Synthesis and SAR of novel 4,5-diarylimidazolines as potent P2X7 receptor antagonists.
A series of 4,5-diarylimidazoline libraries were prepared using high-throughput solid-phase and microwave techniques. The compounds were evaluated as P2X(7) antagonists and their SAR is described.
Merriman
Gregory H
GH
Aventis Inc., 1041 Route 202-206, Bridgewater, New Jersey, NJ 08807-0800, USA. gregory.merriman@aventis.com
Ma
Liang
L
Shum
Patrick
P
McGarry
Daniel
D
Volz
Frank
F
Sabol
Jeffrey S
JS
Gross
Alexandre
A
Zhao
Zhicheng
Z
Rampe
David
D
Wang
Lin
L
Wirtz-Brugger
Friederike
F
Harris
Bruce A
BA
Macdonald
Douglas
D
D000818:Animals; D002460:Cell Line; D006224:Cricetinae; D006841:Hydrocarbons, Aromatic / Q000737:chemistry*; D007093:Imidazoles / Q000138:chemical synthesis / Q000494:pharmacology*; D048288:Imidazolines / Q000138:chemical synthesis / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D058919:Purinergic P2 Receptor Antagonists; D058486:Receptors, Purinergic P2X7; D013329:Structure-Activity Relationship
D006841:Hydrocarbons, Aromatic; D007093:Imidazoles; D048288:Imidazolines; D058919:Purinergic P2 Receptor Antagonists; D058486:Receptors, Purinergic P2X7