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Full-Text Articles in Physical Sciences and Mathematics
Synthesis Of 2-Aryl-5-(Arylsulfonyl)-1,3,4-Oxadiazoles As Potent Antibacterial Andantioxidant Agents, S N Murthy Boddapati, Subrahmanyam Talari, A Emmanuel Kola, Bhuvaneswari Chalapaka
Synthesis Of 2-Aryl-5-(Arylsulfonyl)-1,3,4-Oxadiazoles As Potent Antibacterial Andantioxidant Agents, S N Murthy Boddapati, Subrahmanyam Talari, A Emmanuel Kola, Bhuvaneswari Chalapaka
Turkish Journal of Chemistry
Ten novel 2-aryl-5-(arylsulfonyl)-1,3,4-oxadiazoles were produced and assessed for their in vitro antibacterial and antioxidant activities. Diverse spectroscopic methods li1H NMR, 13C NMR, IR, and LCMS were used for the characterization of the prepared samples and all the data was in good agreement with the anticipated structures. The prepared compounds 6a-j were screened for their in vitro antibacterial activity against bacterial strains Pseudomonas aeruginosa, Enterobacter aerogenes, Escherichia coli (grampositive), and Bacillus cerus, Staphylococcus aureus, Bacillus subtilis (gram-negative). The antimicrobial screening outcome revealed that the prepared 2-(3,4-dimethylphenyl)-5-tosyl-1,3,4-oxadiazole (6j), 2-(3-isopropylphenyl)-5-tosyl-1,3,4-oxadiazole (6c), and 2-(2-ethylphenyl)-5-tosyl-1,3,4-oxadiazole (6i) are most potent among all the examined compounds. Furthermore, …
Synthesis Of Novel Oxadiazole Derivatives And Their Cytotoxic Activity Against Various Cancer Cell Lines, Bi̇lgesu Onur Sucu, Eli̇f Beyza Koç
Synthesis Of Novel Oxadiazole Derivatives And Their Cytotoxic Activity Against Various Cancer Cell Lines, Bi̇lgesu Onur Sucu, Eli̇f Beyza Koç
Turkish Journal of Chemistry
Caffeic acid (CA), ferulic acid (FA) and caffeic acid phenethyl ester (CAPE) have a broad anticancer effect on various cell lines. In this study, nine ferulic and caffeic acid-based 1,2,4 and 1,3,4 oxadiazole molecular hybrids were synthesized and their cytotoxic activity was evaluated mainly against Glioblastoma (GBM) cell lines. Compounds 1 and 5 exhibited the highest inhibitory activity against three different GBM cell lines (LN229, T98G, and U87), without toxicity to healthy human mesenchymal stem cells (hMSC). In addition, their cytotoxicity was also evaluated against three additional cancer cell lines and more inhibitory results were found than GBM cell lines. …
Treatment Of Industrial Contaminants With Zero-Valent Iron- And Zero-Valent Aluminiumactivatedpersulfate: A Case Study With 3,5-Dichlorophenol And 2,4-Dichloroaniline, Olga Koba Ucun, Bahareh Montazeri̇, İdi̇l Arslan Alaton, Tuğba Ölmez Hanci
Treatment Of Industrial Contaminants With Zero-Valent Iron- And Zero-Valent Aluminiumactivatedpersulfate: A Case Study With 3,5-Dichlorophenol And 2,4-Dichloroaniline, Olga Koba Ucun, Bahareh Montazeri̇, İdi̇l Arslan Alaton, Tuğba Ölmez Hanci
Turkish Journal of Chemistry
Zero-valent iron (ZVI)- and zero-valent aluminium (ZVA)-activated persulfate (PS) oxidation procedure was applied to remove the industrial pollutants 3,5-dichlorophenol (3,5-DCP; 12.27 μM) and 2,4-dichloroaniline (2,4-DCA; 12.34 μM) from aqueous solutions. The effects of PS concentration and pH were investigated to optimize heterogeneous treatment systems. Negligible removals were obtained for both pollutants by individual applications of nanoparticles (1 g/L) and PS (1.00 mM). PS activation with ZVI resulted in 59% (1.00 mM PS; 1 g/L ZVI; pH 5.0; 120 min) and 100% (0.75 mM PS; 1 g/L ZVI; pH 5.0; 80 min) 3,5-DCP and 2,4-DCA removals, respectively. The ZVA/PS treatment system …
Synthesis, Spectral Characterization, And Biological Studies Of 3,5-Disubstituted- 1,3,4-Oxadiazole-2(3h)-Thione Derivatives, Tuğçe Özyazici, Fi̇kretti̇n Şahi̇n, Meri̇ç Köksal Akkoç
Synthesis, Spectral Characterization, And Biological Studies Of 3,5-Disubstituted- 1,3,4-Oxadiazole-2(3h)-Thione Derivatives, Tuğçe Özyazici, Fi̇kretti̇n Şahi̇n, Meri̇ç Köksal Akkoç
Turkish Journal of Chemistry
The reaction of 3,4-dichlorophenyl-1,3,4-oxadiazole-2(3H)-thione with piperidine derivatives via Mannich reaction was used to generate eleven novel compounds in moderate to good yields. Synthesized molecules were characterized according to their structure with 1H NMR, 13C NMR and FT-IR spectral foundations, which were compatible with literature informations. Antimicrobial activity and cytotoxicity studies were done by disc diffusion and NCI-60 sulphordamine B assay methods. The antimicrobial test results revealed that synthesized compounds have better activity against gram-positive species than gram-negative ones. A total analysis of the antibacterial, antifungal, and antiyeast activity revealed that newly synthesized compounds were really active against Bacillus cereus, Bacillus …
Synthesis And Bioactivity Of Sulfide Derivatives Containing 1,3,4-Oxadiazole And Pyridine, Gang Yu, Shunhong Chen, Feng He, Dexia Luo, Yu Zhang, Jian Wu
Synthesis And Bioactivity Of Sulfide Derivatives Containing 1,3,4-Oxadiazole And Pyridine, Gang Yu, Shunhong Chen, Feng He, Dexia Luo, Yu Zhang, Jian Wu
Turkish Journal of Chemistry
A series of novel sulfide derivatives containing 1,3,4-oxadiazole and pyridine were synthesized, characterized, and tested for their antibacterial activity against tobacco bacterial wilt and rice bacterial blight and for insecticidal activity toward diamondback moth. The results showed that some compounds had good insecticidal and bactericidal activity, e.g., the activities of compounds 6e and 6g-6j toward tobacco bacterial wilt were much better than those of commercial thiodiazole-copper, and some of the synthesized compounds possessed good insecticidal activity against Plutella xylostella. Compounds 6d, 6h, 6j, 6l, 6p, 6r, and 6p displayed over 93% activity at 500 mg L$^{-1}$.
