Gamma-lactams and related compounds as cholesterol absorption inhibitors: homologs of the beta-lactam cholesterol absorption inhibitor SCH 484611

✍ Scribed by Sundeep Dugar; Michael P. Kirkup; John W. Clader; Sue-Ing Lin; Razia Rizvi; Mark E. Snow; Harry R. Davis Jr.; Stuart W. McCombie

• Publisher: Elsevier Science
• Year: 1995
• Tongue: English
• Weight: 264 KB
• Volume: 5
• Category: Article
• ISSN: 0960-894X
• DOI: 10.1016/0960-894x(95)00516-6

✦ Synopsis

Our search for potent cholesterol absorption inhibitors led to the discovery of the I~-lactam SCH 48461. Structure activity relationship studies prompted us to this study of y-lactams, ring homologs of 13lactam SCH 48461, to determine their potential as cholesterol absorption inhibitors. The results indicate that the y-lactarns have moderate cholesterol absorption inhibitory properties.

High serum cholesterol levels have been unequivocally implicated as a cause of coronary artery disease (CAD). A diet high in saturated fat and cholesterol has been singled out as a major risk factor for CAD and hence drug therapy to inhibit intestinal cholesterol absorption has been important for control of hyperlipidemia. 2 Though numerous agents that affect cholesterol absorption inhibition (CAI) have been reported, the search for safe and effective inhibitors of cholesterol absorption has continued unabated. 3 Our