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)
 
ID 3775737
Author(s) Singh, Kawaljit; Okombo, John; Brunschwig, Christel; Ndubi, Ferdinand; Barnard, Linley; Wilkinson, Chad; Njogu, Peter M.; Njoroge, Mathew; Laing, Lizahn; Machado, Marta; Prudêncio, Miguel; Reader, Janette; Botha, Mariette; Nondaba, Sindisiwe; Birkholtz, Lyn-Marie; Lauterbach, Sonja; Churchyard, Alisje; Coetzer, Theresa L.; Burrows, Jeremy N.; Yeates, Clive; Denti, Paolo; Wiesner, Lubbe; Egan, Timothy J.; Wittlin, Sergio; Chibale, Kelly
Author(s) at UniBasel Wittlin, Sergio
Year 2017
Title 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.
Publisher American Chemical Society
ISSN/ISBN 0022-2623
edoc-URL http://edoc.unibas.ch/54815/
Full Text on edoc No
Digital Object Identifier DOI 10.1021/acs.jmedchem.6b01641
PubMed ID http://www.ncbi.nlm.nih.gov/pubmed/28094524
 
   

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