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抗溃疡药物的研究。III. 咪唑并[1,2-a]吡啶基乙基苯并恶唑类及相关化合物的合成与抗溃疡活性。一类新型组胺H2受体拮抗剂。

Studies on antiulcer drugs. III. Synthesis and antiulcer activities of imidazo[1,2-a]pyridinylethylbenzoxazoles and related compounds. A novel class of histamine H2-receptor antagonists.

作者信息

Katsura Y, Inoue Y, Nishino S, Tomoi M, Itoh H, Takasugi H

机构信息

New Drug Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Osaka, Japan.

出版信息

Chem Pharm Bull (Tokyo). 1992 Jun;40(6):1424-38. doi: 10.1248/cpb.40.1424.

DOI:10.1248/cpb.40.1424
PMID:1356641
Abstract

A series of imidazo[1,2-a]pyridinylalkylbenzoxazole derivatives was synthesized and tested for histamine H2-receptor antagonist, gastric antisecretory and antiulcer activities. Some of 2-amino-6-[2-(imidazo[1,2-a]pyridin-2-yl)ethyl]benzoxazole derivatives were found to have good pharmacological activities. Among them, 2-amino-6-[2-(7-methoxy-3-methylimidazo[1,2-a]pyridin-2-yl)ethyl] benzoxazole (II-11) and 2-acetamido-6-[2-(7-methylimidazo[1,2-a]pyridin-2-yl)ethyl] benzoxazole (II-38) showed potent antisecretory and cytoprotective activity. The structure-activity relationships of these compounds are discussed.

摘要

合成了一系列咪唑并[1,2 - a]吡啶基烷基苯并恶唑衍生物，并对其进行组胺H2受体拮抗剂、胃抗分泌和抗溃疡活性测试。发现一些2 - 氨基 - 6 - [2 - (咪唑并[1,2 - a]吡啶 - 2 - 基)乙基]苯并恶唑衍生物具有良好的药理活性。其中，2 - 氨基 - 6 - [2 - (7 - 甲氧基 - 3 - 甲基咪唑并[1,2 - a]吡啶 - 2 - 基)乙基]苯并恶唑（II - 11）和2 - 乙酰氨基 - 6 - [2 - (7 - 甲基咪唑并[1,2 - a]吡啶 - 2 - 基)乙基]苯并恶唑（II - 38）表现出强效的抗分泌和细胞保护活性。讨论了这些化合物的构效关系。

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