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Development of 5-nitrothiazole derivatives: Identification of leads against both replicative and latent Mycobacterium tuberculosis |
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| Authors: | Variam Ullas Jeankumar Manoj Chandran Ganesh Samala Mallika Alvala Pulla Venkat Koushik Perumal Yogeeswari Elena G. Salina Dharmarajan Sriram |
| Affiliation: | 1. Antitubercular Drug Discovery Laboratory, Department of Pharmacy, Birla Institute of Technology& Science - Pilani, Hyderabad Campus, Jawahar Nagar, Hyderabad 500 078, India;2. Institution of the Russian Academy of Sciences A.N. Bach Institute of Biochemistry RAS, Moscow, Russia |
| Abstract: | Twenty eight 5-nitrothiazole derivatives were synthesized and evaluated for in vitro activities against Mycobacterium tuberculosis (MTB), cytotoxicity against HEK 293T. Among the compounds, 5-nitro-N-(5-nitrothiazol-2-yl)furan-2-carboxamide (20) was found to be the most active compound in vitro with MICs of 5.48 μM against log-phase culture of MTB and also non-toxic up to 100 μM. |
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