2-(Anilinomethyl) imidazolines as α1 Adrenergic Receptor Agonists: the Discovery of α1a Subtype Selective 2'-Alkylsulfonyl-Substituted Analogues

…, DT Garrison, EC Bigham, DL Saussy…

文献索引：Hodson, Stephen J.; Bishop, Michael J.; Speake, Jason D.; Navas III, Frank; Garrison, Deanna T.; Bigham, Eric C.; Saussy Jr., David L.; Liacos, James A.; Irving, Paul E.; Jeffrey Gobel; Sherman, Bryan W. Journal of Medicinal Chemistry, 2002 , vol. 45, # 11 p. 2229 - 2239

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被引用次数: 19

摘要

A series of 2'-alkylthio-2-(anilinomethyl) imidazolines were prepared to examine the effect of the alkyl group size, sulfur oxidation state, and phenyl ring substitution on ligand binding and agonism of α-adrenergic receptor subtypes α1a, α1b, α1d, α2a, and α2c. Binding at all receptor subtypes decreased for compounds in the sulfone oxidation state as compared to their sulfide analogues. While sulfides were generally potent, nonselective agonists, ...