4.5 Article

Synthesis and evaluation of heteroarylalanine diacids as potent and selective neutral endopeptidase inhibitors

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 21, Issue 11, Pages 3404-3406

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.03.109

Keywords

Neutral endopeptidase; Angiotensin converting enzyme; Zinc metalloproteinases, Oxazole; Oxadiazole

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Heteroarylalanine derivatives 4 were designed as potential inhibitors of neutral endopeptidase (NEP EC 3.4.24.11). Selectivity over other zinc metalloproteinases was explored through occupation of the S2' sub-site within NEP. Structural optimisation led to the identification of 5-phenyl oxazole 4f, a potent and selective NEP inhibitor. A crystal structure of the inhibitor bound complex is reported. (C) 2011 Elsevier Ltd. All rights reserved.

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