68432-95-1Relevant articles and documents
Syntheses, crystal structures, properties of metal coordination polymers based on a novel semi-rigid aromatic carboxylate ligand
Wang, Cui-Cui,Tang, Gui-Mei,Wang, Yong-Tao,Wang, Jin-Hua,Cui, Yue-Zhi,Ng, Seik-Weng
, p. 145 - 155 (2017/01/22)
A set of new metal coordination polymers constructed from a novel semi-rigid aromatic carboxylate ligand, namely, [M(L)(4PBI)(H2O)]n(M?=?Ni, Co and Cu for 1, 2 and 3, respectively) and [Cd(L)(4PBI)]n(4) (H2L?=?3
2-Arylpropionic CXC chemokine receptor 1 (CXCR1) ligands as novel noncompetitive CXCL8 inhibitors
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)
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.
Synthesis and hypolipidemic activity of novel 4-oxo- and 4-thioxo-4H-benzopyran-2-phenylalkanoic acids and esters
Orjales, A.,Berisa, A.,Alonso-Cires, L.
, p. 27 - 31 (2007/10/02)
Novel 4-oxo- and 4-thioxo-4H-benzopyran-2-phenylalkanoic acids and esters have been prepared and evaluated for their hypolipidemic activity.Among these compounds 3'-alkanoyl derivatives show superior activity, decreasing total cholesterol, triglycerides a
