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Synthesis Of Alnustone-Like Diarylpentanoids Via A 4 + 1 Strategy And Assessment Of Their Potential Anticancer Activity, Nesli̇han Çelebi̇oğlu, Özlem Özdemi̇r Tozlu, Hasan Türkez, Hasan Seçen
Synthesis Of Alnustone-Like Diarylpentanoids Via A 4 + 1 Strategy And Assessment Of Their Potential Anticancer Activity, Nesli̇han Çelebi̇oğlu, Özlem Özdemi̇r Tozlu, Hasan Türkez, Hasan Seçen
Turkish Journal of Chemistry
Twelve compounds with a 1,5-diaryl-1-penten-3-one structure were synthesized and their cytotoxic activities were evaluated. The 1,5-diaryl-1-penten-3-one compounds were obtained via in situ enaminations of 4-phenyl-2-butanone and 4-(4-hydroxyphenyl)-2- butanone in the presence of pyrrolidine-AcOH, followed by condensation with six different benzaldehydes. The synthesized compounds were tested for their cytotoxic activity against human glioblastoma (U87-MG), breast (MCF-7), and prostate (PC-3) cancer cell lines. Some of the novel compounds exhibited remarkable cytotoxic action, especially against MCF-7 cancer cells.
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. …
Integrated 3d-Qsar, Molecular Docking, And Molecular Dynamics Simulation Studies On 1,2,3-Triazole Based Derivatives For Designing New Acetylcholinesterase Inhibitors, Khalil El Khatabi, Ilham Aanouz, Reda El-Mernissi, Atul Kumar Singh, Mohammed Aziz Ajana, Tahar Lakhlifi, Shashank Kumar, Mohammed Bouachrine
Integrated 3d-Qsar, Molecular Docking, And Molecular Dynamics Simulation Studies On 1,2,3-Triazole Based Derivatives For Designing New Acetylcholinesterase Inhibitors, Khalil El Khatabi, Ilham Aanouz, Reda El-Mernissi, Atul Kumar Singh, Mohammed Aziz Ajana, Tahar Lakhlifi, Shashank Kumar, Mohammed Bouachrine
Turkish Journal of Chemistry
Alzheimer's disease (AD) is a multifactorial and polygenic disease. It is the most prevalent reason for dementia in the aging population. A dataset of twenty-six 1,2,3-triazole-based derivatives previously synthetized and evaluated for acetylcholinesterase inhibitory activity were subjected to the three-dimensional quantitative structure-activity relationship (3D-QSAR) study. Good predictability was achieved for comparative molecular field analysis (CoMFA) (Q2 = 0.604, R2 = 0.863, rext2 = 0.701) and comparative molecular similarity indices analysis (CoMSIA) (Q2 = 0.606, R2 = 0.854, rext2 = 0.647). The molecular features characteristics provided by the 3D-QSAR contour plots were quite useful for designing and improving the activity of …
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, Characterization And Crystal Structures Of Platinum(Ii) Saccharinate Complexes With 1,5-Cyclooctadiene, Ceyda İçsel
Synthesis, Characterization And Crystal Structures Of Platinum(Ii) Saccharinate Complexes With 1,5-Cyclooctadiene, Ceyda İçsel
Turkish Journal of Chemistry
Two new platinum(II) complexes, namely [PtCl(sac)(COD)] (1) and [Pt(sac)$_{2}$(COD)] (2) (sac $=$ saccharinate and COD $=$ 1,5-cyclooctadiene), were synthesized and characterized by elemental analysis, IR, NMR, ESI-MS spectroscopic and thermal analysis (TG/DTA) methods. The platinum(II) complexes were prepared from the reaction of [PtCl$_{2}$(COD)] with Na(sac) • 2H$_{2}$O. The addition of the sac ligand resulted in the replacement of 1 and 2 chlorido ligands in [PtCl$_{2}$(COD)] to yield 1 and 2, respectively. The structures of the complexes were determined by single crystal X-ray diffraction and showed a distorted square planar coordination geometry around platinum(II). COD acted as a $\pi $-donor ligand, …
Design, Synthesis, And Evaluation Of The Antimycobacterial Activity Of 3-Mercapto-1,2,4-Triazole--Pyrrole Hybrids, Gheorghe Roman, Andra-Cristina Bostanaru, Valentin Nastasa, Mihai Mares
Design, Synthesis, And Evaluation Of The Antimycobacterial Activity Of 3-Mercapto-1,2,4-Triazole--Pyrrole Hybrids, Gheorghe Roman, Andra-Cristina Bostanaru, Valentin Nastasa, Mihai Mares
Turkish Journal of Chemistry
