Synthesis and biological evaluation of 2,3-diarylthiophenes as selective Cox-2 inhibitors .2. Replacing the heterocycle

被引:56
作者
Gauthier, JY
Leblanc, Y
Black, WC
Chan, CC
Cromlish, WA
Gordon, R
Kennedey, BP
Lau, CK
Leger, S
Wang, ZY
Ethier, D
Guay, J
Mancini, J
Riendeau, D
Tagari, P
Vickers, P
Wong, E
Xu, LJ
Prasit, P
机构
[1] Merck Frosst Ctr. Therapeut. Res., Dorval, Que. H9R 4P8
关键词
D O I
10.1016/0960-894X(95)00564-A
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The thiophene ring of DuP 697 was replaced by a variety of heterocycles and the products were tested for their ability to inhibit human Cox-2 and Cox-1, the isozymes of cyclooxygenase.
引用
收藏
页码:87 / 92
页数:6
相关论文
共 23 条
[1]   GASTROINTESTINAL DAMAGE ASSOCIATED WITH THE USE OF NONSTEROIDAL ANTIINFLAMMATORY DRUGS [J].
ALLISON, MC ;
HOWATSON, AG ;
TORRANCE, CJ ;
LEE, FD ;
RUSSELL, RI .
NEW ENGLAND JOURNAL OF MEDICINE, 1992, 327 (11) :749-754
[2]   1.3-CYCLOADDITIONEN MIT TRIMETHYLSILYL-AZID - UBER ISOMERE N-ACETYL-1.2.3-TRIAZOLE [J].
BIRKOFER, L ;
WEGNER, P .
CHEMISCHE BERICHTE-RECUEIL, 1966, 99 (08) :2512-&
[3]  
CHAN CC, 1995, J PHARMACOL EXP THER, V274, P1531
[4]  
DRAYTON CJ, 1984, COMP HETEROCYCLIC CH
[5]  
GANS KR, 1990, J PHARMACOL EXP THER, V254, P180
[6]  
Gauthier J.Y., 1995, PCT Int. Appl. WO 95 00,501, Patent No. [9500501, 95 00,501]
[7]  
HABER SB, 1989, Patent No. 4820827
[8]   HUMAN CYCLOOXYGENASE-2 CDNA [J].
HLA, T ;
NEILSON, K .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1992, 89 (16) :7384-7388
[9]   DIARYL INDENES AND BENZOFURANS - NOVEL CLASSES OF POTENT AND SELECTIVE CYCLOOXYGENASE-2 INHIBITORS [J].
HUANG, HC ;
CHAMBERLAIN, TS ;
SEIBERT, K ;
KOBOLDT, CM ;
ISAKSON, PC ;
REITZ, DB .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1995, 5 (20) :2377-2380
[10]   SIMULTANEOUS QUANTIFICATION OF AN ANTIINFLAMMATORY COMPOUND (DUP-697) AND A POTENTIAL METABOLITE (X6882) IN HUMAN PLASMA AND URINE BY HIGH-PERFORMANCE LIQUID-CHROMATOGRAPHY [J].
JOSHI, AS ;
RAGHAVAN, N ;
WILLIAMS, RM ;
TAKAHASHI, K ;
SHINGU, H ;
KING, SYP .
JOURNAL OF CHROMATOGRAPHY B-BIOMEDICAL APPLICATIONS, 1994, 660 (01) :143-150