首页 | 本学科首页   官方微博 | 高级检索  
检索        


Imidazo[1,2-a]quinoxalin-4-amines: A novel class of nonxanthine A1-adenosine receptor antagonists
Authors:Stefano Ceccarelli  Alessandra D'Alessandro  Michela Prinzivalli  Sergio Zanarella
Institution:aBiomedica Foscama Research Centre, via Morolense 87, 03013 Ferentino (FR), Italy
Abstract:The syntheses and A1 adenosine receptor affinities of a number of imidazo1,2-a]quinoxalin-4-amines are reported. Structure—activity relationships within the series and in comparison with other similar tricyclic nonxanthine adenosine antagonists are discussed, leading to a putative common binding mode of these nitrogen-containing heterocycles to A1 adenosine receptors. Secondary amino compounds displayed the best affinities toward A1 receptors, while the tertiary amines were almost devoid of activity, thus suggesting a crucial role for the hydrogen bond-forming 4-NH group. Remarkably higher potencies for 1-methyl and N-cyclopentyl derivatives were also found. 4-Cyclopentylamino-1-methylimidazo1,2-a]quinoxaline (TRFI 165) is the most potent compound in this series, having Ki(A1) = 7.9 nM. It is also provided with a good A1 selectivity both versus A2a and A3 subtypes and was selected for further pharmacological studies.
Keywords:adenosine receptors  imidazo[1  2-a]quinoxaline  tricyclic heteroaromatic systems  nonxanthine A1-adenosine antagonists  IRFI 165
本文献已被 ScienceDirect 等数据库收录!
设为首页 | 免责声明 | 关于勤云 | 加入收藏

Copyright©北京勤云科技发展有限公司  京ICP备09084417号