title: Pyridyl amides as potent inhibitors of T-type calcium channels.
abstract: A novel series of amide T-type calcium channel antagonists were prepared and evaluated using in vitro and in vivo assays. Optimization of the screening hit 3 led to identification of the potent and selective T-type antagonist 37 that displayed in vivo efficacy in rodent models of epilepsy and sleep.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. thomas_reger@merck.com
authors.forename: Thomas S
authors.initials: TS
authors.lastname: Reger
authors.forename: Zhi-Qiang
authors.initials: ZQ
authors.lastname: Yang
authors.forename: Kelly-Ann S
authors.initials: KA
authors.lastname: Schlegel
authors.forename: Youheng
authors.initials: Y
authors.lastname: Shu
authors.forename: Christa
authors.initials: C
authors.lastname: Mattern
authors.forename: Rowena
authors.initials: R
authors.lastname: Cube
authors.forename: Kenneth E
authors.initials: KE
authors.lastname: Rittle
authors.forename: Georgia B
authors.initials: GB
authors.lastname: McGaughey
authors.forename: George D
authors.initials: GD
authors.lastname: Hartman
authors.forename: Cuyue
authors.initials: C
authors.lastname: Tang
authors.forename: Jeanine
authors.initials: J
authors.lastname: Ballard
authors.forename: Yuhsin
authors.initials: Y
authors.lastname: Kuo
authors.forename: Thomayant
authors.initials: T
authors.lastname: Prueksaritanont
authors.forename: Cindy E
authors.initials: CE
authors.lastname: Nuss
authors.forename: Scott M
authors.initials: SM
authors.lastname: Doran
authors.forename: Steven V
authors.initials: SV
authors.lastname: Fox
authors.forename: Susan L
authors.initials: SL
authors.lastname: Garson
authors.forename: Yuxing
authors.initials: Y
authors.lastname: Li
authors.forename: Richard L
authors.initials: RL
authors.lastname: Kraus
authors.forename: Victor N
authors.initials: VN
authors.lastname: Uebele
authors.forename: John J
authors.initials: JJ
authors.lastname: Renger
authors.forename: James C
authors.initials: JC
authors.lastname: Barrow
mesh_terms: D000577:Amides / Q000494:pharmacology*; D000818:Animals; D002121:Calcium Channel Blockers / Q000494:pharmacology*; D020747:Calcium Channels, T-Type / Q000187:drug effects*; D051379:Mice; D051381:Rats; D017208:Rats, Wistar
chemical_list: D000577:Amides; D002121:Calcium Channel Blockers; D020747:Calcium Channels, T-Type