Chemistry Commons^™

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 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.

Synthesis And Characterization Of Five New Tetrakis(N-Phenylacetamidato) Dirhodium(Ii) Amine Complexes And One Molybdenum Cofactor Described Crystallographically, Cragin K. Harris

Electronic Theses and Dissertations

Six new crystal structures were determined using a Rigaku Mercurcy 375/MCCD(XtaLab mini) diffractometer. The structure of a molybdenum cofactor was solved resulting in an R1 (R1 = Σ ||Fo| - |Fc|| / Σ |Fo|) of 3.61% despite the presence of a disordered DMSO molecule. New Tetrakis(N-phenylacetamidato) Dirhodium(II) complexes were synthesized and characterized. Two 2,2-cis-[Rh2(NPhCOCH3)4]•(C3H4N2)x where x= 1 or 2 were successfully crystallized and solved with R1 values below 5%. Additional studies were conducted via NMR to observe formation of both products. Three potential catalysts were synthesized starting with 3,1-[Rh₂(NPhCOCH₃)₄]. The resulting compounds were a …

New Methods For Synthesis Of Organic Peroxides And Application Of Peroxide Electrophiles To Synthesis Of Functionalized Ethers, Shiva Kumar Kyasa

Department of Chemistry: Dissertations, Theses, and Student Research

New Method for Synthesis of Alkyl Hydroperoxides: There are a number of methods reported for synthesis of alkyl hydroperoxides, but most of them suffer either from poor yields or the formation of unwanted side products. I will be discussing new methodology for efficient synthesis of pure samples of 1° and 2° alkyl hydroperoxides via alkylation of readily available cyclododecanone 1,1-dihydroperoxide followed by hydrolysis of the resulting bis peroxyacetals.

Peroxide Electrophiles for Synthesis of Functionalized Ethers: Peroxides are underexplored functional groups as precursors for C-O bond formation and ether synthesis. The reactivity of dialkyl peroxides towards organometallics such as alkyl lithium …

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 …

Microwave-Assisted Regioselective [1,3]-Dipolar Cycloaddition Of 3-Methyl-2-(Substitutedbenzylidene)-5-Oxopyrazolidin-2-Ium-1-Ides To Benzothiophene 1,1-Dioxide, Yaşar Dürüst, Eda Sağirli, Akin Sağirli

Turkish Journal of Chemistry

A series of pyrazolidinium ylides was reacted with benzothiophene 1,1-dioxide to afford (3R,5S,5aS,10bS)-3-methyl-5-substitutedphenyl-2,3,5,5a-tetrahydrobenzo[4,5]thieno[3,2-c]pyrazolo[1,2-a]pyrazol-1(10bH)-one 6,6-dioxides under microwave irradiation and their structures were identified by means of spectral/physical characteristics including X-ray diffraction data and HRMS measurements.

Microwave-Assisted Synthesis Of Novel 8-Chloro-[1,2,4]Triazolo[4,3-$A$]Pyridine Derivatives, Linjiong Zhang, Mingyan Yang, Beizhen Hu, Zhaohui Sun, Xinghai Liu, Jianquan Weng, Chengxia Tan

Turkish Journal of Chemistry

A series of novel 1,2,4-triazolo[4,3-$a$]pyridine derivatives were synthesized from 2,3-dichloropyridine and hydrazine hydrate as starting materials by multistep reactions under microwave assistance, and their structures were characterized by $^{1}$H NMR, MS, and elemental analysis. This method provides several advantages such as high yields, facile work-up, and environmental friendliness.

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 …

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.

Physicochemical Characterization Of Novel 1,1 0-Phenanthrolines, Dominic Millheim

Masters Theses

1,10-Phenanthroline is a well-known and often-used ligand with a variety of interesting properties and applications to both organic and inorganic chemistry. Interest in novel 1,10-phenanthrolines substituted at the 5- and 6- position has grown recently due to their interesting fluorometric and spectroscopic properties. They have been evaluated recently for applications including chemical sensors, chemical indicators, pharmacological targets and bioactive reagents.

