Lead Selection of a New Aminomethylphenol, JPC-3210, for Malaria Treatment and Prevention-Reference-Cited by-同舟云学术

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

Published:2016-05 Issue:5 Volume:60 Page:3115-3118
ISSN:0066-4804
Container-title:Antimicrobial Agents and Chemotherapy
language:en
Short-container-title:Antimicrob Agents Chemother

Author:

Chavchich Marina¹,Birrell Geoffrey W.¹,Ager Arba L.²,MacKenzie Donna O.¹,Heffernan Gavin D.³,Schiehser Guy A.³,Jacobus Laura R.³,Shanks G. Dennis¹,Jacobus David P.³,Edstein Michael D.¹

Affiliation:

1. Department of Drug Evaluation, Australian Army Malaria Institute, Enoggera, Brisbane, Queensland, Australia

2. University of Miami, Miami, Florida, USA

3. Jacobus Pharmaceutical Company, Princeton, New Jersey, USA

Abstract

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.

Publisher

American Society for Microbiology

Subject

Infectious Diseases,Pharmacology (medical),Pharmacology

Link

https://journals.asm.org/doi/pdf/10.1128/AAC.03066-15

Reference21 articles.

1. World Health Organization. 2014. World malaria report 2014. World Health Organization Geneva Switzerland. http://www.who.int/malaria/publications/world_malaria_report_2014/en/.

2. The effect of malaria control on Plasmodium falciparum in Africa between 2000 and 2015

3. Artemisinin Resistance inPlasmodium falciparumMalaria

4. In vivo susceptibility of Plasmodium falciparum to artesunate in Binh Phuoc Province, Vietnam

5. Dihydroartemisinin–Piperaquine Failure in Cambodia

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