Abstract
The high throughput screening of two chemical libraries against Mycobacterium tuberculosis led to the design of hybrid compounds by using nitrile oxide cycloaddition chemistry. One of the hybrids shows an excellent MIC against M. tuberculosis H37Rv. As this molecule shows no CYP3A4 inhibition and a maximum tolerated dose of ≥200 mgkg-1 po in mice, it represents a potential drug candidate for TB therapy. (Chemical Equation Presented)
Original language | English (US) |
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Pages (from-to) | 811-813 |
Number of pages | 3 |
Journal | ChemMedChem |
Volume | 2 |
Issue number | 6 |
DOIs | |
State | Published - Jun 11 2007 |
Externally published | Yes |
Keywords
- Isoxazole
- MIC
- Mefloquine
- Nitrile oxide cycloaddition
- Tuberculosis
ASJC Scopus subject areas
- Biochemistry
- Molecular Medicine
- Pharmacology
- Drug Discovery
- Pharmacology, Toxicology and Pharmaceutics(all)
- Organic Chemistry