SYNTHESIS AND ANTIHYPERLIPIDEMIC ACTIVITY OF CERTAIN NICOTINIC ACID DERIVATIVES

Document Type : Original Article

Authors

Departments of Pharmaceutical Chemistry, and (Pharmacology and Toxicology)*, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt

Abstract

3-Ethoxycarbonyl-4,6-dimethyl-2(1H)-pyridone I was prepared and converted to the corresponding sodium salt II. The latter reacted with certain chloroacetanilides to afford the corresponding ethers III. In addition 3-cyano-4,6-dimethyl-2(1H)-pyridone IV was prepared and converted to the corresponding potassium salt V which was allowed to react with  chloroacetyl and  -chloropropionyl derivatives of certain aromatic amines to afford VI. Furthermore, IV was converted to 3-cyano-4,6-dimethyl pyridine-2-thione IX. Potassium salt of the latter upon reaction with  -chloroacetyl and  -chloropropionyl derivatives of some aromatic amines gave the expected thioethers X. Compounds III2, V4, X1 and X12 were selected for testing for antihyperlipidemic effect and revealed promising hypolipidemic effect on cholesterol, triglyceride, LDL and have no effect on HDL.