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Issue 5, 2014
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α-Aminophosphonates as novel anti-leishmanial chemotypes: synthesis, biological evaluation, and CoMFA studies

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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).

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

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The article was received on 17 Dec 2013, accepted on 19 Feb 2014 and first published on 20 Feb 2014


Article type: Concise Article
DOI: 10.1039/C3MD00388D
Author version available: Download Author version (PDF)
Citation: Med. Chem. Commun., 2014,5, 665-670
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    α-Aminophosphonates as novel anti-leishmanial chemotypes: synthesis, biological evaluation, and CoMFA studies

    S. Bhagat, P. Shah, S. K. Garg, S. Mishra, P. Kamal Kaur, S. Singh and A. K. Chakraborti, Med. Chem. Commun., 2014, 5, 665
    DOI: 10.1039/C3MD00388D

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