title: Synthesis and antidiabetic activity of 5,7-dihydroxyflavonoids and analogs.
abstract: In a study to evaluate the structural elements essential for the antidiabetic activity of flavonoids, we synthesized two series of flavonoids, 5,7-dihydroxyflavanones and 5,7-dihydroxyflavones. In a screening for potential antidiabetic activity, most of the flavonoids showed a remarkable in vitro activity, and compounds 1f, 2d, and 3c were significantly more effective than the positive control, metformin. The biological activity was mainly affected by structural modification at the ring B moiety of the flavonoid skeleton. The results suggest that 5,7-dihydroxyflavonoids can be considered as promising candidates in the development of new antidiabetic lead compounds.
authors.affiliation: School of Pharmaceutical Sciences, Research Center of Basic Medical Sciences, Tianjin Medical University, Tianjin 300070, P. R. China.
authors.forename: Liu-Shuan
authors.initials: LS
authors.lastname: Chang
authors.forename: Chun-Bao
authors.initials: CB
authors.lastname: Li
authors.forename: Nan
authors.initials: N
authors.lastname: Qin
authors.forename: Mei-Na
authors.initials: MN
authors.lastname: Jin
authors.forename: Hong-Quan
authors.initials: HQ
authors.lastname: Duan
mesh_terms: D055372:AMP-Activated Protein Kinases / Q000378:metabolism; D044950:Flavanones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D005419:Flavonoids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D056945:Hep G2 Cells; D006801:Humans; D007004:Hypoglycemic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015398:Signal Transduction / Q000187:drug effects
chemical_list: D044950:Flavanones; D005419:Flavonoids; D007004:Hypoglycemic Agents; C016063:pinocembrin; D055372:AMP-Activated Protein Kinases