疟原虫 FPPS/GGPPS 的非双膦酸盐抑制剂。
Nonbisphosphonate inhibitors of Plasmodium falciparum FPPS/GGPPS.
机构信息
Department of Biochemistry, Stanford Medical School, Stanford University, Stanford, CA 94305, USA.
Research, Takeda Pharmaceutical Company Ltd, 26-1, Muraokahigashi 2-chome Fujisawa, Kanagawa 251-8555, Japan.
出版信息
Bioorg Med Chem Lett. 2021 Jun 1;41:127978. doi: 10.1016/j.bmcl.2021.127978. Epub 2021 Mar 22.
A series of novel thiazole-containing amides were synthesized. A structure-activity relationship study of these compounds led to the identification of potent and selective PfFPPS/GGPPS inhibitors with good in vitro ADME profiles. The most promising candidate molecules were progressed to mouse in vivo PK studies and demonstrated adequate free drug exposure to warrant further investigation.
合成了一系列新型含噻唑的酰胺。对这些化合物的构效关系研究鉴定出了具有良好体外 ADME 特性的有效且选择性的 PfFPPS/GGPPS 抑制剂。最有前途的候选分子被推进到小鼠体内 PK 研究中，并证明具有足够的游离药物暴露量，值得进一步研究。
Zotero 插件