A series of eighteen novel esters of salicylanilides with benzenesulfonic acid were designed, synthesized and characterized by IR, ¹H-NMR and ¹³C-NMR. They were evaluated in vitro as potential antimycobacterial agents towards Mycobacterium tuberculosis, Mycobacterium avium and two strains of Mycobacterium kansasii. In general, the minimum inhibitory concentrations range from 1 to 500 µmol/L. The most active compound against M. tuberculosis was 4-chloro-2-(4-(trifluoromethyl)phenylcarbamoyl)-phenyl benzenesulfonate, with MIC of 1 µmol/L and towards M. kansasii its isomer 5-chloro-2-(4-(trifluoromethyl)phenylcarbamoyl)phenyl benzenesulfonate (MIC of 2-4 µmol/L). M. avium was the less susceptible strain. However, generally, salicylanilide benzenesulfonates did not surpass the activity of other salicylanilide esters with carboxylic acids.
- MeSH
- antibakteriální látky chemická syntéza chemie farmakologie MeSH
- benzensulfonáty chemická syntéza chemie farmakologie MeSH
- esterifikace MeSH
- estery chemická syntéza chemie farmakologie MeSH
- hydrofobní a hydrofilní interakce MeSH
- mikrobiální testy citlivosti MeSH
- Mycobacterium účinky léků MeSH
- racionální návrh léčiv MeSH
- salicylanilidy chemická syntéza chemie farmakologie MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
