Synthesis, Spectral Characterization, in silico Molecular Docking and Pharmacological Screening of Some Quinazoline Analogues as Anticonvulsants

A new analogues of 2-methyl-3-(6-substituted-benzothiazol-2-yl)-3H-quinazolin-4-one [Dm1-Dm5] and their 6-bromo analogues [Dm6-Dm10], similarly a new analogues of 2-methyl-3-(pyridin-4-yl-formamide)-3H-quinazolin-4-one [Em1] and its 6-bromo analogue [Em2] were synthesized and characterized by melting point, elemental and spectral [FTIR, (1H and 13C) NMR and MS] methods. The anticonvulsant activity of selected analogues was assessed against maximal electroshock (MES) induced convulsions model in albino mice. The selected analogues were injected intraperitoneally at dose 20 mg/kg body weight and LD50, ED50 and TI values were determined. Among the tested analogues, electron withdrawing groups (-NO2, -Br) containing analogues (Dm4, Dm8, Dm10) shows better potency than the electron releasing groups containing analogues. The activity was determined to be significant at p < 0.05 with regard to standard diazepam. Similarly, the electron withdrawing groups containing compounds shows better docking score against the protein 6X3X.