Arylaminoethyl amides as inhibitors of the cysteine protease cathepsin K -: Investigating P1′ substituents

被引:22
作者
Altmann, E [1 ]
Green, J
Tintelnot-Blomley, M
机构
[1] Novartis Pharma AG, Arthrit & Bone Metab Therapeut Area, CH-4002 Basel, Switzerland
[2] Novartis Pharma AG, Nervous Syst Therapeut Area, CH-4002 Basel, Switzerland
关键词
D O I
10.1016/S0960-894X(03)00344-5
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Modeling, synthesis and in vitro activities of a series of arylaminoethyl amide based inhibitors of the cysteine protease cathepsin K are described. (C) 2003 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1997 / 2001
页数:5
相关论文
共 17 条
[1]   Arylaminoethyl amides as novel non-covalent cathepsin K inhibitors [J].
Altmann, E ;
Renaud, J ;
Green, J ;
Farley, D ;
Cutting, B ;
Jahnke, W .
JOURNAL OF MEDICINAL CHEMISTRY, 2002, 45 (12) :2352-2354
[2]   HUMAN CATHEPSIN O2, A NOVEL CYSTEINE PROTEASE HIGHLY EXPRESSED IN OSTEOCLASTOMAS AND OVARY MOLECULAR-CLONING, SEQUENCING AND TISSUE DISTRIBUTION [J].
BROMME, D ;
OKAMOTO, K .
BIOLOGICAL CHEMISTRY HOPPE-SEYLER, 1995, 376 (06) :379-384
[3]   Cysteine proteases as therapeutic targets [J].
Brömme, D .
DRUG NEWS & PERSPECTIVES, 1999, 12 (02) :73-82
[4]   Cathepsin K, but not cathepsins B, L, or S, is abundantly expressed in human osteoclasts [J].
Drake, FH ;
Dodds, RA ;
James, IE ;
Connor, JR ;
Debouck, C ;
Richardson, S ;
LeeRykaczewski, E ;
Coleman, L ;
Rieman, D ;
Barthlow, R ;
Hastings, G ;
Gowen, M .
JOURNAL OF BIOLOGICAL CHEMISTRY, 1996, 271 (21) :12511-12516
[5]   Novel, nonpeptidic cyanamides as potent and reversible inhibitors of human cathepsins K and L [J].
Falgueyret, JP ;
Oballa, RM ;
Okamoto, O ;
Wesolowski, G ;
Aubin, Y ;
Rydzewski, RM ;
Prasit, P ;
Riendeau, D ;
Rodan, SB ;
Percival, MD .
JOURNAL OF MEDICINAL CHEMISTRY, 2001, 44 (01) :94-104
[6]   The collagenolytic activity of cathepsin K is unique among mammalian proteinases [J].
Garnero, P ;
Borel, O ;
Byrjalsen, I ;
Ferreras, M ;
Drake, FH ;
McQueney, MS ;
Foged, NT ;
Delmas, PD ;
Delaissé, JM .
JOURNAL OF BIOLOGICAL CHEMISTRY, 1998, 273 (48) :32347-32352
[7]   Characterization of novel cathepsin K mutations in the pro and mature polypeptide regions causing pycnodysostosis [J].
Hou, WS ;
Brömme, D ;
Zhao, YM ;
Mehler, E ;
Dushey, C ;
Weinstein, H ;
Miranda, CS ;
Fraga, C ;
Greig, F ;
Carey, J ;
Rimoin, DL ;
Desnick, RJ ;
Gelb, BD .
JOURNAL OF CLINICAL INVESTIGATION, 1999, 103 (05) :731-738
[8]   Identification of potent and selective mechanism-based inhibitors of the cysteine protease cruzain using solid-phase parallel synthesis [J].
Huang, L ;
Lee, A ;
Ellman, JA .
JOURNAL OF MEDICINAL CHEMISTRY, 2002, 45 (03) :676-684
[9]   MOLECULAR-CLONING OF HUMAN CDNA FOR CATHEPSIN-K - NOVEL CYSTEINE PROTEINASE PREDOMINANTLY EXPRESSED IN BONE [J].
INAOKA, T ;
BILBE, G ;
ISHIBASHI, O ;
TEZUKA, K ;
KUMEGAWA, M ;
KOKUBO, T .
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1995, 206 (01) :89-96
[10]   Protease inhibitors: Current status and future prospects [J].
Leung, D ;
Abbenante, G ;
Fairlie, DP .
JOURNAL OF MEDICINAL CHEMISTRY, 2000, 43 (03) :305-341