Synthesis, Characterization, And Nonlinear Optical Properties Of Some New Series Of S-(5-Aryl-1,3,4-Oxadiazol-2-Yl) 2-Chloroethanethioate Derivatives, Zahra Dono Ghezelbash, Hamideh Motiei, Miri Mahmoody, Karim Akbari Delmaghani
Synthesis, Characterization, And Nonlinear Optical Properties Of Some New Series Of S-(5-Aryl-1,3,4-Oxadiazol-2-Yl) 2-Chloroethanethioate Derivatives, Zahra Dono Ghezelbash, Hamideh Motiei, Miri Mahmoody, Karim Akbari Delmaghani
Turkish Journal of Chemistry
In the present investigation, some novel S-(5-aryl-1,3,4-oxadiazol-2-yl)2-chloroethanethioate (3a-3e) derivatives were synthesized and their impact on optical properties was studied. They have also been characterized by elemental analysis and various spectroscopic methods including FTIR, $^{1}$H NMR, $^{13}$C NMR, and UV-Vis techniques. The nonlinear refractive indexes of 3a-3e were also measured in dichloromethane via Z-scan method using a continuous wave diode-pumped laser at 532 nm wavelength. The nonlinear refractive coefficient of compounds was obtained from ${10}^{11}\, \, {m}^{{2}}{/W}$ order. Regarding the appropriate nonlinearity of these compounds, they could be considered good candidates for biooptical and photonic applications. All the synthesized compounds (3a-3e) …
Synthesis And Evaluation Of Novel 1,3,4-Thiadiazole--Fluoroquinolone Hybrids As Antibacterial, Antituberculosis, And Anticancer Agents, Asli Demi̇rci̇, Kaan Gökçe Karayel, Esra Tatar, Si̇nem Öktem Okullu, Ni̇han Ünübol, Paki̇ze Nesli̇han Taşli, Zühtü Tanil Kocagöz, Fi̇kretti̇n Şahi̇n, İlkay Küçükgüzel
Synthesis And Evaluation Of Novel 1,3,4-Thiadiazole--Fluoroquinolone Hybrids As Antibacterial, Antituberculosis, And Anticancer Agents, Asli Demi̇rci̇, Kaan Gökçe Karayel, Esra Tatar, Si̇nem Öktem Okullu, Ni̇han Ünübol, Paki̇ze Nesli̇han Taşli, Zühtü Tanil Kocagöz, Fi̇kretti̇n Şahi̇n, İlkay Küçükgüzel
Turkish Journal of Chemistry
A series of 5-substituted-1,3,4-thiadiazole-based fluoroquinolone derivatives were designed as potential antibacterial and anticancer agents using a molecular hybridization approach. The target compounds 16-25 were synthesized by reacting the corresponding $N$-(5-substituted-1,3,4-thiadiazol-2-yl)-2-chloroacetamides with ciprofloxacin or norfloxacin. The purity and identity of the synthesized compounds were determined by the use of chromatographic and spectral techniques (NMR, IR, MS, etc.) besides elemental analysis. Antibacterial, antituberculosis, and anticancer activity of the target compounds were evaluated against selected strains and cancer cell lines. Compound 20 was appreciated as the most active agent representing antibacterial activity against Escherichia coli and Staphylococcus aureus with MIC values of 4 …
Biological Study On Novel Coumarinyl 1,3,4-Oxadiazoles, Maja Molnar, Ana Amic, Valentina Pavic, Tihomir Kovac, Marija Kovac, Elizabeta Has-Schön
Biological Study On Novel Coumarinyl 1,3,4-Oxadiazoles, Maja Molnar, Ana Amic, Valentina Pavic, Tihomir Kovac, Marija Kovac, Elizabeta Has-Schön
Turkish Journal of Chemistry
Coumarinyl 1,3,4-oxadiazoles were synthesized from Schiff bases and acetic anhydride. All compounds were characterized by melting points and their structures confirmed by mass and $^{1}$H and $^{13}$C NMR spectrometry. These novel coumarinyl derivatives were subjected to antibacterial, antifungal, anta atoxigenic, and antioxidant activity. Their activity varied depending on their structure, where 2-(3-acetyl-5-(((4-methyl-2-oxo-2H-chromen-7-yl)oxy)methyl)- 2,3-dihydro-1,3,4-oxadiazol-2-yl)-1,4-phenylene diacetate showed significant antioxidant and antibacterial activity on B. subtilis. 4-(3-Acetyl-5-(((4-methyl-2-oxo-2H-chromen-7-yl)oxy)methyl)-2,3-dihydro-1,3,4-oxadiazol-2-yl)-1,2-phenylene diacetate was found to possess excellent antifungal and antia atoxigenic activity.
