Journal of Medicinal Chemistry · 1983 · 23 citations · 0 references
Life SciencesMedicinal ChemistryPharmacologyBiochemical PharmacologyCardiovascular PharmacotherapyLipid BiochemistryCholesterol MetabolismFatty Acid MetabolismLipid MetabolismLipid-lowering TherapySterol MetabolismTriacylglycerol MetabolismAcyl-coa DehydrogenasesAcyltransferase EnzymesArterial Wall ThickeningBenzoic Acid DerivativesCholesterol EsterificationPharmacological Inhibition Of Cholesterol BiosynthesisSterol EsterificationTriglyceride Lowering
The syntheses of a series of (aralkylamino)- and (alkylamino)benzoic acids, as well as the corresponding esters and sodium salts, are described. The compounds were evaluated in vivo in rats for serum sterol and triglyceride lowering activity and in vitro for activity in inhibiting the principle cholesterol-esterifying enzyme of the arterial wall, fatty acyl-CoA:cholesterol acyltransferase (ACAT). Based on a combination of these two activities, cataben sodium (150) was selected for development as a hypolipidemic and potential antiatherosclerotic agent.