1,10-Phenanthroline, an epoxidated synthetic intermediate, and a novel 5,6- disubstituted aminoalcohol derivative were studied to determine the degree of influence that iterative physical and chemical transformations have on the donor properties of the N-C-C-N pocket. Multiple analytical techniques including potentiometry …

Electrochemistry Of Glucose Oxidase Modified On Porin-Phospholipid Biomimic Membrane, Kun-Qi Wang, Zuo-Ming Zhang, Wei Xing, Chang-Peng Liu, Xing Zhou

Journal of Electrochemistry

Biomimic membrane with nano-channels, which is made up of porin MspA and 1,2-Dimyristoyl-sn-glycero-3-phosphocholine (DMPC) is constructed on glassy carbon substrate, and glucose oxidase (GOD) is modified on it. The direct electrochemical reaction and electrocatalytic behavior to oxygen and glucose of GOD on the GOD/MspA-DMPC/GC electreode are expounded by the cyclic voltammetric method. The study shows that GOD immobilized on porin MspA and DMPC biomimic membrane displays direct and surface-controlled electrochemical reaction nearby formal potential (E0′) of the flavoprotein active centre (FAD/FADH), and the electrochemical reaction contains two electrons and two protons exchange in 0.1 mmol·L^-1 phosphate buffer solution (PBS) …

Crystal Structure Of 4,5-Bis-(3,4,5-Trimethoxyphenyl)-2H-1,2,3-Triazole Methanol Monosolvate, Nikhil Reddy Madadi, Narsimha Reddy Penthala, Shobanbabu Bommagani, Sean Parkin, Peter A. Crooks

Chemistry Faculty Publications

The title compound, C₂₀H₂₃N₃O₆·CH₃OH, was synthesized by [3 + 2] cyclo­addition of (Z)-2,3-bis­(3,4,5-tri­meth­oxy­phen­yl)acrylo­nitrile with sodium azide and ammonium chloride in DMF/water. The central nitro­gen of the triazole ring is protonated. The dihedral angles between the triazole ring and the 3,4,5-tri­meth­oxy­phenyl ring planes are 34.31 (4) and 45.03 (5)°, while that between the 3,4,5-tri­meth­oxy­phenyl rings is 51.87 (5)°. In the crystal, the mol­ecules, along with two methanol solvent mol­ecules are linked into an R ⁴ ₄(10) centrosymmetric dimer by N—H⋯O and O—H⋯N hydrogen bonds.

Inhibition Of The Thioesterase Activity Of Human Fatty Acid Synthase By 1,4- And 9,10-Diones, Herman H. Odens

Faculty Works

Fatty acid synthase (FASN) is the enzyme that synthesizes fatty acids de novo in human cells. Although FASN is generally expressed at low levels in most normal tissues, its expression is highly upregulated in many cancers. Consistent with this notion, inhibition of FASN activity has demonstrated potential to halt proliferation and induce cell death in vitro and to block tumor growth in vivo. Consequently, FASN is widely recognized as a valuable therapeutic target. In this report, we describe a variety of 1,4-quinones and 9,10- anthraquinones, including several natural compounds and some newly synthesized compounds, that potently inhibit the thioesterase (TE) …

Studies On The Synthesis Of Orthogonally Protected Azalanthionines, And Of Routes Towards B-Methyl Azalanthionines, By Ring-Opening Of N-Activated Aziridine-2-Crboxylates, Keith O'Brien, Keith Ó Proinsias, Fintan Kelleher

Articles

Orthogonally protected azalanthionines were successfully synthesised by the ring-opening of N-activated aziridine-2-carboxylates with protected diaminopropanoic acids (DAPs). The required DAPs were also prepared by ring-opening of N-activated aziridine-2-carboxylates with para-methoxybenzylamine, but it was found that the choice of aziridine protecting groups dictated both the success of the reaction as well as the regioselectivity of the isolated products. Attempts to extend the methodology to the preparation of the more sterically demanding b-methyl azalanthionines have, so far, been unsuccessful.

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 Phase Transition Studies Of New Dimer Compounds Connected To A 1,3-Dimethylbarbituric Acid Core, Abdulkarim-Talaq Mohammad, Guan-Yeow Yeap, Hasnah Osman

Turkish Journal of Chemistry

A series of dimeric unsymmetrical liquid crystals derived from heterocyclic 1,3-dimethylbarbituric acid exhibiting smectic A and nematic phase are reported. All compounds were prepared by the condensation of 4'-(R-(4-formylphenoxy)butoxy)biphenyl-4-carboxylate with 1,3-dimethylbarbituric acid in ethanol. The mesomorphic properties were investigated by DSC and POM, where the type of phase depends on the length of spacer alkoxy chains and the length of the terminal chain. While the SmA phase was observed upon the heating and cooling run when the spacer alkoxy chains carbon numbers increased (n = 6), the N phase was observed when the length of spacer alkoxy chains increased (n …

Te(Ii)-Induced Heterocyclization Of 1,2-Alkadienephosphonates, Dobromir Dimitrov Enchev

Turkish Journal of Chemistry

The reactivity of some 1,2-alkadienephosphonates towards phenyltelluryl halides was investigated. A plausible mechanism of the reaction is discussed.

