Metronidazole–Deoxybenzoin Derivatives as Anti‐Helicobacter pylori Agents with Potent Inhibitory Activity against HPE‐Induced Interleukin‐8

Abstract

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.

Microwave-Assisted Efficient Synthesis of 2-Hydroxydeoxybenzoins from the Alkali Degradation of Readily Prepared 3-Aryl-4-hydroxycoumarins in Water

“…Among the various methods to date, classic methods, such as Hoesch reactions, 20,21) Nencki reactions 22,23) and FriedelCrafts acylation reactions 24,25) of polyphenols with substituted phenylacetonitriles or phenylacetic acids are attractive for the ready synthesis of polyhydroxydeoxybenzoins. However, these methods are only applicable for symmetrical polyphenols, such as resorcinol, phloroglucinol, benzene-1,2,3-triol, pyrocatechol and hydroquinone.…”