Synthesis and Antimycobacterial Activity of a Novel Series of Isonicotinylhydrazide Derivatives |
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Authors: | Sandip Jaju Mahesh Palkar Veeresh Maddi Pradeepkumar Ronad Shivalingarao Mamledesai Darbhamulla Satyanarayana Mangala Ghatole |
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Affiliation: | 1. Department of Pharmaceutical Chemistry, KLES' College of Pharmacy, Vidyanagar, Hubli, Karnataka, India. Fax: +91 836 237‐1694;2. Department of Pharmaceutical Chemistry, NGSM Institute of Pharmaceutical Sciences, Paneer, Deralakatte, Mangalore, Karnatka, India;3. Department of Microbiology, Dr. V. M. Medical College, Solhapur, Maharastra, India |
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Abstract: | 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 1H‐NMR). All the title compounds were tested for their in‐vitro antimycobacterial activity against Mycobacterium tuberculosis H37Rv 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. |
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Keywords: | Antimycobacterial activity Azetidinones Isonicotinyl hydrazide Mycobacterium tuberculosis Thiazolidinones |
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