58975-53-4Relevant articles and documents
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 antidepressant activity of di substituted-5-Aryl-1,2,4- triazoles
Radhika,Venkatesham,Sarangapani, Manda
, p. 3509 - 3513 (2013/02/25)
A series of 5-Aryl-1H-1,2,4-triazole-3-thiol (3) were synthesized. Alkylation of thiol group with N,Ndimethyl/ diethyl/dicyclo hexyl-(2-chloro ethyl) amine gave compounds N,N-disubstituted-2-(5-Aryl-1H-1,2,4-triazol-3- ylthio)ethanamine (4). These compounds were characterized on the basis of IR, 1H NMR, Mass spectral data, and elemental analysis. The newly synthesized compounds were screened for their antidepressant activity by using tail suspension test in mice. Springer Science+Business Media, LLC 2011.
Synthesis and antimicrobial activity of o- and p-hydroxybenzoic acid thiosemicarbazides
Nurkenov,Satpaeva,Kulakov,Akhmetova,Zhaugasheva
experimental part, p. 668 - 671 (2012/10/08)
The ortho- and para-hydroxybenzoic acid thiosemicarbazide derivatives which are potentially biologically active substances were obtained by the reaction of the corresponding hydrazides with various isothiocyanates. Their structures were determined using I
Synthesis and characterization of some novel quinolinothiazines of biological interest
Kalluraya, Balakrishna,Nayak, Janardhana,Adhikari, Adithya,Sujith,Shetty, N. Sucheta,Winter, Manuela
experimental part, p. 1870 - 1883 (2009/08/07)
A series of 3-aryl-4H-5-(61/81-substituted-31-formyl-21-quinolinyl) thia-1,2,4-triazoles were prepared by the reaction of 2-chloro-3-formyl-6/8- substituted quinoline with 3-substituted 4H-5-mercapto-1,2,4-triazole. These thia-triazoles 5 on reaction with substituted acetophenone gave a novel series of 2-substituted-s-triazolo[5,1-b]-6/8-substituted quinolino-9-arylacetyl[1,3] thiazines 8 rather than the expected 1-aryl-3-[21-(5-substituted-4H-1,2,4- triazole-5-thia)-61/81-substituted quinoline-31-yl]-2-propen-1-ones 7. The new compounds were screened for their antibacterial activity against Gram-positive and Gram-negative bacteria and antifungal activity against Candida albicans. Most of the tested compounds showed significant antibacterial activity much higher than that of the standard drug Nitrofurazone. The structures of the new compounds were established based on analytical and spectral data. In a typical example, the structure of thiazine 8e was further confirmed by single crystal x-ray data. Copyright Taylor & Francis Group, LLC.
