title: Synthesis and SAR of novel 4,5-diarylimidazolines as potent P2X7 receptor antagonists.
abstract: 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.
authors.affiliation: Aventis Inc., 1041 Route 202-206, Bridgewater, New Jersey, NJ 08807-0800, USA. gregory.merriman@aventis.com
authors.forename: Gregory H
authors.initials: GH
authors.lastname: Merriman
authors.forename: Liang
authors.initials: L
authors.lastname: Ma
authors.forename: Patrick
authors.initials: P
authors.lastname: Shum
authors.forename: Daniel
authors.initials: D
authors.lastname: McGarry
authors.forename: Frank
authors.initials: F
authors.lastname: Volz
authors.forename: Jeffrey S
authors.initials: JS
authors.lastname: Sabol
authors.forename: Alexandre
authors.initials: A
authors.lastname: Gross
authors.forename: Zhicheng
authors.initials: Z
authors.lastname: Zhao
authors.forename: David
authors.initials: D
authors.lastname: Rampe
authors.forename: Lin
authors.initials: L
authors.lastname: Wang
authors.forename: Friederike
authors.initials: F
authors.lastname: Wirtz-Brugger
authors.forename: Bruce A
authors.initials: BA
authors.lastname: Harris
authors.forename: Douglas
authors.initials: D
authors.lastname: Macdonald
mesh_terms: 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
chemical_list: D006841:Hydrocarbons, Aromatic; D007093:Imidazoles; D048288:Imidazolines; D058919:Purinergic P2 Receptor Antagonists; D058486:Receptors, Purinergic P2X7