@article { ISI:000371344600027,
	title = {Synthesis, biological evaluation and molecular docking study of some novel indole and pyridine based 1,3,4-oxadiazole derivatives as potential antitubercular agents},
	journal = {Bioorganic \& Medicinal Chemistry Letters},
	volume = {26},
	number = {7},
	year = {2016},
	month = {APR },
	pages = {1776-1783},
	publisher = {PERGAMON-ELSEVIER SCIENCE LTD},
	address = {THE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLAND},
	abstract = {<p>A series of indole and pyridine based 1,3,4-oxadiazole derivatives 5a-t were synthesized and evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis H37Ra (MTB) and Mycobacterium bovis BCG both in active and dormant state. Compounds 5b, 5e, 5g and 5q exhibited very good antitubercular activity. All the newly synthesized compounds 5a-t were further evaluated for antiproliferative activity against HeLa, A549 and PANC-1 cell lines using modified MTT assay and found to be noncytotoxic. On the basis of cytotoxicity and MIC values against Mycobacterium bovis BCG, selectivity index (SI) of most active compounds 5b, 5e, 5g and 5q was calculated (SI = GI(50)/MIC) in active and dormant state. Compounds 5b, 5e and 5g demonstrated SI values \&gt;= 10 against all three cell lines and were found to safe for advance screening. Compounds 5a-t were further screened for their antibacterial activity against four bacteria strains to assess their selectivity towards MTB. In addition, the molecular docking studies revealed the binding modes of these compounds in active site of enoyl reductase (InhA), which in turn helped to establish a structural basis of inhibition of mycobacteria. The potency, low cytotoxicity and selectivity of these compounds make them valid lead compounds for further optimization. (C) 2016 Elsevier Ltd. All rights reserved.</p>},
	keywords = {1, 3, 4-Oxadiazole, Antitubercular activity, Cytotoxicity, Indole, Molecular docking, Pyridine},
	issn = {0960-894X},
	doi = {10.1016/j.bmcl.2016.02.043},
	author = {Desai, N. C. and Somani, Hardik and Trivedi, Amit and Bhatt, Kandarp and Nawale, Laxman and Khedkar, Vijay M. and Jha, Prakash C. and Sarkar, Dhiman}
}
@article {44197,
	title = {Synthesis and biological evaluation of new 2-aryl-4-((4-aryl-1H-1,2,3-triazol-1-yl)methyl)thiazole derivatives},
	journal = {Research on Chemical Intermediates},
	volume = {44},
	year = {2018},
	month = {FEB},
	pages = {1247-1260},
	type = {Article},
	abstract = {<p>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.</p>},
	keywords = {1, 2, 3-Triazole, antibacterial activity, Antitubercular activity, Thiazole},
	issn = {0922-6168},
	doi = {10.1007/s11164-017-3164-4},
	author = {Shinde, Vikas and Mahulikar, Pramod and Mhaske, Pravin C. and Nawale, Laxman and Sarkar, Dhiman}
}
