63327-57-1Relevant articles and documents
A versatile and selective chemo-enzymatic synthesis of β-protected aspartic and γ-protected glutamic acid derivatives
Nuijens, Timo,Kruijtzer, John A.W.,Cusan, Claudia,Rijkers, Dirk T.S.,Liskamp, Rob M.J.,Quaedflieg, Peter J.L.M.
experimental part, p. 2719 - 2721 (2009/09/06)
Two versatile, high yielding, and efficient chemo-enzymatic methods for the synthesis of β-protected Asp and γ-protected Glu derivatives using Alcalase are described. The first method is based on the α-selective enzymatic hydrolysis of symmetrical aspartyl and glutamyl diesters. The second method involving mixed diesters comprises a three-step protocol using (i) α-selective enzymatic methyl-esterification, (ii) chemical β-esterification, and finally (iii) α-selective enzymatic methyl ester hydrolysis. The yields of the purified β- and γ-esters range from 77% to 91%.
Synthesis of β-(S-methyl)thioaspartic acid and derivatives
Heredia-Moya, Jorge,Kirk, Kenneth L.
, p. 5908 - 5913 (2008/12/21)
β-(S-Methyl)thioaspartic acid occurs as a posttranslational modification at position 88 in Escherichia coli ribosomal protein S12, a position that is a mutational hotspot resulting in both antibiotic-resistant and antibiotic-sensitive phenotypes. Critical
CASPASE INHIBITORS BASED ON PYRIDAZINONE SCAFFOLD
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Page/Page column 75-76, (2008/06/13)
The present invention relates to a pyridazinone derivative which can be used as a caspase inhibitor, process for the preparation thereof, and pharmaceutical composition for inhibiting caspase comprising the same.
Isoxazoline derivative and a process for the preparation thereof
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Page/Page column 44-45, (2010/02/07)
The present invention provides to an isoxazoline derivative of formula (I), the pharmaceutically acceptable salts, esters and stereochemically isomeric forms thereof, and the use of the derivative in inhibiting the activity of caspases. The present invent
Straightforward and diastereoselective synthesis of tetrafunctionalized thiol synthons for the design of metallopeptidase inhibitors
David, Christelle,Bischoff, Laurent,Roques, Bernard P.,Fournié-Zaluski, Marie-Claude
, p. 209 - 215 (2007/10/03)
Tetrafunctionalized thiol-containing synthons with different side-chains have been prepared with good yields by a straightforward diastereoselective and general methodology. The key step of the synthesis consisted of a tandem reduction and Wittig-Horner r
Investigation of subsite preferences in aminopeptidase A (EC 3.4.11.7) led to the design of the first highly potent and selective inhibitors of this enzyme
David, Christelle,Bischoff, Laurent,Meudal, Hervé,Mothé, Aurélie,De Mota, Nadia,DaNascimento, Sophie,Llorens-Cortes, Catherine,Fournié-Zaluski, Marie-Claude,Roques, Bernard P.
, p. 5197 - 5211 (2007/10/03)
The study of the physiological roles of the membrane-bound zinc- aminopeptidase A (glutamyl aminopeptidase, EC 3.4.11.7) needs the design of efficient and selective inhibitors of this enzyme. An acute exploration of aminopeptidase A active site was perfor
Synthesis of (3R)- and (3S)-3,4-diamino-butyric acid from L-aspartic acid
Misiti,Santaniello,Zappia
, p. 883 - 891 (2007/10/02)
A short and convenient synthesis for both enantiomers of GABOB amino-analogue 1a,b is reported, starting from L-aspartic acid. The protected diester 3 is the common intermediate for the synthetic pathway.