INTERPHENYLENE 7-OXABICYCLO[2.2.1]HEPTANES - SQ-33961 - A NEW POTENT, LONG-ACTING THROMBOXANE ANTAGONIST

被引:9
作者
MISRA, RN
BROWN, BR
SHER, PM
PATEL, MM
GOLDENBERG, HJ
MICHEL, IM
HARRIS, DN
机构
[1] Bristol-Myers Squibb, Pharmaceutical Research Institute, Princeton, NJ 08543-4000
关键词
D O I
10.1016/S0960-894X(01)81106-9
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis and initial biological evaluation of a novel series of chiral interphenylene 7-oxabicyclo-[2.2.1]heptane TxA2 antagonists with 4-amido oxazole omega chains is described. Within this series SQ 33,961 has been identified as a highly potent TxA2 antagonist with an exceptionally long in vivo duration of action.
引用
收藏
页码:461 / 464
页数:4
相关论文
共 12 条
[1]   NICKEL PEROXIDE DEHYDROGENATION OF OXYGEN-CONTAINING, SULFUR-CONTAINING, AND NITROGEN-CONTAINING HETEROCYCLES [J].
EVANS, DL ;
MINSTER, DK ;
JORDIS, U ;
HECHT, SM ;
MAZZU, AL ;
MEYERS, AI .
JOURNAL OF ORGANIC CHEMISTRY, 1979, 44 (04) :497-501
[2]  
HALL SE, 1991, IN PRESS MED RES REV, V11
[3]  
HALUSHKA P V, 1989, Drugs of Today, V25, P383
[4]   THROMBOXANES - NEW GROUP OF BIOLOGICALLY-ACTIVE COMPOUNDS DERIVED FROM PROSTAGLANDIN ENDOPEROXIDES [J].
HAMBERG, M ;
SVENSSON, J ;
SAMUELSSON, B .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1975, 72 (08) :2994-2998
[5]   9-ALPHA-HOMO-9,11-EPOXY-5,13-PROSTADIENOIC ACID ANALOGS - SPECIFIC STABLE AGONIST (SQ 26,538) AND ANTAGONIST (SQ 26,536) OF THE HUMAN-PLATELET THROMBOXANE RECEPTOR [J].
HARRIS, DN ;
PHILLIPS, MB ;
MICHEL, IM ;
GOLDENBERG, HJ ;
HEIKES, JE ;
SPRAGUE, PW ;
ANTONACCIO, MJ .
PROSTAGLANDINS, 1981, 22 (02) :295-307
[6]  
HEDBERG A, 1988, J PHARMACOL EXP THER, V245, P786
[7]  
HSER PM, 1991, 201ST AM CHEM SOC NA
[8]   INTRAVENOUS ARACHIDONATE IN MOUSE - MODEL FOR EVALUATION OF ANTITHROMBOTIC DRUGS [J].
KOHLER, C ;
WOODING, W ;
ELLENBOGEN, L .
THROMBOSIS RESEARCH, 1976, 9 (01) :67-80
[9]  
MISRA RN, 1991, IN PRESS J MED CHEM, V34
[10]   OXIDATION WITH NICKEL PEROXIDE .1. OXIDATION OF ALCOHOLS [J].
NAKAGAWA, K ;
NAKATA, T ;
KONAKA, R .
JOURNAL OF ORGANIC CHEMISTRY, 1962, 27 (05) :1597-&