Synthesis and Biological Evaluation of 3, 8-dimethyl-5-isopropylazulene Derivatives as Anti-gastric Ulcer Agent

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• 作者：Tingting Cao ; Yong Li ; Ziyao Yang ; Mingxing Yuan ; Ying Li ; Hongjun Yang ; Yuchuan Feng and Shufan Yin
• 刊名：Chemical Biology & Drug Design
• 出版年：2016
• 出版时间：August 2016
• 年：2016
• 卷：88
• 期：2
• 页码：264-271
• 全文大小：908K
• ISSN：1747-0285

文摘

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.