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

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.

SUBMITTER: Molette J

PROVIDER: S-EPMC4027556 | biostudies-literature | 2013 Nov

REPOSITORIES: biostudies-literature

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

Molette Jérôme J Routier Julie J Abla Nada N Besson Dominique D Bombrun Agnes A Brun Reto R Burt Howard H Georgi Katrin K Kaiser Marcel M Nwaka Solomon S Muzerelle Mathilde M Scheer Alexander A

ACS medicinal chemistry letters 20130922 11

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. ...[more]

PMID: 24900603

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