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抗溃疡药物研究。IV。咪唑并[1,2 - a]吡啶基乙基苯并噻唑类和苯并咪唑类的合成及抗溃疡活性。

Studies on antiulcer drugs. IV. Synthesis and antiulcer activities of imidazo[1,2-a]pyridinylethylbenzothiazoles and -benzimidazoles.

作者信息

Katsura Y, Inoue Y, Nishino S, Tomoi M, 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 Jul;40(7):1818-22. doi: 10.1248/cpb.40.1818.

Abstract

A series of 6-[2-(imidazo[1,2-a]pyridin-2-yl)ethyl]benzothiazoles (II) and benzimidazole analogues (III) was synthesized and tested for histamine H2-receptor antagonist, gastric antisecretory and anti-stress ulcer activity. A benzimidazole derivative (IIIa) exhibited strong antisecretory activity, whereas the corresponding benzothiazole derivative (IIb) lacked this potency in in vivo test. In contrast to compound IIIa, however, compound IIb demonstrated good inhibition against stress induced ulcer. The structure-activity relationships of these compounds are discussed.

摘要

合成了一系列6-[2-(咪唑并[1,2-a]吡啶-2-基)乙基]苯并噻唑(II)和苯并咪唑类似物(III),并对其进行组胺H2受体拮抗剂、胃抗分泌和抗应激溃疡活性测试。一种苯并咪唑衍生物(IIIa)表现出较强的抗分泌活性,而相应的苯并噻唑衍生物(IIb)在体内试验中缺乏这种效力。然而,与化合物IIIa相比,化合物IIb对应激诱导的溃疡表现出良好的抑制作用。讨论了这些化合物的构效关系。

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