Potential antiatherosclerotic agents. 2. (Aralkylamino)- and (alkylamino)benzoic acid analogs of cetaben
| Autor: | Vern Gordon Devries, Robert G. Shepherd, Elwood E. Largis, Marvin F Reich, Jay D. Albright, S. A. Schaffer, Miner Thomas G, Janis Upeslacis |
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| Rok vydání: | 1983 |
| Předmět: |
Male
Arteriosclerosis Stereochemistry Sodium Sterol O-acyltransferase Drug Evaluation Preclinical chemistry.chemical_element Hyperlipidemias Structure-Activity Relationship chemistry.chemical_compound In vivo Drug Discovery Methods para-Aminobenzoates Animals Organic chemistry Aminobenzoates Triglycerides Benzoic acid chemistry.chemical_classification Triglyceride Rats Inbred Strains Sterol In vitro Rats Sterols Enzyme chemistry Molecular Medicine Indicators and Reagents lipids (amino acids peptides and proteins) 4-Aminobenzoic Acid Acyltransferases Sterol O-Acyltransferase |
| Zdroj: | Journal of Medicinal Chemistry. 26:1378-1393 |
| ISSN: | 1520-4804 0022-2623 |
| DOI: | 10.1021/jm00364a009 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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