Synthesis and Biological Evaluation of 3, 8‐dimethyl‐5‐isopropylazulene Derivatives as Anti‐gastric Ulcer Agent |
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| Authors: | Ziyao Yang Mingxing Yuan Ying Li Hongjun Yang Yuchuan Feng Shufan Yin |
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| Institution: | 1. College of Chemistry & Environment Protection Engineering, Southwest University for Nationalities, Chengdu, Sichuan Province, China;2. College of Chemistry, Sichuan University, Chengdu, Sichuan Province, China |
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| Abstract: | 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. |
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| Keywords: | anti‐gastric ulcer guaiazulene sodium guaiazulene sulfonate ulcer index |
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