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

…, P Castro, AL Machado, CAM Fraga, C Lugnier…

Index: Lima, Lidia M; Castro, Paulo; Machado, Alexandre L; Fraga, Carlos Alberto M; Lugnier, Claire; de Moraes, Vera Lucia Goncalves; Barreiro, Eliezer J Bioorganic and medicinal chemistry, 2002 , vol. 10, # 9 p. 3067 - 3073

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Citation Number: 147

Abstract

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 ...