Synthesis, Evaluation and Qsar Analysis of 5-nitrofuran-2-yl/4-nitrophenyl Methylene Substituted Hydrazides as Antitubercular Agents
نویسندگان
چکیده
A series of novel N'-((5-nitrofuran-2-yl/4-nitrophenyl) methylene) substituted hydrazides (3a-3i & 4a-4i) was synthesized, and tested for in vitro antimycobacterial activity, and their quantitative structure activity relationship (QSAR) of hydrazide derivatives is reported here. The results of anti-mycobacterial activity study indicated that the presence of halogen substitution at benzohydrazide moiety improved the activity of these derivatives. Preliminary structure activity relationship analysis revealed that 5-nitrofuran-2-yl-methylene analogs more potent than 4nitrobenzylidene substituted analogs. QSAR model was developed correlating the antimycobacterial activity with the structural features of the compounds and the predictive capability of the models was estimated using validation parameters. The QSAR analysis results indicated the radial distribution function (RDF030v, RDF135m & RDF120u) might be helpful in describing the antimycobacterial activity of hydrazides.
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