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Issue 4, 2012
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Novel selective inhibitors of neutral endopeptidase: discovery by screening and hit-to-lead optimisation

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Abstract

A diverse library of carboxylic acids was synthesized on solid-support. The screening on hNEP identified a low molecular weight hit. Structure–activity relationships around the hit highlighted the critical role of configuration for both chiral centers. The path, that involves a side reaction, to the potent and selective NEP optimised inhibitor is presented.

Graphical abstract: Novel selective inhibitors of neutral endopeptidase: discovery by screening and hit-to-lead optimisation

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Publication details

The article was received on 15 Nov 2011, accepted on 08 Jan 2012 and first published on 10 Jan 2012


Article type: Concise Article
DOI: 10.1039/C2MD00287F
Citation: Med. Chem. Commun., 2012,3, 469-474
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    Novel selective inhibitors of neutral endopeptidase: discovery by screening and hit-to-lead optimisation

    J. El Bakali, L. Maingot, J. Dumont, H. Host, A. Hocine, N. Cousaert, S. Dassonneville, F. Leroux, B. Deprez and R. Deprez-Poulain, Med. Chem. Commun., 2012, 3, 469
    DOI: 10.1039/C2MD00287F

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