Synthesis and Biological Evaluation of 3, 8-dimethyl-5-isopropylazulene Derivatives as Anti-gastric Ulcer Agent.

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.

• Authors: Tingting Cao, Yong Li, Ziyao Yang, Mingxing Yuan, Ying Li, Hongjun Yang, Yuchuan Feng, Shufan Yin
• Journal: Chemical biology & drug design (Chem Biol Drug Des) Vol. 88 Issue 2 Pg. 264-71 (Aug 2016) ISSN: 1747-0285 [Electronic] England
• PMID: 26938488 (Publication Type: Journal Article)
• Copyright: © 2016 John Wiley & Sons A/S.

Chemical References

• Anti-Ulcer Agents
• Azulenes
• azulene

Topics

• Animals
• Anti-Ulcer Agents (chemical synthesis, pharmacology, therapeutic use)
• Azulenes (chemistry, pharmacology)
• Drug Evaluation, Preclinical
• Male
• Mice