Discovery of CNS Penetrant CXCR2 Antagonists for the Potential Treatment of CNS Demyelinating Disorders
Structure-activity relationship exploration of the historical biarylurea series led to the identification of novel CNS penetrant CXCR2 antagonists with nanomolar potency, favorable PK profile, and good developability potentials. More importantly, the key
Discovery of potent and orally bioavailable N,N′-diarylurea antagonists for the CXCR2 chemokine receptor
A series of 3-substituted N,N′-diarylureas was prepared and CXCR2 receptor affinities as well as pharmacokinetic properties were examined. A series of 3-substituted N,N′-diarylureas was prepared and the structure-activity relationship relative to CXCR2 re
Jin, Qi,Nie, Hong,McCleland, Brent W.,Widdowson, Katherine L.,Palovich, Michael R.,Elliott, John D.,Goodman, Richard M.,Burman, Miriam,Sarau, Henry M.,Ward, Keith W.,Nord, Melanie,Orr, Bonnie M.,Gorycki, Peter D.,Busch-Petersen, Jakob
p. 4375 - 4378
(2007/10/03)
Evaluation of Potent and Selective Small-Molecule Antagonists for the CXCR2 Chemokine Receptor
N,N′-Diarylureas were prepared, and the structure-activity relationship relative to the CXCR2 receptor was examined. This led to the identification of a potent and highly selective CXCR2 antagonist, which in addition was shown to be functionally active bo
Widdowson, Katherine L.,Elliott, John D.,Veber, Daniel F.,Nie, Hong,Rutledge, Melvin C.,McCleland, Brent W.,Xiang, Jia-Ning,Jurewicz, Anthony J.,Hertzberg, Robert P.,Foley, James J.,Griswold, Don E.,Martin, Lenox,Lee, Judithann M.,White, John R.,Sarau, Henry M.
p. 1319 - 1321
(2007/10/03)
IL-8 RECEPTOR ANTAGONISTS
Novel IL-8 receptor antagonists and methods of using them are provided.
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(2008/06/13)
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