29527-37-5Relevant academic research and scientific papers
Synthesis and invitro Evaluation of West Nile Virus Protease Inhibitors Based on the 2-{6-[2-(5-Phenyl-4H-{1,2,4]triazol-3-ylsulfanyl)acetylamino]benzothiazol-2-ylsulfanyl}acetamide Scaffold
Samanta, Sanjay,Lim, Ting Liang,Lam, Yulin
, p. 994 - 1001 (2013/07/27)
In recent years, clinical symptoms resulting from West Nile virus (WNV) infection have worsened in severity, with an increased frequency in neuroinvasive diseases among the elderly. As there are presently no successful therapies against WNV for use in humans, continual efforts to develop new chemotherapeutics against this virus are highly desired. The viral NS2B-NS3 protease is a promising target for viral inhibition due to its importance in viral replication and its unique substrate preference. In this study, a WNV NS2B-NS3 protease inhibitor with a 2-{6-[2-(5-phenyl-4H-[1,2,4]triazol-3-ylsulfanyl)acetylamino]benzothiazol-2-ylsulfanyl}acetamide scaffold was identified during screening. Optimization of this initial hit by synthesis and screening of a focused compound library with this scaffold led to the identification of a novel uncompetitive inhibitor (1a24, IC50=3.4±0.2μM) of the WNV NS2B-NS3 protease. Molecular docking of 1a24 into the WNV protease showed that the compound interferes with productive interactions of the NS2B cofactor with the NS3 protease and is an allosteric inhibitor of the WNV NS3 protease.
Synthesis and primary cytotoxicity evaluation of new diaryltriazenes
Unsalan,Rollas
, p. 185 - 191 (2008/02/10)
A series of triazenes derived from 5-(4-aminophenyl)-2,4-dihydro-4- substituted-3H-1,2,4-triazole-3-thiones 1a-c, aminoglutethimide or para-aminobenzoic acid have been synthesized for in vitro anticancer properties against three cell lines. The selected c
Some 3-Thioxo/Alkylthio-1,2,4-triazoles with a Substituted Thiourea Moiety as Possible Antimycobacterials
Kuecuekguezel, Ilkay,Kuecuekguezel, S. Gueniz,Rollas, Sevim,Kiraz, Muammer
, p. 1703 - 1708 (2007/10/03)
A series of novel N-alkyl/aryl-N'-[4-(4-alkyl/aryl-2,4-dihydro-3H-1,2,4-triazole-3-thione-5-yl)phenyl]thioureas 1-19 and three S-alkylated representatives of the former, N-alkyl/aryl-N'-[4-(3-aralkylthio-4-alkyl/aryl-4H-1,2,4-triazole-5-yl)phenyl]thioureas 20-22, were synthesized and tested for antimycobacterial activity against Mycobacterium tuberculosis H37Rv as well as Mycobacterium fortuitum ATCC 6841 which is a rapid growing opportunistic pathogen. Compounds 4 and 9-11 were found to possess the same MIC value with that of Tobramycin against M. fortuitum ATCC 6841 whereas 1-3 and 21 had positive response against M. tuberculosis H37Rv at varying degrees. Compound 21 was identified as the most potent derivative of the 1-22 series by an MIC value of 6.25 μg/ml and selectivity index of 1.6
Cytoprotection utilizing aryltriazol-3-thiones
-
, (2008/06/13)
5-Aryltriazol-3-thiones are useful for inhibiting adhesion of Mac-1 and thereby providing cytoprotection for diseases mediated by Mac-1 adhesion.
