Document Report Card

ID: ALA3098117

Journal: ACS Med Chem Lett

Title: Identification and optimization of an aminoalcohol-carbazole series with antimalarial properties.

Authors: Molette J, Routier J, Abla N, Besson D, Bombrun A, Brun R, Burt H, Georgi K, Kaiser M, Nwaka S, Muzerelle M, Scheer A.

Abstract: Recent observations on the emergence of artemisinin resistant parasites have highlighted the need for new antimalarial treatments. An HTS campaign led to the identification of the 1-(1-aminopropan-2-ol)carbazole analogues as potent hits against Plasmodium falciparum K1 strain. The SAR study and optimization of early ADME and physicochemical properties direct us to the selection of a late lead compound that shows good efficacy when orally administrated in the in vivo P. berghei mouse model.

CiteXplore: 24900603

DOI: 10.1021/ml400015f