Nonbisphosphonate inhibitors of Plasmodium falciparum FPPS/GGPPS.

Stephanie Kabeche, Jumpei Aida, Thamina Akther, Takashi Ichikawa, Atsuko Ochida, Michael J Pulkoski-Gross, Mark Smith, Paul S Humphries, Ellen Yeh

Bioorganic & medicinal chemistry letters 2021 Jun 01

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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. Copyright © 2021 Elsevier Ltd. All rights reserved.

Citation

Stephanie Kabeche, Jumpei Aida, Thamina Akther, Takashi Ichikawa, Atsuko Ochida, Michael J Pulkoski-Gross, Mark Smith, Paul S Humphries, Ellen Yeh. Nonbisphosphonate inhibitors of Plasmodium falciparum FPPS/GGPPS. Bioorganic & medicinal chemistry letters. 2021 Jun 01;41:127978