A conventional and solid-state synthesis, biological activity, and molecular docking studies of 6-arylbenzo[4,5]imidazo[1,2-a] [1,8]naphthyridin-10-ols

Abstract

Abstract An effective, practical, and simple approach toward the preparation of highly-substituted 6-arylbenzo[4, 5]imidazo[1,2-a][1,8]naphthyridin-10-ols 6(a-h) by the reaction of 3-aryl-1,8-naphthyridin-2-amines 3(a-h) with benzoquinone 4 in acid catalyzed cyclization under solid-state method, as well as conventional conditions, has been described. The products are obtained in good yields and in a solid of high purity. The major advantages of solid states are easy workup, low costs, short reaction time, good efficacy, and environment-friendly procedure. The newly synthesized compounds were thoroughly characterized using spectral data and elemental analyses. All compounds were screened for their biological evaluation. Predominantly 6b and 6c compounds showed the highest antibacterial activity. Moreover, all the synthesized compounds were docked against topoisomerase II DNA gyrase enzyme. Graphical Abstract