3
Views
0
CrossRef citations to date
0
Altmetric
Cardiovascular Agents (Including Blood Products)

Patent Evaluation: Novel Endothelin Receptor Antagonists Isolated from Microbispora

Pages 1924-1925 | Published online: 02 Mar 2011
 

Summary

Novelty: Three novel cyclic depsipeptides derived from a culture of Microbispora sp. MA6857 are claimed as endothelin receptor antagonists. They are claimed for the treatment of cardiovascular disorders, including hypertension, cerebral and cardiac ischaemia and postischaemic venal failure, and for the treatment of asthma and of cyclosporin nephrotoxicity.

Biology: The binding of the cyclopeptides was determined in a method similar to the assay described by Ambar et al. (Biochem. Biophys. Res. Comm. (1989) 158:195-201) and by Khoog et al. (FEBS Letters (1989) 253:199-202); the method is fully described. Results for rat aorta and rat hippocampus binding are presented. The specified compound had Kis against 125I-endothelin I binding of 100 nM (aorta) and 200 nM (hippocampus).

Chemistry: Three cyclic depsipeptides are specifically claimed. Detailed 1H and 13C nmr data are given. Experimental details for the isolation of the claimed compounds from cultures of Microbispora are presented.

Structure:

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.