title: Inhibition of Alpha-Glucosidase by Synthetic Derivatives of Lupane, Oleanane, Ursane and Dammarane Triterpenoids.
abstract: A variety of new and earlier synthesized lupane, oleanane, ursane and dammarane triterpenoids have been investigated for their inhibitory activity against α-glucosidase. 2,3-Indole-21 β-acetyl-20β,28-epoxy-18α,19βH-ursane and 3-oxo-3A-homo-3a-aza-20(S)-hydroxydammar-24(25)-ene were synthesized for the first time. The compounds 3, 4, 8-11 and 14 demonstrated strong in vitro inhibitory activity towards α-glucosidase with IC₅₀ values of 37.5-115.1 µM. 3-Deoxy-3a-homo-3a-aza-28-cinnamoyloxy-20(29)-lupene, with an IC₅₀ of 6.67 µM was 60-fold more active than the market drug acarbose.
authors.forename: El'mira F
authors.initials: EF
authors.lastname: Khusnutdinova
authors.forename: Irina E
authors.initials: IE
authors.lastname: Smirnova
authors.forename: Gul'nara V
authors.initials: GV
authors.lastname: Giniyatullina
authors.forename: Natal'ya I
authors.initials: NI
authors.lastname: Medvedeva
authors.forename: Emil Yu
authors.initials: EY
authors.lastname: Yamansarov
authors.forename: Dmitri V
authors.initials: DV
authors.lastname: Kazakov
authors.forename: Oxana B
authors.initials: OB
authors.lastname: Kazakova
authors.forename: Pham T
authors.initials: PT
authors.lastname: Linh
authors.forename: Do Quoc
authors.initials: do Q
authors.lastname: Viet
authors.forename: DoThi Thu
authors.initials: DT
authors.lastname: Huong
mesh_terms: D065089:Glycoside Hydrolase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D009828:Oleanolic Acid / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology; D014315:Triterpenes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000520:alpha-Glucosidases; D000097669:Dammaranes; D053978:Pentacyclic Triterpenes
chemical_list: D065089:Glycoside Hydrolase Inhibitors; D009828:Oleanolic Acid; D014315:Triterpenes; D000520:alpha-Glucosidases; D000097669:Dammaranes; C413246:oleanane; C000606873:ursane; D053978:Pentacyclic Triterpenes; C480546:lupane