A series of 3-mercapto-1,2,4-triazole--pyrrole hybrids was designed as antimycobacterial agents by employing 5-(4-(1$H$-pyrrol-1-yl)phenyl)-4$H$-1,2,4-triazole-3-thiol as the scaffold onto which several types of moieties were introduced in the triazole ring at N-4 and N-2 and as substituents of the mercapto function. The aforementioned moieties are an allyl or a phenyl moiety at N-4; an aminomethyl group at N-2; or methyl, substituted benzyl, ethoxycarbonylmethyl, or substituted phenacyl at sulfur. Investigation of the compounds in the resulting library as growth inhibitors of Mycobacterium smegmatis showed that their minimum inhibitory concentration was higher than 64 mg/L.
1,2-Dibromotetrachloroethane: An Efficient Reagent For Many Transformations By Modified Appel Reaction, Selçuk Eşsi̇z, Ari̇f Daştan
1,2-Dibromotetrachloroethane: An Efficient Reagent For Many Transformations By Modified Appel Reaction, Selçuk Eşsi̇z, Ari̇f Daştan
Turkish Journal of Chemistry
An efficient and facile method has been developed for the synthesis of alkyl bromides from various alcohols under mild conditions using a triphenylphosphine (PPh$_{3})$/1,2-dibromotetrachloroethane (DBTCE) complex in excellent yields and very short time (5 min). This method can also be applied for the transformation of chiral alcohols to their corresponding bromides in very high enantiomeric excess. The PPh$_{3}$/DBTCE complex is also successfully applied to ring-opening reactions of cyclic ethers in mild conditions. Esterification, amidation, and formation of acid anhydrides under very mild experimental conditions are also successfully accomplished by following a modification of the Appel reaction protocol in this work.
Crystal Structure And Hirshfeld Surface Analysis Of 1,2-Ethylene-Bis (Para-Methyl Pyridinium) Dichromate As A New Selective And Mild Agent In Oxidation Of Alcohols, Mostafa Gholizadeh, Mehrdad Pourayoubi, Mohammad Reza Houssiendokht, Hadi Amiri Rudbari, Masoumeh Farimaneh, Anahid Saneei, Giuseppe Bruno
Crystal Structure And Hirshfeld Surface Analysis Of 1,2-Ethylene-Bis (Para-Methyl Pyridinium) Dichromate As A New Selective And Mild Agent In Oxidation Of Alcohols, Mostafa Gholizadeh, Mehrdad Pourayoubi, Mohammad Reza Houssiendokht, Hadi Amiri Rudbari, Masoumeh Farimaneh, Anahid Saneei, Giuseppe Bruno
Turkish Journal of Chemistry
1,2-Ethylene-bis(para-methyl pyridinium) dichromate, (C$_{14}$H$_{18}$N$_{2})$[Cr$_{2}$O$_{7}$], is used as a new oxidizing agent in conversion of some alcohols to their corresponding carbonyl compounds in CH$_{3}$CN solvent and also under solvent-free conditions. In both procedures, high conversion percentages are observed. However, a much shorter reaction time is achieved in solvent-free conditions. For allylic alcohols, the C=C bond is not oxidized and the examined saturated alcohol in this work (i.e. cyclo-hexanol) remains intact, which illustrates the mild nature of reagent used. The structure of the reagent is investigated by single-crystal X-ray diffraction analysis. The C--H$\cdots$O and O$\cdots \pi$ interactions are the most important features …
Characterization And Purification Of 1,2,4-Triazole-Containing Phthalocyanines Synthesized By Microwave Method And Structure Elucidation By Spectroscopic Techniques, Asi̇ye Nas, Ümi̇t Demi̇rbaş, Nurhan Gümrükçüoğlu, Hali̇t Kanteki̇n
Characterization And Purification Of 1,2,4-Triazole-Containing Phthalocyanines Synthesized By Microwave Method And Structure Elucidation By Spectroscopic Techniques, Asi̇ye Nas, Ümi̇t Demi̇rbaş, Nurhan Gümrükçüoğlu, Hali̇t Kanteki̇n
Turkish Journal of Chemistry
The complexes of peripherally tetra-substituted metal-free (8), lead(II) 9), and zinc(II) (10) phthalocyanine derivatives were synthesized for the first time in this work. The structures of these new complex compounds have been elucidated using many spectral methods such as electronic absorption, FT-IR, $^{1}$H NMR, $^{13}$C NMR, elemental analysis, and mass spectra. The thermogravimetric behavior of compounds 8-10 was determined by thermogravimetric analysis method in addition to these spectral methods.
