135731-20-3Relevant academic research and scientific papers
Novel sulfonamide-based carbamates as selective inhibitors of bche
?těpánková, ?árka,Enriz, Ricardo D.,Garro, Adriana D.,Ho?ek, Jan,Imramovsky, Ale?,Jampílek, Josef,Jendrzejewska, Izabela,Magar, Pratibha,Parravicini, Oscar,Pauk, Karel,Svr?ková, Katarina
, (2021/09/04)
A series of 14 target benzyl [2-(arylsulfamoyl)-1-substituted-ethyl]carbamates was prepared by multi-step synthesis and characterized. All the final compounds were tested for their abil-ity to inhibit acetylcholinesterase (AChE) and butyrylcholinesterase
PROTEASOME INHIBITOR COMPRISING A SIGNAL-EMITTING MOIETY
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, (2017/03/14)
The present invention relates to compounds such as peptides which act as proteasome inhibitors. The compounds are covalently linked with a signal emitting compound or a precursor thereof, via an ester such as a sulfonic ester group for imaging of the inhibition of the proteasome. The compound is for use in the quantification of proteasomal inhibition, diagnosis and/or prevention and/or treatment of autoimmune diseases, cancer, neurodegenerative diseases, viral infections and/or diseases associated with inflammation. The invention further relates to methods to produce the compounds.
Selective inhibition of the immunoproteasome by ligand-induced crosslinking of the active site
Dubiella, Christian,Cui, Haissi,Gersch, Malte,Brouwer, Arwin J.,Sieber, Stephan A.,Krüger, Achim,Liskamp, Rob M. J.,Groll, Michael
, p. 11969 - 11973 (2015/03/04)
The concept of proteasome inhibition ranks among the latest achievements in the treatment of blood cancer and represents a promising strategy for modulating autoimmune diseases. In this study, we describe peptidic sulfonyl fluoride inhibitors that selecti
Synthesis and biological evaluation of novel irreversible serine protease inhibitors using amino acid based sulfonyl fluorides as an electrophilic trap
Brouwer, Arwin J.,Ceylan, Tarik,Jonker, Anika M.,Linden, Tima Van Der,Liskamp, Rob M.J.
scheme or table, p. 2397 - 2406 (2011/05/12)
We have designed and synthesized novel irreversible serine protease inhibitors containing aliphatic sulfonyl fluorides as an electrophilic trap. These substituted taurine sulfonyl fluorides derived from taurine or protected amino acids were conveniently s
Synthesis of novel N-protected β3-amino nitriles: study of their hydrolysis involving a nitrilase-catalyzed step
Veitia, Maite Sylla-Iyarreta,Brun, Pierre Louis,Jorda, Pierre,Falguieres, Annie,Ferroud, Clotilde
experimental part, p. 2077 - 2089 (2010/03/04)
Several commercially available nitrilases were investigated with regard to their potential to hydrolyze N-protected β3-amino nitriles into their corresponding N-protected β3-amino acids. The biotransformations were obtained in different proportions depending on the nitrilase involved. The best hydrolysis results were achieved for the N-Cbz-β3-amino nitrile from l-alanine using the NIT-107, in a phosphate buffer at 0.05 M. However, no biotransformation into the corresponding acids was observed for the N-sulfonylamide β3-amino nitriles. Two simple and efficient procedures to prepare the β3-amino nitriles from their analogous α-amino acids are described. Thirty four new substances were synthesized and characterized over the course of this work.
Synthesis of β-aminoethanesulfonyl fluorides or 2-substituted taurine sulfonyl fluorides as potential protease inhibitors
Brouwer, Arwin J.,Ceylan, Tarik,Linden, Tima van der,Liskamp, Rob M.J.
scheme or table, p. 3391 - 3393 (2009/09/05)
Substituted taurine sulfonyl fluorides derived from taurine or protected amino acids are conveniently synthesized from β-aminoethanesulfonyl chlorides using KF/18-crown-6 or from β-aminoethanesulfonates using DAST.
Synthesis and applications of β-aminoethanesulfonyl azides
Brouwer, Arwin J.,Merkx, Remco,Dabrowska, Katarzyna,Rijkers, Dirk T. S.,Liskamp, Rob M. J.
, p. 455 - 460 (2007/10/03)
A very efficient method for the synthesis of β-aminoethanesulfonyl azides is descibed. These aliphatic sulfonyl azides are accessible starting from a variety of protected amino acids, including those having functionalized side chains. Furthermore, these s
An efficient synthesis of N-protected β-aminoethanesulfonyl chlorides: Versatile building blocks for the synthesis of oligopeptidosulfonamides
Brouwer,Monnee,Liskamp
, p. 1579 - 1584 (2007/10/03)
A very efficient method for the synthesis of β-aminoethanesulfonyl chlorides is described. These aliphatic functionalized sulfonyl chlorides are accessible starting from a variety of protected amino acids, including those having functionalized side chains
2-6-diaminopurine precursors
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, (2008/06/13)
The present invention relates to compounds of formula (IV): STR1 wherein Ra and Rb each represent a hydrogen atom or together form an alkylidene group.
Design and synthesis of novel conformationally restricted HIV protease inhibitors
Salituro, Francesco G.,Baker, Christopher T.,Court, John J.,Deininger, David D.,Kim, Eunice E.,Li, Biquin,Novak, Perry M.,Rao, Bhisetti G.,Pazhanisamy,Porter, Margaret D.,Schairer, Wayne C.,Tung, Roger D.
, p. 3637 - 3642 (2007/10/03)
A set of HIV protease inhibitors represented by compound 2 has previously been described. Structural and conformational analysis of this compound suggested that conformational restriction of the P1/P2 portion of the molecule could lead to a novel set of potent protease inhibitors. Thus, probe compounds 3-7 were designed, synthesized, and found to be potent inhibitors of HIV protease.
