Title of article :
Carboxylic acid bioisosteres acylsulfonamides, acylsulfamides, and sulfonylureas as novel antagonists of the CXCR2 receptor
Author/Authors :
Michael P. Winters، نويسنده , , Carl Crysler، نويسنده , , Nalin Subasinghe، نويسنده , , Declan Ryan، نويسنده , , Lynette Leong، نويسنده , , Shuyuan Zhao، نويسنده , , Robert Donatelli، نويسنده , , Edward Yurkow، نويسنده , , Marie Mazzulla، نويسنده , , Lisa Boczon، نويسنده , , Carl L. Manthey، نويسنده , , Christopher Molloy، نويسنده , , Holly Raymond، نويسنده , , Lynne Murray، نويسنده , , Laura McAlonan، نويسنده , , Bruce Tomczuk، نويسنده ,
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.
Keywords :
IL-8 , Indole , COPD , CXCR1 , Carboxylic acid bioisosteres , Acylsulfonamides , chemokine , CXCR2 , Sulfonylureas , Neutrophils , asthma , Acylsulfamides
