Tian, Maoqun; Abdelrahman, Aliaa; Baqi, Younis; Fuentes, Eduardo; Azazna, Djamil; Spanier, Claudia; Densborn, Sabrina; Hinz, Sonja; Schmid, Ralf; Mueller, Christa E. published the artcile< Discovery and Structure Relationships of Salicylanilide Derivatives as Potent, Non-acidic P2X1 Receptor Antagonists>, Name: 5-Chloro-2-methoxybenzenesulfonyl chloride, the main research area is inflammation P2X1 receptor calcium influx allosteric modulators antagonists.
Antagonists for the ATP-gated ion channel receptor P2X1 have potential as antithrombotics and for treating hyperactive bladder and inflammation. In this study, salicylanilide derivatives were synthesized based on a screening hit. P2X1 antagonistic potency was assessed in 1321N1 astrocytoma cells stably transfected with the human P2X1 receptor by measuring inhibition of the ATP-induced calcium influx. Structure-activity relationships were analyzed, and selectivity vs. other P2X receptor subtypes was assessed. The most potent compounds, N-[3,5-bis(trifluoromethyl)phenyl]-5-chloro-2-hydroxybenzamide (1, IC50 0.0192 μM)(I) and N-[3,5-bis(trifluoromethyl)phenyl]-4-chloro-2-hydroxybenzamide (14, IC50 0.0231 μM)(II), displayed >500-fold selectivity vs. P2X2 and P2X3, and 10-fold selectivity vs. P2X4 and P2X7 receptors, and inhibited collagen-induced platelet aggregation. They behaved as neg. allosteric modulators, and mol. modeling studies suggested an extracellular binding site. Besides selective P2X1 antagonists, compounds with ancillary P2X4 and/or P2X7 receptor inhibition were discovered. These compounds represent the first potent, non-acidic, allosteric P2X1 receptor antagonists reported to date.
Journal of Medicinal Chemistry published new progress about Asthma. 22952-32-5 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2O3S, Name: 5-Chloro-2-methoxybenzenesulfonyl chloride.
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics