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
2017Author
Kawaljit, Singh
Okombo, John
Christel, Brunschwig
Ndubi, Ferdinand
Linley, Barnard
Chad, Wilkinson
Njogu, Peter M.
Njoroge, Mathew
Lizahn, Laing
Marta, Machado
Miguel, Prudêncio
Janette, Reader
Mariette, Botha
Sindisiwe, Nondaba
Lyn-Marie, Birkholtz
Sonja, Lauterbach
Alisje, Churchyard
Coetzer, Theresa L.
Burrows, Jeremy N.
Clive, Yeates
Paolo, Denti
Lubbe, Wiesner
Egan, Timothy J.
Sergio, Wittlin
Kelly, Chibale
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.
URI
https://www.ncbi.nlm.nih.gov/pubmed/28094524http://pubs.acs.org/doi/abs/10.1021/acs.jmedchem.6b01641
http://hdl.handle.net/11295/100890
Citation
J Med Chem. 2017 Feb 23;60(4):1432-1448. doi: 10.1021/acs.jmedchem.6b01641. Epub 2017 Feb 7.Publisher
University of Nairobi
Rights
Attribution-NonCommercial-NoDerivs 3.0 United StatesUsage Rights
http://creativecommons.org/licenses/by-nc-nd/3.0/us/Collections
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