title: Muscarinic acetylcholine receptor antagonists: SAR and optimization of tyrosine ureas.
abstract: SAR exploration of multiple regions of a tyrosine urea template led to the identification of very potent muscarinic acetylcholine receptor antagonists such as 10b with good subtype selectivity for M(3) over M(1). The structure-activity relationships (SAR) and optimization of the tyrosine urea series are described.
authors.affiliation: Centers of Excellence for Drug Discovery and Molecular Discovery Research, GlaxoSmithKline, 709 Swedeland Road, King of Prussia, PA 19406, USA. jianjin@unc.edu
authors.forename: Jian
authors.initials: J
authors.lastname: Jin
authors.forename: Yonghui
authors.initials: Y
authors.lastname: Wang
authors.forename: Dongchuan
authors.initials: D
authors.lastname: Shi
authors.forename: Feng
authors.initials: F
authors.lastname: Wang
authors.forename: Wei
authors.initials: W
authors.lastname: Fu
authors.forename: Roderick S
authors.initials: RS
authors.lastname: Davis
authors.forename: Qi
authors.initials: Q
authors.lastname: Jin
authors.forename: James J
authors.initials: JJ
authors.lastname: Foley
authors.forename: Henry M
authors.initials: HM
authors.lastname: Sarau
authors.forename: Dwight M
authors.initials: DM
authors.lastname: Morrow
authors.forename: Michael L
authors.initials: ML
authors.lastname: Moore
authors.forename: Ralph A
authors.initials: RA
authors.lastname: Rivero
authors.forename: Michael
authors.initials: M
authors.lastname: Palovich
authors.forename: Michael
authors.initials: M
authors.lastname: Salmon
authors.forename: Kristen E
authors.initials: KE
authors.lastname: Belmonte
authors.forename: Jakob
authors.initials: J
authors.lastname: Busch-Petersen
mesh_terms: D001249:Asthma / Q000188:drug therapy; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D006801:Humans; D020128:Inhibitory Concentration 50; D008956:Models, Chemical; D015394:Molecular Structure; D018727:Muscarinic Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D011976:Receptors, Muscarinic / Q000737:chemistry*; D012492:Salts / Q000737:chemistry; D013329:Structure-Activity Relationship; D014443:Tyrosine / Q000737:chemistry*; D014508:Urea / Q000737:chemistry*
chemical_list: D018727:Muscarinic Antagonists; D011976:Receptors, Muscarinic; D012492:Salts; D014443:Tyrosine; D014508:Urea