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
Date
2017-02-23Author
Singh, K
Okombo, J
Brunschwig, C
Ndubi, F
Barnard, L
Wilkinson, C
Njogu, PM
Njoroge, M
Laing, L
Machado, M
Prudêncio, M
Reader, J
Type
ArticleLanguage
enMetadata
Show full item recordAbstract
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.
Citation
J Med Chem. 2017 Feb 23;60(4):1432-1448.Publisher
ASC
Collections
- Faculty of Health Sciences (FHS) [10377]