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Synthesis and Antimycobacterial Activity of a Novel Series of Isonicotinylhydrazide Derivatives
Author(s) -
Jaju Sandip,
Palkar Mahesh,
Maddi Veeresh,
Ronad Pradeepkumar,
Mamledesai Shivalingarao,
Satyanarayana Darbhamulla,
Ghatole Mangala
Publication year - 2009
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200900001
Subject(s) - antimycobacterial , chemistry , hydrazide , triethylamine , isoniazid , minimum inhibitory concentration , stereochemistry , chloroacetyl chloride , benzene , mycobacterium tuberculosis , in vitro , combinatorial chemistry , organic chemistry , chloride , tuberculosis , biochemistry , medicine , pathology
A novel series of 14 new isonicotinyl hydrazide derivatives 2a – g , 3a – g containing a 4‐thiazolidinone / 2‐azetidinone nucleus were synthesized by reacting N ′‐substituted arylidene / heteroarylidene isonicotinyl hydrazide 1a – g with thioglycollic acid in the presence of dry benzene and with chloroacetyl chloride in the presence of triethylamine, respectively. Structures of all newly synthesized compounds were characterized on the basis of elemental analyses and spectral data (IR and 1 H‐NMR). All the title compounds were tested for their in‐vitro antimycobacterial activity against Mycobacterium tuberculosis H 37 Rv using Alamar‐Blue susceptibility test, and the activity is expressed as the minimum inhibitory concentration (MIC) in μg/mL. Among the series, compounds 2b , 2g , 3b , and 3g displayed an encouraging antimycobacterial activity profile as compared to that of the reference drugs isoniazid / rifampicin.