A Rapid And Sensitive Spectrofluorometric Method For The Determination Of Au(Iii) Based On Fluorescence Quenching Of A 1,3,5-Triphenyl-2-Pyrazoline, Aysel Başoğlu, Ümmühan Ocak, Seda Fandakli, Nuretti̇n Yayli
A Rapid And Sensitive Spectrofluorometric Method For The Determination Of Au(Iii) Based On Fluorescence Quenching Of A 1,3,5-Triphenyl-2-Pyrazoline, Aysel Başoğlu, Ümmühan Ocak, Seda Fandakli, Nuretti̇n Yayli
Turkish Journal of Chemistry
A simple, rapid, sensitive, and low-cost spectrofluorometric method was developed for the determination of Au(III) using 5-(2,3-dimethoxyphenyl)-3-(4-methoxyphenyl)-1-phenyl-4,5-dihydro-1H-pyrazole (L) in ethanol/water. The method is based on the change in the fluorescence intensity at 464 nm after excitation at 355 nm as a result of the reaction between the ligand and Au(III). The fluorescent emission of ligand at 464 nm decreased with the increasing of Au(III) concentration. The ligand concentration, pH effect, response time, and effect of foreign ions were determined. From the results of fluorescence titration experiments, it was found that the ligand (1 $\times $ 10$^{-7}$ M) was selective and …
Synthesis And Characterizations Of Novel Thiazolyl-Thiadiazole Derivatives As Telomerase Activators, İsmai̇l Kayaği̇l, Ayşe Gül Mutlu, Ülkü Bayhan, İnanç Yilmaz, Şeref Demi̇rayak
Synthesis And Characterizations Of Novel Thiazolyl-Thiadiazole Derivatives As Telomerase Activators, İsmai̇l Kayaği̇l, Ayşe Gül Mutlu, Ülkü Bayhan, İnanç Yilmaz, Şeref Demi̇rayak
Turkish Journal of Chemistry
Pyridine-3/4-thiocarboxamide derivatives were used as starting materials for the synthesis of the target compounds. The pyridine-3/4-thiocarboxamide derivatives were reacted with ethyl 2-chloroacetoacetate in ethanol to give the thiazole derivatives (1, 2). The two ethyl thiazole-carboxylate derivatives (1, 2) thus obtained were treated with sodium hydroxide solution and ethanol and converted to carboxylic acids (3, 4). The carboxylic acid derivatives (3, 4) were reacted with thiosemicarbazide in phosphoroxy trichloride and aminothiadiazole rings (5, 6) were formed. Thus, two thiazolyl-thiadiazole amine derivatives (5, 6) were obtained. These two derivatives (5, 6) were converted into two chloroacetamidothiadiazole derivatives (7, 8) by reaction with …
The Synthesis Of New Oxindoles As Analogs Of Natural Product 3,3$^\Prime $-Bis(Indolyl)Oxindole And In Vitro Evaluation Of The Enzyme Activity Of G6pd And 6pgd, Si̇nan Bayindir, Adnan Ayna, Yusuf Temel, Mehmet Çi̇ftci̇
The Synthesis Of New Oxindoles As Analogs Of Natural Product 3,3$^\Prime $-Bis(Indolyl)Oxindole And In Vitro Evaluation Of The Enzyme Activity Of G6pd And 6pgd, Si̇nan Bayindir, Adnan Ayna, Yusuf Temel, Mehmet Çi̇ftci̇
Turkish Journal of Chemistry
Natural and synthetic derivatives that contain an indole core are being used in medical treatments and technological processes. Therefore, the development of new synthetic methods for the synthesis of indole derivatives is very popular. In this study, new oxindoles with reaction of 4,7-dihydro-1$H$-indole (2) and isatin (4) were synthesized as analogs of natural product 3,3$^\prime $-bis(indolyl)oxindole. The biological properties of the compounds obtained during this study were also studied, showing that compounds 5, 7, and 12 inhibited the activity of G6PD with an IC$_{50}$ of 99 $\mu $M, 231 $\mu $M, and 304 $\mu $M respectively. The activity of rat …
Synthesis Of 5-Aryl-$N$-(Trichloroacetyl)-1,3,4-Oxadiazole-2-Carboxamide Via Three-Component Reaction Of Trichloroacetyl Isocyanate, ($N$-Isocyanimino)Triphenylphosphorane, And Benzoic Acid Derivatives, Nahid Shajari, Ali Reza Kazemizadeh, Ali Ramazani
Synthesis Of 5-Aryl-$N$-(Trichloroacetyl)-1,3,4-Oxadiazole-2-Carboxamide Via Three-Component Reaction Of Trichloroacetyl Isocyanate, ($N$-Isocyanimino)Triphenylphosphorane, And Benzoic Acid Derivatives, Nahid Shajari, Ali Reza Kazemizadeh, Ali Ramazani
Turkish Journal of Chemistry
The three-component reaction of benzoic acid derivatives, ($N$-isocyanimino)triphenylphosphorane, and trichloroacetyl isocyanate in a 1:1:1 ratio in CH$_{3}$CN occurred at room temperature, and the 5-aryl-$N$-(trichloroacetyl)-1,3,4-oxadiazole-2-carboxamide derivatives produced were formed in high yields. The reaction proceeded smoothly and cleanly under mild reaction conditions and no side reactions were observed. The structures of the products were confirmed by IR, $^{1}$H NMR, $^{13}$C NMR, mass spectroscopy, and elemental analysis.
