title: Discovery and parallel synthesis of a new class of cathepsin K inhibitors.
abstract: Peptidomimetic aminomethyl ketones have been identified as a new class of cathepsin K inhibitors. Traditional and high-speed parallel synthesis techniques were applied to investigate this series. Structure-activity relationships were established, and certain analogues were characterized with IC(50) values in the range 200-500 nM.
authors.affiliation: Department of Chemistry Research, Bayer Research Center, 400 Morgan Lane, West Haven, CT 06516, USA. roger.smith.b@bayer.com
authors.forename: R A
authors.initials: RA
authors.lastname: Smith
authors.forename: A
authors.initials: A
authors.lastname: Bhargava
authors.forename: C
authors.initials: C
authors.lastname: Browe
authors.forename: J
authors.initials: J
authors.lastname: Chen
authors.forename: J
authors.initials: J
authors.lastname: Dumas
authors.forename: H
authors.initials: H
authors.lastname: Hatoum-Mokdad
authors.forename: R
authors.initials: R
authors.lastname: Romero
mesh_terms: D056657:Cathepsin K; D002403:Cathepsins / Q000037:antagonists & inhibitors*; D015853:Cysteine Proteinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry; D015195:Drug Design; D020128:Inhibitory Concentration 50; D007659:Ketones / Q000737:chemistry*; D007700:Kinetics; D018716:Molecular Mimicry; D013329:Structure-Activity Relationship
chemical_list: D015853:Cysteine Proteinase Inhibitors; D007659:Ketones; D002403:Cathepsins; D056657:Cathepsin K