Literature DB >> 26856849

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

Marina Chavchich1, Geoffrey W Birrell1, Arba L Ager2, Donna O MacKenzie1, Gavin D Heffernan3, Guy A Schiehser3, Laura R Jacobus3, G Dennis Shanks1, David P Jacobus3, Michael D Edstein4.   

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.
Copyright © 2016, American Society for Microbiology. All Rights Reserved.

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Year:  2016        PMID： 26856849      PMCID： PMC4862471          DOI： 10.1128/AAC.03066-15

Source DB:  PubMed          Journal:  Antimicrob Agents Chemother        ISSN： 0066-4804            Impact factor:   5.191


  17 in total

1.  Clinical studies of atovaquone, alone or in combination with other antimalarial drugs, for treatment of acute uncomplicated malaria in Thailand.

Authors:  S Looareesuwan; C Viravan; H K Webster; D E Kyle; D B Hutchinson; C J Canfield
Journal:  Am J Trop Med Hyg       Date:  1996-01       Impact factor: 2.345

2.  Dihydroartemisinin-piperaquine failure in Cambodia.

Authors:  David L Saunders; Pattaraporn Vanachayangkul; Chanthap Lon
Journal:  N Engl J Med       Date:  2014-07-31       Impact factor: 91.245

3.  Spiroindolones, a potent compound class for the treatment of malaria.

Authors:  Matthias Rottmann; Case McNamara; Bryan K S Yeung; Marcus C S Lee; Bin Zou; Bruce Russell; Patrick Seitz; David M Plouffe; Neekesh V Dharia; Jocelyn Tan; Steven B Cohen; Kathryn R Spencer; Gonzalo E González-Páez; Suresh B Lakshminarayana; Anne Goh; Rossarin Suwanarusk; Timothy Jegla; Esther K Schmitt; Hans-Peter Beck; Reto Brun; Francois Nosten; Laurent Renia; Veronique Dartois; Thomas H Keller; David A Fidock; Elizabeth A Winzeler; Thierry T Diagana
Journal:  Science       Date:  2010-09-03       Impact factor: 47.728

4.  A technique for the selection of long-acting antimalarial compounds using a rodent malaria model.

Authors:  P Schofield; R E Howells; W Peters
Journal:  Ann Trop Med Parasitol       Date:  1981-10

5.  JPC-2997, a new aminomethylphenol with high in vitro and in vivo antimalarial activities against blood stages of Plasmodium.

Authors:  Geoffrey W Birrell; Marina Chavchich; Arba L Ager; Hong-Ming Shieh; Gavin D Heffernan; Wenyi Zhao; Peter E Krasucki; Kurt W Saionz; Jacek Terpinski; Guy A Schiehser; Laura R Jacobus; G Dennis Shanks; David P Jacobus; Michael D Edstein
Journal:  Antimicrob Agents Chemother       Date:  2014-10-20       Impact factor: 5.191

6.  Identification of an antimalarial synthetic trioxolane drug development candidate.

Authors:  Jonathan L Vennerstrom; Sarah Arbe-Barnes; Reto Brun; Susan A Charman; Francis C K Chiu; Jacques Chollet; Yuxiang Dong; Arnulf Dorn; Daniel Hunziker; Hugues Matile; Kylie McIntosh; Maniyan Padmanilayam; Josefina Santo Tomas; Christian Scheurer; Bernard Scorneaux; Yuanqing Tang; Heinrich Urwyler; Sergio Wittlin; William N Charman
Journal:  Nature       Date:  2004-08-19       Impact factor: 49.962

7.  Reduced artemisinin susceptibility of Plasmodium falciparum ring stages in western Cambodia.

Authors:  Benoit Witkowski; Nimol Khim; Pheaktra Chim; Saorin Kim; Sopheakvatey Ke; Nimol Kloeung; Sophy Chy; Socheat Duong; Rithea Leang; Pascal Ringwald; Arjen M Dondorp; Rupam Tripura; Françoise Benoit-Vical; Antoine Berry; Olivier Gorgette; Frédéric Ariey; Jean-Christophe Barale; Odile Mercereau-Puijalon; Didier Menard
Journal:  Antimicrob Agents Chemother       Date:  2012-12-03       Impact factor: 5.191

8.  Plasmodium falciparum: cloning by single-erythrocyte micromanipulation and heterogeneity in vitro.

Authors:  A M Oduola; N F Weatherly; J H Bowdre; R E Desjardins
Journal:  Exp Parasitol       Date:  1988-06       Impact factor: 2.011

