title: 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.affiliation: College of Chemistry, Sichuan University, 29 Wangjiang Road, Chengdu, 610064, Sichuan Province, China.
authors.forename: Tingting
authors.initials: T
authors.lastname: Cao
authors.affiliation: College of Chemistry, Sichuan University, 29 Wangjiang Road, Chengdu, 610064, Sichuan Province, China.
authors.forename: Yong
authors.initials: Y
authors.lastname: Li
authors.affiliation: College of Chemistry & Environment Protection Engineering, Southwest University for Nationalities, Section 4, Southern First Ring Road, Chengdu, 610041, Sichuan Province, China.
authors.forename: Ziyao
authors.initials: Z
authors.lastname: Yang
authors.affiliation: College of Chemistry, Sichuan University, 29 Wangjiang Road, Chengdu, 610064, Sichuan Province, China.
authors.forename: Mingxing
authors.initials: M
authors.lastname: Yuan
authors.affiliation: College of Chemistry, Sichuan University, 29 Wangjiang Road, Chengdu, 610064, Sichuan Province, China.
authors.forename: Ying
authors.initials: Y
authors.lastname: Li
authors.affiliation: College of Chemistry & Environment Protection Engineering, Southwest University for Nationalities, Section 4, Southern First Ring Road, Chengdu, 610041, Sichuan Province, China.
authors.forename: Hongjun
authors.initials: H
authors.lastname: Yang
authors.affiliation: College of Chemistry & Environment Protection Engineering, Southwest University for Nationalities, Section 4, Southern First Ring Road, Chengdu, 610041, Sichuan Province, China.
authors.forename: Yuchuan
authors.initials: Y
authors.lastname: Feng
authors.affiliation: College of Chemistry, Sichuan University, 29 Wangjiang Road, Chengdu, 610064, Sichuan Province, China.
authors.forename: Shufan
authors.initials: S
authors.lastname: Yin
mesh_terms: D000818:Animals; D000897:Anti-Ulcer Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use*; D052176:Azulenes / Q000737:chemistry* / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D008297:Male; D051379:Mice
chemical_list: D000897:Anti-Ulcer Agents; D052176:Azulenes; C005525:azulene
keywords: anti-gastric ulcer; guaiazulene; sodium guaiazulene sulfonate; ulcer index