2. Academic Validation
  3. Nonbisphosphonate inhibitors of Plasmodium falciparum FPPS/GGPPS

Nonbisphosphonate inhibitors of Plasmodium falciparum FPPS/GGPPS

  • Bioorg Med Chem Lett. 2021 Jun 1:41:127978. doi: 10.1016/j.bmcl.2021.127978.
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
Affiliations

Affiliations

  • 1 Department of Biochemistry, Stanford Medical School, Stanford University, Stanford, CA 94305, USA.
  • 2 Research, Takeda Pharmaceutical Company Ltd, 26-1, Muraokahigashi 2-chome Fujisawa, Kanagawa 251-8555, Japan.
  • 3 Department of ChEM-H, Stanford University, Stanford, CA 94305, USA.
PMID: 33766764 DOI: 10.1016/j.bmcl.2021.127978
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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