Title of article
Design and synthesis of potent thiol-based inhibitors of endothelin converting enzyme-1
Author/Authors
Cynthia A. Fink، نويسنده , , Michael Moskal، نويسنده , , Fariborz Firooznia، نويسنده , , Denton Hoyer، نويسنده , , David Symonsbergen، نويسنده , , Dongchu Wei، نويسنده , , Ying Qiao، نويسنده , , Paula Savage، نويسنده , , Michael E. Beil، نويسنده , , Angelo J. Trapani، نويسنده , , Arco Y. Jeng، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2000
Pages
3
From page
2037
To page
2039
Abstract
Through directed screening of compounds prepared as metalloprotease inhibitors a compound, CGS 30084, that had potent endothelin converting enzyme-1 (ECE-1) in vitro inhibitory activity (IC50=77 nM) was identified. Herein we report the synthesis and optimization of ECE-1 inhibitory activity of additional analogues from this lead. Compound 3c, the thioacetate methyl ester derivative of compound 4c, was found to be a long acting inhibitor of ECE-1 activity in rats after oral administration.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2000
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
791033
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