Synthesis Of Novel Triazoles Bearing 1,2,4-Oxadiazole And Phenylsulfonyl Groups By 1,3-Dipolar Cycloaddition Of Some Organic Azides And Their Biological Activities, Yaşar Dürüst, Hamza Karakuş, Muhsi̇ne Zeynep Yavuz, Ali̇ Akçahan Gepdi̇remen

Turkish Journal of Chemistry

1,3-Dipolar cycloaddition of 5-azidomethyl-3-p-substituted phenyl-1,2,4-oxadiazoles to phenyl vinyl sulfone and bismaleimide gives rise straightforwardly to 1-((3-(p-substituted) phenyl-1,2,4-oxadiazol-5-yl)methyl)-4-(phenylsul\-fonyl)-4,5-dihydro-1H-1,2,3-triazoles and bisdihydropyrrolo[3,4-d][1,2,3]triazole-4,6(3aH,5H)-diones. The structures of the new cycloadducts were elucidated by means of IR, NMR (^1H, ^{13}C, 2D), mass spectra, and physical characteristics (mp and R_f values). In addition, anticancer activities of the cycloadducts against MCF-7 cells were also investigated.

Spectrophotometric Determination Of Molybdenum Using Surfactant-Mediated Liquid--Liquid Extraction, Rameshwar Dass, Jitander Kumar Kapoor, Sunita Gambhir

Turkish Journal of Chemistry

A new spectrophotometric method has been developed for determination of molybdenum using surfactant-mediated liquid--liquid extraction. Molybdenum(V) obtained by ascorbic acid reduction in 2.5 M H_2SO_4 reacted spontaneously with thiocyanate and cetyl trimethyl ammonium bromide (CTAB), forming an intense orange yellow complex that was extracted quantitatively into 1,2-dichloroethane and absorbed at 460 nm. The absorbance of the extract was found to be stable for more than 24 h. Beer's law was obeyed over the concentration range 0.1--4.2 \mu g Mo mL^{-1} of the extract. The linear range for an accurate determination was found to be 1.2--2.6 \mu g Mo mL^{-1}. The …

Synthesis And Characterization Of A Novel 3-Amino-1,2,4-Triazole Lead(Ii) Coordination Polymer, Şebnem Esen Sözerli̇, Arzu Özen, İbrahi̇m Kani̇, Deni̇z Demi̇r

Turkish Journal of Chemistry

A novel [Pb_2(\mu-atrz)_2(\mu-CH_3COO)(CH_3COO)]_n (atrz = 3-amino-1,2,4-triazole) complex was synthesized and characterized by IR spectroscopy, thermogravimetric analysis, and single crystal X-ray diffraction. The molecular structure shows that the complex is a coordination polymer in which there are 2 different lead(II) ions with coordination number of 5, Pb(2), and, with a coordination number of 4, Pb(1). Each atrz acts as a bridging ligand between 2 Pb(II) ions through the 2 adjacent nitrogen atoms of the triazole ring. The acetate anions show different types of coordination mode: one acts as a bridge by coordination of the same oxygen atom with Pb(II) ions and …

Convenient Synthesis Of 1,3-Dithiolane-2-Thiones: Cyclic Trithiocarbonates As Conformational Locks, Irina A. Dotsenko, Qinliang Zhao, Andreas H. Franz, Patrick Batoon, Nataliya M. Samoshina, Vyacheslav V. Samoshin

College of the Pacific Faculty Articles

A series of novel 1,3-dithiolane-2-thiones, or cyclic trithiocarbonates, has been prepared by a new simple procedure: a treatment of the corresponding epoxides with the commercially available potassium ethyl xanthogenate, KSC(S)OEt. The stereochemistry of the products was determined by 1 H NMR and in some cases by single-crystal X-ray data. Cyclohexane-based 1,3- dithiolane-2-thiones revealed a trans-fusion of the carbo- and hetero-cycles. The products obtained from the mono-substituted cyclohexene oxides demonstrated an axial position of the substituents. Thus the epoxide transformation into trithiocarbonate can be used as a method for locking cyclic compounds in unstable conformations.

