Synthesis and anti-inflammatory activity of phthalimide derivatives,designed as new thalidomide analogues |
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| Authors: | Lima Lídia M Castro Paulo Machado Alexandre L Fraga Carlos Alberto M Lugnier Claire de Moraes Vera Lúcia Gonçalves Barreiro Eliezer J |
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| Affiliation: | Laboratório de Avalia??o e Síntese de Substancias Bioativas, Faculdade de Farmácia, Universidade Federal do Rio de Janeiro, Brazil. |
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| 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 ED(50)=2.5mg kg(-1), which was correlated with its inhibitory effect on TNF-alpha level. |
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