Title of article
Discovery of potent and orally bioavailable N,N′-diarylurea antagonists for the CXCR2 chemokine receptor
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 ,
Issue Information
روزنامه با شماره پیاپی سال 2004
Pages
4
From page
4375
To page
4378
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
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2004
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
794796
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