title: Discovery of orally active butyrolactam 11beta-HSD1 inhibitors.
abstract: A series of metabolically stable butyrolactam 11beta-HSD1 inhibitors have been synthesized and biologically evaluated. These compounds exhibit excellent HSD1 potency and HSD2 selectivity, pharmacokinetic, and pharmacodynamic profiles.
authors.affiliation: Metabolic Disease Research, Abbott Laboratories, 100 Abbott Park Road, AP-10-304B, Abbott Park, IL 60064, USA. vince.yeh@abbott.com
authors.forename: Vince S C
authors.initials: VS
authors.lastname: Yeh
authors.forename: Ravi
authors.initials: R
authors.lastname: Kurukulasuriya
authors.forename: Steven
authors.initials: S
authors.lastname: Fung
authors.forename: Katina
authors.initials: K
authors.lastname: Monzon
authors.forename: William
authors.initials: W
authors.lastname: Chiou
authors.forename: Jiahong
authors.initials: J
authors.lastname: Wang
authors.forename: Deanne
authors.initials: D
authors.lastname: Stolarik
authors.forename: Hovis
authors.initials: H
authors.lastname: Imade
authors.forename: Robin
authors.initials: R
authors.lastname: Shapiro
authors.forename: Victoria
authors.initials: V
authors.lastname: Knourek-Segel
authors.forename: Eugene
authors.initials: E
authors.lastname: Bush
authors.forename: Denise
authors.initials: D
authors.lastname: Wilcox
authors.forename: Phong T
authors.initials: PT
authors.lastname: Nguyen
authors.forename: Michael
authors.initials: M
authors.lastname: Brune
authors.forename: Peer
authors.initials: P
authors.lastname: Jacobson
authors.forename: J T
authors.initials: JT
authors.lastname: Link
mesh_terms: D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1 / Q000037:antagonists & inhibitors*; D000284:Administration, Oral; D000818:Animals; D006801:Humans; D007769:Lactams / Q000008:administration & dosage / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology*; D024821:Metabolic Syndrome / Q000188:drug therapy; D051379:Mice
chemical_list: D007769:Lactams; D043205:11-beta-Hydroxysteroid Dehydrogenase Type 1