The sulfone moiety is an important core unit in organic synthesis and medicinal chemistry. Amongst different heteroaromatic compounds oxadiazoles, thiadiazoles triazoles form the basis of many pharmaceuticals agrochemicals. In fact, pyridine exhibits diversified biological activities. presence pharmacophores same attracting approach to develop new drugs due synergetic effect. Besides, applicati...

A series of 4-amino-3-[[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]thio]-5-(substituted phenyl)[1,2,4]triazoles (5a-f) and the isomeric 4-amino-2-[2-[4-(2-methoxyphenyl)-1piperazinyl]ethyl]-5-(substitutedphenyl)-2,4-dihydro-3H[1,2,4]triazole-3-thiones (6a-f) and a series of 3-[[2-[4-(2-methoxy or 2-nitrophenyl)1-piperazinyl]ethyl]thio]-5-(substituted phenyl)[1,2,4]triazoles (8a-i) were synthesi...

Triazoles with different substituent groups are found to possess diverse applications in the field of medicine and industry. A series of 4-(substituted ethanoyl)amino-3-mercapto-5-(4-nitro)phenyl-1,2,4-triazoles (NU-1 to NU-15) were synthesized as novel antimicrobial agents starting from 4-nitrobenzoic acid. The chemical structures of these newly synthesized compounds were elucidated by IR, 1H ...

An effective strategy for the synthesis of N-2-substituted-1,2,3-triazoles with excellent yields and regioselectivity has been developed.

2-Aryl-1,2,3-triazoles were synthesized by cyclization of the corresponding glyoxal arylosazones, generated from commercial arylhydrazines. The deproto-metallation of 2-phenyl-1,2,3-triazole was attempted using different 2,2,6,6-tetramethylpiperidino-based mixed lithium-metal (Zn, Cd, Cu, Co, Fe) combinations, giving results in the case of Zn, Cd, and Cu. The lithium-zinc combination was next s...

An efficient one-pot synthesis of 1,2,3-triazole derivatives of dihydropyrimidinones has been developed using two multicomponent reactions. The aldehyde-1,2,3-triazoles were obtained in good yields from in situ-generated organic azides and O-propargylbenzaldehyde. The target heterocycles were synthesized through the Biginelli reaction in which the aldehyde-1,2,3-triazoles reacted with ethyl ace...

Objective(s) Inhibitors of p38 MAP kinase are considered as suitable target in the treatment of inflammatory diseases such as rheumatoid arthritis and bowel inflammatory diseases. The development of 5-alkylthio-1-aryl-2-(4-pyridinyl) triazoles as inhibitors of p38 MAP kinase is described. These are analogues of 4- pyridinyl imidazole p38 MAP kinase inhibitor reported by Merck Research Laborator...

In this article, the pharmacological, microbiological and clinical development progress from Phase II and III clinical trials with the new generation triazoles albaconazole, isavuconazole, posaconazole, ravuconazole and voriconazole are reviewed. These drugs exhibit a favorable toxicity profile and possess high activity against resistant and emerging fungal pathogens. Pharmacokinetic may be aff...

Two classes of 1,4-disubstituted 1,2,3-triazoles were synthesized using one-pot reaction of α-tosyloxy ketones/α-halo ketones, sodium azide, and terminal alkynes in the presence of aq PEG (1:1, v/v) using the click chemistry approach and evaluated for Src kinase inhibitory activity. Structure-activity relationship analysis demonstrated that insertion of C(6)H(5)- and 4-CH(3)C(6)H(4)- at positio...

Using N-sulfonyl triazoles as substrates, compounds as diverse as 2-imino tetrahydrofurans, 13and 15membered ring aza-macrocycles can be prepared selectively via formal [1 + 4], [5 + 4 + 4] and [3 + 4 + 4 + 4] condensations of a-imino carbenes and oxetanes under Rh(II)-catalysis or thermal activation. Spirocyclic N-heterocycles are also accessible by means of Buchwald–Hartwig and Pictet–Spengle...