Thalidomide analogs and PDE4 inhibition

被引：67

作者：

Muller, GW ^{[1
]}

Shire, MG ^{[1
]}

Wong, LM ^{[1
]}

Corral, LG ^{[1
]}

Patterson, RT ^{[1
]}

Chen, YX ^{[1
]}

Stirling, DI ^{[1
]}

机构：

[1] Celgene Corp, Warren, NJ 07059 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 19期

关键词：

D O I：

10.1016/S0960-894X(98)00475-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

N-Phthaloyl 3-amino-3-arylpropionic acid analogs of thalidomide that are potent inhibitors of tumor necrosis factor-a are reported. These compounds were found to be potent inhibitors of phosphodiesterase 4. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

收藏

页码：2669 / 2674

页数：6

相关论文

共 13 条

[1] A RAPID AND EFFICIENT METHOD FOR DEHYDRATION OF PRIMARY AMIDES TO NITRILES - PREPARATION OF ACRYLONITRILE DERIVATIVES [J].

BARGAR, TM ;

RILEY, CM .

SYNTHETIC COMMUNICATIONS, 1980, 10 (06) :479-487

[2] SYNTHESIS AND IN-VITRO PROFILE OF A NOVEL SERIES OF CATECHOL BENZIMIDAZOLES - THE DISCOVERY OF POTENT, SELECTIVE PHOSPHODIESTERASE TYPE-IV INHIBITORS WITH GREATLY ATTENUATED AFFINITY FOR THE [H-3] ROLIPRAM BINDING-SITE [J].

CHENG, JB ;

COOPER, K ;

DUPLANTIER, AJ ;

EGGLER, JF ;

KRAUS, KG ;

MARSHALL, SC ;

MARFAT, A ;

MASAMUNE, H ;

SHIRLEY, JT ;

TICKNER, JE ;

UMLAND, JP .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1995, 5 (17) :1969-1972

[3] Taming TNF: strategies to restrain this proinflammatory cytokine [J].

Eigler, A ;

Sinha, B ;

Hartmann, G ;

Endres, S .

IMMUNOLOGY TODAY, 1997, 18 (10) :487-492

[4]

HILL PA, 1994, FASEB J, V8, pA217

[5]

LOMBARDO LJ, 1995, CURR PHARM DESIGN, V1, P255

[6] THALIDOMIDE EXERTS ITS INHIBITORY-ACTION ON TUMOR-NECROSIS-FACTOR-ALPHA BY ENHANCING MESSENGER-RNA DEGRADATION [J].

MOREIRA, AL ;

SAMPAIO, EP ;

ZMUIDZINAS, A ;

FRINDT, P ;

SMITH, KA ;

KAPLAN, G .

JOURNAL OF EXPERIMENTAL MEDICINE, 1993, 177 (06) :1675-1680

[7] Structural modifications of thalidomide produce analogs with enhanced tumor necrosis factor inhibitory activity [J].

Muller, GW ;

Corral, LG ;

Shire, MG ;

Wang, H ;

Moreira, A ;

Kaplan, G ;

Stirling, DI .

JOURNAL OF MEDICINAL CHEMISTRY, 1996, 39 (17) :3238-3240

[8] Enhanced potency of perfluorinated thalidomide derivatives for inhibition of LPS-induced tumor necrosis factor-α production is associated with a change of mechanism of action [J].

Niwayama, S ;

Loh, C ;

Turk, BE ;

Liu, JO ;

Miyachi, H ;

Hashimoto, Y .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1998, 8 (09) :1071-1076

[9]

Palacios JM, 1995, FARMACO, V50, P819

[10] THALIDOMIDE SELECTIVELY INHIBITS TUMOR-NECROSIS-FACTOR-ALPHA PRODUCTION BY STIMULATED HUMAN MONOCYTES [J].

SAMPAIO, EP ;

SARNO, EN ;

GALILLY, R ;

COHN, ZA ;

KAPLAN, G .

JOURNAL OF EXPERIMENTAL MEDICINE, 1991, 173 (03) :699-703