Lead Selection of a New Aminomethylphenol, JPC-3210, for Malaria Treatment and Prevention | Zendy

Marina Chavchich | Zendy; Geoffrey W. Birrell | Zendy; Arba L. Ager | Zendy; Donna Mackenzie | Zendy; Gavin D. Heffernan | Zendy; Guy A. Schiehser | Zendy; Laura R. Jacobus | Zendy; G. Dennis Shanks | Zendy; David P. Jacobus | Zendy; Michael D. Edstein | Zendy

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Lead Selection of a New Aminomethylphenol, JPC-3210, for Malaria Treatment and Prevention

Author(s) -

Marina Chavchich,

Geoffrey W. Birrell,

Arba L. Ager,

Donna Mackenzie,

Gavin D. Heffernan,

Guy A. Schiehser,

Laura R. Jacobus,

G. Dennis Shanks,

David P. Jacobus,

Michael D. Edstein

Publication year - 2016

Publication title -

antimicrobial agents and chemotherapy

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.07

H-Index - 259

eISSN - 1070-6283

pISSN - 0066-4804

DOI - 10.1128/aac.03066-15

Subject(s) - malaria , selection (genetic algorithm) , medicine , computer science , immunology , artificial intelligence

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.

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