Synthesis and structure-activity relationships of new disubstituted phenyl-containing 3,4-diamino-3-cyclobutene-1,2-diones as CXCR2 receptor antagonists |
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| Authors: | Lai Gaifa Merritt J Robert He Zhenmin Feng Daming Chao Jianhua Czarniecki Michael F Rokosz Laura L Stauffer Tara M Rindgen Diane Taveras Arthur G |
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| Institution: | Pharmacopeia, Inc., 3000 Eastpark Boulevard, Cranbury, NJ 08512, USA. galai@pcop.com |
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| Abstract: | A series of 3,4- and 3,5-disubstituted phenyl-containing cyclobutenedione analogues were synthesized and evaluated as CXCR2 receptor antagonists. Variations in the disubstitution pattern of the phenyl ring afforded new compounds with potent CXCR2 binding affinity in the low nanomolar ranges. Moreover, two potent compounds 19 and 26 exhibited good oral pharmacokinetic profiles. |
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