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Synthesis and Biological Evaluation of 3, 8‐dimethyl‐5‐isopropylazulene Derivatives as Anti‐gastric Ulcer Agent
Author(s) -
Cao Tingting,
Li Yong,
Yang Ziyao,
Yuan Mingxing,
Li Ying,
Yang Hongjun,
Feng Yuchuan,
Yin Shufan
Publication year - 2016
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12753
Subject(s) - omeprazole , ulcer index , ethanol , stomach , chemistry , in vivo , pharmacology , gastroenterology , medicine , gastric mucosa , biochemistry , biology , microbiology and biotechnology
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.