Conformationally restricted 3,4-diarylfuranones (2,3a,4,5-tetrahydronaphthofuranones) as selective cyclooxygenase-2 inhibitors

被引：59

作者：

Pal, M

Veeramaneni, VR

Nagabelli, M

Kalleda, SR

Misra, P

Casturi, SR

Yeleswarapu, KR

机构：

[1] Dr Reddys Labs Ltd, Dept Chem, Discovery Res, Hyderabad 500050, Andhra Pradesh, India

[2] Dr Reddys Labs Ltd, Dept Biol, Discovery Res, Hyderabad 500050, Andhra Pradesh, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 10期

关键词：

D O I：

10.1016/S0960-894X(03)00282-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A number of naphthofuranones were synthesized and tested for COX-1 and COX-2 inhibition. Few of them were identified as selective COX-2 inhibitors. Structure-activity relationship studies within the series are discussed. (C) 2003 Elsevier Science Ltd. All rights reserved.

引用

页码：1639 / 1643

页数：5

共 27 条

[1]

ALMANSA C, 2002, 17 INT S MED CHEM SE

[2] Conformationally restricted 1,5-diarylpyrazoles are selective COX-2 inhibitors [J].

Bertenshaw, SR ;

Talley, JJ ;

Rogier, DJ ;

Graneto, MJ ;

Koboldt, CM ;

Zhang, Y .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1996, 6 (23) :2827-2830

[3] A human whole blood assay for clinical evaluation of biochemical efficacy of cyclooxygenase inhibitors [J].

Brideau, C ;

Kargman, S ;

Liu, S ;

Dallob, AL ;

Ehrich, EW ;

Rodger, IW ;

Chan, CC .

INFLAMMATION RESEARCH, 1996, 45 (02) :68-74

[4]

Chan CC, 1999, J PHARMACOL EXP THER, V290, P551

[5] 2-pyridinyl-3-(4-methylsulfonyl)phenylpyridines:: Selective and orally active cyclooxygenase-2 inhibitors [J].

Friesen, RW ;

Brideau, C ;

Chan, CC ;

Charleson, S ;

Deschênes, D ;

Dubé, D ;

Ethier, D ;

Fortin, R ;

Gauthier, JY ;

Girard, Y ;

Gordon, R ;

Greig, GM ;

Riendeau, D ;

Savoie, C ;

Wang, ZY ;

Wong, E ;

Visco, D ;

Xu, LJ ;

Young, RN .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1998, 8 (19) :2777-2782

[6] NS-398, A NEW ANTIINFLAMMATORY AGENT, SELECTIVELY INHIBITS PROSTAGLANDIN-G/H SYNTHASE CYCLOOXYGENASE (COX-2) ACTIVITY IN-VITRO [J].

FUTAKI, N ;

TAKAHASHI, S ;

YOKOYAMA, M ;

ARAI, I ;

HIGUCHI, S ;

OTOMO, S .

PROSTAGLANDINS, 1994, 47 (01) :55-59

[7]

GANS KR, 1990, J PHARMACOL EXP THER, V254, P180

[8] Design and synthesis of celecoxib and rofecoxib analogues as selective cyclooxygenase-2 (COX-2) inhibitors: Replacement of sulfonamide and methylsulfonyl pharmacophores by an azido bioisostere [J].

Habeeb, AG ;

Rao, PNP ;

Knaus, EE .

JOURNAL OF MEDICINAL CHEMISTRY, 2001, 44 (18) :3039-3042

[9] 1,2-diarylpyrroles as potent and selective inhibitors of cyclooxygenase-2 [J].

Khanna, IK ;

Weier, RM ;

Yu, Y ;

Collins, PW ;

Miyashiro, JM ;

Koboldt, CM ;

Veenhuizen, AW ;

Currie, JL ;

Seibert, K ;

Isakson, PC .

JOURNAL OF MEDICINAL CHEMISTRY, 1997, 40 (11) :1619-1633

[10] Sar in the alkoxy lactone series:: The discovery of DFP, a potent and orally active COX-2 inhibitor [J].

Leblanc, Y ;

Roy, P ;

Boyce, S ;

Brideau, C ;

Chan, CC ;

Charleson, S ;

Gordon, R ;

Grimm, E ;

Guay, J ;

Léger, S ;

Li, CS ;

Riendeau, D ;

Visco, D ;

Wang, Z ;

Webb, J ;

Xu, LJ ;

Prasit, P .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1999, 9 (15) :2207-2212

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