Synthesis Of Orthogonally Protected 1,2-Diaminopropanoic Acids By Ring-Opening Of 3-Unsubstituted N-Activated Aziridine 2-Carboxylates With Para-Methoxybenzylamine: A Study Of The Regioselectivity Of The Reaction, Fintan Kelleher, Keith O'Brien

Articles

Orthogonally protected 1,2-diaminopropanoic acids (DAPs) have been synthesised in good yields by the ring-opening of 3-unsubstituted N-activated aziridine 2-carboxylates with para-methoxybenzylamine. The choice of both the N-activating group and ester alkyl group had a significant influence on the ratio of attack at the a or b positions of the aziridine. However, the regiochemical outcome is not predictable.

New Synthetic Strategy For Novel 6-Arylazo-5-Methyl-3-Aryl-Thiazolo[2,3-C]- [1,2,4]Triazoles And Study Of Their Solvatochromic Properties, Ahmad Sami Shawali, Mohie Eldin Moustafa Zayed

Turkish Journal of Chemistry

Two series of 6-arylazothiazol[2,3-c][1,2,4]triazoles were prepared via oxidative cyclization of the respective aldehyde N-(5-arylazo-4-methylthiazol-2-yl)-hydrazones. The structures of the latter hydrazone precursors and the azo compounds were confirmed by spectral and elemental analyses. The solvatochromism of the title azo dyes is evaluated by means of the Kamlet--Taft equation and discussed.

Synthesis Of Fused Tetrazolone Derivatives, Sevi̇l Özcan, Zeynep Ekmekçi̇, Berk Müjde, Meti̇n Balci

Turkish Journal of Chemistry

New fused tetrazolone derivatives were synthesized using homophthalic and maleic anhydrides. Treatment of anhydrides with trimethylsilyl azide opened the lactone rings and formed the corresponding intermediates, which bore 1,3-dipole and dipolarophile functionalities in ortho positions. The intermediates partially underwent internal 1,3-dipolar cycloaddition to produce fused tetrazolone derivatives. When the carbonyl groups in anhydride were not conjugated with any double bond, then a triazine-fused tetrazolone derivative was formed.

Synthesis, Characterization, And Luminescence Of Zinc(Ii) And Cadmium(Ii) Coordination Complexes: [Zn(Phen)_2(Ch_3coo)](Clo_4), [Zn(Bpy)_2(Clo_4)](Clo_4), And [Cd(Phen)_2(No_3)_2], İbrahi̇m Kani̇, Mehmet Kurtça

Turkish Journal of Chemistry

Three metal complexes, [Zn(phen)_2(CH_3COO)](ClO_4) (1), [Zn(bpy)_2(ClO_4)](ClO_4) (2), and [Cd(phen)_2 (NO_3)_2] (3) (phen = 1,10-phenanthroline, bpy = 2,2 {Abedini, 2005 #222} -bipyridine), were synthesized and their structures were determined by single-crystal X-ray diffraction analyses. In 1, Zn(II) is coordinated by 4 nitrogen atoms from 2 phen molecules and 2 oxygen atoms from 1 acetato to form an octahedral configuration. In 2, Zn(II) has pentacoordination geometry with chelating 2 bpy and 1 perchlorato ion. In 3, phen and NO_3^- serve as bidentate ligands coordinating to Cd(II) through their nitrogen and oxygen atoms to form 8 coordination. Three-dimensional frameworks of complexes 1--3 are …

Synthesis And Biological Activities Of Methylenebis-4h-1,2,4-Triazole Derivatives, Yildiz Uygun, Hacer Bayrak, Havva Özkan

Turkish Journal of Chemistry

5,5'-Methylenebis(4--phenyl-4H-1,2,4-triazole-3-thiol) (2) was synthesized starting from hydrazinecarbothioamide compound (1). Treatment of compound 2 with ethyl bromoacetate produced diethyl 5,5'-{methylenebis[(4-phenyl-4H-1,2,4-triazole-5,3-diyl)thio]}diacetate (3), which was converted to the corresponding diacetohydrazide derivative (4) by treatment with hydrazine hydrate. The reaction of compound 4 with several aldehydes produced the corresponding arylidene hydrazides, 5a--d. Syntheses of Mannich bases 6a--c were carried out by the treatment of compound 2 with several amines in the presence of formaldehyde. (4{[5-({5-[(4-Amino-2-chlorophenyl)thio]-4-phenyl-4H-1,2,4-triazol-3-ylmethyl)-4-phenyl-4H-1,2,4-triazol-3-yl]thio}-3-chlorophenyl)amine (8) was prepared by reduction of 2 nitro groups of 3,3' -methylenebis{5-[(2-chloro-4-nitrophenyl)thio]-4-phenyl-4H-1,2,4-triazole} (7) that were obtained from the condensation of 2} with 3,4-dichloronitrobenzene. The newly synthesized compounds were screened …

