Abstract

Thalidomide ([2-(2,6-dioxo-hexahydro-3-(R,S)-pyridinyl)-1,3-isoindolinedione]), well known by its teratogenic effect, caused birth defects in up to 12,000 children in the 1960s. More recently, this drug was approved by the US Food and Drug Administration for the treatment of erythema nodosum leprosum, under restricted-use program, and a variety of new possible therapeutic applications have been described. This article will accomplish a review of medicinal chemistry aspects of thalidomide and state of the art in the development of new anti-inflammatory and immunomodulator drug candidates designed using thalidomide as lead-compound.

Keywords: CYP450, Teratogenicity, bioactivation, thiothalidomide analogs, CoMFA, cAMP