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
, 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