title: Synthesis and pharmacological study of antihyperlipaemic activity of 2-substituted thieno(2,3-d)pyrimidin-4(3H)-ones.
abstract: A series of 2-substituted thieno(2,3-d)pyrimidin-4-(3H) ones (1-15) was prepared by the reaction of thiophene ortho-aminoester (IV) with a variety of nitriles (V) under acidic conditions, and screened for antihyperlipaemic activity in various animal models. While most of these compounds were found active, 2-chloromethyl-5,6,7,8-tetrahydrobenzo(b)thieno(2,3-d) pyrimidin-4(3H)-one (5) was found to be the most active of all. The serum triglyceride lowering activity exhibited by 5 was found comparable to that of clofibrate and riboflavin tetrabutyrate. Compound 5 was also found to be safe as indicated by acute and chronic toxicity studies in mice and rats.
authors.affiliation: Department of Pharmaceutical Chemistry, Lallubhai Motilal College of Pharmacy, Ahmedabad, India.
authors.forename: C J
authors.initials: CJ
authors.lastname: Shishoo
authors.forename: M B
authors.initials: MB
authors.lastname: Devani
authors.forename: V S
authors.initials: VS
authors.lastname: Bhadti
authors.forename: K S
authors.initials: KS
authors.lastname: Jain
authors.forename: I S
authors.initials: IS
authors.lastname: Rathod
authors.forename: R K
authors.initials: RK
authors.lastname: Goyal
authors.forename: T P
authors.initials: TP
authors.lastname: Gandhi
authors.forename: R B
authors.initials: RB
authors.lastname: Patel
authors.forename: S R
authors.initials: SR
authors.lastname: Naik
mesh_terms: D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D002791:Cholesterol, Dietary / Q000494:pharmacology; D000431:Ethanol; D005260:Female; D006168:Guinea Pigs; D006937:Hypercholesterolemia / Q000517:prevention & control; D006949:Hyperlipidemias / Q000139:chemically induced / Q000517:prevention & control; D000960:Hypolipidemic Agents / Q000138:chemical synthesis* / Q000633:toxicity; D007202:Indicators and Reagents; D007928:Lethal Dose 50; D008055:Lipids / Q000097:blood; D008297:Male; D051379:Mice; D011744:Pyrimidinones / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D011817:Rabbits; D051381:Rats; D011919:Rats, Inbred Strains
chemical_list: D002791:Cholesterol, Dietary; D000960:Hypolipidemic Agents; D007202:Indicators and Reagents; D008055:Lipids; D011744:Pyrimidinones; D000431:Ethanol; C065127:2-chloromethyl-5,6,7,8-tetrahydrobenzo(b)thieno(2,3-d)pyrimidin-4(3H)-one