Malaria is one of the most destructive diseases in the world annually affecting over 200 million people and killing almost one million people per year. Although several antimalarial agents are currently used successfully, the emergence of multidrug resistance signals the importance to developing new antimalarials. Previously, compound ICI56,780 was reported to display causal prophylactic and blood schizonticidal activity in rodent malaria models. Unfortunately, ICI56,780 generated rapid parasitological resistance in P. berghei infected mice. Herein the synthesis of analogues of ICI56,780 with low EC50 values against P. falciparum will be presented. By introducing ortho-substituted aryl groups at the 3-position of the 7-(2-phenoxyethoxy)-4(1H)-quinolone core, good activities with low cross resistance indexes to atovaquone were obtained.

7-(2-phenoxyethoxy)-4(1H)-quinolones as antimalarials

244th National Meeting (2012)

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.