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N-Aryl-2-phenyl-2,3-dihydro-imidazo[1,2-b]pyrazole-1-carboxamides 7-substituted strongly inhibiting both fMLP-OMe- and IL-8-induced human neutrophil chemotaxis.
- Source :
-
European journal of medicinal chemistry [Eur J Med Chem] 2012 Jan; Vol. 47 (1), pp. 573-9. Date of Electronic Publication: 2011 Nov 25. - Publication Year :
- 2012
-
Abstract
- Anomalous activation of neutrophil recruitment is one of the causes of many inflammatory diseases. The chemoattractants N-formyl-methionyl-leucyl-phenylalanine (fMLP), and interleukine 8 (IL8) play a pivotal role in neutrophil chemotaxis regulation in the latter and early stages, respectively, probably by two independent mechanisms. We reported here synthesis and biological evaluation of new N-aryl-2-phenyl-2,3-dihydro-imidazo[1,2-b]pyrazole-1-carboxamides 7-substituted which were designed as possible multi-target antiinflammatory agents. Many of the title compounds showed a good inhibition, in the nano molar range, of human neutrophil chemotaxis selectively acting toward fMLP-OMe (methylester of fMLP) or IL8 stimulus; whereas, two compounds showed an interesting dual activity inhibiting both fMLP-OMe and IL8-induced chemotaxis at nano molar concentration.<br /> (Copyright © 2011 Elsevier Masson SAS. All rights reserved.)
- Subjects :
- Humans
Inhibitory Concentration 50
N-Formylmethionine Leucyl-Phenylalanine pharmacology
Structure-Activity Relationship
Chemotaxis drug effects
Interleukin-8 pharmacology
N-Formylmethionine Leucyl-Phenylalanine analogs & derivatives
Neutrophils cytology
Neutrophils drug effects
Pyrazoles chemistry
Pyrazoles pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1768-3254
- Volume :
- 47
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- European journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 22152986
- Full Text :
- https://doi.org/10.1016/j.ejmech.2011.11.031