| Literature DB >> 28094524 |
Kawaljit Singh1,2, John Okombo1, Christel Brunschwig3, Ferdinand Ndubi1, Linley Barnard1, Chad Wilkinson1, Peter M Njogu4, Mathew Njoroge3, Lizahn Laing3, Marta Machado5, Miguel Prudêncio5, Janette Reader6, Mariette Botha6, Sindisiwe Nondaba6, Lyn-Marie Birkholtz6, Sonja Lauterbach7, Alisje Churchyard7, Theresa L Coetzer7, Jeremy N Burrows8, Clive Yeates9, Paolo Denti3, Lubbe Wiesner3, Timothy J Egan1, Sergio Wittlin10,11, Kelly Chibale1,2.
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.Entities:
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Year: 2017 PMID： 28094524 DOI： 10.1021/acs.jmedchem.6b01641
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446