title: Synthesis and pharmacological evaluation of novel limonin derivatives as anti-inflammatory and analgesic agents with high water solubility.
abstract: A novel series of water-soluble derivatives of limonin were synthesized by introducing various tertiary amines onto the C (7)-position of limonin. Ten target compounds were characterized and screened for their anti-inflammatory and analgesic activity in vivo. Compound 3c exhibited the strongest analgesic and anti-inflammatory activity among the limonin and its derivatives tested; its analgesic activity is more potent than that of aspirin and its anti-inflammatory activity is stronger than that of naproxen.
authors.affiliation: Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing, Jiangsu 21009, China.
authors.forename: Yun
authors.initials: Y
authors.lastname: Yang
authors.affiliation: Department of Pharmacology, China Pharmaceutical University, Nanjing, Jiangsu 210009, China.
authors.forename: Xinhui
authors.initials: X
authors.lastname: Wang
authors.affiliation: Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing, Jiangsu 210009, China.
authors.forename: Qihua
authors.initials: Q
authors.lastname: Zhu
authors.affiliation: Department of Pharmacology, China Pharmaceutical University, Nanjing, Jiangsu 210009, China. Electronic address: gonggq@hotmail.com.
authors.forename: Guoqing
authors.initials: G
authors.lastname: Gong
authors.affiliation: Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing, Jiangsu 210009, China.
authors.forename: Danmeng
authors.initials: D
authors.lastname: Luo
authors.affiliation: Department of Pharmacology, China Pharmaceutical University, Nanjing, Jiangsu 210009, China.
authors.forename: Aidou
authors.initials: A
authors.lastname: Jiang
authors.affiliation: Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing, Jiangsu 210009, China.
authors.forename: Liyan
authors.initials: L
authors.lastname: Yang
authors.affiliation: Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing, Jiangsu 21009, China; Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing, Jiangsu 210009, China. Electronic address: xyg64@126.com.
authors.forename: Yungen
authors.initials: Y
authors.lastname: Xu
mesh_terms: D019342:Acetic Acid / Q000037:antagonists & inhibitors; D000588:Amines / Q000737:chemistry; D000700:Analgesics / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D004431:Ear, External / Q000187:drug effects / Q000473:pathology; D036701:Limonins / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D051379:Mice; D010146:Pain / Q000139:chemically induced / Q000188:drug therapy*; D010147:Pain Measurement / Q000187:drug effects; D012995:Solubility; D014867:Water / Q000737:chemistry*; D014992:Xylenes
chemical_list: D000588:Amines; D000700:Analgesics; D000894:Anti-Inflammatory Agents, Non-Steroidal; D036701:Limonins; D014992:Xylenes; D014867:Water; C001546:limonin; D019342:Acetic Acid
keywords: Analgesic activity; Anti-inflammatory activity; Limonin derivatives; Solubility