Gamma-lactams and related compounds as cholesterol absorption inhibitors: Homologs of the beta-lactam cholesterol absorption inhibitor SCH 48461

被引:24
作者
Dugar, S
Kirkup, MP
Clader, JW
Lin, SI
Rizvi, R
Snow, ME
Davis, HR
McCombie, SW
机构
[1] Schering Plough Research Institute, Kenilworth, NJ 07033
关键词
D O I
10.1016/0960-894X(95)00516-6
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Our search for potent cholesterol absorption inhibitors led to the discovery of the p-lactam SCH 48461. Structure activity relationship studies prompted us to this study of gamma-lactams, ring homologs of beta-lactam SCH 48461, to determine their potential as cholesterol absorption inhibitors. The results indicate that the gamma-lactams have moderate cholesterol absorption inhibitory properties.
引用
收藏
页码:2947 / 2952
页数:6
相关论文
共 10 条
[1]   2-AZETIDINONES AS INHIBITORS OF CHOLESTEROL ABSORPTION [J].
BURNETT, DA ;
CAPLEN, MA ;
DAVIS, HR ;
BURRIER, RE ;
CLADER, JW .
JOURNAL OF MEDICINAL CHEMISTRY, 1994, 37 (12) :1733-1736
[2]   SUBSTITUTED (1,2-DIARYLETHYL)AMIDE ACYL-COA-CHOLESTEROL ACYLTRANSFERASE INHIBITORS - EFFECT OF POLAR GROUPS ON IN-VITRO AND IN-VIVO ACTIVITY [J].
CLADER, JW ;
BERGER, JG ;
BURRIER, RE ;
DAVIS, HR ;
DOMALSKI, M ;
DUGAR, S ;
KOGAN, TP ;
SALISBURY, B ;
VACCARO, W .
JOURNAL OF MEDICINAL CHEMISTRY, 1995, 38 (10) :1600-1607
[3]  
CLADER JW, UNPUB
[4]  
DAVIS HR, 1994, ATHEROSCLEROSIS, V109, P162
[5]   INDIVIDUAL-RESPONSES TO A CHOLESTEROL-LOWERING DIET IN 50 MEN WITH MODERATE HYPERCHOLESTEROLEMIA [J].
DENKE, MA ;
GRUNDY, SM .
ARCHIVES OF INTERNAL MEDICINE, 1994, 154 (03) :317-325
[6]  
LEE HT, 1995, EXPERT OPIN THER PAT, V5, P397
[7]   HYPOCHOLESTEROLEMIC ACTIVITY OF A NOVEL INHIBITOR OF CHOLESTEROL ABSORPTION, SCH-48461 [J].
SALISBURY, BG ;
DAVIS, HR ;
BURRIER, RE ;
BURNETT, DA ;
BOYKOW, G ;
CAPLEN, MA ;
CLEMMONS, AL ;
COMPTON, DS ;
HOOS, LM ;
MCGREGOR, DG ;
SCHNITZERPOLOKOFF, R ;
SMITH, AA ;
WEIG, BC ;
ZILLI, DL ;
CLADER, JW ;
SYBERTZ, EJ .
ATHEROSCLEROSIS, 1995, 115 (01) :45-63
[8]  
SCHINTZERPOLOKO.R, 1991, COMP BIOCH PHYSL, V197, P304
[9]  
1988, CIRCULATION, V77, pA721
[10]  
1993, JAMA-J AM MED ASSOC, V269, P3015