期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 5, 期 8, 页码 947-950出版社
AMER CHEMICAL SOC
DOI: 10.1021/ml500244m
关键词
Liver-stage antimalarial; imidazopyrazines; structure-activity relationship; lead optimization
资金
- Wellcome Trust [WT078285, WT096157]
- Medicines for Malaria Venture (MMV)
- Swiss Tropical and Public Health Institute
- Biomedical Primate Research Centre
- Novartis Institute for Tropical Diseases
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.
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