Development of 5-nitrothiazole derivatives: identification of leads against both replicative and latent Mycobacterium tuberculosis

…, G Samala, M Alvala, PV Koushik, P Yogeeswari…

Index: Jeankumar, Variam Ullas; Chandran, Manoj; Samala, Ganesh; Alvala, Mallika; Koushik, Pulla Venkat; Yogeeswari, Perumal; Salina, Elena G.; Sriram, Dharmarajan Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 24 p. 7414 - 7417

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Citation Number: 4

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 100μM.