Synthesis Of Novel 1,2,4-Triazoles And Triazolo-Thiadiazines As Anticancer Agents, Thoraya Abd El-Reheem Farghaly, Magda Ahmad Abdallah, Huda Kamel Mmahmoud
Synthesis Of Novel 1,2,4-Triazoles And Triazolo-Thiadiazines As Anticancer Agents, Thoraya Abd El-Reheem Farghaly, Magda Ahmad Abdallah, Huda Kamel Mmahmoud
Turkish Journal of Chemistry
A new series of 7-arylazo-5$H$-3-(trifluoromethyl)-6-methyl-1,2,4-triazolo-[3,4-$b$]-1,3,4-thiadiazines was prepared by reaction of 4-amino-3-trifluoromethyl-5-mercapto-1,2,4-triazoles with $N$-aryl-2-oxo-propane hydrazonoyl chloride in dioxane under reflux in the presence of triethylamine. Furthermore, Schiff bases of 4-amino-5-mercapto-1,2,4-triazole derivatives were reacted with a variety of hydrazonoyl chlorides and gave the respective hydrazonothioates. In addition, the novel \textit{bis}-(1,2,4-triazole-3-thione) was reacted with the appropriate hydrazonoyl chloride in dioxane under reflux in the presence of triethylamine to give the corresponding \textit{bis}-(1,2,4-triazolethiohydrazonoate). The structures of the new compounds were established based on elemental and spectral data. The mechanism of the studied reaction was also discussed. Moreover, some of the new products were screened …
Kinetics And Performance Studies Of A Switchable Solvent Tmg (1,1,3,3-Tetramethylguanidine)/1-Propanol/Carbon Dioxide System, Özge Yüksel, Mustafa Çağdaş Öztürk, Ayça Şeker, Erdoğan Alper
Kinetics And Performance Studies Of A Switchable Solvent Tmg (1,1,3,3-Tetramethylguanidine)/1-Propanol/Carbon Dioxide System, Özge Yüksel, Mustafa Çağdaş Öztürk, Ayça Şeker, Erdoğan Alper
Turkish Journal of Chemistry
The rate constants and the activation energies of the reaction between carbon dioxide and 1,1,3,3-tetramethylguanidine (TMG) in 1-propanol solution were measured by a stopped-flow technique at a temperature range of 288--308 K and at a TMG concentration range of 2.5--10.0 wt %. Based on the pseudo-first-order reaction for CO_2, the reaction was modeled by a termolecular reaction mechanism, which resulted in a rate constant of 199.30 m^3 kmol^{-1} s^{-1} at 298 K. The activation energies were 5.19 kJ/mol and 5.26 kJ/mol at 2.5 and 5.0 wt % TMG, respectively. In addition, carbon dioxide absorption capacity was investigated using a gas--liquid …
Synthesis Of Novel Imidazo[1,2-A]Pyridines And Evaluation Of Their Antifungal Activities, Füsun Göktaş, Nesri̇n Cesur, Di̇lek Şatana, Meltem Uzun
Synthesis Of Novel Imidazo[1,2-A]Pyridines And Evaluation Of Their Antifungal Activities, Füsun Göktaş, Nesri̇n Cesur, Di̇lek Şatana, Meltem Uzun
Turkish Journal of Chemistry
New 2-(imidazo[1,2-a]pyridin-2-ylcarbonyl)-N-substituted hydrazinecarbothioamides (4a--j), N'-(3-substituted-4-oxo-1,3-thiazolidin-2-ylidene)imidazo[1,2-a]pyridine-2-carbohydrazides (5a--f), and N-(nonsubstituted/4-substituted phenyl)-5-(imidazo[1,2-a]pyridine-2-yl)-1,3,4-oxadiazole-2-amines (6a--d) were synthesized from imidazo[1,2-a]pyridine-2-carbohydrazide (3) and evaluated for antifungal activity against Microsporum gypseum NCPF 580, M. canis, Trichophyton tonsurans NCPF 245, T. rubrum, Candida albicans ATCC 10231, and C. parapsilosis ATCC 22019 using amphotericin B as the standard. The chemical structures of the compounds were confirmed by elemental analysis, IR, ^1H NMR, ^{13}C NMR, HMBC (^{13}C, ^1H), and mass spectra. Most of the tested compounds showed moderate antifungal activity. Hydrazinecarbothioamide derivatives 4h and 4f exhibited the highest activity against M. canis (MIC: 2 \mu g mL^{-1} and 4 \mu g …
Synthesis And Characterization Of New (E)-N'-(Substituted Benzylidene)-2-(3-(2-Methyl)-4-Oxo-3,4-Dihydroquinazolin-2-Ylthio)Acetohydrazides, Aamer Saeed, Shams-Ul Mahmood, Ulrich Flörke
Synthesis And Characterization Of New (E)-N'-(Substituted Benzylidene)-2-(3-(2-Methyl)-4-Oxo-3,4-Dihydroquinazolin-2-Ylthio)Acetohydrazides, Aamer Saeed, Shams-Ul Mahmood, Ulrich Flörke
Turkish Journal of Chemistry
A small library of new azomethine derivatives of 3-aryl-2-thioxo-2,3-dihydroquinazolin-4(1H)-ones was synthesized. The key intermediates 2-thioxo-quinazolinones (3a--e), obtained in 2 steps from the corresponding anilines, were treated with methyl chloroacetate to afford S-substituted esters (4a,d), which were then converted into corresponding acetohydrazides (5a,d). Further, acetohydrazide (5d) was converted to the azomethines derivatives (6a--k) by reacting with a number of suitably substituted benzaldehydes. FTIR, ^1H NMR, ^{13}C NMR, GC-MS, and elemental analyses were used to confirm the assigned structures of the synthesized compounds. Further, compounds 3a, 5, and 6j were also confirmed by X-ray diffraction data.
