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American Chemical Society, ACS Medicinal Chemistry Letters, 8(5), p. 947-950, 2014

DOI: 10.1021/ml500244m

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Lead Optimization of Imidazopyrazines: A New Class of Antimalarial with Activity on Plasmodium Liver Stages

Journal article published in 2014 by Bin Zou, Advait Nagle, Arnab K. Chatterjee, Seh Yong Leong, Liying Jocelyn Tan, Wei Lin Sandra Sim, Pranab Mishra, Prasuna Guntapalli, David C. Tully, Suresh B. Lakshminarayana, Chek Shik Lim, Yong Cheng Tan, Siti Nurdiana Abas, Christophe Bodenreider, Kelli L. Kuhen and other authors.
This paper is available in a repository.
This paper is available in a repository.

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Abstract

Imidazopyridine 1 was identified from a phenotypic screen against P. falciparum (Pf) blood stages and subsequently optimized for activity on liver-stage schizonts of the rodent parasite P. yoelii (Py) as well as hypnozoites of the simian parasite P. cynomolgi (Pc). We applied these various assays to the cell-based lead optimization of the imidazopyrazines, exemplified by 3 (KAI407), and show that optimized compounds within the series with improved pharmacokinetic properties achieve causal prophylactic activity in vivo and may have the potential to target the dormant stages of P. vivax malaria.