Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1368659 | Bioorganic & Medicinal Chemistry Letters | 2005 | 5 Pages |
Abstract
We have previously reported the design of a lead compound 1a for the joint inhibition of neprilysin (NEP, EC 3.4.24.11), angiotensin converting enzyme (ACE, EC 3.4.15.1) and endothelin converting enzyme (ECE-1, EC 3.4.24.71), three metallopeptidases which are implicated in the regulation of fluid homeostasis and vascular tone. We report here the synthesis and biological activities of analogues derived from this lead with inhibitory potencies in the nanomolar range for the three enzymes. Compounds 8b and 15c are the most potent triple inhibitors described to date.
This paper reports the synthesis and pharmacology of the first triple NEP, ACE, ECE inhibitor.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Nicolas Inguimbert, Hervé Poras, Franck Teffo, Françoise Beslot, Mohamed Selkti, Alain Tomas, Elizabeth Scalbert, Caroline Bennejean, Pierre Renard, Marie-Claude Fournié-Zaluski, Bernard-Pierre Roques,