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Nonbisphosphonate inhibitors of Plasmodium falciparum FPPS/GGPPS. Bioorganic & medicinal chemistry letters Kabeche, S., Aida, J., Akther, T., Ichikawa, T., Ochida, A., Pulkoski-Gross, M. J., Smith, M., Humphries, P. S., Yeh, E. 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.

View details for DOI 10.1016/j.bmcl.2021.127978

View details for PubMedID 33766764