Orally active esters of dihydroartemisinin: Synthesis and antimalarial activity against multidrug-resistant Plasmodium yoelii in mice.

Bioorganic & Medicinal Chemistry Letters
Chandan SinghS K Puri

Abstract

A series of artemisinin derived esters 7a-j, incorporating pharmacologically privileged substructure, such as biphenyl, adamantane and fluorene, have been prepared and evaluated for antimalarial activity against multidrug-resistant (MDR) Plasmodium yoelii nigeriensis by oral route. Several of these compounds were found to be more active than the antimalarial drugs beta-arteether 4 and artesunic acid 5. Ester 7i, the most active compound of the series, provided 100% and 80% protection to the infected mice at 24 mg/kg x 4 days and 12 mg/kg x 4 days, respectively. In this model beta-arteether provided 100% and 20% protection at 48 mg/kg x 4 days and 24 mg/kg x 4 days, respectively.

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Citations

Feb 26, 2013·Chemical Reviews·Lukas WankaPeter R Schreiner
Aug 2, 2014·European Journal of Medicinal Chemistry·Ajay KumarDhirender Kaushik
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Jan 29, 2021·European Journal of Medicinal Chemistry·Om P S PatelLesetja J Legoabe
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Mar 12, 2015·The Journal of Organic Chemistry·Ganesh MajjiBhisma K Patel

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