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$^{-1}$.
An Efficient Protocol For The Synthesis Of Brominated Norbornene, Norbornadiene, And Benzonorbornadiene, Selçuk Eşsi̇z
An Efficient Protocol For The Synthesis Of Brominated Norbornene, Norbornadiene, And Benzonorbornadiene, Selçuk Eşsi̇z
Turkish Journal of Chemistry
An efficient protocol for the synthesis of 2-bromonorbornene, 2-bromonorbornadiene, 2-bromoben- zonorbornadiene, 2,3-dibromonorbornene, 2,3-dibromonorbornadiene, and 2,3-dibromobenzonorbornadiene in good yields has been developed. 1,2-Dibromotetrachloroethane is used as the brominating agent for these reactions. The results are discussed in comparison with alternative methods in the literature.
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.
Synthesis, Biological Evaluation, And In Silico Study Of Some Unique Multifunctional 1,2,4-Triazole Acetamides, Almas Sattar, Aziz Ur Rehman, Muhammad Athar Abbasi, Sabahat Zahra Saddiqui, Shahid Rasool, Hira Khalid, Muhammad Arif Lodhi, Farman Ali Khan
Synthesis, Biological Evaluation, And In Silico Study Of Some Unique Multifunctional 1,2,4-Triazole Acetamides, Almas Sattar, Aziz Ur Rehman, Muhammad Athar Abbasi, Sabahat Zahra Saddiqui, Shahid Rasool, Hira Khalid, Muhammad Arif Lodhi, Farman Ali Khan
Turkish Journal of Chemistry
The imperative demand for antibacterial agents and enzyme inhibitors prompted us to synthesize some new compounds, 6a-6k, bearing multifunctional moieties. The target acetamides were derived from 4-phenyl-5-(1-tosylpiperidin-4-yl)-4$H$-1,2,4-triazole-3-thiol (3). The structural analysis was carried out using modern spectroscopic techniques including IR, NMR, and EIMS spectral analysis. The antibacterial activity was screened against five bacterial strains including three gram-negative and two gram-positive ones. Enzyme inhibition was carried out against lipoxygenase enzyme and results were supported by in silico study. The synthesized compounds were proved to be potent antibacterial agents and enzyme inhibitors.
