Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century

…, PA Winstanley, A Mukhtar, R Bonar-Law…

文献索引：O'Neill, Paul M.; Park, B. Kevin; Shone, Alison E.; Maggs, James L.; Roberts, Phillip; Stocks, Paul A.; Biagini, Giancarlo A.; Bray, Patrick G.; Gibbons, Peter; Berry, Neil; Winstanley, Peter A.; Mukhtar, Amira; Bonar-Law, Richard; Hindley, Stephen; Bambal, Ramesh B.; Davis, Charles B.; Bates, Martin; Hart, Timothy K.; Gresham, Stephanie L.; Lawrence, Ron M.; Brigandi, Richard A.; Gomez-delas-Heras, Federico M.; Gargallo, Domingo V.; Ward, Stephen A. Journal of Medicinal Chemistry, 2009 , vol. 52, # 5 p. 1408 - 1415

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被引用次数: 58

摘要

N-tert-Butyl isoquine (4)(GSK369796) is a 4-aminoquinoline drug candidate selected and developed as part of a public− private partnership between academics at Liverpool, MMV, and GSK pharmaceuticals. This molecule was rationally designed based on chemical, toxicological, pharmacokinetic, and pharmacodynamic considerations and was selected based on excellent activity against Plasmodium falciparum in vitro and rodent malaria ...