Synthesis of novel N-(2-substituted 4-oxothiazolidin-3-yl) isonicotinamide derivatives as anti mycobacterial agents

In the present work, the intermediate Schiff’s bases (imines) 1(a-j) were synthesized by refluxing isoniazid with aromatic and heterocyclic aldehydes in ethanol. Cyclocondensation of 1(a-j) (imines) with thioglycolic acid in dimethylformamide as solvent, in presence of anhydrous zinc chloride as a catalyst, was carried out under microwave irradiation, to give a series of N-(2-substituted-4-oxothiazolidin-3-yl) isonicotinamide derivatives 2(a-j) in good yield. The synthesized compounds were evaluated for their in vitro anti-mycobacterial activity against M. tuberculosis H37Rv using tube dilution method. Some of the compounds exhibited a significant anti mycobacterial activity when compared with first line drugs such as isoniazid (INH) and rifampicin (RIP)

Author(s): Anna Pratima G. Nikalje, M. Pathan, M. Ghodke and D. Rajani

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