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Molecules 2017, 22(6), 915; doi:10.3390/molecules22060915

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

1
Superacid Group/Organic Synthesis Team, Université de Poitiers, IC2MP—UMR CNRS 7285, 86073 Poitiers CEDEX 09, France
2
STIM—ERL CNRS 7368 Université de Poitiers, 86073 Poitiers Cedex 9, France
3
Laboratoire de Physiologie Animale, Université de Ouagadougou, 03 BP 7021 Ouagadougou 01, Burkina Faso
4
Department of Neurofarba, Sez, Chimica Farmaceutica e Nutraceutica, University of Florence, 50019 Sesto Fiorentino, Italy
*
Authors to whom correspondence should be addressed.
Academic Editor: Jean-Yves Winum
Received: 9 May 2017 / Revised: 23 May 2017 / Accepted: 23 May 2017 / Published: 31 May 2017
(This article belongs to the Special Issue Carbonic Anhydrase Inhibitors from Natural Products)
View Full-Text   |   Download PDF [1557 KB, uploaded 5 June 2017]   |  

Abstract

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. View Full-Text
Keywords: dodoneine; carbonic anhydrase; L-type calcium channel; molecular diversity; superacid dodoneine; carbonic anhydrase; L-type calcium channel; molecular diversity; superacid
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Carreyre, H.; Carré, G.; Ouedraogo, M.; Vandebrouck, C.; Bescond, J.; Supuran, C.T.; Thibaudeau, S. 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. Molecules 2017, 22, 915.

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