Cholesterol lowering bile acid binding agents: novel lipophilic polyamines.

Autor: Thomas EW; Upjohn Company, Kalamazoo, Michigan 49001., Cudahy MM, Spilman CH, Dinh DM, Watkins TL, Vidmar TJ
Jazyk: angličtina
Zdroj: Journal of medicinal chemistry [J Med Chem] 1992 Apr 03; Vol. 35 (7), pp. 1233-45.
DOI: 10.1021/jm00085a011
Abstrakt: 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.
Databáze: MEDLINE