4.5 Article

Thiol-based angiotensin-converting enzyme 2 inhibitors:: P1 modifications for the exploration of the S1 subsite

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 18, Issue 2, Pages 732-737

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.11.048

Keywords

angiotensin-converting enzyme 2; metalloproteases; protease inhibitors; thiols

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Screening of a metalloprotease library led to the identification of a thiol-based dual ACE/NEP inhibitor as a potent ACE2 inhibitor. Modifications of the P-1 benzyl moiety led to improvements in ACE2 potency as well as to increased selectivity versus ACE and NEP. (c) 2007 Elsevier Ltd. All rights reserved.

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