Antiulcer agents. 1. Gastric antisecretory and cytoprotective properties of substituted imidazo[1,2-a]pyridines
作者:James J. Kaminski、James A. Bristol、Chester Puchalski、Raymond G. Lovey、Arthur J. Elliott、Henry Guzik、Daniel M. Solomon、David J. Conn、Martin S. Domalski
DOI:10.1021/jm00145a006
日期:1985.7
A novel class of antiulcer agents, the substituted imidazo[1,2-a]pyridines, is described. The present compounds are not histamine (H2) receptor antagonists nor are they prostaglandin analogues, yet they exhibit both gastric antisecretory and cytoprotective properties. The mechanism of gastric antisecretory activity may involve inhibition of the H+/K+-ATPase enzyme. Structure-activity studies led to
描述了新型的抗溃疡剂,取代的咪唑并[1,2-a]吡啶。本发明的化合物既不是组胺(H 2)受体拮抗剂,也不是前列腺素类似物,但它们既具有胃分泌作用又具有细胞保护作用。胃抗分泌活性的机制可能涉及抑制H + / K + -ATPase酶。结构活性研究导致鉴定出3-(氰基甲基)-2-甲基-8-(苯甲氧基)咪唑并[1,2-a]吡啶,SCH 28080(27),已被选择用于进一步开发和临床评价。