Lead optimization of 3-carboxyl-4 (1 H)-quinolones to deliver orally bioavailable antimalarials

…, F Zhu, J Min, WA Guiguemde, A Pradhan…

Index: Zhang, Yiqun; Clark, Julie A.; Connelly, Michele C.; Zhu, Fangyi; Min, Jaeki; Guiguemde, W. Armand; Pradhan, Anupam; Iyer, Lalitha; Furimsky, Anna; Gow, Jason; Parman, Toufan; El Mazouni, Farah; Phillips, Margaret A.; Kyle, Dennis E.; Mirsalis, Jon; Guy, R. Kiplin Journal of Medicinal Chemistry, 2012 , vol. 55, # 9 p. 4205 - 4219

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Citation Number: 46

Abstract

Malaria is a protozoal parasitic disease that is widespread in tropical and subtropical regions of Africa, Asia, and the Americas and causes more than 800,000 deaths per year. The continuing emergence of multidrug-resistant Plasmodium falciparum drives the ongoing need for the development of new and effective antimalarial drugs. Our previous work has explored the preliminary structural optimization of 4 (1 H)-quinolone ester derivatives, a ...