title: Cholesterol lowering bile acid binding agents: novel lipophilic polyamines.
abstract: A series of novel lipophilic polyamines was synthesized by the sodium cyanoborohydride-mediated reductive amination of various ketones and aldehydes with the polyamine tris(2-aminoethyl)amine. Two of these compounds, N,N-bis[2-(cyclododecylamino)ethyl]-N'-benzyl-1,2-ethanediamine trihydrochloride (36.3HCl) and N,N-bis[2-(cyclododecylmethylamino)ethyl]-N',N'-dimethyl-1,2-ethan ediamine (23), are 29 and 24 times more potent than colestipol hydrochloride, respectively, for lowering animal serum cholesterol levels.
authors.affiliation: Upjohn Company, Kalamazoo, Michigan 49001.
authors.forename: E W
authors.initials: EW
authors.lastname: Thomas
authors.forename: M M
authors.initials: MM
authors.lastname: Cudahy
authors.forename: C H
authors.initials: CH
authors.lastname: Spilman
authors.forename: D M
authors.initials: DM
authors.lastname: Dinh
authors.forename: T L
authors.initials: TL
authors.lastname: Watkins
authors.forename: T J
authors.initials: TJ
authors.lastname: Vidmar
mesh_terms: D000818:Animals; D000924:Anticholesteremic Agents / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D001647:Bile Acids and Salts / Q000378:metabolism*; D008078:Cholesterol, LDL / Q000097:blood; D015243:Cholesterol, VLDL / Q000097:blood; D003084:Colestipol / Q000494:pharmacology; D003370:Coturnix / Q000097:blood; D015394:Molecular Structure; D011073:Polyamines / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000924:Anticholesteremic Agents; D001647:Bile Acids and Salts; D008078:Cholesterol, LDL; D015243:Cholesterol, VLDL; D011073:Polyamines; D003084:Colestipol