454471-77-3Relevant academic research and scientific papers
Discovery of CNS Penetrant CXCR2 Antagonists for the Potential Treatment of CNS Demyelinating Disorders
Xu, Heng,Lu, Hongfu,Xu, Zhongmiao,Luan, Linbo,Li, Chengyong,Xu, Yan,Dong, Kelly,Zhang, Jinqiang,Li, Xiong,Li, Yvonne,Liu, Gentao,Gong, Sophie,Zhao, Yong-Gang,Liu, Ailian,Zhang, Yueting,Zhang, Wei,Cai, Xin,Xiang, Jia-Ning,Elliott, John D.,Lin, Xichen
supporting information, p. 397 - 402 (2016/05/19)
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
Comparison of N,N′-diarylsquaramides and N,N′-diarylureas as antagonists of the CXCR2 chemokine receptor
McCleland, Brent W.,Davis, Roderick S.,Palovich, Michael R.,Widdowson, Katherine L.,Werner, Michelle L.,Burman, Miriam,Foley, James J.,Schmidt, Dulcie B.,Sarau, Henry M.,Rogers, Martin,Salyers, Kevin L.,Gorycki, Peter D.,Roethke, Theresa J.,Stelman, Gary J.,Azzarano, Leonard M.,Ward, Keith W.,Busch-Petersen, Jakob
, p. 1713 - 1717 (2007/10/03)
N,N′-diarylsquaramides were prepared and evaluated as antagonists of CXCR2. The compounds were found to be potent and selective antagonists of CXCR2. Significant differences in SAR was observed relative to the previously described N,N′-diarylurea series. As was the case in the N,N′-diarylurea series, placing sulfonamide substituent adjacent to the acidic phenol significantly reduced the clearance in rat pharmacokinetic studies.
Discovery of potent and orally bioavailable N,N′-diarylurea antagonists for the CXCR2 chemokine receptor
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)
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
