title: Design and synthesis of 8-substituted benzamido-phenylxanthine derivatives as MAO-B inhibitors.
abstract: Monoamine oxidase-B (MAO-B) inhibitor has been used as neuroprotectants to treat the motor deficits of Parkinson's disease (PD). We designed and synthesized a class of 8-substituted benzamido-phenylxanthine derivatives as MAO-B inhibitors. The compounds have various inhibitory effects, with compound 6a having a K(i) value of 0.26 μM. Their promising activity in vitro suggests potential use in the treatment of PD.
authors.affiliation: School of Pharmacy, Wenzhou Medical College, Wenzhou, PR China.
authors.forename: Bo
authors.initials: B
authors.lastname: Song
authors.forename: Tong
authors.initials: T
authors.lastname: Xiao
authors.forename: Xiaolu
authors.initials: X
authors.lastname: Qi
authors.forename: Ling-Na
authors.initials: LN
authors.lastname: Li
authors.forename: Kuiyou
authors.initials: K
authors.lastname: Qin
authors.forename: Siyun
authors.initials: S
authors.lastname: Nian
authors.forename: Guo-Xin
authors.initials: GX
authors.lastname: Hu
authors.forename: Yinfei
authors.initials: Y
authors.lastname: Yu
authors.forename: Guang
authors.initials: G
authors.lastname: Liang
authors.forename: Faqing
authors.initials: F
authors.lastname: Ye
mesh_terms: D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002460:Cell Line; D015195:Drug Design; D004789:Enzyme Activation / Q000187:drug effects; D006801:Humans; D051379:Mice; D015394:Molecular Structure; D008996:Monoamine Oxidase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D019800:Phenol / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D011687:Purines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D014970:Xanthines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: C572259:(E)-2-styryl-1-methylbenzimidazole; D000577:Amides; D001562:Benzimidazoles; D008996:Monoamine Oxidase Inhibitors; D011687:Purines; D014970:Xanthines; C111599:istradefylline; D019800:Phenol