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

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...

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Bibliographic Details
Published in:Molecules (Basel, Switzerland) Switzerland), 2017-06, Vol.22 (6), p.915
Main Authors: Carreyre, Hélène, Carré, Grégoire, Ouedraogo, Maurice, Vandebrouck, Clarisse, Bescond, Jocelyn, Supuran, Claudiu T., Thibaudeau, Sébastien
Format: Article
Language:English
Subjects:
Aorta
Calcium channels (L-type)
Calcium currents
Calcium ions
Carbonic anhydrase
Case studies
Chemical Sciences
dodoneine
Hypertension
L-type calcium channel
Lead
Lead compounds
molecular diversity
Natural products
Organic chemistry
Pharmacology
Proteins
Review
superacid
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Summary: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.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules22060915