1. Synthesis and Biological Evaluation of 3, 8-dimethyl-5-isopropylazulene Derivatives as Anti-gastric Ulcer Agent
- Author
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Yuchuan Feng, Ying Li, Yuan Mingxing, Hongjun Yang, Cao Tingting, Shu-Fan Yin, Li Yong, and Yang Ziyao
- Subjects
Male ,Drug Evaluation, Preclinical ,Positive control ,Pharmacology ,Ulcer index ,01 natural sciences ,Biochemistry ,Azulenes ,Mice ,chemistry.chemical_compound ,In vivo ,Drug Discovery ,Guaiazulene ,medicine ,Animals ,Sodium guaiazulene sulfonate ,Omeprazole ,Biological evaluation ,010405 organic chemistry ,Chemistry ,Anti-ulcer Agent ,Organic Chemistry ,Anti-Ulcer Agents ,digestive system diseases ,0104 chemical sciences ,010404 medicinal & biomolecular chemistry ,Molecular Medicine ,medicine.drug - 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.
- Published
- 2016