2,3-benzodiazepin-1,4-diones as peptidomimetic inhibitors of γ-secretase

被引:28
作者
Prasad, CVC
Vig, S
Smith, DW
Gao, Q
Polson, CT
Corsa, JA
Guss, VL
Loo, A
Barten, DM
Zheng, M
Felsenstein, KM
机构
[1] Bristol Myers Squibb Co, Pharmaceut Res Inst, Dept Discovery Chem, Wallingford, CT 06492 USA
[2] Bristol Myers Squibb Pharamaceut Res Inst, Dept Analyt R&D, Wallingford, CT 06492 USA
[3] Bristol Myers Squibb Co, Pharmaceut Res Inst, Dept Neurosci Biol, Wallingford, CT 06492 USA
[4] Bristol Myers Squibb Co, Pharmaceut Res Inst, Dept Drug Metab & Pharmacokinet, Wallingford, CT 06492 USA
关键词
D O I
10.1016/j.bmcl.2004.04.056
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
2,3-Benzodiazepin-1,4-diones were designed as peptidomimetics at the carboxy terminus of hydroxyamides. Inhibition of brain Abeta production was improved by one of the compounds containing constrained modification. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码:3535 / 3538
页数:4
相关论文
共 18 条
[11]   Amyloid precursor protein processing and A beta(42) deposition in a transgenic mouse model of Alzheimer disease [J].
JohnsonWood, K ;
Lee, M ;
Motter, R ;
Hu, K ;
Gordon, G ;
Barbour, R ;
Khan, K ;
Gordon, M ;
Tan, H ;
Games, D ;
Lieberburg, I ;
Schenk, D ;
Seubert, P ;
McConlogue, L .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1997, 94 (04) :1550-1555
[12]   BENZOCYCLOALKYL AMINES AS NOVEL C-TERMINI FOR HIV PROTEASE INHIBITORS [J].
LYLE, TA ;
WISCOUNT, CM ;
GUARE, JP ;
THOMPSON, WJ ;
ANDERSON, PS ;
DARKE, PL ;
ZUGAY, JA ;
EMINI, EA ;
SCHLEIF, WA ;
QUINTERO, JC ;
DIXON, RAF ;
SIGAL, IS ;
HUFF, JR .
JOURNAL OF MEDICINAL CHEMISTRY, 1991, 34 (03) :1228-1230
[13]  
MATTSON MP, 1992, J NEUROSCI, V12, P379
[14]   Hydroxytriamides as potent γ-secretase inhibitors [J].
Prasada, CVC ;
Noonan, JW ;
Sloan, CP ;
Lau, W ;
Vig, S ;
Parker, MF ;
Smith, DW ;
Hansel, SB ;
Polson, CT ;
Barten, DM ;
Felsenstein, KM ;
Roberts, SB .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2004, 14 (08) :1917-1921
[15]   PHYSIOLOGICAL PRODUCTION OF THE BETA-AMYLOID PROTEIN AND THE MECHANISM OF ALZHEIMERS-DISEASE [J].
SELKOE, DJ .
TRENDS IN NEUROSCIENCES, 1993, 16 (10) :403-409
[16]   Neuroscience - Alzheimer's disease: Genotypes, phenotype, and treatments [J].
Selkoe, DJ .
SCIENCE, 1997, 275 (5300) :630-631
[17]   AN INCREASED PERCENTAGE OF LONG AMYLOID-BETA PROTEIN SECRETED BY FAMILIAL AMYLOID-BETA PROTEIN-PRECURSOR (BETA-APP(717)) MUTANTS [J].
SUZUKI, N ;
CHEUNG, TT ;
CAI, XD ;
ODAKA, A ;
OTVOS, L ;
ECKMAN, C ;
GOLDE, TE ;
YOUNKIN, SG .
SCIENCE, 1994, 264 (5163) :1336-1340
[18]   NEUROTROPHIC AND NEUROTOXIC EFFECTS OF AMYLOID BETA-PROTEIN - REVERSAL BY TACHYKININ NEUROPEPTIDES [J].
YANKNER, BA ;
DUFFY, LK ;
KIRSCHNER, DA .
SCIENCE, 1990, 250 (4978) :279-282