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Bioorg Med Chem Lett. 2008 Jan 15;18(2):732-7. Epub 2007 Nov 19.

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

Author information

1
Department of Medicinal Chemistry, GlaxoSmithKline, Research Triangle Park, NC 27709, USA. david.n.deaton@gsk.com

Abstract

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.

PMID:
18078750
DOI:
10.1016/j.bmcl.2007.11.048
[Indexed for MEDLINE]

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