Potential antiatherosclerotic agents. 2. (Aralkylamino)- and (alkylamino) benzoic acid analogues of cetaben.
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.
D010129:4-Aminobenzoic Acid / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D000217:Acyltransferases / Q000037:antagonists & inhibitors*; D062365:Aminobenzoates / Q000138:chemical synthesis*; D000818:Animals; D001161:Arteriosclerosis / Q000188:drug therapy*; D004353:Drug Evaluation, Preclinical; D006949:Hyperlipidemias / Q000188:drug therapy; D007202:Indicators and Reagents; D008297:Male; D008722:Methods; D051381:Rats; D011919:Rats, Inbred Strains; D002785:Sterol O-Acyltransferase / Q000037:antagonists & inhibitors*; D013261:Sterols / Q000097:blood; D013329:Structure-Activity Relationship; D014280:Triglycerides / Q000097:blood; D062366:para-Aminobenzoates
D062365:Aminobenzoates; D007202:Indicators and Reagents; D013261:Sterols; D014280:Triglycerides; D062366:para-Aminobenzoates; C018246:cetaben; D000217:Acyltransferases; D002785:Sterol O-Acyltransferase; D010129:4-Aminobenzoic Acid