Design and synthesis of 8-substituted benzamido-phenylxanthine derivatives as MAO-B inhibitors

…, T Xiao, X Qi, LN Li, K Qin, S Nian, GX Hu, Y Yu…

Index: Song, Bo; Xiao, Tong; Qi, Xiaolu; Li, Ling-Na; Qin, Kuiyou; Nian, Siyun; Hu, Guo-Xin; Yu, Yinfei; Liang, Guang; Ye, Faqing Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 4 p. 1739 - 1742

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Citation Number: 11

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 Ki value of 0.26 μM. Their promising activity in vitro suggests potential use in the treatment of PD.