cas 266359-83-5, Repertaxin | Articles data

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Modified acidic nonsteroidal anti-inflammatory drugs as dual inhibitors of mPGES-1 and 5-LOX
mPGES-1 is a promising target for development of new anti-inflammatory drugs. We aimed to create mPGES-1 inhibitors by modifying the structure of NSAIDs by replacing the carboxylic acid functionality by sulfonamide moieties. Compounds were also tested for
Elkady, Mahmoud,Niess, Raimund,Bauer, Julia,Luderer, Susann,Ambrosi, Giulia,Laufer, Stefan A.,Schaible, Anja M.,Werz, Oliver
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p. 8958 - 8962,5
(2020/09/16)

A new and efficient method for the facile synthesis of N-acyl sulfonamides under Lewis acid catalysis
The N-acylation of sulfonamides with carboxylic acid anhydrides in the presence of Lewis acids is described. Several Lewis acids such as BF3·Et2O, ZnCl2, MoCl5, TiCl4, B(C6F5)su
Raji Reddy, Chada,Mahipal, Bodugam,Yaragorla, Srinivasa Rao
p. 7528 - 7532
(2008/03/14)

2-Arylpropionic CXC chemokine receptor 1 (CXCR1) ligands as novel noncompetitive CXCL8 inhibitors
The CXC chemokine CXCL8/IL-8 plays a major role in the activation and recruitment of polymorphonuclear (PMN) cells at inflammatory sites. CXCL8 activates PMNs by binding the seven-transmembrane (7-TM) G-protein-coupled receptors CXC chemokine receptor 1 (CXCR1) and CXC chemokine receptor 2 (CXCR2). (R)-Ketoprofen (1) was previously reported to be a potent and specific noncompetitive inhibitor of CXCLS-induced human PMNs chemotaxis. We report here molecular modeling studies showing a putative interaction site of 1 in the TM region of CXCR1. The binding model was confirmed by alanine scanning mutagenesis and photoaffinity labeling experiments. The molecular model driven medicinal chemistry optimization of 1 led to a new class of potent and specific inhibitors of CXCL8 biological activity. Among these, repertaxin (13) was selected as a clinical candidate drug for prevention of post-ischemia reperfusion injury.
Allegretti, Marcello,Bertini, Riccardo,Cesta, Maria Candida,Bizzarri, Cinzia,Di Bitondo, Rosa,Di Cioccio, Vito,Galliera, Emanuela,Berdini, Valerio,Topai, Alessandra,Zampella, Giuseppe,Russo, Vincenzo,Di Bello, Nicoletta,Nano, Giuseppe,Nicolini, Luca,Locati, Massimo,Fantucci, Piercarlo,Florio, Saverio,Colotta, Francesco
p. 4312 - 4331
(2007/10/03)

Predicting human serum albumin affinity of interleukin-8 (CXCL8) inhibitors by 3D-QSPR approach
A novel class of 2-(R)-phenylpropionamides has been recently reported to inhibit in vitro and in vivo interleukin-8 (CXCL8)-induced biological activities. These CXCL8 inhibitors are derivatives of phenylpropionic nonsteroidal antiinflammatory drugs (NSAID
Aureli, Loretta,Cruciani, Gabriele,Cesta, Maria Candida,Anacardio, Roberto,De Simone, Lucio,Moriconi, Alessio
p. 2469 - 2479
(2007/10/03)

Chemical Properties

Melting Point: 103-105℃
Density: 1.137g/cm³
Solubility:Soluble in DMSO (up to 100 mg/ml) or in Ethanol (up to 25 mg/ml)
Storage Temp.:Sealed in dry,Room Temperature
PKA: 4.28±0.40(Predicted)
PSA: 75.11000
LogP: 3.98550

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Chemical Properties

Melting Point: 103-105℃

Density: 1.137g/cm³

Solubility:Soluble in DMSO (up to 100 mg/ml) or in Ethanol (up to 25 mg/ml)

Storage Temp.:Sealed in dry,Room Temperature

PKA: 4.28±0.40(Predicted)

PSA: 75.11000

LogP: 3.98550

Global suppliers and manufacturers of 266359-83-5total 23 suppliers on LookChem

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266359-83-5

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More Articles about upstream products of 266359-83-5

Chemical Properties

Melting Point: 103-105℃

Density: 1.137g/cm3

Solubility:Soluble in DMSO (up to 100 mg/ml) or in Ethanol (up to 25 mg/ml)

Storage Temp.:Sealed in dry,Room Temperature

PKA: 4.28±0.40(Predicted)

PSA: 75.11000

LogP: 3.98550

Global suppliers and manufacturers of 266359-83-5total 23 suppliers on LookChem

Density: 1.137g/cm³