期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 63, 期 9, 页码 4732-4748出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.0c00003
关键词
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资金
- Tres Cantos Open Lab Foundation [TC188]
- European Union's Seventh Framework Programme [291799]
- Canadian Institute of Health Research Grant [PJT-148646]
Screening of a GSK-proprietary library against intracellular Mycobacterium tuberculosis identified 1, a thioalkylbenzoxazole hit. Biological profiling and mutant analysis revealed that this compound is a prodrug that is bioactivated by the mycobacterial enzyme MymA. A hit-expansion program including design, synthesis, and profiling of a defined set of analogues with optimized drug-like properties led to the identification of an emerging lead compound, displaying potency against intracellular bacteria in the low micromolar range, high in vitro solubility and permeability, and excellent microsomal stability.
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