Article history: Received on: 07/02/2017 Accepted on: 21/03/2017 Available online: 30/07/2017 The current therapy of epilepsy is associated with a number of side effects including sedation and hypnosis. Newer improved molecules are needed with lesser side effects and with improved physical properties. In view of these facts, a series of novel 4, 5-disubstituted-1,2,4-triazoles (6a-o) were synth...

A series of heterocyclic compounds bearing the well-known free radical scavenging 3,4,5-trimethoxybenzyloxy group, was synthesized. The key compound 4-(3,4,5-trimethoxybenzyl-oxy)benzohydrazide was converted into thiosemicarbazide derivatives, which were subsequently cyclized with NaOH to provide 1,2,4-triazole derivatives. Alternative treatment of the acid hydrazide with carbon disulfide in th...

The chiral-discriminating abilities of new triazole-linked host compounds (6, 7) toward amino acid esters were evaluated by the FABMS/EL-guest method. Two types of host appending saccharide derivatives were synthesized by the copper-catalyzed Huisgen-1,3-dipolar cycloaddition (CuAAC). Host compounds binding constants and chiral-discriminating abilities toward the enantiomeric alanine esters wer...

A number of 1,4-dihydropyridine derivatives (9a?d, 10a?d and 11a?d) were designed synthesized by the reaction 1,3,4-oxadiazole-5-thiones 1,2,4-triazole-5-thiones to 2,6-dibromomethyl-3,5-diethoxycarbonyl-4-(3- -nitrophenyl)-1,4-dihydropyridine. The compounds characterized using FT-IR, 1H-NMR, 13C-NMR spectral data, ESI-MS elemental analysis. cytotoxicity was evaluated in human breast cancer (MC...

In the present study, a new series of 2,5-disubstituted-1,3,4-thiadiazole tethered 1,2,4-triazole, 1,3,4-thiadiazole, 1,3,4-oxadiazole and Schiff base derivatives were synthesized and characterized by IR, ¹H-NMR, (13)C-NMR, MS and elemental analyses. All compounds were screened for their antibacterial, antifungal and antiproliferative activity. Some of the synthesized derivatives have displayed...

There are some reports which indicate that several triazole derivatives have inotropic activity; however, the cellular site and mechanism of action at cardiovascular level is very confusing. In order, to have a clear understanding of these phenomena, a triazole derivative was synthesized to evaluate its biological activity on left ventricular pressure and characterize the molecular mechanism. T...

Sixteen 1,4-diaryl-1,2,3-triazole compounds 4-19 derived from the tetrahydrofuran neolignans veraguensin 1, grandisin 2, and machilin G 3 were tested against Leishmania (Leishmania) amazonensis intracellular amastigotes. Triazole compounds 4-19 were synthetized via Click Chemistry strategy by 1,3-dipolar cycloaddition between terminal acetylenes and aryl azides containing methoxy and methylened...

Indirubin derivatives and analogs comprise a significant group of ATP-competitive inhibitors. The inhibitory effects of ChEMBL474807 (1-(4-amino-1,2,5-oxadiazol-3-yl)-5-(piperidin-1-ylmethyl)-N'-(pyridin-4-ylmethylene)-1H-1,2,3-triazole-4-carbohydrazide) on two enzymes, namely glycogen synthase kinase-3β (GSK-3β) and cyclin-dependent kinase-2 (CDK-2), were analyzed. The close resemblance of the...