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  • 2-Phenyl-2,3-dihydro-1H-imidazo[1,2-b]pyrazole derivatives: new potent inhibitors of fMLP-induced neutrophil chemotaxis.

2-Phenyl-2,3-dihydro-1H-imidazo[1,2-b]pyrazole derivatives: new potent inhibitors of fMLP-induced neutrophil chemotaxis.

Bioorganic & medicinal chemistry letters (2007-05-04)
Olga Bruno, Chiara Brullo, Francesco Bondavalli, Angelo Ranise, Silvia Schenone, Maria Sofia Falzarano, Katia Varani, Susanna Spisani
ABSTRACT

It is well known that both acute and chronic autoimmune inflammatory disorders arise following a breakdown in control of neutrophil activation and recruitment. In the search for new anti-inflammatory agents, we synthesized some new 2-phenyl-2,3-dihydro-1H-imidazo[1,2-b]pyrazole derivatives and tested them in vitro in order to evaluate their ability to interfere with human neutrophil functions. All tested compounds showed strong inhibition of fMLP-OMe-induced chemotaxis, although they appeared unable to block degranulation and the fMLP-OMe-induced respiratory burst, and were inactive in binding experiments.

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Sigma-Aldrich
Cyclosporin A, 97.0-101.5% (on dried basis)
Sigma-Aldrich
N-Formyl-Met-Leu-Phe, ≥97% (HPLC)
Sigma-Aldrich
Cyclosporin A, from Tolypocladium inflatum, ≥95% (HPLC), solid
Sigma-Aldrich
Cyclosporin A, BioReagent, from Tolypocladium inflatum, Molecular Biology, ≥95%
Sigma-Aldrich
N-Formyl-Met-Leu-Phe, BioXtra, ≥99.0% (TLC)
Supelco
Cyclosporin A, VETRANAL®, analytical standard