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 …
The Synthesis Of New 3,4-(Bisaryl)-1,8-Naphthalimide And 2,3-(Bisaryl)-7$H$-Benzimidazo[2,1-A]Benzo[D]Isoquinolin-7-One Compounds And An Investigation Of Their Photochromic Properties, Ersi̇n Orhan, Mahmut Köse, Tolga Yazan
The Synthesis Of New 3,4-(Bisaryl)-1,8-Naphthalimide And 2,3-(Bisaryl)-7$H$-Benzimidazo[2,1-A]Benzo[D]Isoquinolin-7-One Compounds And An Investigation Of Their Photochromic Properties, Ersi̇n Orhan, Mahmut Köse, Tolga Yazan
Turkish Journal of Chemistry
Three new photochromic compounds, 3-(2,5-dimethyl-3-thienyl)-4-(2-phenyl-5-methyl-4-thiazolyl)-1,8-napht- halimide (1-O), 2,3-bis(2-phenyl-5-methyl-4-thiazolyl)-7$H$-benzimidazo[2,1-a]benzo[de]isoquinolin-7-one (2-O), and 2,5-dimethyl-3-thienyl)-7$H$-benzimidazo[2,1-a]benzo[de]isoquinolin-7-one (3-O), were synthesized and their photochromic properties were studied. Compound 1-O was synthesized by two consecutive Suzuki coupling reactions using 2,5-dimethylthiophene-3-boronic acid and 5-methyl-2-phenylthiazole-4-boronic acid. Photochromic compounds 2-O and 3-O were prepared by multistep reactions starting with 3-iodo-4-bromo-1,8-naphthalic anhydride and 2,5-dimethylthiophene-3-boronic acid or 2-phenyl-5-methylthiazole-4-boronic acid. All photochromic compounds showed a color change from colorless (or light yellow) to blue-green, purple, or orange colors (depending on the nature of the structures) on exposure to UV light at 365 nm in ethyl acetate solutions. The colored solutions can be reversed to …
Investigation Of The Hydrogen Bond Donating Ability Of 1,8-Naphthalenediol By Nmr Spectroscopy And Its Use As A Hydrogen Bonding Catalyst, Yunus Emre Türkmen
Investigation Of The Hydrogen Bond Donating Ability Of 1,8-Naphthalenediol By Nmr Spectroscopy And Its Use As A Hydrogen Bonding Catalyst, Yunus Emre Türkmen
Turkish Journal of Chemistry
The hydrogen bond donating ability of 1,8-naphthalenediol was investigated via a series of $^{1}$H, $^{13}$C, and $^{31}$P NMR experiments. Complexation studies using triphenylphosphine oxide and cyclohexanone as hydrogen bond acceptors revealed that 1,8-naphthalenediol is a more effective hydrogen bond donor compared to 1-naphthol and 8-methoxy-1-naphthol. Afterwards, its effectiveness as a hydrogen bonding catalyst was demonstrated in the Friedel-Crafts-type addition reaction of indole to trans-$\beta $-nitrostyrene.
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 …
Synthesis Of Acetamide Derivatives Of 1,2,4-Triazole Bearing Azinane And Their Binding Interactions With Bovine Serum Albumin Using Spectroscopic Techniques, Javed Iqbal, Aziz Ur Rehman, Muhammad Athar Abbasi, Sabahat Zahra Siddiqui, Hira Khalid, Sabina Jhaumeer Laulloo, Nausheen Joondan, Aniisah Banu Taupass, Shahid Rasool, Syed Adnan Ali Shah
Synthesis Of Acetamide Derivatives Of 1,2,4-Triazole Bearing Azinane And Their Binding Interactions With Bovine Serum Albumin Using Spectroscopic Techniques, Javed Iqbal, Aziz Ur Rehman, Muhammad Athar Abbasi, Sabahat Zahra Siddiqui, Hira Khalid, Sabina Jhaumeer Laulloo, Nausheen Joondan, Aniisah Banu Taupass, Shahid Rasool, Syed Adnan Ali Shah
Turkish Journal of Chemistry
A new series of acetamide derivatives containing 1,2,4-triazole and azinane moieties has been synthesized and characterized using $^{1}$H NMR, $^{13}$C NMR, IR, and EI-MS spectroscopic analysis. The intermediate triazole was synthesized through a sequential synthesis of carboxylate and carbohydrazide. The bovine serum albumin (BSA) binding of the newly synthesized 1,2,4-triazole derivatives was evaluated along with thermodynamics, site-selective binding, and synchronous study. The results obtained by BSA binding as well as thermodynamic studies justify that all the compounds show spontaneous interaction with BSA and could be effectively distributed and eliminated from the body. Therefore, the triazole-based analogs might be a useful …
