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. I. 8-Ethoxycarbonyl-5, 6-dihydrothiazolo[2, 3-c][1, 4]thiazine Derivatives
Masashi HASEGAWA, Atsushi NAKAYAMA, Toru HOSOKAMI, Yoichi KUREBAYASHI, Takuya IKEDA, Yoshimasa SHIMOTO, Shoichiro IDE, Yuko HONDA, Norio SUZUKI
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Keywords: ethyl 5, 6-dihydrothiazolo[2, 3-c][1, 4]thiazine-8-carboxylate, bicyclic thiazoline, hepatoprotective agent, galactosamine-induced hepatic injury, monoclonal antibody-induced hepatic injury, structure-activity relationship
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1995 Volume 43 Issue 1 Pages 78-83

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Abstract

A series of bicyclic thiazoline derivatives (4a-s) 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, ethyl 3-(N-methylcarbamoyl)-5, 6-dihydrothiazolo[2, 3-c][1, 4]thiazine-8-carboxylate (4p) exhibited remarkable hepatoprotective activity and lower toxicity. This compound suppressed galactosamine-induced hepatic injury at 100 mg/kg by gavage and further prevented monoclonal antibody-induced hepatic injury at 30 mg/kg by intraperitoneal injection, as evaluated by measuring changes in serum transaminase activities.

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© The Pharmaceutical Society of Japan
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