title: 2,6-disubstituted and 2,6,8-trisubstituted purines as adenosine receptor antagonists.
abstract: Purines have long been exploited as adenosine receptor antagonists. The substitution pattern about the purine ring has been well investigated, and certain criteria have become almost a prerequisite for good affinity at the adenosine A(1) receptor. The adaptation of the pharmacophore and the initial series of pyrimidines developed in an earlier publication resulted in a series of purines with an entirely new substitution pattern. One compound in particular, 8-cyclopentyl-2,6-diphenylpurine (31, LUF 5962) has been shown to be very promising with an affinity of 0.29 nM at the human adenosine A(1) receptor.
authors: Leiden/Amsterdam Center for Drug Research, Division of Medicinal Chemistry, P.O. Box 9502, 2300 RA Leiden, The Netherlands.
authors: Lisa C W
authors: LC
authors: Chang
authors: Ronald F
authors: RF
authors: Spanjersberg
authors: Jacobien K
authors: JK
authors: von Frijtag Drabbe Künzel
authors: Thea
authors: T
authors: Mulder-Krieger
authors: Johannes
authors: J
authors: Brussee
authors: Adriaan P
authors: AP
authors: Ijzerman