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  • Carboxylic acid bioisosteres acylsulfonamides, acylsulfamides, and sulfonylureas as novel antagonists of the CXCR2 receptor.

Carboxylic acid bioisosteres acylsulfonamides, acylsulfamides, and sulfonylureas as novel antagonists of the CXCR2 receptor.

Bioorganic & medicinal chemistry letters (2008-03-01)
Michael P Winters, Carl Crysler, Nalin Subasinghe, Declan Ryan, Lynette Leong, Shuyuan Zhao, Robert Donatelli, Edward Yurkow, Marie Mazzulla, Lisa Boczon, Carl L Manthey, Christopher Molloy, Holly Raymond, Lynne Murray, Laura McAlonan, Bruce Tomczuk
PMID18308567
ABSTRACT

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.