104062-70-6Relevant articles and documents
Novel 2-oxoamide inhibitors of human group IVA phospholipase A2
Kokotos, George,Kotsovolou, Stavroula,Six, David A.,Constantinou-Kokotou, Violetta,Beltzner, Christopher C.,Dennis, Edward A.
, p. 2891 - 2893 (2002)
A novel class of potent human cytosolic phospholipase A2 (GIVA PLA2) inhibitors was developed. These inhibitors were designed to contain the 2-oxoamide functionality and a free carboxyl group. Among the compounds tested, a longchain
Crystal Structures of Staphylococcus aureus Methionine Aminopeptidase Complexed with Keto Heterocycle and Aminoketone Inhibitors Reveal the Formation of a Tetrahedral Intermediate
Douangamath, Alice,Dale, Glenn E.,D'Arcy, Allan,Almstetter, Michael,Eckl, Robert,Frutos-Hoener, Annabelle,Henkel, Bernd,Illgen, Katrin,Nerdinger, Sven,Schulz, Henk,MacSweeney, Aengus,Thormann, Michael,Treml, Andreas,Pierau, Sabine,Wadman, Sjoerd,Oefner, Christian
, p. 1325 - 1328 (2004)
High-resolution crystal structures of Staphylococcus aureus methionine aminopeptidase I in complex with various keto heterocycles and aminoketones were determined, and the intermolecular ligand interactions with the enzyme are reported. The compounds are effective inhibitors of the S. aureus enzyme because of the formation of an uncleavable tetrahedral intermediate upon binding. The electron densities unequivocally show the enzyme-catalyzed transition-state analogue mimicking that for amide bond hydrolysis of substrates.
AN EFFICIENT METHOD FOR PREPARATION OF OPTICALLY ACTIVE N-PROTECTED α-AMINO ALDEHYDES FROM N-PROTECTED α-AMINO ALCOHOLS
Soucek, Milan,Urban, Jan
, p. 693 - 696 (1995)
N-Protected α-amino aldehydes of high optical purity were prepared in excellent yields from corresponding α-amino alcohols by 1,1,1-tris(acetoxy)-1,1-dihydro-1,2-benzodioxol-3(H)-one (periodinane) oxidation.
Triazolo-peptidomimetics: novel radiolabeled minigastrin analogs for improved tumor targeting
Grob, Nathalie M.,H?ussinger, Daniel,Deupi, Xavier,Schibli, Roger,Behe, Martin,Mindt, Thomas L.
, p. 4484 - 4495 (2020/06/08)
MG11 is a truncated analog of minigastrin, a peptide with high affinity and specificity toward the cholecystokinin-2 receptor (CCK2R), which is overexpressed by different tumors. Thus, radiolabeled MG11 derivatives have great potential for use in cancer d
1,2,3-Triazoles as amide bond mimics: Triazole scan yields protease-resistant peptidomimetics for tumor targeting
Valverde, Ibai E.,Bauman, Andreas,Kluba, Christiane A.,Vomstein, Sandra,Walter, Martin A.,Mindt, Thomas L.
, p. 8957 - 8960 (2013/09/02)
The triazole makes the difference: Replacement of amide bonds in the backbone of peptides by 1,4-disubstituted 1,2,3-triazole isosteres affords peptidomimetics with retained receptor affinity and cell-internalization properties, enhanced proteolytic stability, and improved tumor-targeting capabilities. Copyright