title: Design, synthesis and inhibitory activities of 8-(substituted styrol-formamido)phenyl-xanthine derivatives on monoamine oxidase B.
abstract: The design and synthesis of two series of 8-(substituted styrol-formamido)phenyl-xanthine derivatives are described. Their in vitro monoamine oxidase B (MAO-B) inhibition were tested and the effect of substituents on the N-7, phenyl and the substituted positions are discussed. It was observed that compound 9b displayed significant MAO-B inhibition activity and selectivity, fluorine substitution plays a key role in the selectivity of MAO-B inhibition, and the styrol-formamido group at position-3' may enhance the activity and selectivity of 8-phenyl-xanthine analogues. These results suggest that such compounds may be utilized for the development of new candidate MAO-B inhibitors for treatment of Parkinson's disease.
authors.affiliation: School of Pharmacy, Wenzhou Medical College, Department of Heurology, the First Affiliated Hospital of Wenzhou Medical College, Zhejiang, PR China.
authors.forename: Suwen
authors.initials: S
authors.lastname: Hu
authors.forename: Siyun
authors.initials: S
authors.lastname: Nian
authors.forename: Kuiyou
authors.initials: K
authors.lastname: Qin
authors.forename: Tong
authors.initials: T
authors.lastname: Xiao
authors.forename: Lingna
authors.initials: L
authors.lastname: Li
authors.forename: Xiaolu
authors.initials: X
authors.lastname: Qi
authors.forename: Faqing
authors.initials: F
authors.lastname: Ye
authors.forename: Guang
authors.initials: G
authors.lastname: Liang
authors.forename: Guoxin
authors.initials: G
authors.lastname: Hu
authors.forename: Jincai
authors.initials: J
authors.lastname: He
authors.forename: Yinfei
authors.initials: Y
authors.lastname: Yu
authors.forename: Bo
authors.initials: B
authors.lastname: Song
mesh_terms: D005461:Fluorine / Q000737:chemistry; D008995:Monoamine Oxidase / Q000378:metabolism*; D008996:Monoamine Oxidase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D020058:Styrene / Q000737:chemistry; D019820:Xanthine / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D008996:Monoamine Oxidase Inhibitors; D019820:Xanthine; D005461:Fluorine; D020058:Styrene; D008995:Monoamine Oxidase