α-Aminophosphonates as novel anti-leishmanial chemotypes: synthesis, biological evaluation, and CoMFA studies

Bhagat, Srikant ; Shah, Parth ; Garg, Sanjeev K. ; Mishra, Shweta ; Kamal Kaur, Preet ; Singh, Sushma ; Chakraborti, Asit K. (2014) α-Aminophosphonates as novel anti-leishmanial chemotypes: synthesis, biological evaluation, and CoMFA studies MedChemComm, 5 (5). pp. 665-670. ISSN 2040-2503

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Official URL: http://pubs.rsc.org/en/Content/ArticleLanding/2014...

Related URL: http://dx.doi.org/10.1039/C3MD00388D

Abstract

A series of twenty six structurally diverse α-aminophosphonates have been synthesized and evaluated for in vitro anti-leishmanial activity and cytotoxicity using the MTT assay. Among them, seven compounds (1–7) exhibited anti-leishmanial potency against the L. donovani promastigote with IC50 values in the low micromolar range. The structure–activity relationships were quantitatively evaluated by a statistically reliable CoMFA model with high predictive abilities (r2pred = 0.87, r2ncv = 0.985).

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