Thromboxane modulating agents .1. Design of 1-[(arylsulfonyl)amino] alkylindole derivatives as dual thromboxane synthase inhibitor thromboxane receptor antagonists

被引:13
作者
Dickinson, RP
Dack, KN
Steele, J
机构
[1] Department of Discovery Chemistry, Pfizer Central Research, Sandwich
关键词
D O I
10.1016/0960-894X(95)00529-4
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The design of a series of dual thromboxane synthase inhibitor/thromboxane receptor antagonists based on an indole thromboxane synthase inhibitor template is described. The indole-5-propanoic acid derivatives 17, 22 and 23 were found to be potent dual agents in vitro.
引用
收藏
页码:3017 / 3022
页数:6
相关论文
共 16 条
[1]  
Bhagwat Shripad S., 1994, Drugs of the Future, V19, P765
[2]  
COLLINGTON EW, 1990, ANNU REP MED CHEM, V25, P99
[3]  
COY JH, 1974, J CHEM SOC P2, P35
[4]  
COZZI P, 1991, CURR OPINION THERAPE, P1343
[5]   SELECTIVE THROMBOXANE SYNTHETASE INHIBITORS .1. 1-[(ARYLOXY)ALKYL]-1H-IMIDAZOLES [J].
CROSS, PE ;
DICKINSON, RP ;
PARRY, MJ ;
RANDALL, MJ .
JOURNAL OF MEDICINAL CHEMISTRY, 1985, 28 (10) :1427-1432
[6]  
CROSS PE, 1987, ANNU REP MED CHEM, V22, P95
[7]   THE BIOCHEMICAL PHARMACOLOGY OF THROMBOXANE SYNTHASE INHIBITION IN MAN [J].
FITZGERALD, GA ;
REILLY, IAG ;
PEDERSEN, AK .
CIRCULATION, 1985, 72 (06) :1194-1201
[8]   COMPARISON OF THE DISPOSITION OF 2 NOVEL COMBINED THROMBOXANE SYNTHASE INHIBITORS THROMBAXANE-A(2) RECEPTOR ANTAGONISTS IN THE ISOLATED-PERFUSED RAT-LIVER [J].
GARDNER, IB ;
WALKER, DK ;
LENNARD, MS ;
SMITH, DA ;
TUCKER, GT .
XENOBIOTICA, 1995, 25 (02) :185-197
[9]   ROLE OF PROAGGREGATORY AND ANTIAGGREGATORY PROSTAGLANDINS IN HEMOSTASIS - STUDIES WITH COMBINED THROMBOXANE SYNTHASE INHIBITION AND THROMBOXANE RECEPTOR ANTAGONISM [J].
GRESELE, P ;
ARNOUT, J ;
DECKMYN, H ;
HUYBRECHTS, E ;
PIETERS, G ;
VERMYLEN, J .
JOURNAL OF CLINICAL INVESTIGATION, 1987, 80 (05) :1435-1445
[10]  
GRESELE P, 1984, THROMB HAEMOSTASIS, V52, P364