Candidate Selection and Preclinical Evaluation of N-tert-Butyl Isoquine (GSK369796), An Affordable and Effective 4-Aminoquinoline Antimalarial for the 21st Century

Author:

O’Neill Paul M.1,Park B. Kevin1,Shone Alison E.1,Maggs James L.1,Roberts Phillip1,Stocks Paul A.1,Biagini Giancarlo A.1,Bray Patrick G.1,Gibbons Peter1,Berry Neil1,Winstanley Peter A.1,Mukhtar Amira1,Bonar-Law Richard1,Hindley Stephen1,Bambal Ramesh B.1,Davis Charles B.1,Bates Martin1,Hart Timothy K.1,Gresham Stephanie L.1,Lawrence Ron M.1,Brigandi Richard A.1,Gomez-delas-Heras Federico M.1,Gargallo Domingo V.1,Ward Stephen A.1

Affiliation:

1. Department of Chemistry, University of Liverpool, Liverpool, L69 7ZD, United Kingdom, University of Liverpool, MRC Centre for Drug Safety Science, Department of Pharmacology, School of Biomedical Sciences, University of Liverpool, Liverpool L69 3GE, United Kingdom, Liverpool School of Tropical Medicine, Pembroke Place, Liverpool L3 5QA, United Kingdom, Drug Metabolism and Pharmacokinetics, GlaxoSmithKline Drug Discovery, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, GlaxoSmithKline,...

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Reference37 articles.

1. Medical need, scientific opportunity and the drive for antimalarial drugs

2. For a discussion of how chloroquine resistance may have evolved:

3. A Requiem for Chloroquine

4. A critical role for PfCRT K76T in Plasmodium falciparum verapamil-reversible chloroquine resistance

5. For phase 1 studies on the chloroquine analogue AQ13, see:

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