Nano Archive

6-Amino-4-oxo-1,3-diphenyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonyl derivatives as a new class of potent inhibitors of Interleukin-8-induced neutrophil chemotaxis

Cesarini, Sara and Spallarossa, Andrea and Ranise, Angelo and Bruno, Olga and Arduino, Nicoletta and Bertolotto, Maria and Dallegri, Franco and Tognolini, Massimiliano and Gobbetti, Thomas and Barocelli, Elisabetta (2009) 6-Amino-4-oxo-1,3-diphenyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonyl derivatives as a new class of potent inhibitors of Interleukin-8-induced neutrophil chemotaxis. Bioorganic & Medicinal Chemistry, 17 (10). 3580 - 3587.

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Official URL: http://www.sciencedirect.com/science/article/B6TF8...

Abstract

A series of 6-amino-4-oxo-1,3-diphenyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonyl derivatives was synthesized. The compounds demonstrated to be novel, potent and selective inhibitors of Interleukin-8-induced human neutrophil chemotaxis. A SAR study was performed by varying the carbonyl function at position 5 and the chain linked to the amino group at position 6 of the scaffold. All the compounds of the series displayed inhibitory activity at nano- or picomolar concentrations against Interleukin-8-driven migration and no activity against fMLP- and C5a-induced chemotaxis. The binding tests of selected compounds on CXCR1 and CXCR2 receptors were negative. The most potent derivative showed in vivo efficacy in a mouse model of Zymosan-induced peritonitis.

Item Type:Article
Uncontrolled Keywords:eutrophil; Chemotaxis; Interleukin-8; Inhibitors; Peritonitis
Subjects:Biomedical Science > Nanomedicine
ID Code:5670
Deposited By:SPI
Deposited On:04 Aug 2009 10:39
Last Modified:04 Aug 2009 10:39

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