6-(2-Furanyl)-9H-purin-2-amine derivatives as A2A adenosine antagonists

Structure-activity relationships have been investigated through substitutions at the 9-position of the 2-amino-6-(2-furanyl) purine (5) to identify novel and selective A(2A) adenosine receptor antagonists. Several potent and selective antagonists were identified. In particular, compounds 20, 25, and...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2005-04, Vol.15 (8), p.2119-2122
Hauptverfasser:	KISELGOF, Eugenia, TULSHIAN, Deen B, ARIK, Leyla, HONGTAO ZHANG, FAWZI, Ahmad
Format:	Artikel
Sprache:	eng
Schlagworte:	Adenosine A2 Receptor Antagonists Biological and medical sciences Cell Line Humans Medical sciences Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems Pharmacology. Drug treatments Protein Binding - drug effects Protein Binding - physiology Pyrimidines - chemistry Pyrimidines - metabolism Pyrimidines - pharmacology Receptor, Adenosine A2A - metabolism Receptor, Adenosine A2A - physiology Triazoles - chemistry Triazoles - metabolism Triazoles - pharmacology
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Beschreibung
Zusammenfassung:	Structure-activity relationships have been investigated through substitutions at the 9-position of the 2-amino-6-(2-furanyl) purine (5) to identify novel and selective A(2A) adenosine receptor antagonists. Several potent and selective antagonists were identified. In particular, compounds 20, 25, and 26 show very high affinity with excellent selectivity.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2005.02.031