Assessment of a pretomanid analogue library for African trypanosomiasis: Hit-to-lead studies on 6-substituted 2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]thiazine 8-oxides.

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Title

Assessment of a pretomanid analogue library for African trypanosomiasis: Hit-to-lead studies on 6-substituted 2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]thiazine 8-oxides.

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Description

A 900 compound nitroimidazole-based library derived from our pretomanid backup program with TB Alliance was screened for utility against human African trypanosomiasis (HAT) by the Drugs for Neglected Diseases initiative. Potent hits included 2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]thiazine 8-oxides, which surprisingly displayed good metabolic stability and excellent cell permeability. Following comprehensive mouse pharmacokinetic assessments on four hits and determination of the most active...

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Format

Research paper

Research format

Journal article

Date created

2018-01

Creator

Thompson, Andrew / Marshall, Andrew J / Maes, Louis / Yarlett, Nigel / Bacchi, Cyrus J / Gaukel, Eric / Wring, Stephen A / Launay, Delphine / Braillard, Stephanie / Chatelain, Eric / Mowbray, Charles E / Denny, William

URL

http://hdl.handle.net/2292/42407

Related subjects

Animals / Humans / Mice / Trypanosomiasis, African / Disease Models, Animal / Nitroimidazoles / Administration, Oral / Molecular Structure / Structure-Activity Relationship / Dose-Response Relationship, Drug / Small Molecule Libraries

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