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

ACS Med Chem Lett. 2013 Sep 22;4(11):1037-41. doi: 10.1021/ml400015f. eCollection 2013 Nov 14.


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.

Keywords: IC50; Malaria; Plasmodium berghei; Plasmodium falciparum; SAR; WHO; carbazole; hERG.