期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 55, 期 9, 页码 4205-4219出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm201642z
关键词
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资金
- St. Jude High Throughput Screening Core
- National Institutes of Health
- NIAID [AI075517, AI075594]
- American Lebanese Syrian Associated Charities (ALSAC)
- St. Jude Children's Research Hospital
- Welch Foundation [I-1257]
Malaria is a protozoal parasitic disease that is widespread in tropical and subtropical regions of Africa, Asia, and the Americas and causes more than 800,000 deaths per year. The continuing emergence of multidrug-resistant Plasmodium falciparum drives the ongoing need for the development of new and effective antimalarial drugs. Our previous work has explored the preliminary structural optimization of 4(1H)-quinolone ester derivatives, a new series of antimalarials related to the endochins. Herein, we report the lead optimization of 4(1H)-quinolones with a focus on improving both antimalarial potency and bioavailability. These studies led to the development of orally efficacious antimalarials including quinolone analogue 20g, a promising candidate for further optimization.
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