期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 56, 期 12, 页码 5213-5217出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm4005972
关键词
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资金
- Foundation for Polish Science
- NHMRC
- ARC
The malaria parasite Plasmodium falciparum employs two metallo-aminopeptidases, PfA-M1 and PfA-M17, which are essential for parasite survival. Compounds that inhibit the activity of either enzyme represent leads for the development of new antimalarial drugs. Here we report the synthesis and structure-activity relationships of a small library of phosphonic acid arginine mimetics that probe the SI pocket of both enzymes and map the necessary interactions that would be important for a dual inhibitor.
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