Design, synthesis and SAR evaluation of mercaptooxadiazole analogs as anti-tubercular, anti-diabetic and anti-bacterial agents
Chemical Data Collections(2020)
摘要
Diabetes and tuberculosis are the chronic diseasea, highly affected mankind. Globally 422 million adults suffer from diabetes and two million deaths occur due to tuberculosis. A library of the mercaptooxadiazole analogs were synthesized by cyclization of benzohydrazide, followed by the nucleophillic alkylation/arylation. Characterization was done by FT-IR, LCMS and NMR spectral techniques. The newly synthesized compounds were screened for the antibacterial, antioxidant, anti-diabetic and anti-tubercular (anti-TB) activities. Some of the compounds show superior in-vitro anti-TB activity with 1.6 μg/ml as MIC value and a better anti-diabetic activity with 62% inhibitory potency. The level of toxicity of active compounds was determined with normal cell line (L292) by MTT assay and was found to be non-toxic over the MIC values. Experimental data hypothesized that compound 5e is the most prominent non-toxic drug candidature with lengthened activity against bacterial, fungal, tubercular and diabetic activities.
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关键词
Oxadiazole,in-vitro and in-silico,anti-TB,Anti-diabetic,Anti-bacterial
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