Design and synthesis of novel indole-quinoxaline hybrids to target phosphodiesterase 4 (PDE4)

Abstract

A series of novel hybrid molecules were designed rationally by connecting an indole moiety with a quinoxaline ring through a linker as potential inhibitors of PDE4. Their design was validated initially in silico by performing docking studies using a representative molecule. Subsequent synthesis of a focused library of related hybrid molecules was accomplished using Pd/CACu mediated coupling-cyclization as a key step. Some of the synthesized compounds showed PDE4 inhibition in vitro and one of them appeared to be promising.