9.  Artemisinin resistance in Plasmodium falciparum malaria.

Authors:  Arjen M Dondorp; François Nosten; Poravuth Yi; Debashish Das; Aung Phae Phyo; Joel Tarning; Khin Maung Lwin; Frederic Ariey; Warunee Hanpithakpong; Sue J Lee; Pascal Ringwald; Kamolrat Silamut; Mallika Imwong; Kesinee Chotivanich; Pharath Lim; Trent Herdman; Sen Sam An; Shunmay Yeung; Pratap Singhasivanon; Nicholas P J Day; Niklas Lindegardh; Duong Socheat; Nicholas J White
Journal:  N Engl J Med       Date:  2009-07-30       Impact factor: 91.245

10.  Development of cultured Plasmodium falciparum blood-stage malaria cell banks for early phase in vivo clinical trial assessment of anti-malaria drugs and vaccines.

Authors:  Danielle I Stanisic; Xue Q Liu; Sai Lata De; Michael R Batzloff; Tanya Forbes; Christopher B Davis; Silvana Sekuloski; Marina Chavchich; Wendy Chung; Katharine Trenholme; James S McCarthy; Tao Li; B Kim Lee Sim; Stephen L Hoffman; Michael F Good
Journal:  Malar J       Date:  2015-04-07       Impact factor: 2.979
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  7 in total

1.  Characterization of the Preclinical Pharmacology of the New 2-Aminomethylphenol, JPC-3210, for Malaria Treatment and Prevention.

Authors:  Geoffrey W Birrell; Gavin D Heffernan; Guy A Schiehser; John Anderson; Arba L Ager; Pablo Morales; Donna MacKenzie; Karin van Breda; Marina Chavchich; Laura R Jacobus; G Dennis Shanks; David P Jacobus; Michael D Edstein
Journal:  Antimicrob Agents Chemother       Date:  2018-03-27       Impact factor: 5.191

2.  In Vivo Efficacy and Pharmacokinetics of the 2-Aminomethylphenol Antimalarial JPC-3210 in the Aotus Monkey-Human Malaria Model.

Authors:  Fiona J McCallum; Geoffrey W Birrell; Marina Chavchich; Ivor Harris; Nicanor Obaldia; Karin Van Breda; Gavin D Heffernan; David P Jacobus; Dennis Shanks; Michael D Edstein
Journal:  Antimicrob Agents Chemother       Date:  2020-02-21       Impact factor: 5.191

3.  Multi-omic Characterization of the Mode of Action of a Potent New Antimalarial Compound, JPC-3210, Against Plasmodium falciparum.

Authors:  Geoffrey W Birrell; Matthew P Challis; Amanda De Paoli; Dovile Anderson; Shane M Devine; Gavin D Heffernan; David P Jacobus; Michael D Edstein; Ghizal Siddiqui; Darren J Creek
Journal:  Mol Cell Proteomics       Date:  2019-12-13       Impact factor: 5.911

Review 4.  Recent metabolomic developments for antimalarial drug discovery.

Authors:  Lúcia Mamede; Fanta Fall; Matthieu Schoumacher; Allison Ledoux; Pascal De Tullio; Joëlle Quetin-Leclercq; Michel Frédérich
Journal:  Parasitol Res       Date:  2022-10-04       Impact factor: 2.383

5.  Comparison of the Pharmacokinetics and Ex Vivo Antimalarial Activities of Artesunate-Amodiaquine and Artemisinin-Piperaquine in Healthy Volunteers for Preselection Malaria Therapy.

Authors:  Nguyen Ngoc Quang; Marina Chavchich; Chu Xuan Anh; Geoffrey W Birrell; Karin van Breda; Thomas Travers; Kerryn Rowcliffe; Michael D Edstein
Journal:  Am J Trop Med Hyg       Date:  2018-05-03       Impact factor: 2.345

6.  Arylmethylamino steroids as antiparasitic agents.

Authors:  Reimar Krieg; Esther Jortzik; Alice-Anne Goetz; Stéphanie Blandin; Sergio Wittlin; Mourad Elhabiri; Mahsa Rahbari; Selbi Nuryyeva; Kerstin Voigt; Hans-Martin Dahse; Axel Brakhage; Svenja Beckmann; Thomas Quack; Christoph G Grevelding; Anthony B Pinkerton; Bruno Schönecker; Jeremy Burrows; Elisabeth Davioud-Charvet; Stefan Rahlfs; Katja Becker
Journal:  Nat Commun       Date:  2017-02-17       Impact factor: 14.919

Review 7.  Drugs in Development for Malaria.

Authors:  Elizabeth A Ashley; Aung Pyae Phyo
Journal:  Drugs       Date:  2018-06       Impact factor: 9.546
  7 in total

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