共 18 条
Synthesis and SAR of arylaminoethyl amides as noncovalent inhibitors of cathepsin S: P3 cyclic ethers
被引:30
作者:

Tully, David C.
论文数: 0 引用数: 0
h-index: 0
机构:
Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA

Liu, Hong
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h-index: 0
机构:
Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA

Chatterjee, Arnab K.
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h-index: 0
机构:
Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA

Alper, Phil B.
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h-index: 0
机构:
Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA

Epple, Robert
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h-index: 0
机构:
Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA

Williams, Jennifer A.
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h-index: 0
机构:
Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA

Roberts, Michael J.
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h-index: 0
机构:
Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA

Woodmansee, David H.
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h-index: 0
机构:
Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA

Masick, Brian T.
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h-index: 0
机构:
Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA

Tumanut, Christine
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h-index: 0
机构:
Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA

Li, Jun
论文数: 0 引用数: 0
h-index: 0
机构:
Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA

Spraggon, Glen
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h-index: 0
机构:
Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA

Hornsby, Michael
论文数: 0 引用数: 0
h-index: 0
机构:
Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA

Chang, Jonathan
论文数: 0 引用数: 0
h-index: 0
机构:
Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA

Tuntland, Tove
论文数: 0 引用数: 0
h-index: 0
机构:
Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA

Hollenbeck, Thomas
论文数: 0 引用数: 0
h-index: 0
机构:
Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA

Gordon, Perry
论文数: 0 引用数: 0
h-index: 0
机构:
Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA

Harris, Jennifer L.
论文数: 0 引用数: 0
h-index: 0
机构:
Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA

Karanewsky, Donald S.
论文数: 0 引用数: 0
h-index: 0
机构:
Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA
机构:
[1] Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA
关键词:
cathepsin S;
cysteine protease inhibitor;
noncovalent inhibitor;
peptidomimetic;
X-ray structure;
D O I:
10.1016/j.bmcl.2006.07.033
中图分类号:
R914 [药物化学];
学科分类号:
100701 ;
摘要:
The synthesis and structure-activity relationship of a series of arylaminoethyl amide cathepsin S inhibitors are reported. Optimization of P3 and P2 groups to improve overall physicochemical properties resulted in significant improvements in oral bioavailability over early lead compounds. An X-ray structure of compound 37 bound to the active site of cathepsin S is also reported.
引用
收藏
页码:5112 / 5117
页数:6
相关论文
共 18 条
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Tully, DC
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Tumanut, C
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Li, J
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Hollenbeck, T
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Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA

Karanewsky, DS
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Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA Novartis Res Fdn, Genom Inst, San Diego, CA 92121 USA
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机构: Biotechnol Res Inst, Montreal, PQ H4P 2R2, Canada

Danley, DE
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机构: Biotechnol Res Inst, Montreal, PQ H4P 2R2, Canada

Griffor, MC
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机构: Biotechnol Res Inst, Montreal, PQ H4P 2R2, Canada

Kamath, AV
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机构: Biotechnol Res Inst, Montreal, PQ H4P 2R2, Canada

Wang, LK
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机构: Biotechnol Res Inst, Montreal, PQ H4P 2R2, Canada

Laird, ER
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机构: Biotechnol Res Inst, Montreal, PQ H4P 2R2, Canada

Seddon, AP
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机构: Biotechnol Res Inst, Montreal, PQ H4P 2R2, Canada

Ménard, R
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机构: Biotechnol Res Inst, Montreal, PQ H4P 2R2, Canada

Cygler, M
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机构: Biotechnol Res Inst, Montreal, PQ H4P 2R2, Canada

Rath, VL
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机构: Biotechnol Res Inst, Montreal, PQ H4P 2R2, Canada