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Design and synthesis of highly potent benzodiazepine gamma-secretase inhibitors: preparation of (2S,3R)-3-(3,4-difluorophenyl)-2-(4-fluorophenyl)-4- hydroxy-N-((3S)-1-methyl-2-oxo-5- phenyl-2,3-dihydro-1H-benzo[e][1,4]-diazepin-3-yl)butyramide by use of an asymmetric Ireland-Claisen rearrangement.
Churcher I, Williams S, Kerrad S, Harrison T, Castro JL, Shearman MS, Lewis HD, Clarke EE, Wrigley JD, Beher D, Tang YS, Liu W. Churcher I, et al. Among authors: harrison t. J Med Chem. 2003 Jun 5;46(12):2275-8. doi: 10.1021/jm034058a. J Med Chem. 2003. PMID: 12773031
A new series of potent benzodiazepine gamma-secretase inhibitors.
Churcher I, Ashton K, Butcher JW, Clarke EE, Harrison T, Lewis HD, Owens AP, Teall MR, Williams S, Wrigley JD. Churcher I, et al. Among authors: harrison t. Bioorg Med Chem Lett. 2003 Jan 20;13(2):179-83. doi: 10.1016/s0960-894x(02)00909-5. Bioorg Med Chem Lett. 2003. PMID: 12482419
Quantitative measurement of changes in amyloid-beta(40) in the rat brain and cerebrospinal fluid following treatment with the gamma-secretase inhibitor LY-411575 [N2-[(2S)-2-(3,5-difluorophenyl)-2-hydroxyethanoyl]-N1-[(7S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl]-L-alaninamide].
Best JD, Jay MT, Otu F, Ma J, Nadin A, Ellis S, Lewis HD, Pattison C, Reilly M, Harrison T, Shearman MS, Williamson TL, Atack JR. Best JD, et al. Among authors: harrison t. J Pharmacol Exp Ther. 2005 May;313(2):902-8. doi: 10.1124/jpet.104.081174. Epub 2005 Mar 2. J Pharmacol Exp Ther. 2005. PMID: 15743924
2,332 results