Quinazoline derivatives with antitubercular activity
Language English Country France Media print
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
11204949
DOI
10.1016/s0014-827x(00)00100-2
PII: S0014-827X(00)00100-2
Knihovny.cz E-resources
- MeSH
- Alkylation MeSH
- Antitubercular Agents chemical synthesis pharmacology MeSH
- Quinazolines chemical synthesis pharmacology MeSH
- Mass Spectrometry MeSH
- Magnetic Resonance Spectroscopy MeSH
- Microbial Sensitivity Tests MeSH
- Mycobacterium drug effects MeSH
- Spectrophotometry, Infrared MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- Antitubercular Agents MeSH
- Quinazolines MeSH
4-Quinazolinol was prepared by the reaction of anthranilic acid and formamide. The hydroxy group was converted into the thiol function by treatment with phosphorus(V)sulfide, and the subsequent alkylation of the thiol group was carried out with alkylhalides under the conditions of phase-transfer catalysis. The structure of the substances was confirmed by 1H, 13C NMR, IR, and MS. Most of the synthesized compounds exhibited antimycobacterial activity against the strains of Mycobacterium tuberculosis, Mycobacerium avium, Mycobacterium fortuitum, Mycobacterium kansasii and Mycobacterium intracellulare. 4-(S-Butylthio)quinazoline (3c) was even more active than isoniazide against atypical strains of mycobacteria.
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