Title of article
Synthesis and biological activity of novel potent endothelin-converting enzyme-1 inhibitors
Author/Authors
Fariborz Firooznia، نويسنده , , Candido Gude، نويسنده , , Kenneth Chan، نويسنده , , Cynthia A. Fink، نويسنده , , Ying Qiao، نويسنده , , Yoshitaka Satoh، نويسنده , , Nicholas Marcopoulos، 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 2001
Pages
4
From page
375
To page
378
Abstract
Through directed screening of metalloprotease inhibitors, CGS 30084 (1) has been identified as a potent endothelin-converting enzyme-1 (ECE-1) inhibitor in vitro (IC50=77 nM). Herein we report the syntheses and biological activities of analogues derived from this lead, based on modifications of the biphenyl moiety. Compound 10, the thioacetate methyl ester prodrug derivative of compound 6m, was found to be an orally active and potent inhibitor of ECE-1 activity in rats.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2001
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
800350
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