Bioorganic & Medicinal Chemistry Letters 2012-02-15

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

Bo Song, Tong Xiao, Xiaolu Qi, Ling-Na Li, Kuiyou Qin, Siyun Nian, Guo-Xin Hu, Yinfei Yu, Guang Liang, Faqing Ye

Index: Bioorg. Med. Chem. Lett. 22(4) , 1739-42, (2012)

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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.Copyright © 2012 Elsevier Ltd. All rights reserved.