Design, synthesis and SAR evaluation of mercaptooxadiazole analogs as anti-tubercular, anti-diabetic and anti-bacterial agents
| Autor: | H. K. Kumara, Mahesh Bhat, Mounika Tirukoti, S.K. Meenakshi, D. Channe Gowda, S. V. Mamatha |
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| Rok vydání: | 2020 |
| Předmět: |
Drug
Antioxidant Tuberculosis 010405 organic chemistry Chemistry medicine.medical_treatment media_common.quotation_subject General Chemistry Pharmacology 010402 general chemistry medicine.disease 01 natural sciences 0104 chemical sciences Diabetes mellitus Toxicity medicine MTT assay Anti bacterial Anti tubercular media_common |
| Zdroj: | Chemical Data Collections. 26:100343 |
| ISSN: | 2405-8300 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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