Anti-Ulcer/Cytoprotective: The Gastric Anti-Ulcer Activity of 2-Carboxyalkoxychalcone Derivatives

Summary

Novelty: Cytoprotective and antisecretory properties are claimed for new carboxyalkoxy chalcones as is their use in anti-ulcer therapy. The compounds are related to previously described chalcones such as sofalcone.

Biology: Biological activity is presented for three assays. In the stress-induced rat model, sixty-six compounds show inhibition of ulceration up to 93%, at 50 mg/kg, po. In a rat gastric mucosal protection assay four compounds are inhibitory up to 84%, at 50 mg/kg, and in a 2-DG induced antisecretory assay (rat, ip), one compound (below) gives 54% inhibition, at 30 mg/kg; five control chalcones are less active.

Chemistry: Two reaction schemes and fifty-seven examples detail the synthetic methodology, with many compounds appearing in tabular form. The compound tested in the 2-DG assay is 4-t-butyl-2-carboxymethoxy-4′-(3-methyl-2-butenyloxy)chalcone.