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Literature DB >> 25147620

Lead optimization of imidazopyrazines: a new class of antimalarial with activity on Plasmodium liver stages.

Bin Zou¹, Advait Nagle², Arnab K Chatterjee², Seh Yong Leong¹, Liying Jocelyn Tan¹, Wei Lin Sandra Sim¹, Pranab Mishra², Prasuna Guntapalli², David C Tully², Suresh B Lakshminarayana¹, Chek Shik Lim¹, Yong Cheng Tan¹, Siti Nurdiana Abas¹, Christophe Bodenreider¹, Kelli L Kuhen², Kerstin Gagaring², Rachel Borboa², Jonathan Chang², Chun Li², Thomas Hollenbeck², Tove Tuntland², Anne-Marie Zeeman³, Clemens H M Kocken³, Case McNamara², Nobutaka Kato², Elizabeth A Winzeler⁴, Bryan K S Yeung¹, Thierry T Diagana¹, Paul W Smith¹, Jason Roland².

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.

Entities: Chemical Disease Species

Keywords: Liver-stage antimalarial; imidazopyrazines; lead optimization; structure−activity relationship

Year: 2014 PMID： 25147620 PMCID： PMC4137381 DOI： 10.1021/ml500244m

Source DB: PubMed Journal: ACS Med Chem Lett ISSN： 1948-5875 Impact factor: 4.345

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