Synthesis of isonicotinic acid N'-arylidene-N-[2-oxo-2-(4-aryl-piperazin-1-yl)-ethyl]-hydrazides as antituberculosis agents.
A new series of antituberculosis agents 6-9 was designed, synthesized and evaluated for antituberculosis activity against Mycobacterium tuberculosis H37Rv and clinical isolates in an agar dilution method. Compound 9h showed comparable in vitro activity (MIC) to isoniazid against M. tuberculosis H37Rv and clinical isolates (sensitive strains) and superior activity against resistant strains of M. tuberculosis.
Sinha
Neelima
N
Medicinal Chemistry Division, New Chemical Entity Research, Lupin Research Park, 46/47A, Village Nande, Taluka Mulshi, Pune 411 042, Maharashtra, India. neelimasinha@lupinpharma.com
Jain
Sanjay
S
Tilekar
Ajay
A
Upadhayaya
Ram Shankar
RS
Kishore
Nawal
N
Jana
Gour Hari
GH
Arora
Sudershan K
SK
D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D007539:Isonicotinic Acids / Q000138:chemical synthesis* / Q000494:pharmacology*; D015394:Molecular Structure; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D013329:Structure-Activity Relationship
D000995:Antitubercular Agents; D007539:Isonicotinic Acids