ABSTRACT
Objective: To search for new compounds with better water-solubility and higher antianxiety activities. Methods: A series of 2-arylimidazo[1,2-a] pyridine-3-acetamide derivitives were designed and synthesized. The anxiolytic activities were evaluated by BZDR competitive binding assay in vitro and the elevated-plus maze test in mice, the structure-activity relationship (SAR) has been studied. Results and Conclusion: Twenty-eight new compounds have been synthesized. Their structures were confirmed by 1H NMR and MS. According to the results of BZDR affinity test, compounds I1, I 8, I10, I13, I19 showed as good affinity as the positive control (Ro5-4864). The corresponding inhibition was 87%, 89%, 85%, 89% and 76% respectively at the concentration of 100 nmol/L, while that of Ro5-4864 was 82%. I8 and I10, which display better water-solubility and better BZDR affinity in vitro, show significant antianxiety effects in vivo.