Synthesis and anti-inflammatory activity of phthalimide derivatives, designed as new thalidomide analogues

被引：239

作者：

Lima, LM

Castro, P

Machado, AL

Fraga, CAM

Lugnier, C

de Moraes, VLG

Barreiro, EJ ^{[1
]}

机构：

[1] Univ Fed Rio de Janeiro, Fac Farm, Lab Avaliacao & Sintese Subst Bioativas, Rio De Janeiro, Brazil

[2] Univ Fed Rio de Janeiro, Inst Quim, Rio De Janeiro, Brazil

[3] Univ Fed Rio de Janeiro, Dept Bioquim Med, Rio De Janeiro, Brazil

[4] CNRS, URA 660, Illkirch Graffenstaden, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2002年 / 10卷 / 09期

关键词：

D O I：

10.1016/S0968-0896(02)00152-9

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 [生物化学与分子生物学]; 081704 [应用化学];

摘要：

This paper describes the synthesis and anti-inflammatory activity of new N-phenyl-phthalimide sulfonamides (3a-e) and the isosters N-phenyl-phthalimide amides (4a-e), designed as hybrids of thalidomide (1) and aryl sulfonamide phosphodiesterase inhibitor (2), In these series, compound 3e (LASSBio 468). having a sulfonyl-thiomorpholine moiety, showed potent inhibitory activity on LPS-induced neutrophil recruitment with ED50 = 2.5 mg kg(-1), which was correlated with its inhibitory effect on TNF-alpha level. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：3067 / 3073

页数：7

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