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

oleh: Bethala Jawahar Luther, Chekuri Sharmila Rani, Namburi Suresh, Mandava V. Basaveswara Rao, Ravikumar Kapavarapu, Chakali Suresh, P. Vijaya Babu, Manojit Pal

Format: Article
Diterbitkan: Elsevier 2019-12-01

Deskripsi

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/CCu 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. Keywords: Indole, Quinoxaline, Pd/C, PDE4