Publication details
Antimicrobial effect of salicylamide derivatives against intestinal sulfate-reducing bacteria
| Authors | |
|---|---|
| Year of publication | 2016 |
| Type | Article in Periodical |
| Magazine / Source | Journal of Applied Biomedicine |
| MU Faculty or unit | |
| Citation | |
| Web | http://dx.doi.org/10.1016/j.jab.2016.01.005 |
| Doi | http://dx.doi.org/10.1016/j.jab.2016.01.005 |
| Field | Microbiology, virology |
| Keywords | Sulfate-reducing bacteria; Desulfovibrio piger; Desulfomicrobium sp.; Salicylamides; Bowel disease; Lipophilicity; Structure–activity relationships |
| Description | Sulfate-reducing bacteria (SRB) are most likely involved in both the initiation and maintenance of inflammatory bowel disease (IBD); unfortunately present antibacterial chemotherapeutics used in the treatment of IBD have been ineffective. Thus, the antimicrobial activity of salicylamide derivatives against two different genera of intestinal SRB, Desulfovibrio and Desulfomicrobium, was investigated. Six 2-(phenylcarbamoyl)phenyl N-[(benzyloxy)carbonyl]alkanoates and three 2-hydroxy-N-[(2S)-1-oxo-1-(phenylamino)alkan-2-yl]benzamides showed MIC values in the range from 0.22 to 0.35 microM against Desulfovibrio piger Vib-7 and in the range from 0.27 to 8.52 microM against Desulfomicrobium sp. Rod-9, while MIC values of ciprofloxacin were 41.2 microM and 39.3 microM. The highest potency against the two strains was observed for 4-chloro-N-{(2S)-1-[(3,4-dichlorophenyl)amino]-3-methyl-1-oxobutan-2-yl}-2-hydroxybenzamide (MIC 0.22 microM and 0.27 microM). 4-Chloro-2-[(4-nitrophenyl)carbamoyl]phenyl (2S)-2-{[(benzyloxy)carbonyl]amino}-3-methylbutanoate showed high activity against D. piger Vib-7 (MIC = 0.26 microM), while 4-chloro-2-[(4-methylphenyl)carbamoyl]phenyl (2S)-2-[(tert-butoxycarbonyl)amino]-3-(1H-indol-2-yl)propanoate expressed high activity against Desulfomicrobium sp. Rod-9 (MIC = 0.31 microM). Structure–activity relationships are discussed. |