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Wiley-VCH Verlag, ChemInform, 24(43), p. no-no, 2012

DOI: 10.1002/chin.201224121

Elsevier, European Journal of Medicinal Chemistry, (47), p. 573-579

DOI: 10.1016/j.ejmech.2011.11.031

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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

Journal article published in 2012 by Chiara Brullo, Susanna Spisani, Rita Selvatici ORCID, Olga Bruno
This paper is available in a repository.
This paper is available in a repository.

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Abstract

Keywords: N-Aryl-2-phenyl-2,3-dihydro-imidazo[1,2-b]pyrazole-1-carboxamides IL8 fMLP-OMe Chemotaxis Human neutrophils Inflammation a b s t r a c t 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 (methyl-ester 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.