Synthesis, spectroscopic characterization, X-ray structure, and in vivo neurotropic activity of new 1,5-benzodiazepin-2-ones

The paper reports the synthesis and in vivo pharmacological studies of a series of N-alkyl-1,5-benzodiazepine-2-ones. In this work, 19 novel benzodiazepine derivatives have been prepared and characterized by spectroscopic methods including 2D nuclear magnetic resonance techniques. Crystal structure of 1-benzyl-8-methyl-4-phenyl-1H-benzo[b][1,4]diazepin-2(3H)-one has also been determined by X-ray diffraction. Prediction of activity spectra for substances prediction and docking studies onto human serum albumin were conducted. Two compounds under these investigation showed high antihypoxic, tranquilizing, and anticonvulsant activity in vivo.