2. Academic Validation
  3. Discovery of 2-hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5- methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide (SCH 527123): a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist

Discovery of 2-hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5- methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide (SCH 527123): a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist

  • J Med Chem. 2006 Dec 28;49(26):7603-6. doi: 10.1021/jm0609622.
Michael P Dwyer 1,  Younong Yu,  Jianping Chao,  Cynthia Aki,  Jianhua Chao,  Purakkattle Biju,  Viyyoor Girijavallabhan,  Diane Rindgen,  Richard Bond,  Rosemary Mayer-Ezel,  James Jakway,  R William Hipkin,  James Fossetta,  Waldemar Gonsiorek,  Hong Bian,  Xuedong Fan,  Carol Terminelli,  Jay Fine,  Daniel Lundell,  J Robert Merritt,  Laura L Rokosz,  Bernd Kaiser,  Ge Li,  Wei Wang,  Tara Stauffer,  Lynne Ozgur,  John Baldwin,  Arthur G Taveras
Affiliations

Affiliation

  • 1 Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. michael.dwyer@spcorp.com
PMID: 17181143 DOI: 10.1021/jm0609622
Abstract

Structure-activity studies on lead cyclobutenedione 3 led to the discovery of 4 (SCH 527123), a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist with excellent cell-based activity. Compound 4 displayed good oral bioavailability in rat and may be a potential therapeutic agent for the treatment of various inflammatory diseases.

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