221286-65-3Relevant academic research and scientific papers
The synthesis of ketomethylene pseudopeptide analogues of dipeptide aldehyde inhibitors of calpain
Angelastro, Michael R.,Marquart, Angela L.,Mehdi, Shujaath,Koehl, Jack R.,Vaz, Roy J.,Philippe, Bey,Peet, Norton P.
, p. 139 - 140 (2007/10/03)
The ketomethylene phenylalanal and alanal analogues of Cbz-Val-Phe-H and Cbz-Val-Ala-H have been prepared and the K(i) values versus chicken gizzard smooth muscle calpain were determined. The ketomethylene isosteres were significantly less potent than the corresponding dipeptide aldehydes, and this loss in activity is attributed to the absence of a critical interaction between the P1-P2 amide bond and the peptide binding region of calpain.
Aminoalkyl-substituted α-methylene-γ-butyrolactones from α-amino acids using an indium-mediated Barbier allyl addition
Steurer, Steffen,Podlech, Joachim
, p. 1551 - 1560 (2007/10/03)
The indium-mediated reaction of Z-protected α-amino aldehydes 1-6 with 2-(bromomethyl)acrylates 8/9 in aqueous solvents has been investigated. The preference for the formation of syn-configured homoallyl alcohols 10-16 (diastereoselectivities ranging from
