title: Sulfide analogues as potent and selective M(2) muscarinic receptor antagonists.
abstract: We have discovered highly potent, selective sulfide M(2) receptor antagonists with low molecular weight and different structural features compared with our phase I clinical candidate Sch 211803. Analogue 30 showed superior M(2) receptor selectivity profile over Sch 211803. More importantly, this study provided new leads for the discovery of M(2) receptor antagonists as potential drug candidates.
authors.affiliation: Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. yuguang.wang@spcorp.com
authors.forename: Yuguang
authors.initials: Y
authors.lastname: Wang
authors.forename: Samuel
authors.initials: S
authors.lastname: Chackalamannil
authors.forename: Zhiyong
authors.initials: Z
authors.lastname: Hu
authors.forename: Brian A
authors.initials: BA
authors.lastname: McKittrick
authors.forename: William
authors.initials: W
authors.lastname: Greenlee
authors.forename: Vilma
authors.initials: V
authors.lastname: Ruperto
authors.forename: Ruth A
authors.initials: RA
authors.lastname: Duffy
authors.forename: Jean E
authors.initials: JE
authors.lastname: Lachowicz
mesh_terms: D001665:Binding Sites; D001667:Binding, Competitive; D018727:Muscarinic Antagonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D043643:Receptor, Muscarinic M1; D043585:Receptor, Muscarinic M2; D043587:Receptor, Muscarinic M3; D043588:Receptor, Muscarinic M4; D011976:Receptors, Muscarinic / Q000187:drug effects* / Q000378:metabolism; D013440:Sulfides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D018727:Muscarinic Antagonists; D043643:Receptor, Muscarinic M1; D043585:Receptor, Muscarinic M2; D043587:Receptor, Muscarinic M3; D043588:Receptor, Muscarinic M4; D011976:Receptors, Muscarinic; D013440:Sulfides