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 language | English (US) |
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Pages (from-to) | 3115-3118 |
Number of pages | 4 |
Journal | Antimicrobial agents and chemotherapy |
Volume | 60 |
Issue number | 5 |
DOIs | |
State | Published - May 2016 |
ASJC Scopus subject areas
- Pharmacology
- Pharmacology (medical)
- Infectious Diseases