title: Exploration of cathepsin S inhibitors characterized by a triazole P1-P2 amide replacement.
abstract: This paper details exploration of a class of triazole-based cathepsin S inhibitors originally reported by Ellman and co-workers. SAR studies involving modifications across the whole inhibitor provide a perspective on the strengths and weaknesses of this class of inhibitors. In addition, we put the unique characteristics of this class of compounds into perspective with other classes of cathepsin S inhibitors.
authors.affiliation: Department of Medicinal Chemistry, Immunology and Inflammation, Boehringer Ingelheim Pharmaceutical, Inc., 900 Ridgebury Road, Ridgefield, CT 06877, USA. Neil.Moss@comcast.com
authors.forename: Neil
authors.initials: N
authors.lastname: Moss
authors.forename: Zhaoming
authors.initials: Z
authors.lastname: Xiong
authors.forename: Mike
authors.initials: M
authors.lastname: Burke
authors.forename: Derek
authors.initials: D
authors.lastname: Cogan
authors.forename: Donghong A
authors.initials: DA
authors.lastname: Gao
authors.forename: Kathleen
authors.initials: K
authors.lastname: Haverty
authors.forename: Alexander
authors.initials: A
authors.lastname: Heim-Riether
authors.forename: Eugene R
authors.initials: ER
authors.lastname: Hickey
authors.forename: Raj
authors.initials: R
authors.lastname: Nagaraja
authors.forename: Matthew
authors.initials: M
authors.lastname: Netherton
authors.forename: Kathy
authors.initials: K
authors.lastname: O'Shea
authors.forename: Philip
authors.initials: P
authors.lastname: Ramsden
authors.forename: Racheline
authors.initials: R
authors.lastname: Schwartz
authors.forename: Daw-Tsun
authors.initials: DT
authors.lastname: Shih
authors.forename: Yancey
authors.initials: Y
authors.lastname: Ward
authors.forename: Erick
authors.initials: E
authors.lastname: Young
authors.forename: Qing
authors.initials: Q
authors.lastname: Zhang
mesh_terms: D000577:Amides / Q000737:chemistry*; D002403:Cathepsins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006207:Half-Life; D006801:Humans; D008862:Microsomes, Liver / Q000378:metabolism; D011480:Protease Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D011485:Protein Binding; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D014230:Triazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics
chemical_list: D000577:Amides; D011480:Protease Inhibitors; D013876:Thiophenes; D014230:Triazoles; D002403:Cathepsins; C028217:cathepsin S