4_23_15

Syntrix Publication in Bioorganic & Medicinal Chemistry Letters

Congratulations to Syntrix scientists on their latest publication, which appeared in the journal Bioorganic & Medicinal Chemistry Letters.  Abstract: Blockade of undesired neutrophil migration to sites of inflammation remains an area of substantial pharmaceutical interest.  To effect this blockade, a validated therapeutic target is antagonism of the chemokine receptor CXCR2.  Herein we report the discovery of 6-(2-boronic acid-5-trifluoromethoxy-benzylsulfanyl)-N-(4-fluoro-phenyl)-nicotinamide 6, an antagonist with activity at both CXCR1 and CXCR2 receptors (IC50 values 31 and 21 nM, respectively).  Compound 6 exhibited potent inhibition of neutrophil influx in a rat model of pulmonary inflammation, and is hypothesized to interact with a unique intracellular binding site on CXCR2.  Compound 6 (SX-576) is undergoing further investigation as a potential therapy for pulmonary inflammation.