Synthesis And Characterization Of Ni(Ii) And Cu(Ii) Complexes Derived From Novel Phenolic Mannich Bases, Nurgün Büyükkidan, Sali̇h Özer
Synthesis And Characterization Of Ni(Ii) And Cu(Ii) Complexes Derived From Novel Phenolic Mannich Bases, Nurgün Büyükkidan, Sali̇h Özer
Turkish Journal of Chemistry
The novel phenolic Mannich bases 2,2'-(2-hydroxy-4,5- dimethylbenzylazanediyl)diethanol (1) and 2-((2-(4-(2-hydroxy-4,5- dimethylbenzyl)piperazin-1-yl)ethylamino)methyl)-4,5-dimethylphenol (2) have been synthesized in good yield by using a microwave-induced technique from 3,4-dimethylphenol and corresponding amines in the presence of formaldehyde. Metal complexes of 1 and 2 for Ni(II) (3 and 5) and for Cu(II) (4 and 6) have also been prepared and all compounds have been characterized by elemental and spectral analyses. Thermal, magnetic, and electronic studies have also been reported for metal complexes. Electronic spectra and magnetic susceptibility measurements suggested tetrahedral geometry for Ni(II) (3), square planar geometry for Cu(II) (4) complexes of 1, and octahedral …
Synthesis Of Linezolid-Like Molecules And Evaluation Of Their Antimicrobial Activities, Serap Başoğlu, Meltem Yolal, Ahmet Demi̇rbaş, Hakan Bektaş, Rza Abbasoğlu, Nesli̇han Demi̇rbaş
Synthesis Of Linezolid-Like Molecules And Evaluation Of Their Antimicrobial Activities, Serap Başoğlu, Meltem Yolal, Ahmet Demi̇rbaş, Hakan Bektaş, Rza Abbasoğlu, Nesli̇han Demi̇rbaş
Turkish Journal of Chemistry
3-Fluoro-4-(morpholin-4-yl)aniline (2), prepared from 3,4-difluoronitrobenzene, was converted to the corresponding Schiff base (3) by treatment with indol-3-carbaldehyde. The treatment of thiourea 4 and carbothioamide derivatives 9 with ethyl bromoacetate or 4-substituted phenacyl bromides generated the corresponding thiazolidinone (5 and 13) and thiazoline (6 and 12) derivatives, respectively. The acidic or basic treatment of carbothioamide 9 produced 1,3,4-thiadiazole (11) or 1,2,4-triazole (10) compounds, respectively. The structural assignments of the new compounds were based on elemental analysis and spectral (IR, ^1H-NMR, ^{13}C-NMR, and LC-MS) data. The antimicrobial activity study revealed that all compounds showed good antitubercular activities.
Four-Component Synthesis Of 1,3,4-Oxadiazole Derivatives From N-Isocyaniminotriphenylphosphorane, Aromatic Carboxylic Acids, Aromatic Bis-Aldehydes, And Secondary Amines, Ali Ramazani, Zahra Karimi, Ali Souldozi, Yavar Ahmadi
Four-Component Synthesis Of 1,3,4-Oxadiazole Derivatives From N-Isocyaniminotriphenylphosphorane, Aromatic Carboxylic Acids, Aromatic Bis-Aldehydes, And Secondary Amines, Ali Ramazani, Zahra Karimi, Ali Souldozi, Yavar Ahmadi
Turkish Journal of Chemistry
The 1:1 iminium intermediate generated by the addition of a secondary amine to aromatic bis-aldehydes (isophthalaldehyde and terphthalaldehyde) is trapped by the N-isocyaniminotriphenylphosphorane in the presence of a aromatic carboxylic acid derivative, which leads to the formation of corresponding iminophosphorane intermediate. Then disubstituted 1,3,4-oxadiazole derivatives are formed via intramolecular aza-Wittig reaction of the iminophosphorane intermediates. The reactions were completed in neutral conditions at room temperature and the corresponding disubstituted 1,3,4-oxadiazole derivatives were produced in excellent yields.
One-Pot Synthesis Of Fully Substituted 1,3,4-Oxadiazole Derivatives From Aromatic Carboxylic Acids, Cyclobutanone And N-Isocyaniminotriphenylphosphorane, Mohsen Valizadeh Holagh, Abel Mohammadali Oglu Maharramv, Mirza Aliakbar Oglu Allahverdiyev, Ali Ramazani, Yavar Ahmadi, Ali Souldozi
One-Pot Synthesis Of Fully Substituted 1,3,4-Oxadiazole Derivatives From Aromatic Carboxylic Acids, Cyclobutanone And N-Isocyaniminotriphenylphosphorane, Mohsen Valizadeh Holagh, Abel Mohammadali Oglu Maharramv, Mirza Aliakbar Oglu Allahverdiyev, Ali Ramazani, Yavar Ahmadi, Ali Souldozi
Turkish Journal of Chemistry
Reactions of N-isocyaniminotriphenylphosphorane with cyclobutanone in the presence of aromatic (or heteroaromatic) carboxylic acids proceeded smoothly at room temperature and in neutral conditions to afford sterically congested 1-(5-aryl-1,3,4-oxadiazol-2-yl)- 1-cyclobutanol derivatives in high yields. The reaction proceeded smoothly and cleanly under mild conditions and no side reactions were observed. The structures of the products were deduced from their IR, ^1HNMR, and ^{13}CNMR spectra, and mass spectrometry.
