Literature DB >> 20097070

Structure-activity relationships amongst 4-position quinoline methanol antimalarials that inhibit the growth of drug sensitive and resistant strains of Plasmodium falciparum.

Erin Milner1, William McCalmont, Jayendra Bhonsle, Diana Caridha, Dustin Carroll, Sean Gardner, Lucia Gerena, Montip Gettayacamin, Charlotte Lanteri, Thulan Luong, Victor Melendez, Jay Moon, Norma Roncal, Jason Sousa, Anchalee Tungtaeng, Peter Wipf, Geoffrey Dow.   

Abstract

Utilizing mefloquine as a scaffold, a next generation quinoline methanol (NGQM) library was constructed to identify early lead compounds that possess biological properties consistent with the target product profile for malaria chemoprophylaxis while reducing permeability across the blood-brain barrier. The library of 200 analogs resulted in compounds that inhibit the growth of drug sensitive and resistant strains of Plasmodium falciparum. Herein we report selected chemotypes and the emerging structure-activity relationship for this library of quinoline methanols. Published by Elsevier Ltd.

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Year:  2010        PMID： 20097070     DOI： 10.1016/j.bmcl.2010.01.001

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  11 in total

1.  Characterization of in vivo metabolites of WR319691, a novel compound with activity against Plasmodium falciparum.

Authors:  Erin Milner; Jason Sousa; Brandon Pybus; Victor Melendez; Sean Gardner; Kristina Grauer; Jay Moon; Dustin Carroll; Jennifer Auschwitz; Montip Gettayacamin; Patricia Lee; Susan Leed; William McCalmont; Suzanne Norval; Anchalee Tungtaeng; Qiang Zeng; Michael Kozar; Kevin D Read; Qigui Li; Geoffrey Dow
Journal:  Eur J Drug Metab Pharmacokinet       Date:  2011-07-13       Impact factor: 2.441

2.  A chemotype that inhibits three unrelated pathogenic targets: the botulinum neurotoxin serotype A light chain, P. falciparum malaria, and the Ebola filovirus.

Authors:  Igor Opsenica; James C Burnett; Rick Gussio; Dejan Opsenica; Nina Todorović; Charlotte A Lanteri; Richard J Sciotti; Montip Gettayacamin; Nicoletta Basilico; Donatella Taramelli; Jonathan E Nuss; Laura Wanner; Rekha G Panchal; Bogdan A Solaja; Sina Bavari
Journal:  J Med Chem       Date:  2011-01-25       Impact factor: 7.446

Review 3.  Recent advances in malaria drug discovery.

Authors:  Marco A Biamonte; Jutta Wanner; Karine G Le Roch
Journal:  Bioorg Med Chem Lett       Date:  2013-03-27       Impact factor: 2.823

4.  Anti-malarial activity of a non-piperidine library of next-generation quinoline methanols.

Authors:  Erin Milner; William McCalmont; Jayendra Bhonsle; Diana Caridha; Jose Cobar; Sean Gardner; Lucia Gerena; Duane Goodine; Charlotte Lanteri; Victor Melendez; Norma Roncal; Jason Sousa; Peter Wipf; Geoffrey Stuart Dow
Journal:  Malar J       Date:  2010-02-11       Impact factor: 2.979

5.  The use of a prodrug approach to minimize potential CNS exposure of next generation quinoline methanols while maintaining efficacy in in vivo animal models.

Authors:  Jason C Sousa; Erin Milner; Dustin Carroll; William McCalmont; Sean Gardner; Jay Moon; Jacob D Johnson; Patricia Lee; Jennifer Auschwitz; Norma Roncal; Diana Caridha; Anchalee Tungteung; Qiang Zeng; Sean Reyes; Bryan Smith; Qigui Li; Michael P Kozar; Victor Melendez; Geoffrey Dow
Journal:  Eur J Drug Metab Pharmacokinet       Date:  2014-04-07       Impact factor: 2.441

6.  Expanding the Antimalarial Drug Arsenal-Now, But How?

Authors:  Brian T Grimberg; Rajeev K Mehlotra
Journal:  Pharmaceuticals (Basel)       Date:  2011-05-01

7.  Central nervous system exposure of next generation quinoline methanols is reduced relative to mefloquine after intravenous dosing in mice.

Authors:  Geoffrey S Dow; Erin Milner; Ian Bathurst; Jayendra Bhonsle; Diana Caridha; Sean Gardner; Lucia Gerena; Michael Kozar; Charlotte Lanteri; Anne Mannila; William McCalmont; Jay Moon; Kevin D Read; Suzanne Norval; Norma Roncal; David M Shackleford; Jason Sousa; Jessica Steuten; Karen L White; Qiang Zeng; Susan A Charman
Journal:  Malar J       Date:  2011-06-06       Impact factor: 2.979

8.  A small-fish model for behavioral-toxicological screening of new antimalarial drugs: a comparison between erythro- and threo-mefloquine.

Authors:  Hans Maaswinkel; Liqun Zhu; Wei Weng
Journal:  BMC Res Notes       Date:  2015-04-02

9.  An oral quinoline derivative, MPT0B392, causes leukemic cells mitotic arrest and overcomes drug resistant cancer cells.

Authors:  Min-Wu Chao; Han-Li Huang; Wei-Chun HuangFu; Kai-Cheng Hsu; Yi-Min Liu; Yi-Wen Wu; Chao-Feng Lin; Yi-Lin Chen; Mei-Jung Lai; Hsueh-Yun Lee; Jing-Ping Liou; Che-Ming Teng; Chia-Ron Yang
Journal:  Oncotarget       Date:  2017-04-25

10.  Mefloquine targets the Plasmodium falciparum 80S ribosome to inhibit protein synthesis.

Authors:  Wilson Wong; Xiao-Chen Bai; Brad E Sleebs; Tony Triglia; Alan Brown; Jennifer K Thompson; Katherine E Jackson; Eric Hanssen; Danushka S Marapana; Israel S Fernandez; Stuart A Ralph; Alan F Cowman; Sjors H W Scheres; Jake Baum
Journal:  Nat Microbiol       Date:  2017-03-13       Impact factor: 17.745
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