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

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

Luther, Bethala Jawahar;Rani, Chekuri Sharmila;Suresh, Namburi;Rao, Mandava V. Basaveswara;Kapavarapu, Ravikumar;Suresh, Chakali;Babu, P. Vijaya;Pal, Manojit;
arabian journal of chemistry 2019 Vol. 12 pp. 3108-3117
103
luther2019designarabian

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/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

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