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  • Title: Synthesis and structure-activity relationships of 3,4-diaminocyclobut-3-ene-1,2-dione CXCR2 antagonists.
    Author: Merritt JR, Rokosz LL, Nelson KH, Kaiser B, Wang W, Stauffer TM, Ozgur LE, Schilling A, Li G, Baldwin JJ, Taveras AG, Dwyer MP, Chao J.
    Journal: Bioorg Med Chem Lett; 2006 Aug 01; 16(15):4107-10. PubMed ID: 16697193.
    Abstract:
    A novel series of 3,4-diaminocyclobut-3-ene-1,2-diones was prepared and found to show potent inhibitory activity of CXCR2 binding and IL-8-mediated chemotaxis of a CXCR2-expressing cell line. Microsome stability and Caco2 studies were subsequently used to show that compounds of this chemotype are predicted to have good oral bioavailability and are thus suitable for pharmaceutical development.
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