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Arzneimittelforschung ; 46(10): 981-5, 1996 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-8931892

RESUMO

A series of 2-aminomethyl-3-aryl-5,6,7,8-tetrahydrobenzo(b)/5,6-dimethylthieno (2,3-d) pyrimidin-4-ones (IX) were prepared by the displacement reaction between various amines and 2-chloromethyl-3-aryl-5,6, 7,8-tetrahydrobenzo(b)/5, 6-dimethylthieno(2, 3-d) pyrimidin-4-ones (VIII), which are obtained by the cyclization of corresponding chloroacetylamino derivatives (VII) under acidic condition. Compounds VII were obtained by the interaction of VI and chloroacetylchloride in glacial acetic acid. Compounds VIII were converted to corresponding 2-acetoxymethyl derivatives (X) with potassium acetate in glacial acetic acid. Selected compounds were screened for antihyperlipaemic activity in albino rats, whereby most of these compounds were found to be active. The serum cholesterol and triglyceride lowering activities exhibited by compounds 1 and 3 were found to be comparable to that of gemfibrozil. Compounds 1 and 3 were also found to be safe as indicated by their acute toxicity study.


Assuntos
Hipolipemiantes/síntese química , Pirimidinas/síntese química , Animais , Colesterol/sangue , Feminino , Genfibrozila/farmacologia , Hipolipemiantes/farmacologia , Hipolipemiantes/toxicidade , Dose Letal Mediana , Lipídeos/sangue , Masculino , Camundongos , Pirimidinas/farmacologia , Pirimidinas/toxicidade , Ratos , Ratos Wistar , Triglicerídeos/sangue
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