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目的设计合成具有心肌保护作用的糖碳苷化合物。方法针对红景天苷可被糖苷水解酶水解的缺点,将其改造为糖碳苷并改变苯环上的取代基进行新药设计,获得红景天苷的糖碳苷类似物。通过体外心肌细胞的缺氧-复氧损伤模型评价其心肌保护活性。结果与结论合成了10个糖碳苷类新化合物。初步药理评价表明,大多数化合物对缺氧-复氧损伤心肌具有明显的保护作用,其中5个化合物的活性强于红景天苷,并呈剂量依赖关系。
Objective To design and synthesize glycoside compounds with cardioprotective effects. Methods Salidroside can be hydrolyzed by glycoside hydrolase shortcomings, it is transformed into glycosides and change the substituents on the benzene ring for new drug design, to obtain glycosides of salidroside analogs. Myocardial protective activity was evaluated by hypoxia-reoxygenation injury model of cardiomyocytes in vitro. RESULTS AND CONCLUSIONS Ten new glycosidic compounds were synthesized. Preliminary pharmacological evaluation showed that most of the compounds have obvious protective effects on myocardium injured by hypoxia-reoxygenation, of which 5 compounds are more active than salidroside in a dose-dependent manner.