Literature DB >> 17236763

Comparison of N,N'-diarylsquaramides and N,N'-diarylureas as antagonists of the CXCR2 chemokine receptor.

Brent W McCleland1, Roderick S Davis, Michael R Palovich, Katherine L Widdowson, Michelle L Werner, Miriam Burman, James J Foley, Dulcie B Schmidt, Henry M Sarau, Martin Rogers, Kevin L Salyers, Peter D Gorycki, Theresa J Roethke, Gary J Stelman, Leonard M Azzarano, Keith W Ward, Jakob Busch-Petersen.   

Abstract

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.

Entities:  

Mesh:

Substances:

Year:  2006        PMID: 17236763     DOI: 10.1016/j.bmcl.2006.12.067

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

Review 1.  Emerging strategies for cancer immunoprevention.

Authors:  J C Roeser; S D Leach; F McAllister
Journal:  Oncogene       Date:  2015-09-14       Impact factor: 9.867

2.  Activities of N,N'-Diarylurea MMV665852 analogs against Schistosoma mansoni.

Authors:  Noemi Cowan; Philipp Dätwyler; Beat Ernst; Chunkai Wang; Jonathan L Vennerstrom; Thomas Spangenberg; Jennifer Keiser
Journal:  Antimicrob Agents Chemother       Date:  2015-01-12       Impact factor: 5.191

  2 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.