Comparison Of Chemical Nano Structure, Rheological And Mechanical Properties Of Long Oil Alkyd Resin Synthesized Using Polybasic Acids Catalyst, Ar Ilkhani

Tanzania Journal of Science

In this research, chemical nano structures, rheological and mechanical properties of long oil alkyd resin which was synthesized using different polybasic acid catalysts have been studied. These catalyst were phosphoric acid, 1,2,4-benzene tricarboxylic acid and succinic acid. The new compounds were compared with reference formula of long oil alkyd resin. For this idea, same formula of clear air drying varnishes were prepared based on different long oil resins which have been synthesized using different catalysts and reference long oil alkyd resin. FTIR spectroscopy was employed to investigate the nano chemical structures of the resins and varnishes. The rheological properties of …

A Microwave-Assisted Bismuth Nitrate-Catalyzed Unique Route Toward 1,4-Dihydropyridines, Debasish Bandyopadhyay, Stephanie Maldonado, Bimal K. Banik

School of Integrative Biological & Chemical Sciences (Formerly Dept. of Chemistry)

The classical Hantzsch reaction is one of the simplest and most economical methods for the synthesis of biologically important and pharmacologically useful 1,4-dihydropyridine derivatives. Bismuth nitrate pentahydrate under microwave irradiation is proven to act as a very efficient catalyst for a one-pot, three-component synthesis of 1,4-dihydropyridines in excellent yields from diverse amines/ammonium acetate, aldehydes and 1,3-dicarbonyl compounds within 1-3 min under solvent-free conditions. The present environmentally benign procedure for the synthesis of 1,4-dihydropyridines is suitable for library synthesis and it will find application in the synthesis of potent biologically active molecules. The excellent yield and extreme rapidity of the method …

Design And Synthesis Of New 1,2,4-Triazole Derivatives Containing Morpholine Moiety As Antimicrobial Agents, Deni̇z Şahi̇n, Hacer Bayrak, Ahmet Demi̇rbaş, Nesli̇han Demi̇rbaş, Şengül Alpay Karaoğlu

Turkish Journal of Chemistry

2-Morpholine-4ylethyl-3H-1,2,4-triazole-3-ones (2a, 2b) were obtained from the condensation between the corresponding ethoxycarbonylhydrazones and 2-morpholinoethanamine. 2a was converted to acetohydrazide (4) via the formation of an ester derivative (3). Treatment of 2a and 2b with several aryl sulfonyl chlorides afforded the corresponding 2-arylsulfonyl-1,2,4-triazole-3-ones (5a-c and 6). The reaction of hydrazide (4) with benzyl iso- and benzyl isothiocyanate produced the corresponding carboxamide (8a) and carbothioamide (8b). The basic treatment of 8b yielded 5-mercapto-4H-1,2,4-triazol-3-yl)methyl]-2,4-dihydro-3H-1,2,4-triazol-3-one (10). The synthesis of 1,3-thiazol-2(3H)-ylidene-1,2,4-triazol-1- ylacetohydrazide (11) and 1,3-oxazole-2(3H)-ylidene-1,2,4-triazole- 1-yl)acetohydrazide (9) derivatives was performed from the reaction of 8a and 8b with substituted phenacyl bromides. All the newly synthesized …

Design, Synthesis, And Biological Evaluation Of Indole-Based 1,4-Disubstituted Piperazines As Cytotoxic Agents, Meri̇ç Köksal Akkoç, Mi̇ne Yarim Yüksel, İrem Durmaz, Rengül Çeti̇n Atalay

Turkish Journal of Chemistry

A series of 3-[(4-substitutedpiperazin-1-yl)methyl]-1H-indole derivatives were synthesized, and their structures were confirmed by spectral analysis. All the compounds were tested for their cytotoxic activity in vitro against 3 human tumor cell lines: human liver (HUH7), breast (MCF7), and colon (HCT116). Among the designed derivatives, most of the compounds showed significant cytotoxicity against liver and colon cancer cell lines with lower IC_{50} concentrations than the standard drug 5-fluorouracil. Compound 3s, with 3,4-dichlorophenyl substituent on the piperazine ring, was the most active in suppressing the growth of all screened cancer cells.