Mario Bianchi

Gastric anti-secretory, anti-ulcer and cytoprotective properties of substituted (E)-4-phenyl- and heteroaryl-4-oxo-2-butenoic acids

Abstract A class of anti-secretory, anti-ulcer and cytoprotective agents, the substituted (E) -4-phenyl and heteroaryl-4-oxo-2-butenoic acids, is described. This chemical structure is not related to those of any known anti-cholinergic drugs, histamine H 2 -receptor antagonists or prostaglandins. Five compounds, 4-(2-methoxyphenyl)- 15 , 4-(4-methoxyphenyl)- 22 , 4-(3,4-dimethoxyphenyl)- 32 , 4-(3,4,5-trimethoxyphenyl)- 40 , and 4-(2-furanyl)-4-oxo-2-butenoic acid 44 , have cytoprotective activity at a very low dose (0.6 mg/kg, p.o. ) and anti-secretory and anti-ulcer activities at higher doses. One of these compounds, RU 38086 40 , has been selected for clinical evaluation.