A new aminomethylphenol , JPC - 2997 , with 1 high in vitro and in vivo antimalarial 2 activity against blood stages of 3 Plasmodium
نویسندگان
چکیده
5 Geoffrey W. Birrell, Marina Chavchich, Arba L. Ager, Hong-Ming 6 Shieh, Gavin D. Heffernan, Wenyi Zhao, Peter E. Krasucki, Kurt W. 7 Saionz2, Jacek Terpinski2, Guy A. Schiehser2, Laura R. Jacobus2, G. 8 Dennis Shanks1, David P. Jacobus2 and Michael D. Edstein1* 9 10 Department of Drug Evaluation, Australian Army Malaria Institute, Enoggera, 11 Brisbane, Queensland 4051, Australia 12 Jacobus Pharmaceutical Company, Princeton, New Jersey, USA 13 University of Miami, Miami, Florida, USA 14 15 *Corresponding author: 16 Dr Mike Edstein; Telephone: +61-7-33324930; Fax: +61-7-33324800 and E17 mail: [email protected] 18 # These authors contributed equally to this study 19 20 Short Running Title: A new aminomethylphenol effective against Plasmodium 21 22
منابع مشابه
JPC-2997, a new aminomethylphenol with high in vitro and in vivo antimalarial activities against blood stages of Plasmodium.
4-(tert-Butyl)-2-((tert-butylamino)methyl)-6-(6-(trifluoromethyl)pyridin-3-yl)-phenol (JPC-2997) is a new aminomethylphenol compound that is highly active in vitro against the chloroquine-sensitive D6, the chloroquine-resistant W2, and the multidrug-resistant TM90-C2B Plasmodium falciparum lines, with 50% inhibitory concentrations (IC50s) ranging from 7 nM to 34 nM. JPC-2997 is >2,500 times les...
متن کاملLead Selection of a New Aminomethylphenol, JPC-3210, for Malaria Treatment and Prevention.
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...
متن کاملEvaluation of the 2-Aminomethylphenol JPC-2997 in Aotus Monkeys Infected with Plasmodium falciparum.
Previously, we reported JPC-2997 [4-(tert-Butyl)-2-((tertbutylamino)methyl)-6-(6-(trifluoromethyl)pyridin-3-yl)phenol] to possess high in vitro antimalarial activity against Plasmodium falciparum lines, low cytotoxicity in mammalian cell lines, a long blood elimination half-life in Aotus monkeys (10.8 days), and potent in vivo efficacy against animal malaria models (1). Herein, as planned by Bi...
متن کاملAntimalarial evaluation of selected medicinal plant extracts used in Iranian traditional medicine
Objective(s): In an attempt to discover new natural active extracts against malaria parasites, the present study evaluated the antiplasmodial properties of selected plants based on Iranian traditional medicine. Materials and Methods: Ten plant species found in Iran were selected and collected based on the available literature about the Iranian traditional medicine. The methanolic extracts of th...
متن کاملAntiplasmodial activity and cytotoxicity of ethanol extract of Zea mays root
Objective:Zea mays root decoction that has been traditionally used for the treatment of malaria by various tribes in Nigeria, was evaluated for antimalarial potential against malaria parasites using in vivo and in vitro models. Materials and Methods: The root extract of Zea mays was investigated for antimalarial activity against Plasmodium berghei in mice using rodent malaria models; suppressiv...
متن کامل