40290-56-0Relevant academic research and scientific papers
Tripeptide analogues of MG132 as protease inhibitors
Pehere, Ashok D.,Nguyen, Steven,Garlick, Sarah K.,Wilson, Danny W.,Hudson, Irene,Sykes, Matthew J.,Morton, James D.,Abell, Andrew D.
supporting information, p. 436 - 441 (2019/01/04)
The 26S proteasome and calpain are linked to a number of important human diseases. Here, we report a series of analogues of the prototypical tripeptide aldehyde inhibitor MG132 that show a unique combination of high activity and selectivity for calpains over proteasome. Tripeptide aldehydes (1–3) with an aromatic P3 substituent show enhanced activity and selectivity against ovine calpain 2 relative to chymotrypsin-like activity of proteasome. Docking studies reveal the key contacts between inhibitors and calpain to confirm the importance of the S3 pocket with respect to selectivity between calpains 1 and 2 and the proteasome.
General and versatile approach to the synthesis of optically active 5-alkylpiperazine-2-carboxylic acids
Falorni,Giacomelli,Satta,Cossu
, p. 391 - 395 (2007/10/02)
General and convenient syntheses of optically active 5-alkylpiperazine-2-carboxylic acids are described. The methods are based on cyclization of L- or D-serine with α-amino acids and occur without loss of optical purity. The presented procedures are based
Chiral Ligands Containing Heteroatoms. 11. Optically Active 2-Hydroxymethyl Piperazines as Catalyst in the Enantioselective Addition of Diethylzinc to Benzaldehyde
Falorni, Massimo,Satta, Michele,Conti, Sandra,Giacomelli, Giampaolo
, p. 2389 - 2398 (2007/10/02)
Starting from enantiomerically pure serine, a series of (2R,5S) and (2S,5S)-2-hydroxymethyl-5-alkyl piperazines 1-5 were prepared in good yields without any racemization.The use of these compounds as chiral catalysts for the enantioselective addition of d
