Studies on substituted benzo[h]quinazolines, benzo[g]indazoles, pyrazoles, 2,6-diarylpyridines as anti-tubercular agents.
Various substituted 5,6-dihydro-8-methoxybenzo[h]quinazolin-2-amine, 1-(3-(4-alkoxyphenyl)-7-methoxy-3,3a,4,5-tetrahydro-2H benzo[g]indazol-2-yl)ethanone, pyrazole and 2,6-diarylpyridine derivatives have been synthesized in good yields by an efficient methodology. The synthesized compounds (4-23) were evaluated for their in vitro anti-tubercular activity against Mycobacterium tuberculosis H37Rv strain. Compounds 6a, 6c, 8a, 19a and 19e exhibited significant anti-tubercular activity at MIC values 50, 100, 50, 25 and 100μM concentration. In vitro cytotoxicity data using THP-1 cells indicated that most active compound 19a is safe as its MIC value is much lower than the cytotoxic value.
Medicinal Chemistry Department, CSIR-Central Institute of Medicinal and Aromatic Plants, P.O. CIMAP, Kukrail Road, Lucknow 226015, India.
Hardesh K
HK
Maurya
Ruby
R
Verma
Saba
S
Alam
Shweta
S
Pandey
Vinay
V
Pathak
Sandeep
S
Sharma
Kishore K
KK
Srivastava
Arvind S
AS
Negi
Atul
A
Gupta
D000995:Antitubercular Agents / Q000737:chemistry* / Q000494:pharmacology; D002460:Cell Line; D006801:Humans; D007191:Indazoles / Q000737:chemistry* / Q000494:pharmacology; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D011720:Pyrazoles / Q000737:chemistry* / Q000494:pharmacology; D011725:Pyridines / Q000737:chemistry* / Q000494:pharmacology; D011799:Quinazolines / Q000737:chemistry* / Q000494:pharmacology; D014376:Tuberculosis / Q000188:drug therapy
D000995:Antitubercular Agents; D007191:Indazoles; D011720:Pyrazoles; D011725:Pyridines; D011799:Quinazolines
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