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
| Autor: | Yoichi Kurebayashi, Shoichiro Ide, Norio Suzuki, Takuya Ikeda, Hasegawa Masashi, Yuko Honda, Atsushi Nakayama, Toru Hosokami, Yoshimasa Shimoto |
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| Rok vydání: | 1995 |
| Předmět: |
Male
Stereochemistry medicine.medical_treatment Intraperitoneal injection Thiazines Chemical synthesis Rats Sprague-Dawley chemistry.chemical_compound Structure-Activity Relationship Thiazine Drug Discovery medicine Structure–activity relationship Animals Hepatoprotective Agent Bicyclic molecule Chemistry Thiazoline Liver Diseases Antibodies Monoclonal General Chemistry General Medicine Rats Thiazoles Liver Toxicity |
| Zdroj: | Chemicalpharmaceutical bulletin. 43(1) |
| ISSN: | 0009-2363 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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