Title of article
Synthesis and biological activity of potent heterocyclic thiol-based inhibitors of endothelin-converting enzyme-1
Author/Authors
Fariborz Firooznia، نويسنده , , Candido Gude، نويسنده , , Kenneth Chan، نويسنده , , Jenny Tan، نويسنده , , Cynthia A. Fink، نويسنده , , Paula Savage، نويسنده , , Michael E. Beil، نويسنده , , Charles W. Bruseo، نويسنده , , Angelo J. Trapani، نويسنده , , Arco Y. Jeng، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2002
Pages
4
From page
3059
To page
3062
Abstract
Directed screening of metalloprotease inhibitors identified CGS 30084 (1) as a potent inhibitor of endothelin-converting enzyme-1 (ECE-1) in vitro (IC50=77 nM). Herein we report the syntheses and biological activities of analogues containing modified biphenyl moieties, bearing heterocyclic proximal rings. Compound 20, the thioacetate ethyl ester prodrug derivative of compound 19a, was found to be an orally active and potent inhibitor of ECE-1 activity in rats.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2002
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
792599
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