Synthesis And Antimicrobial And Antioxidant Activities Of Hybrid Molecules Containing Benzotriazole And 1,2,4-Triazole, Mahesh Chand, Reena Kaushik, Subhash Chand Jain
Synthesis And Antimicrobial And Antioxidant Activities Of Hybrid Molecules Containing Benzotriazole And 1,2,4-Triazole, Mahesh Chand, Reena Kaushik, Subhash Chand Jain
Turkish Journal of Chemistry
Eleven novel 1,2,4-triazolylbenzotriazoles have been prepared using 1-(hydrazinylcarbonylmethyl)-1$H$-benzot- riazole (3) as a potent intermediate. Compound 3, however, was obtained from benzotriazole in two steps. All synthesized compounds were characterized by detailed spectral studies like IR, $^{1}$H NMR, $^{13}$C NMR, and mass spectrometry. All synthesized compounds were evaluated for their \textit{in vitro} antimicrobial activity against seven strains of bacteria and four strains of fungi. Compounds 13, 17, 19, 20, and 21}were found to possess antibacterial activity comparable to that of ciprofloxacin against a Klebsiella pneumoniae strain. Except for compounds2 and 13, all compounds showed good antifungal activity against an Aspergillus niger …
$S$-Substituted Derivatives Of 1,2,4-Triazol-3-Thiol As New Drug Candidates For Type Ii Diabetes, Aziz Ur Rehman, Khadija Nafeesa, Muhammad Athar Abbasi, Sabahat Zahra Saddiqui, Shahid Rasool, Syed Adnan Ali Shah, Muhammad Ashraf, Muhammad Arif Lodhi, Farman Ali Khan, Bakht Jahan
$S$-Substituted Derivatives Of 1,2,4-Triazol-3-Thiol As New Drug Candidates For Type Ii Diabetes, Aziz Ur Rehman, Khadija Nafeesa, Muhammad Athar Abbasi, Sabahat Zahra Saddiqui, Shahid Rasool, Syed Adnan Ali Shah, Muhammad Ashraf, Muhammad Arif Lodhi, Farman Ali Khan, Bakht Jahan
Turkish Journal of Chemistry
The therapeutic applications of 1,2,4-triazoles motivated us to synthesize some new derivatives. Two series of $S$-substituted derivatives (8a-8j, 12a-12i) of 5-$\{$1-[(4-chlorophenyl)sulfonyl]-3-piperidinyl$\}$-4-phenyl-4$H$-1,2,4-triazol-3-thiol (6) have been synthesized and evaluated for their biological potential. Using 4-chlorobenzene sulfonyl chloride (1) and ethyl piperidine-3-carboxylate (2), ethyl 1-[(4-chlorophenyl)sulfonyl]piperidine-3-carboxylate (3) was synthesized and converted into 3,4,5-trisubstituted 1,2,4-triazole (6) through formation of the corresponding carbohydrazide (4) and hydrazinecarbothioamide (5). Compound 6 was transformed into 8a-8j by alkyl halides (7a-7j) and into 12a-12i by $N$-aralkyl/aryl-2-bromoacetamides (11a-11i) in an aprotic solvent. The electrophiles, 11a-11i, were synthesized by gearing up $N$-substituted aralkyl/aryl amines (10a-10i) with 2-bromoacetyl bromide (9) under dynamic pH …
Efficient Multicomponent Synthesis Of 1,2,3-Triazoles Catalyzed By Cu(Ii) Supported On Pei@Fe$_{3}$O$_{4}$ Mnps In A Water/Peg$_{300}$ System, Zeinab Hassanpour, Aziz Maleki, Morteza Hosseini, Lena Gorgannezhad, Vajihe Nejadshafiee, Ali Ramazani, Ismaeil Haririan, Abbas Shafiee, Mehdi Khoobi
Efficient Multicomponent Synthesis Of 1,2,3-Triazoles Catalyzed By Cu(Ii) Supported On Pei@Fe$_{3}$O$_{4}$ Mnps In A Water/Peg$_{300}$ System, Zeinab Hassanpour, Aziz Maleki, Morteza Hosseini, Lena Gorgannezhad, Vajihe Nejadshafiee, Ali Ramazani, Ismaeil Haririan, Abbas Shafiee, Mehdi Khoobi
Turkish Journal of Chemistry
