New generation dopaminergic agents 4. Exploiting the 2-methyl chroman scaffold. Synthesis and evaluation of two novel series of 2-(aminomethyl)- 3,4,7,9-tetrahydro-2H-pyrano[2,3-e]indole and indol-8-one derivatives

Article abstract of DOI:10.1016/S0040-4020(98)00349-4

The rational design, synthesis, and evaluation of two novel series of 2- (aminomethyl)-3,4,7,9-tetrahydro-2H-pyrano[2,3-e]indole and indolone derivatives are disclosed, based on the recently discovered D₂ agonist phenolic template prototype [i.e. the 7-OH-2-(aminomethyl)chroman nucleus]. The indolones were observed to have higher affinity and intrinsic activity than the corresponding indoles.