Design, synthesis, and biological evaluation of novel 4-alkylamino-1-hydroxymethylimidazo [1, 2-a] quinoxalines as adenosine A 1 receptor antagonists

CH Liu, B Wang, WZ Li, LH Yun, Y Liu, RB Su…

Index: Liu, Chun-He; Wang, Bo; Li, Wei-Zhang; Yun, Liu-Hong; Liu, Ying; Su, Rui-Bing; Li, Jin; Liu, He Bioorganic and Medicinal Chemistry, 2004 , vol. 12, # 17 p. 4701 - 4707

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Citation Number: 19

Abstract

A series of 4-alkylamino-1-hydroxymethylimidazo [1, 2-a] quinoxalines have been synthesized and evaluated for their adenosine A1 receptor inhibitory activity in the radioligand binding assays. The compounds were tested for the inhibition percent (IP) and the affinity toward A1AR (Ki) that IP were more than 90% in the nanomolar range. 4- Cyclopentylamino-7, 8-dichloro-1-hydroxymethylimidazo [1, 2-a] quinoxaline 18 is the ...