1,3-Diarylcycloalkanopyrazoles and diphenyl hydrazides as selective inhibitors of cyclooxygenase-2

被引:73
作者
Sui, ZH [1 ]
Guan, JH [1 ]
Ferro, MP [1 ]
McCoy, K [1 ]
Wachter, MP [1 ]
Murray, WV [1 ]
Singer, M [1 ]
Steber, M [1 ]
Ritchie, DM [1 ]
Argentieri, DC [1 ]
机构
[1] RW Johnson Pharmaceut Res Inst, Raritan, NJ 08869 USA
关键词
D O I
10.1016/S0960-894X(00)00041-X
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Novel 1,3-diarylcycloalkanopyrazoles 1, and diphenyl hydrazides 2 were identified as selective inhibitors of cyclooxygenase-2. The 1,3-diaryl substitution pattern of the pyrazole ring in 1 differentiates these compounds from most of the known selective COX-2 inhibitors that contain two aryl rings at the adjacent positions on a heterocyclic or a phenyl ring. Similarly, the two phenyl rings in 2 are also separated by three atoms. SAR of both phenyl rings in 1 and 2, and the aliphatic ring in 1 will be discussed. (C) 2000 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:601 / 604
页数:4
相关论文
共 14 条
[1]  
CARTER JS, 1997, EXPERT OPIN THER PAT, V8, P21
[2]  
COLEMAN RA, 1994, PHARMACOL REV, V46, P205
[3]  
Huisgen R., 1962, TETRAHEDRON, V17, P3, DOI DOI 10.1016/S0040-4020(01)99001-5
[4]  
KARGMAN S, 1994, J CELL BIOCH S B, V18, P319
[5]   Synthesis and biological activity of annulated pyrazoles as selective COX-2 inhibitors. I. [J].
Kim, HH ;
Park, JG ;
Moon, TC ;
Chang, HW ;
Jahng, Y .
ARCHIVES OF PHARMACAL RESEARCH, 1999, 22 (04) :372-379
[6]  
LANEUVILLE O, 1994, J PHARMACOL EXP THER, V271, P927
[7]  
MEADE EA, 1993, J LIPID MEDIATOR, V6, P119
[8]  
MICHELL JA, 1993, P NATL ACAD SCI USA, V90, P11693
[9]  
MURRAY W, 1991, SYNTHESIS-STUTTGART, P18
[10]  
ONEILL GP, 1994, MOL PHARMACOL, V45, P245