Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 5, Issue 8, Pages 947-950Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ml500244m
Keywords
Liver-stage antimalarial; imidazopyrazines; structure-activity relationship; lead optimization
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Funding
- Wellcome Trust [WT078285, WT096157]
- Medicines for Malaria Venture (MMV)
- Swiss Tropical and Public Health Institute
- Biomedical Primate Research Centre
- Novartis Institute for Tropical Diseases
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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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