Design, synthesis, and pharmacological investigation of iodined salicylimines, new prototypes of antimicrobial drug candidates.
A series of 3,5-diiodo-salicylalidene Schiff bases (compounds 1-35) has been synthesized and tested for antimicrobial activity. The compounds were assayed for antibacterial activities by the MTT method. Some of the compounds inhibit the growth of a broad range of bacteria including the species of Bacillus subtilis, Staphylococcus aureus, Streptococcus faecalis, Pseudomonas aeruginosa, Escherichia coli, and Enterobacter cloacae. Among them, compounds 2-[(4-chloro-phenylimino)methyl]-4,6-diiodo-phenol 11 and 2,4-diiodo-6-[(2-morpholin-4-yl-ethylimino)methyl]phenol 19 showed the most potent antibacterial activity with MIC of 3.1, 12.9, 3.3, 6.5, 12.9, 3.3 and 3.2, 12.8, 3.2, 12.8, 12.8, 3.2 muM against B. subtilis, S. aureus, S. faecalis, P. aeruginosa, E. Coli, and E. cloacae, respectively.
Key Laboratory of Anhai Educational Department, Anhai University of Technology, Maanshan, P.R. China.
Suo-Ping
SP
Xu
Peng-Cheng
PC
Lv
Lei
L
Shi
Hai-Liang
HL
Zhu
D000447:Aldehydes / Q000737:chemistry*; D000588:Amines / Q000737:chemistry*; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D015195:Drug Design; D054879:Halogenation; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D012545:Schiff Bases / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000447:Aldehydes; D000588:Amines; D000900:Anti-Bacterial Agents; D012545:Schiff Bases; C013243:salicylaldehyde