Back to Search Start Over

Synthesis and biological evaluation of new 2-aryl-4-((4-aryl-1H-1,2,3-triazol-1-yl)methyl)thiazole derivatives

Authors :
Pravin C. Mhaske
Laxman Nawale
Pramod P. Mahulikar
Dhiman Sarkar
Vikas Shinde
Source :
Research on Chemical Intermediates. 44:1247-1260
Publication Year :
2017
Publisher :
Springer Science and Business Media LLC, 2017.

Abstract

A series of 2-aryl-4-((4-aryl-1H-1,2,3-triazol-1-yl)methyl)thiazole derivatives (8a–p) have been synthesized. The structure of the newly synthesized compounds was determined by spectral analysis. The title compounds were screened for their preliminary antitubercular activity against Mycobacterium tuberculosis H37Ra (MTB, ATCC 25177) and Mycobacterium bovis BCG (BCG, ATCC 35743). Further, the synthesized compounds were screened for antimicrobial activity against standard Gram-negative bacteria Escherichia coli (NCIM 2576) and Pseudomonas flurescence (NCIM 2059) and Gram-positive bacteria Staphylococcus aureus (NCIM 2602) and Bacillus subtilis (NCIM 2162). Among all the synthesized compounds, 8a–c, f–h, m exhibited good activity against dormant M. bovis BCG strain. Compounds 8h, j exhibited good activity against all tested bacterial strains. All active compounds were screened for cytotoxicity and found inactive. Their high potency and promising antimycobacterial activity suggest that these compounds could serve as good leads for further optimization and development.

Details

ISSN :
15685675 and 09226168
Volume :
44
Database :
OpenAIRE
Journal :
Research on Chemical Intermediates
Accession number :
edsair.doi...........f68a7eceb7eede891ad8a9bc0762c379
Full Text :
https://doi.org/10.1007/s11164-017-3164-4