Bioactive Natural Product and Superacid Chemistry for Lead Compound Identification: A Case Study of Selective hCA III and L-Type Ca2+ Current Inhibitors for Hypotensive Agent Discovery

Autor: Hélène Carreyre, Grégoire Carré, Maurice Ouedraogo, Clarisse Vandebrouck, Jocelyn Bescond, Claudiu T. Supuran, Sébastien Thibaudeau
Jazyk: angličtina
Rok vydání: 2017
Předmět:
Zdroj: Molecules, Vol 22, Iss 6, p 915 (2017)
Druh dokumentu: article
ISSN: 1420-3049
DOI: 10.3390/molecules22060915
Popis: Dodoneine (Ddn) is one of the active compounds identified from Agelanthus dodoneifolius, which is a medicinal plant used in African pharmacopeia and traditional medicine for the treatment of hypertension. In the context of a scientific program aiming at discovering new hypotensive agents through the original combination of natural product discovery and superacid chemistry diversification, and after evidencing dodoneine’s vasorelaxant effect on rat aorta, superacid modifications allowed us to generate original analogues which showed selective human carbonic anhydrase III (hCA III) and L-type Ca2+ current inhibition. These derivatives can now be considered as new lead compounds for vasorelaxant therapeutics targeting these two proteins.
Databáze: Directory of Open Access Journals