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Antimalarial pyrido[1,2-a]benzimidazoles : lead optimization, parasite life cycle stage profile, mechanistic evaluation, killing kinetics, and in vivo oral efficacy in a mouse model
JournalArticle (Originalarbeit in einer wissenschaftlichen Zeitschrift)
Antimalarial pyrido[1,2-a]benzimidazoles : lead optimization, parasite life cycle stage profile, mechanistic evaluation, killing kinetics, and in vivo oral efficacy in a mouse model
Journal
Journal of medicinal chemistry
Volume
60
Number
4
Pages / Article-Number
1432-1448
Abstract
Further structure-activity relationship (SAR) studies on the recently identified pyrido[1,2-a]benzimidazole (PBI) antimalarials have led to the identification of potent, metabolically stable compounds with improved in vivo oral efficacy in the P. berghei mouse model and additional activity against parasite liver and gametocyte stages, making them potential candidates for preclinical development. Inhibition of hemozoin formation possibly contributes to the mechanism of action.
