Design, Synthesis and Inhibitory Activities of 8-(Substituted styrol-formamido)phenyl-xanthine Derivatives on Monoamine Oxidase B

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  • Hu Suwen
    School of Pharmacy, Wenzhou Medical College
  • Nian Siyun
    School of Pharmacy, Wenzhou Medical College
  • Qin Kuiyou
    School of Pharmacy, Wenzhou Medical College
  • Xiao Tong
    School of Pharmacy, Wenzhou Medical College
  • Li Lingna
    School of Pharmacy, Wenzhou Medical College
  • Qi Xiaolu
    School of Pharmacy, Wenzhou Medical College
  • Ye Faqing
    School of Pharmacy, Wenzhou Medical College
  • Liang Guang
    School of Pharmacy, Wenzhou Medical College
  • Hu Guoxin
    School of Pharmacy, Wenzhou Medical College
  • He Jincai
    Department of Heurology, the First Affiliated Hospital of Wenzhou Medical College
  • Yu Yinfei
    The Optometry Eye Hospital of Wenzhou Medical College
  • Song Bo
    School of Pharmacy, Wenzhou Medical College

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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.

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