1. Synthesis and Biological Evaluation of 3, 8-dimethyl-5-isopropylazulene Derivatives as Anti-gastric Ulcer Agent.
- Author
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Cao T, Li Y, Yang Z, Yuan M, Li Y, Yang H, Feng Y, and Yin S
- Subjects
- Animals, Anti-Ulcer Agents pharmacology, Drug Evaluation, Preclinical, Male, Mice, Anti-Ulcer Agents chemical synthesis, Anti-Ulcer Agents therapeutic use, Azulenes chemistry, Azulenes pharmacology
- 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., (© 2016 John Wiley & Sons A/S.)
- Published
- 2016
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