2
Views
0
CrossRef citations to date
0
Altmetric
Research

Patent Evaluation Cardiovascular & Renal: Phosphinic acid derivatives as endothelin converting enzyme inhibitors

Pages 503-505 | Published online: 29 Feb 2008
 

Abstract

Endothelin-1 is the most potent peptide vasoconstrictor known and has been implicated in the pathogenesis of various cardiovascular, renal and central nervous system diseases. Since the final step of biosynthesis of this vasoactive peptide is catalysed by endothelin converting enzyme, inhibitors of this enzyme are expected to have beneficial effects for diseases associated with an overproduction of endothelin-1. This patent application discloses a series of phosphinic acid derivatives as endothelin converting enzyme inhibitors. The most potent compound inhibits endothelin converting enzyme activity in vitro with an IC50 of 27 nM. In addition, compound 1 is shown to be orally active in an ex vivo assay.

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.