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

  • Chem Biol Drug Des. 2016 Aug;88(2):264-71. doi: 10.1111/cbdd.12753.
Tingting Cao  1 ,  Yong Li  1 ,  Ziyao Yang  2 ,  Mingxing Yuan  1 ,  Ying Li  1 ,  Hongjun Yang  2 ,  Yuchuan Feng  2 ,  Shufan Yin  1
Affiliations
  • 1. College of Chemistry, Sichuan University, 29 Wangjiang Road, Chengdu, 610064, Sichuan Province, China.
  • 2. College of Chemistry & Environment Protection Engineering, Southwest University for Nationalities, Section 4, Southern First Ring Road, Chengdu, 610041, Sichuan Province, China.
PMID: 26938488 DOI: 10.1111/cbdd.12753
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.

Keywords
anti-gastric ulcer; guaiazulene; sodium guaiazulene sulfonate; ulcer index.
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