4.5 Article

Synthesis and antigastric ulcer activity of novel 5-isoproyl-3,8-dimethylazulene derivatives

期刊

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 19, 页码 5722-5725

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PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.08.018

关键词

Guaiazulene; Sodium guaiazulene sulfonate; Sulfonamide; Antigastric ulcer

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5-Isoproyl-3,8-dimethylazulene derivatives were synthesized and evaluated for antigastric ulcer activity in vivo. Some of them possess the best activity against gastric ulcer with ulcer index values lower than the drug reference (omeprazole). The structure-activity relationship (SAR) shows that the lipophilic flat structure contributes to quite potent antigastric ulcer activity. (C) 2011 Elsevier Ltd. All rights reserved.

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