128707-89-1Relevant academic research and scientific papers
(S)-N-(5-Chlorothiophene-2-sulfonyl)-β,β-diethylalaninol a Notch-1-sparing γ-secretase inhibitor
Cole, Derek C.,Stock, Joseph R.,Kreft, Anthony F.,Antane, Madelene,Aschmies, Suzan H.,Atchison, Kevin P.,Casebier, David S.,Comery, Thomas A.,Diamantidis, George,Ellingboe, John W.,Harrison, Boyd L.,Hu, Yun,Jin, Mei,Kubrak, Dennis M.,Lu, Peimin,Mann, Charles W.,Martone, Robert L.,Moore, William J.,Oganesian, Aram,Riddell, David R.,Sonnenberg-Reines, June,Sun, Shaiu-Ching,Wagner, Erik,Wang, Zheng,Woller, Kevin R.,Xu, Zheng,Zhou, Hua,Jacobsen, J. Steven
scheme or table, p. 926 - 929 (2009/09/06)
Accumulation of beta-amyloid (Aβ), produced by the proteolytic cleavage of amyloid precursor protein (APP) by β- and γ-secretase, is widely believed to be associated with Alzheimer's disease (AD). Research around the high-throughput screening hit (S)-4-chlorophenylsulfonyl isoleucinol led to the identification of the Notch-1-sparing (9.5-fold) γ-secretase inhibitor (S)-N-(5-chlorothiophene-2-sulfonyl)-β,β-diethylalaninol 7.b.2 (Aβ 40/42 EC50 = 28 nM), which is efficacious in reduction of Aβ production in vivo.
Asymmetric synthesis of unusual amino acids: An efficient synthesis of optically pure isomers of β-methylphenylalanine
Dharanipragada,VanHulle,Bannister,Bear,Kennedy,Hruby
, p. 4733 - 4748 (2007/10/02)
Substitution of the diastereotopic β-hydrogens of many α-amino acids provides an approach to the three dimensional topographic control of peptide structure. Asymmetric synthesis of the desired amino acids is needed to facilitate these studies. All four in
ASYMMETRIC SYNTHESIS OF UNUSUAL AMINO ACIDS: SYNTHESIS OF OPTICALLY PURE ISOMERS OF β-METHYLPHENYLALANINE
Dharanipragada, Ramalinga,Nicolas, Ernesto,Toth, Geza,Hruby, Victor J.
, p. 6841 - 6844 (2007/10/02)
All the four individual isomers of β-methylphenylalanine have been synthesized in very high optical purities by utilizing in part the chiral imide enolate bromination methodology of Evans and co-workers.
