176907-02-1Relevant articles and documents
Pyrimidine derivatives of n-acetylguanidine: Novel inhibitors of sodium-hydrogen exchanger 1
Ozerov, Alexander,Novikov, Mikhail,Spasov, Alexander,Iezhitsa, Igor,Gurova, Natalia,Gurova, Valeria
, p. 1101 - 1107 (2018/08/28)
Sodium-hydrogen exchanger (Na+/H+) type 1 (NHE-1) inhibitors have been shown to protect the heart during ischaemia and early reperfusion. As such, NHE-1 inhibitors are of special interest for clinical development for the attenuation of both acute and chronic post-myocardial infarction responses. New pyrimidine derivatives of N-acetylguanidine containing fragments of uracil, thymine, and their 3-benzyl derivatives were synthesised. These compounds showed in vitro inhibitory effects on NHE-1 that were significantly higher than those of zoniporide in platelet swelling assays.
Human neutrophil elastase phosphonic inhibitors with improved potency of action
Winiarski, ?ukasz,Oleksyszyn, Józef,Sieńczyk, Marcin
experimental part, p. 6541 - 6553 (2012/09/21)
Herein, we present the synthesis and the measurement of the inhibitory activity of novel peptidyl derivatives of α-aminoalkylphosphonate diaryl esters as human neutrophil elastase inhibitors. Their selectivity against other serine proteases, including porcine pancreatic elastase, chymotrypsin, and trypsin, was also demonstrated. We also describe the preparation of single peptide diastereomers. The most active and selective compound developed possessed a kinact/KI of 2353000 M-1 s -1, which is the most potent irreversible peptidyl inhibitor of human neutrophil elastase reported to date. The peptidyl inhibitors were demonstrated to be stable in PBS buffer and human plasma, as were their complexes with HNE.
Development of a highly water-soluble peptide-based human neutrophil elastase inhibitor; AE-3763 for treatment of acute organ injury
Inoue, Yasunao,Omodani, Tomoki,Shiratake, Ryotaro,Okazaki, Hiroshi,Kuromiya, Akemi,Kubo, Taeko,Sato, Fuminori
experimental part, p. 7477 - 7486 (2011/02/23)
A series of peptide-based transition-state human neutrophil elastase (HNE) inhibitors with N-terminal acidic moieties were synthesized and their inhibitory activity against HNE was evaluated both in vitro and in vivo. Our results show that compounds conta
Design, synthesis, and evaluation of a biomimetic artificial photolyase model
Wiest, Olaf,Harrison, Christopher B.,Saettel, Nicolas J.,Cibulka, Radek,Sax, Mirjam,Koenig, Burkhard
, p. 8183 - 8185 (2007/10/03)
Two new artificial photolyase models that recognize pyrimidine dimers in protic and aprotic organic solvents as well as in water through a combination of charge and hydrogen-bonding interactions and use a mimic of the flavine to achieve repair through red
HETEROCYCLIC COMPOUNDS, INTERMEDIATES THEREOF AND ELASTASE INHIBITORS
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, (2008/06/13)
The present invention relates to a heterocyclic compound of the following formula (I-a), its ester, or a salt thereof, and a human neutrophilic elastase inhibitor containing the same as the active ingredient, etc. wherein A and B are the same or different
Synthesis and Structure of (Carboxymethyl)-Functionalized Cyclobuta-Fused Uracil Dimers
Carell, Thomas,Epple, Robert,Gramlich, Volker
, p. 2191 - 2203 (2007/10/03)
Herein, we report a convenient method for the preparation of four benzyl-ester-protected, (carboxymethyl)-functionalized cyclobuta-fused uracil dimers 1-4, including the desired cis-cisoid-cis,syn-configured isomer 1, a compound which is suitable for the preparation of catalytic antibodies, synthetic receptors, and model compounds, required for the investigation of the DNA-lesion, recognition step and DNA-repair mechanisms. A comprehensive structure determination of each isomer by 1H-NMR, and in the case of the cis-cisoid-cis,syn-and the cis-transoid-cis-cis,syn-dimers by X-ray crystal-structure analysis, is also provided.
Zur DNA-Reparatur durch das Enzym DNA-Photolyase: Synthese von Flavin enthaltenden Modellverbindungen
Carell, Thomas,Epple, Robert,Gramlich, Volker
, p. 676 - 679 (2007/10/03)
Keywords: DNA-Reparatur; Elektronentransfer; Flavine; Nucleobasen