title: Novel vanadyl complexes with quinoxaline N(1),N(4)-dioxide derivatives as potent in vitro insulin-mimetic compounds.
abstract: As a contribution to the development of novel vanadyl complexes with potential insulin-mimetic activity, three new oxovanadium(IV) complexes with the formula VO(L)(2), where L are 3-amino-quinoxaline-2-carbonitrile N(1),N(4)-dioxide derivatives, have been synthesized. Complexes have been characterized by elemental and thermal analyses, fast atom bombardment mass spectroscopy (FAB-MS), conductivity measurements and electronic, Fourier transform infrared (FTIR) and electron paramagnetic resonance (EPR) spectroscopies. The in vitro insulin-mimetic activity of the vanadyl complexes has been estimated by lipolysis inhibition tests, in which the inhibition of the release of free fatty acid from isolated rat adipocytes treated with epinephrine was determined. All the complexes showed inhibitory effects on free fatty acid release. [V(IV)O(3-amino-6(7)-bromoquinoxaline-2-carbonitrile N(1),N(4)-dioxide)(2)] exhibited higher in vitro insulin-mimetic activity than the very active bis(6-methylpicolinato)oxovanadium(IV), VO(6mpa)(2). This new vanadyl complex is expected to exhibit a higher blood glucose lowering activity than VO(6mpa)(2) in diabetic animals.
authors.affiliation: Cátedra de Química Inorgánica, Facultad de Química, Universidad de la República, Gral. Flores 2124, C.C. 1157, 11800 Montevideo, Uruguay.
authors.forename: Pabla
authors.initials: P
authors.lastname: Noblía
authors.forename: Marisol
authors.initials: M
authors.lastname: Vieites
authors.forename: María H
authors.initials: MH
authors.lastname: Torre
authors.forename: Antonio J
authors.initials: AJ
authors.lastname: Costa-Filho
authors.forename: Hugo
authors.initials: H
authors.lastname: Cerecetto
authors.forename: Mercedes
authors.initials: M
authors.lastname: González
authors.forename: María Laura
authors.initials: ML
authors.lastname: Lavaggi
authors.forename: Yusuke
authors.initials: Y
authors.lastname: Adachi
authors.forename: Hiromu
authors.initials: H
authors.lastname: Sakurai
authors.forename: Dinorah
authors.initials: D
authors.lastname: Gambino
mesh_terms: D017667:Adipocytes / Q000187:drug effects / Q000378:metabolism; D000818:Animals; D002478:Cells, Cultured; D004578:Electron Spin Resonance Spectroscopy; D004809:Ephedrine / Q000494:pharmacology; D007004:Hypoglycemic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D007328:Insulin / Q000494:pharmacology; D008066:Lipolysis / Q000187:drug effects; D008297:Male; D018716:Molecular Mimicry; D015394:Molecular Structure; D009942:Organometallic Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011810:Quinoxalines / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D014638:Vanadates / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D007004:Hypoglycemic Agents; D007328:Insulin; D009942:Organometallic Compounds; D011810:Quinoxalines; D014638:Vanadates; C003282:quindoxin; D004809:Ephedrine