3,8-二甲基-5-异丙基薁衍生物作为抗胃溃疡药物的合成及生物学评价
Synthesis and Biological Evaluation of 3, 8-dimethyl-5-isopropylazulene Derivatives as Anti-gastric Ulcer Agent.
作者信息
Cao Tingting, Li Yong, Yang Ziyao, Yuan Mingxing, Li Ying, Yang Hongjun, Feng Yuchuan, Yin Shufan
机构信息
College of Chemistry, Sichuan University, 29 Wangjiang Road, Chengdu, 610064, Sichuan Province, China.
College of Chemistry & Environment Protection Engineering, Southwest University for Nationalities, Section 4, Southern First Ring Road, Chengdu, 610041, Sichuan Province, China.
出版信息
Chem Biol Drug Des. 2016 Aug;88(2):264-71. doi: 10.1111/cbdd.12753. Epub 2016 Mar 24.
Recent studies showed that Guaiazulene (GA) and Sodium guaiazulene sulfonate (GAS-Na) have good anti-gastric ulcer effect. Here, two series of GA derivatives were synthesized and evaluated for their anti-gastric ulcer activity. The data obtained from in vivo testing of these compounds in a rodent ethanol-induced stomach injury model are discussed. Among the tested compounds, A1, A4, and A9 (ulcer index: 1.125 ± 1.246**, 1.714 ± 0.756*, 1.875 ± 1.126*) exhibited better anti-gastric ulcer activity than the positive control Omeprazole (2.005 ± 1.011*). The information got from these studies and the results of 3D-SAR investigation may be useful in the design of novel anti-gastric ulcer agents.
近期研究表明，愈创蓝油烃（GA）和愈创蓝油烃磺酸钠（GAS-Na）具有良好的抗胃溃疡作用。在此，合成了两个系列的GA衍生物，并对其抗胃溃疡活性进行了评估。讨论了这些化合物在啮齿动物乙醇诱导的胃损伤模型中的体内测试数据。在测试的化合物中，A1、A4和A9（溃疡指数：1.125±1.246**，1.714±0.756*，1.875±1.126*）表现出比阳性对照奥美拉唑（2.005±1.011*）更好的抗胃溃疡活性。从这些研究中获得的信息以及3D-SAR研究结果可能有助于新型抗胃溃疡药物的设计。
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