A highly dispersible and magnetically recoverable Cu-PEI@Fe$_{3}$O$_{4}$ MNPs catalyst was prepared and successfully applied in one-pot three-component coupling of terminal alkynes, sodium azide, and alkyl bromides/chlorides in water to give 1,4-disubstituted 1,2,3-triazoles with good to excellent yields. The catalyst was fully characterized with FT-IR, TGA, TEM, SEM, VSM, EDX, cyclic voltammetry, and ICP-AES spectroscopic techniques. Furthermore, the catalyst was easily recycled by an external magnet and successfully reused six times in the reaction without significant loss of its catalytic activity and copper leaching. The large-scale reaction was also carried out in the absence of any base and reducing agent even …
Synthesis And In Vitro Anticancer Evaluation Of 1,4-Phenylene-Bis-Pyrimidine-2-Amine Derivatives, Meli̇ha Burcu Gürdere, Erdoğan Kamo, Ayşe Şahi̇n Yağlioğlu, Yakup Budak, Mustafa Ceylan
Synthesis And In Vitro Anticancer Evaluation Of 1,4-Phenylene-Bis-Pyrimidine-2-Amine Derivatives, Meli̇ha Burcu Gürdere, Erdoğan Kamo, Ayşe Şahi̇n Yağlioğlu, Yakup Budak, Mustafa Ceylan
Turkish Journal of Chemistry
A series of 1,4-phenylene-bis-chalcones 3a-3h were synthesized by the reaction of terephthalaldehyde with substituted arylketones in this study. The novel 1,4-phenylene-bis-pyrimidine-2-amine derivatives 5a-5h were obtained by the addition of guanidine hydrochloride to 1,4-phenylene-bis-chalcone 3a-3h in ethanolic KOH under reflux conditions. The structure of the compounds was explained by means of IR, $^{1}$H NMR, $^{13}$C NMR, and elemental analyses. The anticancer activities of 3a-3h and 5a-5h were investigated against rat brain tumor cells and human uterus carcinoma in vitro$.$ Activity tests were performed as dose-dependent assays at eight concentrations. The positive control was 5-fluorouracil (5-FU). Compounds 3c and 3d were examined …
A Rapid, Eco-Friendly, And Reliable Microplate Method For Determination Of Cr(Vi), Alejandro Coreño Alonso, Gustavo Cruz Jimenez, Leticia Lopez Martinez, Georgina Elena Reyna Lopez, Francisco Javier Acevedo Aguilar
A Rapid, Eco-Friendly, And Reliable Microplate Method For Determination Of Cr(Vi), Alejandro Coreño Alonso, Gustavo Cruz Jimenez, Leticia Lopez Martinez, Georgina Elena Reyna Lopez, Francisco Javier Acevedo Aguilar
Turkish Journal of Chemistry
In the present work, the reaction of Cr(VI) with 1,5-diphenylcarbazide in microplates (enzyme-linked immunosorbent assay microtiter plate) and a subsequent determination in a plate reader at 540 nm were performed. The final volume utilized for each determination was 200 $\mu $L, and the cost and waste were reduced for hexavalent chromium [Cr(VI)] quantification. The use of microplates allowed for the analysis of a large number of samples, reducing analysis time. No statistically significant differences were observed between the results obtained in the analysis of Cr(VI) in real samples by the conventional procedure and by the proposed methodology in this work …
Nanocomposite Copper Metal As An Efficient Heterogeneous Catalyst In Click Synthesis Of 1,2,3-Triazoles In Aqueous Media, Vajihe Nejadshafiee, Hossein Naeimi
Nanocomposite Copper Metal As An Efficient Heterogeneous Catalyst In Click Synthesis Of 1,2,3-Triazoles In Aqueous Media, Vajihe Nejadshafiee, Hossein Naeimi
Turkish Journal of Chemistry
Copper/periodic mesoporous organosilica (Cu/PMO) nanocomposites provided a highly active, reusable, globular, solid-phase catalyst for click chemistry. The reaction proceeds by mixing organohalides, sodium azide, alkyne, and the catalyst in an aqueous medium to afford the desired products. The cost efficiency and recyclability of the catalyst up to six runs without appreciable loss of activity and high yields of products make this procedure greener.