Preparation And Antimicrobial Activity Evaluation Of Some Quinoline Derivatives Containing An Azole Nucleus, Muhammet Özyanik, Serpi̇l Demi̇rci̇, Hakan Bektaş, Nesli̇han Demi̇rbaş, Ahmet Demi̇rbaş, Şengül Alpay Karaoğlu
Preparation And Antimicrobial Activity Evaluation Of Some Quinoline Derivatives Containing An Azole Nucleus, Muhammet Özyanik, Serpi̇l Demi̇rci̇, Hakan Bektaş, Nesli̇han Demi̇rbaş, Ahmet Demi̇rbaş, Şengül Alpay Karaoğlu
Turkish Journal of Chemistry
Quinoline-2-carbohydrazide (2) obtained from quinaldic acid (1) was converted to the corresponding carbothioamide 3 and carboxamide 6 by treatment with benzyliso(thio)cyanate. The basic treatment of 3 and 6 yielded the corresponding 1,2,4-triazole derivatives 4 and 7. The synthesis of 5-(quinolin-2-yl)-1,3,4- oxadiazol-2-thiol (9) was performed from the reaction of 1 with CS_2 in basic media. The Mannich reaction of compounds 4, 7, and 9 resulted in the formation of aminoalkylated derivatives 5a-c, 8, and 10a,b. The condensation of 1 with thiosemicarbazide, carbohydrazide, or thiocarbohydrazide gave the corresponding 1,2,4-triazole derivatives (11-13). The treatment of 4-amino-5-(quinolin-2-yl)- 4H-1,2,4-triazole-3-thiol (13) with 4-chlorophenacyl bromide caused the …
A One-Pot Efficient Four-Component Reaction For The Synthesis Of 2-(Arylamino)-2-(5-Aryl-1-Ethenyl-1,3,4-Oxadiazol-2-Yl)Propyl Benzoate (Or 4-Bromobenzoate) Derivatives, Mohsen Valizadeh Holagh, Abel Mohammadali Oglu Maharramov, Mirza Aliakbar Oglu Allahverdiyev, Ali Ramazani, Yavar Ahmadi, Fatemeh Zeinali Nasrabadi, Ali Souldozi
A One-Pot Efficient Four-Component Reaction For The Synthesis Of 2-(Arylamino)-2-(5-Aryl-1-Ethenyl-1,3,4-Oxadiazol-2-Yl)Propyl Benzoate (Or 4-Bromobenzoate) Derivatives, Mohsen Valizadeh Holagh, Abel Mohammadali Oglu Maharramov, Mirza Aliakbar Oglu Allahverdiyev, Ali Ramazani, Yavar Ahmadi, Fatemeh Zeinali Nasrabadi, Ali Souldozi
Turkish Journal of Chemistry
Reactions of N-isocyaniminotriphenylphosphorane with 2-oxopropyl benzoate (or 2-oxopropyl 4-bromobenzoate) in the presence of 3-phenyl-2-propynoic acid and primary amines proceeded smoothly at room temperature and in neutral conditions to afford sterically congested 1,3,4-oxadiazole derivatives in high yields. The reaction proceeded smoothly and cleanly under mild conditions and no side reactions were observed.
Synthesis And Anti-Helicobacter Pylori Activity Of (4-Nitro-1-Imidazolylmethyl)-1,2,4-Triazoles, 1,3,4-Thiadiazoles, And 1,3,4-Oxadiazoles, Asal Fallah-Tafti, Tahmineh Akbarzadeh, Parastoo Saniee, Farideh Siavoshi, Abbas Shafiee, Alireza Foroumadi
Synthesis And Anti-Helicobacter Pylori Activity Of (4-Nitro-1-Imidazolylmethyl)-1,2,4-Triazoles, 1,3,4-Thiadiazoles, And 1,3,4-Oxadiazoles, Asal Fallah-Tafti, Tahmineh Akbarzadeh, Parastoo Saniee, Farideh Siavoshi, Abbas Shafiee, Alireza Foroumadi
Turkish Journal of Chemistry
A series of [(4-nitro-1H-imidazol-1-yl)methyl]-1,2,4- triazoles and 1,3,4-thiadiazoles were prepared and evaluated for their activity against sensitive and resistant H. pylori strains. Study of the structure-activity relationship of these series of compounds indicated that the type of nitroimidazole moiety and the pendent group on the heteroaryl analog dramatically impact the anti-H. pylori activity. In triazole series, compound 5d, containing a 4-methyl phenyl group on the triazole ring, was the most potent compound tested against both metronidazole-sensitive and -resistant strains at a concentration of 8 \mu g.
