Design and synthesis of sulfonyl-substituted 4,5-diarylthiazoles as selective cyclooxygenase-2 inhibitors

被引：33

作者：

Carter, JS ^{[1
]}

Rogier, DJ ^{[1
]}

Graneto, MJ ^{[1
]}

Seibert, K ^{[1
]}

Koboldt, CM ^{[1
]}

Zhang, Y ^{[1
]}

Talley, JJ ^{[1
]}

机构：

[1] GD Searle Monsanto, St Louis, MO 63198 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 08期

关键词：

D O I：

10.1016/S0960-894X(99)00158-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel sulfone substituted 4,5-diarylthiazoles have been synthesized and evaluated for their inhibition of the two isoforms of human cyclooxygenase (COX-1 and COX-2). This series displays exceptionally selective COX-2 inhibition. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：1167 / 1170

页数：4

共 23 条

[1]

CARTER JS, 1997, EXPERT OPIN THER PAT, V8, P21

[2]

DUCHARNME Y, 1995, Patent No. 00501

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

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 .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1996, 6 (01) :87-92

[4] EXPRESSION AND SELECTIVE-INHIBITION OF THE CONSTITUTIVE AND INDUCIBLE FORMS OF HUMAN CYCLOOXYGENASE [J].

GIERSE, JK ;

HAUSER, SD ;

CREELY, DP ;

KOBOLDT, C ;

RANGWALA, SH ;

ISAKSON, PC ;

SEIBERT, K .

BIOCHEMICAL JOURNAL, 1995, 305 :479-484

[5]

Hantzch, 1888, BER DTSCH CHEM GES, V21, P942

[6]

HOLTZMAN MJ, 1992, J BIOL CHEM, V267, P21438

[7]

ISAKSON P, 1995, P 9 INT C PROST REL

[8]

ISAKSON P, 1994, 208 NAT ACS M

[9] Investigation of the binding of isoform-selective inhibitors to prostaglandin endoperoxide synthases using fluorescence spectroscopy [J].

Lanzo, CA ;

Beechem, JM ;

Talley, J ;

Marnett, LJ .

BIOCHEMISTRY, 1998, 37 (01) :217-226

[10] ENDOGENOUS GLUCOCORTICOIDS REGULATE AN INDUCIBLE CYCLOOXYGENASE ENZYME [J].

MASFERRER, JL ;

SEIBERT, K ;

ZWEIFEL, B ;

NEEDLEMAN, P .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1992, 89 (09) :3917-3921

← 1 2 3 →