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. 2021 Jun 1:41:127978.
doi: 10.1016/j.bmcl.2021.127978. Epub 2021 Mar 22.

Nonbisphosphonate inhibitors of Plasmodium falciparum FPPS/GGPPS

Stephanie Kabeche  1 , Jumpei Aida  2 , Thamina Akther  2 , Takashi Ichikawa  2 , Atsuko Ochida  2 , Michael J Pulkoski-Gross  1 , Mark Smith  3 , Paul S Humphries  3 , Ellen Yeh  1
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Nonbisphosphonate inhibitors of Plasmodium falciparum FPPS/GGPPS

Stephanie Kabeche et al. Bioorg Med Chem Lett. .

Abstract

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.

Keywords: Farnesyl/Geranylgeranyl diphosphate synthase; Malaria; Plasmodium falciparum; SAR; Thiazole.

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