Thalidomide Analogs from Diamines: Synthesis and Evaluation as Inhibitors of TNF-. ALPHA. Production

…, FM Teixeira, MVN Souza, GW Amarante…

Index: De Almeida, Mauro Vieira; Teixeira, Francisco Martins; De Souza, Marcus Vinicius Nora; Amarante, Giovanni Wilson; Alves, Caio Cesar De Souza; Cardoso, Silvia Helena; Mattos, Ana Marcia; Ferreira, Ana Paula; Teixeira, Henrique Couto Chemical and Pharmaceutical Bulletin, 2007 , vol. 55, # 2 p. 223 - 226

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Citation Number: 23

Abstract

Fourteen thalidomide analogs bearing two phthalimido units were prepared in high yields (83—94%) by condensation of different diamines with phthalic or 3-nitrophthalic anhydride. An in vitro investigation of the compounds as inhibitors of the TNF-α production was performed. The inhibition was higher for compounds bearing amino and nitro groups and was modulated by increasing the size of the spacers between the phthalimide groups.

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