Chemical & Pharmaceutical Bulletin 2007-02-01

Thalidomide analogs from diamines: Synthesis and evaluation as inhibitors of TNF-alpha production.

Mauro Vieira de Almeida, Francisco Martins Teixeira, Marcus Vinicius Nora de Souza, Giovanni Wilson Amarante, Caio César de Souza Alves, Sílvia Helena Cardoso, Ana Márcia Mattos, Ana Paula Ferreira, Henrique Couto Teixeira

Index: Chem. Pharm. Bull. 55(2) , 223-6, (2007)

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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-alpha 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.