Synthesis and QSAR of quinazoline sulfonamides as highly potent human histamine H4 receptor inverse agonists

…, FJJ de Kanter, A Jongejan, G Coruzzi…

Index: Smits, Rogier A.; Adami, Maristella; Istyastono, Enade P.; Zuiderveld, Obbe P.; Van Dam, Cindy M. E.; De Kanter, Frans J. J.; Jongejan, Aldo; Coruzzi, Gabriella; Leurs, Rob; De Esch, Iwan J. P. Journal of Medicinal Chemistry, 2010 , vol. 53, # 6 p. 2390 - 2400

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Citation Number: 59

Abstract

Hit optimization of the class of quinazoline containing histamine H4 receptor (H4R) ligands resulted in a sulfonamide substituted analogue with high affinity for the H4R. This moiety leads to improved physicochemical properties and is believed to probe a distinct H4R binding pocket that was previously identified using pharmacophore modeling. By introducing a variety of sulfonamide substituents, the H4R affinity was optimized. The ...