Discovery of (S)-2-((S)-2-(3, 5-difluorophenyl)-2-hydroxyacetamido)-N-((S, Z)-3-methyl-4-oxo-4, 5-dihydro-3H-benzo [d][1, 2] diazepin-5-yl) propanamide (BMS- …

…, J Wang, BG Sleczka, C Dangler, BJ Robertson…

文献索引：Prasad; Zheng, Ming; Vig, Shikha; Bergstrom, Carl; Smith, David W.; Gao, Qi; Yeola, Suresh; Polson, Craig T.; Corsa, Jason A.; Guss, Valerie L.; Loo, Alice; Wang, Jian; Sleczka, Bogdan G.; Dangler, Charles; Robertson, Barbara J.; Hendrick, Joseph P.; Roberts, Susan B.; Barten, Donna M. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 14 p. 4006 - 4011

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被引用次数: 30

摘要

We report on the design of benzodiazepinones as peptidomimetics at the carboxy terminus of hydroxyamides. Structure–activity relationships of diazepinones were investigated and orally active γ-secretase inhibitors were synthesized. Active metabolites contributing to Aβ reduction were identified by analysis of plasma samples from Tg2576 mice. In particular,(S)- 2-((S)-2-(3, 5-difluorophenyl)-2-hydroxyacetamido)-N-((S, Z)-3-methyl-4-oxo-4, 5-dihydro- ...