Metronidazole-deoxybenzoin derivatives as anti-Helicobacter pylori agents with potent inhibitory activity against HPE-induced interleukin-8.
A series of new metronidazole-deoxybenzoin derivatives were synthesized and evaluated for their antimicrobial activity against Helicobacter pylori. Highly selective anti-H. pylori activity was also observed in synthesized compounds. Compound 34 exhibited the most potent activity, similar to the positive control amoxicillin. Furthermore, compounds 17 and 34 were able to significantly decrease H. pylori water extract (HPE)-induced production of interleukin-8 (IL-8) in gastric mucosal cells, which did not show any effect on the cell viability.
Luo
Yin
Y
State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, PR China.
Li
Huan-Qiu
HQ
Zhou
Yang
Y
Li
Zi-Lin
ZL
Yan
Tao
T
Zhu
Hai-Liang
HL
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D001573:Benzoin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D005753:Gastric Mucosa / Q000166:cytology / Q000378:metabolism; D016480:Helicobacter pylori / Q000187:drug effects*; D007093:Imidazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D016209:Interleukin-8 / Q000037:antagonists & inhibitors / Q000378:metabolism*; D008795:Metronidazole / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
C552829:1-(2,3-dihydroxy-4-(2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethoxy)phenyl)-2-(4-nitrophenyl)ethanone; D000900:Anti-Bacterial Agents; D007093:Imidazoles; D016209:Interleukin-8; D008795:Metronidazole; C492807:deoxybenzoin; D001573:Benzoin