新型熊果酸苯并咪(噻)唑连苯酯合成及抗炎活性测定

Synthesis and Anti-inflammatory Activity of Novel Benzimida-zole (Benzothiazole) Phenylursolate

以熊果酸、取代苯甲醛和邻苯二胺或邻氨基苯硫酚为原料,合成了一系列熊果酸苯并咪(噻)唑连苯酯衍生物4a～4h,8个新化合物均未见文献报道,其结构经1H NMR,IR和HRMS加以确认,并对4a～4h进行药理活性筛选,结果表明,化合物4d(150 mg·kg-1),4g(150 mg·kg-1)等具有良好抗炎活性.

A novel series of the benzimidazole or benzothiazole phenyl ester derivatives of ursolic acid 4a～4h were prepared via ursolic acid,substituted benzaldehyde,and o-phenylendiamine or 2-aminothiophenol.The compounds were structurally confirmed by 1H NMR,IR and HRMS techniques.The preliminary bioassay test demonstrated that compounds 4d and 4g had potent anti-inflammatory activity.