Structure-Activity Relationship of novel phenylacetic CXCR1 inhibitors
Manolo Rocco Sablone1, Maria Candida Cesta, Alessio Moriconi
1Research Center, Dompé pha.r.ma s.p.a., via Campo di Pile, 67100, L'Aquila, Italy.
Abstract:
We reported recently the Structure-Activity Relationship (SAR) of a class of CXCL8 allosteric modulators. They invariably share a 2-arylpropionic moiety so far considered a key structural determinant of the biological activity. We show the results of recent SAR studies on a novel series of phenylacetic derivatives supported by a combined approach of mutagenesis experiments and conformational analysis. The results suggest novel insights on the fine role of the propionic/acetic chain in the modulation of CXCL8 receptors.
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