Synthesis And Characterization Of New Symmetrical 3,6-Bis[(25,26,27- Tripropoxy-28-(3-(4-Iodophenyl) Propoxy)-P-Tert-Butyl Calix[4]Arene Ethynyl]-9h- Fluoren-9-One By Sonogashira Coupling As A Novel Precursor For Synthesis Of Quinodimethane (Qdm), Karim Akbari Dilmaghani, Fazel Nasuhi Pur
Synthesis And Characterization Of New Symmetrical 3,6-Bis[(25,26,27- Tripropoxy-28-(3-(4-Iodophenyl) Propoxy)-P-Tert-Butyl Calix[4]Arene Ethynyl]-9h- Fluoren-9-One By Sonogashira Coupling As A Novel Precursor For Synthesis Of Quinodimethane (Qdm), Karim Akbari Dilmaghani, Fazel Nasuhi Pur
Turkish Journal of Chemistry
Novel symmetrical 3,6-bis[(25,26,27-tripropoxy-28-(3-(4-iodophenyl)propoxy)-p-tert-butyl calix[4]arene ethynyl]-9H-fluoren-9-one with a cone conformation was synthesized by palladium-catalyzed coupling of (25,26,27-tripropoxy- 28-(3-(4-iodophenyl)propoxy)-p-tert-butyl calix[4]arene and 3,6-diethynyl-9H-fluoren-9-one. Its structure was confirmed by FT-IR, ^1H-NMR, and ^{13}C-NMR spectroscopy, and elemental analysis and positive ion FAB mass spectrometry.
Synthesis Of Some New Biheterocyclic Triazole Derivatives And Evaluation Of Their Antimicrobial Activity, Hakan Bektaş, Ahmet Demi̇rbaş, Nesli̇han Demi̇rbaş, Şengül Alpay Karaoğlu
Synthesis Of Some New Biheterocyclic Triazole Derivatives And Evaluation Of Their Antimicrobial Activity, Hakan Bektaş, Ahmet Demi̇rbaş, Nesli̇han Demi̇rbaş, Şengül Alpay Karaoğlu
Turkish Journal of Chemistry
2-{3-(4-Substitutedbenzyl)-4-[2-(1H-indol-3-yl)ethyl]-5-oxo-4,5- dihydro-1H-1,2,4-triazol-1-yl}-N'-(aryl-methylene)acetohydrazides (5a-g), 4-amino-2-{-(4-substitutedbenzyl)-5-oxo-4,5-dihydro-1H-1,2,4-triazol- 1-yl}-N'-(arylmethylene)acetohydrazides (6a,b), and 4-[2-(1H-indol- 3-yl)ethyl]-5-(4-substitutedbenzyl)-2-{5-(phenylamino)-1,3,4-thiadiazol- 2-yl]methyl}-2,4-dihydro-3H-1,2,4-triazol-3-ones (8a,b) were synthesized starting from 4-alkyl-5-(4-substitutedbenzyl)-2,4-dihydro- 3H-1,2,4-triazol-3-ones (2a-c) by several steps and their structures were well characterized by elemental analyses, IR, ^1H-NMR, ^{13}C-NMR, and mass spectral studies. They were also screened for their microbial activities. The obtained antimicrobial activity results revealed that 12 among the 24 compounds tested displayed variable growth inhibition effects on the tested gram-positive and gram-negative bacterial strains. None of the compounds showed antifungal activity against yeast-like fungi.
Synthesis And Antimicrobial Activities Of 2-(5-Mercapto)-1,3-Oxadiazol-2-Ylmethyl-1,2,4-Triazol-3-One Derivatives, Nesli̇han Demi̇rbaş, Ahmet Demi̇rbaş, Hakan Bektaş, Şengül Alpay Karaoğlu, Deni̇z Şahi̇n
Synthesis And Antimicrobial Activities Of 2-(5-Mercapto)-1,3-Oxadiazol-2-Ylmethyl-1,2,4-Triazol-3-One Derivatives, Nesli̇han Demi̇rbaş, Ahmet Demi̇rbaş, Hakan Bektaş, Şengül Alpay Karaoğlu, Deni̇z Şahi̇n
Turkish Journal of Chemistry
The synthesis of 4-amino-2-[(5-mercapto-1,3,4-oxadiazol-2- yl)methyl]-5-(4-methylphenyl)-2,4-dihydro-3H-1,2,4-triazol-3-one (2) and 4-amino-2-[(4-amino-5-mercapto-4H-1,2,4-triazol-3-yl)methyl]- 5-(4-methylphenyl)-2,4-dihydro-3H-1,2,4-triazol-3-one (5) was performed starting from 2-[4-amino-3-(4-methylphenyl)-5-oxo-4,5- dihydro-1H-1,2,4-triazol-1-yl]acetohydrazide (1). The treatment of 2 and 5 with 4-fluorobenzaldehyde (for 8) or salicylaldehyde (for 6) afforded the corresponding Schiff bases (6 and 8). The condensation of 5 with phenacyl bromide produced 4-amino-5-(4-methylphenyl)-2- [(6-phenyl-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazin-3-yl)methyl]- 2,4-dihydro-3H-1,2,4-triazol-3-one (7). The alkylation of 2 and 8 was carried out by using methyl iodide in basic media. Compounds 3 and 10a,b were prepared by aminoalkylation of 2 and 8 with 4-fluorophenyl piperazine, morpholine, or 4-methyl piperazine in the presence of formaldehyde. The synthesized compounds were screened for their antimicrobial activities …
A Simple And Efficient Procedure For Synthesis Of Optically Active 1,3,4-Oxadiazole Derivatives Containing L-Amino Acid Moieties, Naser Foroughifar, Akbar Mobinikhaledi, Sattar Ebrahimi
A Simple And Efficient Procedure For Synthesis Of Optically Active 1,3,4-Oxadiazole Derivatives Containing L-Amino Acid Moieties, Naser Foroughifar, Akbar Mobinikhaledi, Sattar Ebrahimi
Turkish Journal of Chemistry
Some new unsymmetrical and optically active 2,5-disubstituted 1,3,4-oxadiazoles 5a-j were efficiently synthesized by cyclization reaction of diacylhydrazides 4a-j. The synthesis of the title compounds was achieved by the reaction of acyl hydrazides 3a-b and N-phetaloyl-L-amino acids 1a-e in the presence of the phosphoroxy chloride (POCl_3) as an anhydrous reagent.
