Design and synthesis of polyethylene glycol-modified biphenylsulfonyl-thiophene-carboxamidine inhibitors of the complement component C1s.
Bioorganic & Medicinal Chemistry Letters(2012)
摘要
Complement C1s protease inhibitors have potential utility in the treatment of diseases associated with activation of the classical complement pathway such as humorally mediated graft rejection, ischemia-reperfusion injury (IRI), vascular leak syndrome, and acute respiratory distress syndrome (ARDS). The utility of biphenylsulfonyl-thiophene-carboxamidine small-molecule C1s inhibitors are limited by their poor in vivo pharmacokinetic properties. Pegylation of a potent analog has provided compounds with good potency and good in vivo pharmacokinetic properties.
更多查看译文
关键词
Complement inhibitors,C1s inhibitors,Pegylation,Pegylated small molecule,Polyethylene glycol-modified,Pharmacokinetics,Polyethylene glycol-modified small molecule,Pegylated molecule pharmacokinetics,Pegylated molecule PK
AI 理解论文
溯源树
样例
生成溯源树,研究论文发展脉络
Chat Paper
正在生成论文摘要