A review on antitubercular activity of some 2-isonicotinoylhydrazinecarboxamide, 5-(pyridin-4-yl)-1,3,4-oxadiazol-2-amine, N'-(E)-heteroaromatic-isonicotino-hydrazide and 1-(7-chloroquinolin-4-yl)-2-(heteroaromatic) methylene hydrazone derivatives

Abstract

* M. Asif * Department of Pharmacy, GRD (PG) IMT, Dehradun, India. Email: * aasif321@gmail.com ABSTRACT The modification of the isoniazid (INH) structure and with N-substituted 5-(pyridine-4-yl)-1,3,4-oxadiazole-2-amine, 5-(pyridin4-yl)-1,3,4-oxadiazol-2-amine derivatives were evaluated in vitro for their anti-tubercular (anti-TB) activity against M. tuberculosis H37Rv, M. avium, M. kansasii and one clinical isolated strain of M. kansasii. 2-Isonicotinoyl-N-(4-octylphenyl) hydrazinecarboxamide displayed an in vitro efficacy comparable to that of INH for M. tuberculosis with MIC of 1–2 μM. Among the halogenated derivatives, the best anti-TB activity was found for 2-isonicotinoyl-N-(2,4,6-trichlorophenyl) hydrazine carboxamide (MIC=4μM). Most of the hydrazinecarboxamides exhibited significant activity against INH-resistant non tuberculous mycobacteria. Two other series of N ́-(E)-heteroaromatic-isonicotino hydrazide derivatives and 1-(7-chloroquinolin4-yl)-2-[(heteroaromatic)methylene]hydrazone derivatives have been for their in vitro anti-TB activity against M. tuberculosis H37Rv. Several compounds were non cytotoxic and exhibited significant MIC value (3.12, 2.50, 1.25, or 0.60 μg/mL) compared with ethambutol (3.12 μg/mL) and rifampicin (2.0 μg/ml). These results can be considered an important point for the rational design of new leads for anti-TB compounds.