Synthesis And Antimicrobial Activities Of Some New 1,2,4-Triazole Derivatives, Nesli̇han Demi̇rbaş, Ahmet Demi̇rbaş, Hacer Bayrak, Hakan Bektaş, Şengül Alpay Karaoğlu
Synthesis And Antimicrobial Activities Of Some New 1,2,4-Triazole Derivatives, Nesli̇han Demi̇rbaş, Ahmet Demi̇rbaş, Hacer Bayrak, Hakan Bektaş, Şengül Alpay Karaoğlu
Turkish Journal of Chemistry
The synthesis of ethyl [3-(cyanomethyl)-5-alkyl-4H-1,2,4-triazol- 4-yl]carbamates (2a-d) was performed starting from ethyl 2-[ethoxy(4- (aryl)methylene]hydrazinecarboxylates (1a, 1b). The treatment of 2a with thiosemicarbazide afforded ethyl [3-[(5-amino-1,3,4-thiadiazol- 2-yl)methyl]-5-(4-nitrophenyl)-4H-1,2,4-triazol-4-yl]carbamates (3a), whereas compound 2b produced 5-{[4-amino-5-(4-methylphenyl)- 4H-1,2,4-triazol-3-yl]methyl}-1,3,4-thiadiazol-2-amine (3b) in the same reaction conditions. The treatment of tert-butyl 2-[2-(4-chlorophenyl)-1-ethoxyethylidene]hydrazinecarboxylate (5) with malonohydrazide or cyanoacethydrazide gave the corresponding 1,2,4-triazol-ylcarbamate derivatives (6 or 9); then the hydrolysis of these compounds resulted in the formation of 3-{[4-amino-5-(4- chlorobenzyl)-4H-1,2,4-triazol-3-yl]methyl}-5-(4-chlorobenzyl)-4H- 1,2,4-triazol-4-amine (7) and [4-amino-5-(4-chlorobenzyl)-4H- 1,2,4-triazole-3-yl]acetonitrile (10), respectively. The synthesis of the Schiff base derivatives 3-(4-chlorobenzyl)-5-{[5-(4-chloroben- zyl)-4-[(2-hydroxyphenyl-methylene)amino]-4H-1,2,4-triazol-3-yl]methyl} -N-(2-hydroxyphenylmethylene)-4H-1,2,4-triazol-4-amine (8), and (5-(4-chlorobenzyl)-4-{[(2,6-dichlorophenyl)methylene]amino}-4H-1,2,4- triazol-3-yl)acetonitrile (12) was performed from the reaction of compounds 7 …
Synthesis And In Vitro Anti-Helicobacter Pylori Activity Of 2-(Substituted Benzylthio)-5-(5-Nitro-2- Furyl)-1, 3, 4-Thiadiazole Derivatives, Negar Mohammadhosseini, Ali Asadipor, Bahram Letafat, Mohsen Vosooghi, Farideh Siavoshi, Abbas Shafiee, Alireza Foroumadi
Synthesis And In Vitro Anti-Helicobacter Pylori Activity Of 2-(Substituted Benzylthio)-5-(5-Nitro-2- Furyl)-1, 3, 4-Thiadiazole Derivatives, Negar Mohammadhosseini, Ali Asadipor, Bahram Letafat, Mohsen Vosooghi, Farideh Siavoshi, Abbas Shafiee, Alireza Foroumadi
Turkish Journal of Chemistry
Starting from (5-nitrofuran-2-yl)methylene diacetate, a new series of 2-[(substituted benzyl)thio]-5-(5-nitro-2-furyl)-1,3,4-thiadiazoles (6a-n) were synthesized and the structures of the compounds were determined using spectroscopic methods including mass spectrometry, ^1H-nuclear magnetic resonance, infrared spectroscopy, and elemental analysis. The in vitro anti-Helicobacter pylori activity of the synthesized compounds was evaluated by the disk diffusion method against the clinical isolates of Helicobacter pylori. The results indicated that most of the synthesized compounds exhibited significant inhibitory activity against H. pylori with respect to standard drug metronidazole. Compound 6l, containing the 2-chloro-6-fluorobenzylthio moiety, was the most potent compound tested.
Synthesis, Characterization, And Optical Properties Of Novel 2,5-Bis[4-(2-(-Arylvinyl)Phenyl]-1,3,4-Oxadiazoles, Dao-Hang He, Yong-Chuang Zhu, Zhuo-Ru Yang, Ai-Xi Hu, Gao Cao
Synthesis, Characterization, And Optical Properties Of Novel 2,5-Bis[4-(2-(-Arylvinyl)Phenyl]-1,3,4-Oxadiazoles, Dao-Hang He, Yong-Chuang Zhu, Zhuo-Ru Yang, Ai-Xi Hu, Gao Cao
Turkish Journal of Chemistry
Six novel 2,5-bis[4-(2-arylvinyl)phenyl]-1,3,4-oxadiazoles were synthesized by introducing 1,3,4-oxadiazole moiety into the stilbene skeleton. The synthesis route included the cyclization of p-toluic acid and hydrazine hydrate catalyzed by polyphosphoric acid (PPA), bromination of 1,3-dibromo-5,5-dimethylhydantoin (DBDMH), esterification, and the Wittig-Horner reaction. All the title compounds were characterized by ^1H-NMR, MS, and elemental analysis. UV-Vis absorption and fluorescence emission spectra in THF solution were investigated; the compounds may have potential for use in organic optical materials.