高級脂肪酸アミド誘導体の研究(第1報)化学構造とコレステロール低下作用との関係

抄録

Many novel amide derivatives of higher fatty acids were synthesized to study the relationship between chemical structure and the serum cholesterol-lowering activity in mice. In a series of cyclohexylamides of higher fatty acids, the cholesterol-lowering activity was enhanced with increasing number of carbon atoms and number of unsaturated double bonds. Introduction of substituents into the cyclohexyl ring of N-cyclohexyllinoleamide did not increase the cholesterollowering activity, while significant improvement of the activity was observed by introduction of a methyl group or a chlorine atom into the phenyl ring of N-phenyllinoleamide. In all the substituted groups tested except the acetyl group, derivatives substituted at 2-position in the N-cyclohexyl-and N-phenyl-linoleamides showed a higher activity than these substituted in other positions. As a result, N-(2-methyl-6-chlorophenyl) linoleamide was found to be the most potent agent in the present study.