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Synthesis and antihyperlipaemic activity of some 2-aminomethyl-3-aryl-5,6,7,8-tetrahydrobenzo(b)/5,6-dimethylthieno++ +(2,3- d) -pyrimidin-4-ones. 1996

A K Gadad, and S G Kapsi, and R I Anegundi, and S R Pattan, and C S Mahajanshetti, and C J Shishoo
Department of Medicinal Chemistry, College of Pharmacy, J.N. Medical College, Belgaum, Karnatak (India).

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.

UI MeSH Term Description Entries
D007928 Lethal Dose 50 The dose amount of poisonous or toxic substance or dose of ionizing radiation required to kill 50% of the tested population. LD50,Dose 50, Lethal
D008055 Lipids A generic term for fats and lipoids, the alcohol-ether-soluble constituents of protoplasm, which are insoluble in water. They comprise the fats, fatty oils, essential oils, waxes, phospholipids, glycolipids, sulfolipids, aminolipids, chromolipids (lipochromes), and fatty acids. (Grant & Hackh's Chemical Dictionary, 5th ed) Lipid
D008297 Male Males
D011743 Pyrimidines A family of 6-membered heterocyclic compounds occurring in nature in a wide variety of forms. They include several nucleic acid constituents (CYTOSINE; THYMINE; and URACIL) and form the basic structure of the barbiturates.
D002784 Cholesterol The principal sterol of all higher animals, distributed in body tissues, especially the brain and spinal cord, and in animal fats and oils. Epicholesterol
D005260 Female Females
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D000960 Hypolipidemic Agents Substances that lower the levels of certain LIPIDS in the BLOOD. They are used to treat HYPERLIPIDEMIAS. Antihyperlipidemic,Antilipemic,Antilipemic Agents,Antilipemic Drug,Hypolipidemic Agent,Hypolipidemic Drug,Antihyperlipemics,Antihyperlipidemics,Antilipemic Drugs,Antilipemics,Hypolipidemic Drugs,Agent, Hypolipidemic,Agents, Antilipemic,Agents, Hypolipidemic,Drug, Antilipemic,Drug, Hypolipidemic,Drugs, Antilipemic,Drugs, Hypolipidemic
D014280 Triglycerides An ester formed from GLYCEROL and three fatty acid groups. Triacylglycerol,Triacylglycerols,Triglyceride
D015248 Gemfibrozil A lipid-regulating agent that lowers elevated serum lipids primarily by decreasing serum triglycerides with a variable reduction in total cholesterol. Apo-Gemfibrozil,Ausgem,Bolutol,CI-719,Chem mart Gemfibrozil,DBL Gemfibrozil,Decrelip,Gemfi 1A Pharma,Gemfibrosil,Gemfibrozilo Bayvit,Gemfibrozilo Bexal,Gemfibrozilo Ur,Gemhexal,Gen-Gemfibrozil,GenRX Gemfibrozil,Healthsense Gemfibrozil,Jezil,Lipazil,Lipox Gemfi,Lipur,Litarek,Lopid,Lopid R,Novo-Gemfibrozil,Nu-Gemfibrozil,PMS-Gemfibrozil,Pilder,SBPA Gemfibrozil,Terry White Chemists Gemfibrozil,Trialmin,Apo Gemfibrozil,ApoGemfibrozil,Bayvit, Gemfibrozilo,CI 719,CI719,Gemfibrozil, GenRX,Gemfibrozil, Healthsense,Gemfibrozil, SBPA,Gen Gemfibrozil,GenGemfibrozil,Novo Gemfibrozil,Nu Gemfibrozil,NuGemfibrozil,PMS Gemfibrozil

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