Synthesis, in vitro lipoxygenase inhibition, docking study and thermal stability analyses of novel indole derivatives

A series of indole derivatives has been synthesized and biologically evaluated to identify potent new lipoxygenase (LOX) inhibitors. All selected indole derivatives were screened for their LOX inhibition studies. Most of compounds showed good in vitro LOX inhibition properties exhibiting IC50 values in the range of 53.61 +/- A 0.14 to 198.61 +/- A 0.11 mu M (mean +/- A SEM), as compared to the standard inhibitor baicalein with IC50 value 22.4 +/- A 1.3 mu M. Structure activity relationship has been discussed and docking stimulation of most active compound 4f has also performed. Thermal stability and melting point of indole derivatives have been performed by thermal gravimetric analysis and differential scanning calorimetry analysis under nitrogen atmosphere at heating rate of 20 A degrees C min(-1). Compound 4f bearing bis-phenyl moiety has been found to be the most potent (IC50 53.61 +/- A 0.14 mu M) and thermally most stable among the tested compounds. Imine (C=N) was found to be the key moiety for increasing the thermal stabilities of indole derivatives. FT-IR, NMR and elemental analysis techniques were performed for structural characterization.