Lead selection of a new aminomethylphenol, JPC-3210, for malaria treatment and prevention

Marina Chavchich, Geoffrey W. Birrell, Arba L. Ager, Donna O. MacKenzie, Gavin D. Heffernan, Guy A. Schiehser, Laura R. Jacobus, G. Dennis Shanks, David P. Jacobus, Michael D. Edstein

Research output: Contribution to journalArticle

12 Scopus citations

Abstract

Structure-activity relationship studies of trifluoromethyl-substituted pyridine and pyrimidine analogues of 2-aminomethylphenols (JPC-2997, JPC-3186, and JPC-3210) were conducted for preclinical development for malaria treatment and/or prevention. Of these compounds, JPC-3210 [4-(tert-butyl)-2-((tert-butylamino)methyl)-6-(5-fluoro-6-(trifluoromethyl)pyridin-3-yl)phenol] was selected as the lead compound due to superior in vitro antimalarial activity against multidrug-resistant Plasmodium falciparum lines, lower in vitro cytotoxicity in mammalian cell lines, longer plasma elimination half-life, and greater in vivo efficacy against murine malaria.

Original languageEnglish (US)
Pages (from-to)3115-3118
Number of pages4
JournalAntimicrobial agents and chemotherapy
Volume60
Issue number5
DOIs
StatePublished - May 2016

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)
  • Infectious Diseases

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    Chavchich, M., Birrell, G. W., Ager, A. L., MacKenzie, D. O., Heffernan, G. D., Schiehser, G. A., Jacobus, L. R., Shanks, G. D., Jacobus, D. P., & Edstein, M. D. (2016). Lead selection of a new aminomethylphenol, JPC-3210, for malaria treatment and prevention. Antimicrobial agents and chemotherapy, 60(5), 3115-3118. https://doi.org/10.1128/AAC.03066-15