Author/Authors :
Qi Jin، نويسنده , , Hong Nie، نويسنده , , Brent W. McCleland، نويسنده , , Katherine L. Widdowson، نويسنده , , Michael R. Palovich، نويسنده , , John D. Elliott، نويسنده , , Richard M. Goodman، نويسنده , , Miriam Burman، نويسنده , , Henry M. Sarau، نويسنده , , Keith W. Ward، نويسنده , , Melanie Nord، نويسنده , , Bonnie M. Orr، نويسنده , , Peter D. Gorycki، نويسنده , , Jakob Busch-Petersen، نويسنده ,
Abstract :
A series of 3-substituted N,N′-diarylureas was prepared and the structure–activity relationship relative to CXCR2 receptor affinity as well as their pharmacokinetic properties were examined. In vitro microsomal metabolism studies indicated that the lower clearance rates of the 3-sulfonamido-substituted compounds were most likely due to the suppression of glucuronidation.
Keywords :
IL-8 , CXCR2 , fax: +1-6102704451 , Diarylureas.* Corresponding authors. Tel.: +1-6102707831 , e-mail: jakob.2.busch-petersen@gsk.com