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

• Autor(a) principal: Luther, Bethala Jawahar
• Data de Publicação: 2019
• Outros Autores: Rani, Chekuri Sharmila, Suresh, Namburi, Basaveswara Rao, Mandava V., Kapavarapu, Ravikumar, Suresh, Chakali, Vijaya Babu, P., Pal, Manojit
• Tipo de documento: Artigo
• Idioma: eng
• Título da fonte: Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
• Texto Completo: http://hdl.handle.net/10316/101617; https://doi.org/10.1016/j.arabjc.2015.08.009
• topic: Indole; Quinoxaline; Pd/C; PDE4

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.