342045-65-2Relevant articles and documents
Lead optimization of 3-carboxyl-4(1 H)-quinolones to deliver orally bioavailable antimalarials
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
supporting information; experimental part, p. 4205 - 4219 (2012/07/02)
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(1H)-quinolone ester derivatives, a new series of antimalarials related to the endochins. Herein, we report the lead optimization of 4(1H)-quinolones with a focus on improving both antimalarial potency and bioavailability. These studies led to the development of orally efficacious antimalarials including quinolone analogue 20g, a promising candidate for further optimization.
Synthesis and structure-activity relationships of antimalarial 4-oxo-3-carboxyl quinolones
Zhang, Yiqun,Guiguemde, W. Armand,Sigal, Martina,Zhu, Fangyi,Connelly, Michele C.,Nwaka, Solomon,Guy, R. Kiplin
experimental part, p. 2756 - 2766 (2010/06/19)
Malaria is endemic in tropical and subtropical regions of Africa, Asia, and the Americas. The increasing prevalence of multi-drug-resistant Plasmodium falciparum drives the ongoing need for the development of new antimalarial drugs. In this light, novel s