Synthesis, Characterization, in silico and in vivo Evaluation of Amino Acid Derived Schiff Bases of QuinolineBenzimidazole Hybrids as Anti- epileptic Agents

Aim/Background: Novel quinoline compounds containing benzimidazole have been synthesized in a number of different ways and screened for anti-epileptic potential through in vivo and in silico studies.Materials and Methods: The novel quinoline-benzimidazole hybrids were synthesized by using substituted carbaldehyde (1,2) and substituted benzimidazole (derived from amino acids) (3a-f). The synthesized derivatives were characterized by IR, 13C-NMR, 1H-NMR, and Mass spectroscopy and anti-convulsant activity was analyzed by in silico studies on the swiss albino mice using the ScPTZ model. Conclusion and Results: Compounds (1H-Benzoimidazol-2-yl)substituted-(2-p-tolyloxy-quinolin-3-ylmethylene)-amine (4a-f) and (Benzoimidazol-2-yl)substituted-(2- ethoxy-quinolin-3-ylmethylene)-amine (5a-f) were synthesized. The synthesized derivativeswere characterized (IR, 13C-NMR, 1H-NMR, andmass spectrometry) and screened for their anticonvulsant potentiality by subcutaneous pentylenetetrazol method using carbamazepine. Additionally, the anti- epileptic potential of the produced compounds is confirmed by in silico study results that were obtained. The study also proved that the synthesized derivatives used aminobutyric acid (GABA A) receptors. At a dose level of 30 mg/kg body weight, 4a, 4b, and 4d were found to be more effective than the other synthesized derivatives.