
European Journal of Medicinal Chemistry p. 59 - 64 (1996)
Update date:2022-08-03
Topics:
Giudice, M. R. Del
Borioni, A.
Mustazza, C.
Gatta, F.
Dionisotti, S.
et al.
Some 1,3,7-trisubstituted-8-styrylxanthine analogues, with the aryl group replaced by a heterocycle or cyclohexane ring, were prepared and evaluated for their interaction with the A1 and A2a adenosine receptors.The highest degree of activity was displayed by the 1,3-dipropyl-7-methyl-8-<2-(3-thienyl)ethenyl>xanthine 4cdi, which was found to be a potent and selective A2a antagonist in binding assays (Ki = 19 nM, A1/A2a ratio = 30). - Keywords: 8-styrylxanthine analogue; adenosine A2a receptor antagonist
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