title: The identification of potent, selective, and bioavailable cathepsin S inhibitors.
abstract: Highly potent, selective, and bioavailable inhibitors of human, mouse, or rat cathepsin S are described. The key structural features combine a sulfonyl moiety attached to a large group in P2 and a small substituent in P3.
authors.affiliation: Merck Frosst Centre for Therapeutic Research, Department of Medicinal Chemistry, Kirkland, QUE, Canada. jacques-yves_gauthier@merck.com
authors.forename: Jacques Yves
authors.initials: JY
authors.lastname: Gauthier
authors.forename: W Cameron
authors.initials: WC
authors.lastname: Black
authors.forename: Isabelle
authors.initials: I
authors.lastname: Courchesne
authors.forename: Wanda
authors.initials: W
authors.lastname: Cromlish
authors.forename: Sylvie
authors.initials: S
authors.lastname: Desmarais
authors.forename: Robert
authors.initials: R
authors.lastname: Houle
authors.forename: Sonia
authors.initials: S
authors.lastname: Lamontagne
authors.forename: Chun Sing
authors.initials: CS
authors.lastname: Li
authors.forename: Frédéric
authors.initials: F
authors.lastname: Massé
authors.forename: Daniel J
authors.initials: DJ
authors.lastname: McKay
authors.forename: Marc
authors.initials: M
authors.lastname: Ouellet
authors.forename: Joël
authors.initials: J
authors.lastname: Robichaud
authors.forename: Jean-François
authors.initials: JF
authors.lastname: Truchon
authors.forename: Vouy-Linh
authors.initials: VL
authors.lastname: Truong
authors.forename: Qingping
authors.initials: Q
authors.lastname: Wang
authors.forename: M David
authors.initials: MD
authors.lastname: Percival
mesh_terms: D000818:Animals; D002403:Cathepsins / Q000037:antagonists & inhibitors*; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015853:Cysteine Proteinase Inhibitors / Q000737:chemistry; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D006801:Humans; D020128:Inhibitory Concentration 50; D051379:Mice; D008956:Models, Chemical; D008958:Models, Molecular; D008968:Molecular Conformation; D015394:Molecular Structure; D011485:Protein Binding; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D015853:Cysteine Proteinase Inhibitors; D002403:Cathepsins; C028217:cathepsin S