Synthesis and evaluation of 2-tosylamino and 2-tosyliminopyrimidine derivatives as inhibitors of some leukocyte functions

被引：6

作者：

Fernandez-Ferri, P

Ubeda, A ^{[1
]}

Guillén, I

Lasri, J

González-Rosende, ME

Akssira, M

Sepúlveda-Arques, J

机构：

[1] Univ Valencia, Dept Farmacol, E-46100 Burjassot, Spain

[2] Univ Valencia, Dept Quim Organ, E-46100 Burjassot, Spain

[3] Univ Cardenal Herrera, CEU, Dept Quim Bioquim & Biol Mol, Fac Ciencias Expt & Salud, Moncada, Valencia, Spain

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2003年 / 38卷 / 03期

关键词：

leukocytes; elastase; lipoxygenase; 2-tosyliminopyrimidines; 2-tosylaminopyrimidines;

D O I：

10.1016/S0223-5234(03)00013-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We have studied the potential anti-inflammatory effects of 20 2-tosylamino and 2-tosyliminopyrimidine new derivatives in human neutrophils. We have evaluated their interference with some leukocyte functions and 5-lipoxygenase activity. All the compounds reduced neutrophil degranulation process at concentrations in the muM range. Besides, compounds with a phenolic substitution inhibited leukotriene B-4 biosynthesis in neutrophils and decreased the cell-free 5-lipoxygenase activity. This study demonstrates that 2-tosylamino and 2-tosyliminopyrimidine derivatives can reduce the activation of neutrophil cells which may have relevance for the modulation of the inflammatory response. (C) 2003 Editions scientifiques et medicales Elsevier SAS. All rights reserved.

引用

页码：289 / 296

页数：8

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