Abstract
A variety of phthalimido(2-aryl-3-(5'-(4''-pyridyl)-1',3',4'-thiadiazol-2'-yl)-4-oxothiazolidin-5- yl)ethanoates 7a-h and 3-N-alkoxyphthalimido-2-isonicotinoylhydrazido-1,3-thiazolidin-4-ones 9a-c were synthesized using thiosemicarbazide of isoniazid 2 by two alternative pathways. The structures of these compounds were confirmed by IR, NMR ( 1 H & 13 C) and Mass spectral studies. Synthesized compounds 7a-h and 9a-c were evaluated for their antimicrobial activity. Some of the compounds exhibited good antimicrobial activity compared to standard drugs. The structure activity relationships of synthesized compounds have also been studied in order to develop the most potential antimicrobial agent for preclinical evaluation.
Highlights
Tuberculosis is believed to be present in about one third of the world’s population.[1]
Most of the drug resistant clinical isolates of the tubercle bacillus are resistant to isoniazid which is a first line antituberculous drug.[3]
This antibiotic was shown to act on Mycobacterium tuberculosis by inhibiting a 2-trans-enoyl-acyl carrier, protein reductase, called InhA.[4]
Summary
Tuberculosis is believed to be present in about one third of the world’s population.[1]. Antimicrobial Screening In the present investigation, various substituted phthalimido[2-aryl-3-(5′-(4′′-pyridyl)-1′,3′,4′thiadiazol-2′-yl)-4-oxothiazolidin-5-yl]ethanoates 7a-h and 3-N-alkoxyphthalimido-2isonicotinoylhydrazido-1,3-thiazolidin-4-ones 9a-c derivatives have been evaluated for their antimicrobial activity.
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