Synthesis and biological evaluation of disubstituted N 6-cyclopentyladenine analogues: the search for a neutral antagonist with high affinity for the adenosine A1 …

…, R van Westhoven, T van den Hoven, J Brussee…

Index: De Ligt, Rianne A. F.; Van Der Klein, Pieter A. M.; Von Frijtag Drabbe Kuenzel, Jacobien K.; Lorenzen, Anna; El Maate, Fatna Ait; Fujikawa, Shelly; Van Westhoven, Rosemarijn; Van Den Hoven, Thijs; Brussee, Johannes; Ijzerman, Ad P. Bioorganic and Medicinal Chemistry, 2004 , vol. 12, # 1 p. 139 - 149

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Citation Number: 34

Abstract

Novel 3, 8-and 8, 9-disubstituted N6-cyclopentyladenine derivatives were synthesised in moderate overall yield from 6-chloropurine. The derivatives were made in an attempt to find a new neutral antagonist with high affinity for adenosine A1 receptors. N6-Cyclopentyl-9- methyladenine (N-0840) was used as a lead compound. Binding affinities of the new analogues were determined for human adenosine A1 and A3 receptors. Their intrinsic ...