Hypolipidemic activity of amine-borane aducts of cyclohexylamine and toluidine in rodents.
The amine-borane adducts of cyclohexylamine and toluidine were observed to be potent hypolipidemic agents in mice, I.P. and rats orally at 8 mg/kg/day lowering both serum cholesterol and triglyceride levels after 14-16 days. These compounds were able to lower tissue lipids including the cholesterol content of the aorta wall. The agents successfully lower VLDL- and LDL-cholesterol content while elevating HDL-cholesterol content significantly. The agents also modulate lipid regulatory enzyme activities in a manner to reduce liver lipid levels. These studies demonstrate that the nitrogen atom does not have to be apart of the aromatic ring as in heterocyclic-amine borane to afford good hypolipidemic activity in rodents.
Burnham
B S
BS
Division of Medicinal Chemistry and Natural Products School of Pharmacy University of North Carolina Chapel Hill N.C. 27599-7360 USA.
Chen
S Y
SY
Sood
A
A
Spielvogel
B F
BF
Hall
I H
IH