Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
Synthesis and Pharmacological Activities of Novel Bicyclic Thiazoline Derivatives as Hepatoprotective Agents. II. (7-Alkoxycarbonyl-2, 3, 5, 6-tetrahydropyrrolo[2, 1-b]thiazol-3-ylidene)acetamide Derivatives
Masashi HASEGAWAAtsushi NAKAYAMAShuichi YOKOHAMAToru HOSOKAMIYoichi KUREBAYASHITakuya IKEDAYoshimasa SHIMOTOShoichiro IDEYuko HONDANorio SUZUKI
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1995 Volume 43 Issue 7 Pages 1125-1131

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Abstract

A series of exomethylenic bicyclic thiazoline derivatives (3a-i) was synthesized and evaluated for hepatoprotective activity against galactosamine-induced and monoclonal antibody-induced acute liver injuries in rats. The structure-activity relationships were investigated. Among the compounds synthesized, N-methyl-(7-isopropoxycarbonyl-6, 6-dimethyl-2, 3, 5, 6-tetrahydropyrrolo[2, 1-b]thiazol-3-ylidene)acetamide (3i) exhibited the most potent hepatoprotective activity. This compound suppressed galactosamine-induced hepatic injury at 100 mg/kg by oral administration and further prevented monoclonal antibody-induced hepatic injury at 30 mg/kg by intraperitoneal injection, as judged from the changes in serum transaminase activities.

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