期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 58, 期 21, 页码 8713-8722出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.5b01605
关键词
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资金
- Medicines for Malaria Ventures (MMV)
- South African Technology Innovation Agency (TIA) [MMV09/0002]
- University of Cape Town
- South African Medical Research Council
- South African Research Chairs Initiative of the Department of Science and Technology
Toward improving pharmacokinetics, in vivo efficacy, and selectivity over hERG, structure activity relationship studies around the central core of antimalarial imidazo-pyridazines were conducted. This study led to the identification of potent pyrazolopyridines, which showed good in vivo efficacy and pharmacokinetics profiles. The lead compounds also proved to be very potent in the parasite liver and gametocyte stages, which makes them of high interest.
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