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Design and Synthesis of Novel Dual‐Action Compounds Targeting the Adenosine A~2A~ Receptor and Adenosine Transporter for Neuroprotection by Jhih-Bin Chen; Eric Minwei Liu; Ting-Rong Chern; Chieh-Wen Yang; Chia-I Lin; Prof. Nai-Kuei Huang; Yun-Lian Lin; Prof. Yijuang Chern; Prof. Jung-Hsin Lin; Prof. Jim-Min Fang is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

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## Abstract A novel compound, __N__^6^‐(4‐hydroxybenzyl)adenosine, isolated from __Gastrodia elata__ and which has been shown to be a potential therapeutic agent for preventing and treating neurodegenerative disease, was found to target both the adenosine A~2A~ receptor (A~2A~R) and the equilibrative nucleoside transporter 1 (ENT1). As A~2A~R and ENT1 are proximal in the synaptic crevice of striatum, where the mutant huntingtin aggregate is located, the dual‐action compounds that concomitantly target these two membrane proteins may be beneficial for the therapy of Huntington’s disease. To design the desired dual‐action compounds, pharmacophore models of the A~2A~R agonists and the ENT1 inhibitors were constructed. Accordingly, potentially active compounds were designed and synthesized by chemical modification of adenosine, particularly at the N^6^ and C^5’^ positions, if the predicted activity was within an acceptable range. Indeed, some of the designed compounds exhibit significant dual‐action properties toward both A~2A~R and ENT1. Both pharmacophore models exhibit good statistical correlation between predicted and measured activities. In agreement with competitive ligand binding

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Author

Jhih-Bin Chen; Eric Minwei Liu; Ting-Rong Chern; Chieh-Wen Yang; Chia-I Lin; Prof. Nai-Kuei Huang; Yun-Lian Lin; Prof. Yijuang Chern; Prof. Jung-Hsin Lin; Prof. Jim-Min Fang

Publisher

John Wiley and Sons; Wiley (John Wiley & Sons); Wiley - V C H Verlag GmbbH & Co.; Wiley (ISSN 1860-7179)

Published

2011

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)