Synthesis And Evaluation Of Some Novel Thiazoles And 1,3-Thiazines As Potent Agents Against The Rabies Virus, Magda Abdalla, Sobhi Gomha, Mohamad Abd Elaziz, Nany Serag
Synthesis And Evaluation Of Some Novel Thiazoles And 1,3-Thiazines As Potent Agents Against The Rabies Virus, Magda Abdalla, Sobhi Gomha, Mohamad Abd Elaziz, Nany Serag
Turkish Journal of Chemistry
A series of novel thiazoles and 1,3-thiazine derivatives were synthesized in good yield via reaction of ethyl 3-(1-(2-thiocarbamoylhydrazono)ethyl)-1,5-diphenyl-1$H$-pyrazole-4-carboxylate with hydrazonoyl halides and arylidenemalononitriles, respectively. The structure of the newly synthesized products was elucidated via elemental analysis, spectral data, and alternative routes whenever possible. Moreover, the antiviral screening of the products was evaluated and the results revealed that some of them have strong to moderate potency against the rabies virus compared with the reference drug.
Isoquinoline-Substituted Triazole And Pyran Derivatives: Synthesis And Computational Studies, Duygu Yeni̇dede, Selçuk Gümüş, Ayşegül Gümüş
Isoquinoline-Substituted Triazole And Pyran Derivatives: Synthesis And Computational Studies, Duygu Yeni̇dede, Selçuk Gümüş, Ayşegül Gümüş
Turkish Journal of Chemistry
The one-pot synthesis of novel 1,4-disubstituted 1,2,3-triazoles from isoquinoline-substituted homopropargyl alcohol backbone is described (42%-88% yields). A ring closing metathesis reaction and an intramolecular Pauson-Khand reaction of enyne system derived from a homopropargyl alcohol backbone to afford the corresponding isoquinoline-substituted dihydropyran and cyclopentenone-pyran, respectively, are also described (54% and 78% yields). Information about the structural, electronic, and physico-chemical properties of the novel compounds, obtained by density functional theory application, is also reported.
Synthesis Of 5-Aryl-$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.
Microwave-Assisted Synthesis Of Condensed 1,4-Dihydropyridines As Potential Calcium Channel Modulators, Erdem Kami̇l Özer, Mi̇yase Gözde Gündüz, Ahmed El-Khouly, Mehmet Yildirim Sara, Rahi̇me Şi̇mşek, Alper Bektaş İski̇t, Osman Ci̇hat Şafak
Microwave-Assisted Synthesis Of Condensed 1,4-Dihydropyridines As Potential Calcium Channel Modulators, Erdem Kami̇l Özer, Mi̇yase Gözde Gündüz, Ahmed El-Khouly, Mehmet Yildirim Sara, Rahi̇me Şi̇mşek, Alper Bektaş İski̇t, Osman Ci̇hat Şafak
Turkish Journal of Chemistry
This study reports the design, synthesis, and calcium channel modulatory activity evaluation of a series of 14 novel fused 1,4-dihydropyridine derivatives. The molecular design of the compounds was based on modifications of nifedipine, which is a calcium channel blocker. The compounds were achieved by one-pot microwave-assisted reaction of 4,4-dimethyl-1,3-cyclohexanedione, 5-chlorosalicylaldehyde/3,5-dichlorosalicylaldehyde, an appropriate alkyl acetoacetate, and ammonium acetate in ethanol according to a modified Hantzsch reaction. The structures of the compounds were confirmed by spectral methods and elemental analysis. To evaluate their relaxant activities, the maximum relaxant response (E$_{\max})$ and pD$_{2}$ values of the compounds and nifedipine were determined on isolated …