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Discovery of Novel Cyanamide-Based Inhibitors of Cathepsin C

  作者 LAINE DRAMANE; PALOVICH MICHAEL; MCCLELAND BRENT; PETITJEAN EMILIE; DELHOM ISABELLE; XIE HAIBO; DENG JIANGHE; LIN GUOLIANG; DAVIS RODERICK; JOLIT ANAIS; NEVINS NEYSA; ZHAO BAOGUANG; VILLA JIM; SCHNECK JESSICA; MCDEVITT PATRICK; MIDGETT ROBERT; KMETT CASEY; UMBRECHT SANDRA; PECK BRIAN; DAVIS ALICIA BACON; BETTOUN DAVID  
  选自 期刊  ACS Medicinal Chemistry Letters;  卷期  2011年2-2;  页码  142-147  
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[摘要]The discovery of potent and selective cyanamide-based inhibitors of the cysteine protease cathepsin C is detailed. Optimization of the template with regard to plasma stability led to the identification of compound 17, a potent cathepsin C inhibitor with excellent selectivity over other cathepsins and potent in vivo activity in a cigarette smoke mouse model.

 
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