羧酸生物电子等排体酰基磺酰胺、酰基磺胺和磺酰脲类作为新型CXCR2受体拮抗剂
Carboxylic acid bioisosteres acylsulfonamides, acylsulfamides, and sulfonylureas as novel antagonists of the CXCR2 receptor.
作者信息
Winters Michael P, Crysler Carl, Subasinghe Nalin, Ryan Declan, Leong Lynette, Zhao Shuyuan, Donatelli Robert, Yurkow Edward, Mazzulla Marie, Boczon Lisa, Manthey Carl L, Molloy Christopher, Raymond Holly, Murray Lynne, McAlonan Laura, Tomczuk Bruce
机构信息
Johnson & Johnson Pharmaceutical Research and Development, 665 Stockton Drive, Exton, PA 19341, USA.
出版信息
Bioorg Med Chem Lett. 2008 Mar 15;18(6):1926-30. doi: 10.1016/j.bmcl.2008.01.127. Epub 2008 Feb 7.
A series of novel acylsulfonamide, acylsulfamide, and sulfonylurea bioisosteres of carboxylic acids were prepared as CXCR2 antagonists. Structure-activity relationships are reported for these series. One potent orally bioavailable inhibitor had excellent PK properties and was active in a lung injury model in hyperoxia-exposed newborn rats.
制备了一系列新型的羧酸酰基磺酰胺、酰基磺酰胺和磺酰脲生物电子等排体作为CXCR2拮抗剂。报道了这些系列的构效关系。一种有效的口服生物可利用抑制剂具有优异的药代动力学性质，并且在高氧暴露新生大鼠的肺损伤模型中具有活性。
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