title: Stereoselective synthesis of bioactive isosteviol derivatives as alpha-glucosidase inhibitors.
abstract: Considerable interest has been attracted in isosteviol and its derivatives because of their large variety of pharmacological activities. In this project, a series of novel compounds containing hydroxyl, hydroxymethyl group and heteroatom-containing frameworks fused with isosteviol structure were synthesized and evaluated as alpha-glucosidase inhibitors, aimed at clarifying the structure-activity correlation. The results indicated that these isosteviol derivatives were capable of inhibiting in vitro alpha-glucosidase with moderate to good activities. Among them, indole derivative 15b exhibited the highest activities and thus may be exploitable as a lead compound for the development of potent alpha-glucosidase inhibitors.
authors.affiliation: Department of Chemistry, New Drug Research & Development Center, Zhengzhou University, Zhengzhou, China.
authors.forename: Ya
authors.initials: Y
authors.lastname: Wu
authors.forename: Jing-Hua
authors.initials: JH
authors.lastname: Yang
authors.forename: Gui-Fu
authors.initials: GF
authors.lastname: Dai
authors.forename: Cong-Jun
authors.initials: CJ
authors.lastname: Liu
authors.forename: Guo-Qiang
authors.initials: GQ
authors.lastname: Tian
authors.forename: Wen-Yan
authors.initials: WY
authors.lastname: Ma
authors.forename: Jing-Chao
authors.initials: JC
authors.lastname: Tao
mesh_terms: D018360:Crystallography, X-Ray; D045786:Diterpenes, Kaurane / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D065089:Glycoside Hydrolase Inhibitors; D006900:Hydroxylation; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D008958:Models, Molecular; D015394:Molecular Structure; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D045786:Diterpenes, Kaurane; D004791:Enzyme Inhibitors; D065089:Glycoside Hydrolase Inhibitors; D007211:Indoles; C515747:isosteviol