A reaction of equimolar equivalents 1-(4-methoxyphenyl)-5-methyl-1H-1,2,3-triazole-4-carbohydrazide (1) and indoline-2,3-dione (2) in boiling ethanol for 4 h under acidic conditions gave 1-(4-methoxyphenyl)-5-methyl-N’-(2-oxoindolin-3-ylidene)-1H-1,2,3-triazole-4-carbohydrazide (3) 88% yield. The structure 3 was ascertained by NMR spectroscopy single-crystal X-ray diffraction.

Phosphodiesterase 7 (PDE7), one of the members of PDE family has been reported as potential therapeutic target involved in inflammation. The present work was designed to synthesize and evaluate the anti-inflammatory activity of some newer substituted triazole derivatives as potential PDE7 inhibitors. A series of substituted triazole derivatives was synthesized and evaluated by in silico studies...

Post-translational modifications (PTMs) are used by organisms to control protein structure and function after translation, but their study is complicated roles not often well understood as PTMs difficult introduce onto proteins selectively. Designing reagents that both good mimics of PTMs, also only modify select amino acid residues in challenging. Frequently, a chemical warhead linker used, cr...

Thirty six novel heterocyclic derivatives of ethyl 2-(2-pyridylacetate) were efficiently synthesized. The new compounds involve the linkage of a 2-pyridyl ring with thiosemicarbazide (compounds 1-7), 1,2,4-triazole (compounds 1a-7a), 1,3,4-thiadiazole (compounds 1b-7b), and 1,3,4-oxadiazole (compounds 1f-7f) moieties. The last group of compounds 1e-7e involves the connection of a 2-pyridyl ring...

A number of 1,3,4-oxadiazole, 3-9, and 1,2,4-triazole derivatives, 13-15, were synthesized starting form the acid hydrazide 1. The 1,3,4-thiadiazole derivative 12 was prepared from the substituted phenylthiosemicarbazide derivative 11 by treatment with sulfuric acid. The aryl hydrazone derivatives 10a-c were synthesized by reaction of the hydrazide 1 with the corresponding ketones. The thioalky...

In the title coordination polymer, [CdCl(2)(C(8)H(8)N(4))(2)](n), the Cd(II) atom, lying on an inversion center, is coordinated by two Cl atoms and two triazole N atoms and two pyridyl N atoms from four 1-(4-pyridyl-meth-yl)-1,2,4-triazole (pmta) ligands in a distorted trans-CdCl(2)N(4) octa-hedral arrangement. The bridg-ing pmta ligands, with a dihedral angle between the triazole and pyridyl r...

Tuberculosis (TB) ranks second, next to AIDS making it most formidable disease if the present age. One of the crucial enzymes involved in cell wall synthesis of Mycobacterium tuberculosis, InhA (enoyl acyl carrier protein reductase) has been authenticated as an effective target for anti-mycobacterial drug development. In the current work, we have developed novel derivatives of 1,2,4-triazole-5-...

BACKGROUND 1,2,4-Triazole3-thiones are good scaffolds for preparation of new lead compounds. Their derivatives attracted the attention of chemists due to their wide spectrum of biological activities. Alkylsulfanyl-1,2,4-triazoles have three nucleophilic sites (nitrogens) ready for reaction with electrophiles. Herein, new regioselective isomers were synthesized by the reaction of benzylsulfanyl-...

The anticonvulsant activity of several 1,2,4-triazole-3-thione derivatives on mouse maximal electroshock-induced seizures was tested in this study. Characteristic features of all active compounds were rapid onset of action and long lasting effect. Structure-activity observations showed that the probability of obtaining compounds exerting anticonvulsant activity was much higher when at least one...

Thiadiazole and their derivatives have been studied extensively because of their wide range of biological activity. They are found to be effective as antibacterial, antimalarial, antiviral, antiinflammatory, anticancer and antianthelminthic agents. Diverse biological activities, such as antibacterial, anti-inflammatory, and antiviral have been associated with 1,3,4Thiadiazole derivatives. The s...