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Design and synthesis of polyethylene glycol-modified biphenylsulfonyl-thiophene-carboxamidine inhibitors of the complement component C1s.

Abstract
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.
AuthorsNalin L Subasinghe, Ehab Khalil, Jeremy M Travins, Farah Ali, Shelley K Ballentine, Heather R Hufnagel, Wenxi Pan, Kristi Leonard, Roger F Bone, Richard M Soll, Carl S Crysler, Nisha Ninan, Jennifer Kirkpatrick, Michael X Kolpak, Karen A Diloreto, Stephen H Eisennagel, Norman D Huebert, Christopher J Molloy, Bruce E Tomczuk, Michael D Gaul
JournalBioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 22 Issue 16 Pg. 5303-7 (Aug 15 2012) ISSN: 1464-3405 [Electronic] England
PMID22795627 (Publication Type: Journal Article)
CopyrightCopyright © 2012 Elsevier Ltd. All rights reserved.
Chemical References
  • Amides
  • Protease Inhibitors
  • Thiophenes
  • Polyethylene Glycols
  • Complement C1s
Topics
  • Amides (chemistry)
  • Animals
  • Complement C1s (antagonists & inhibitors, metabolism)
  • Drug Design
  • Half-Life
  • Polyethylene Glycols (chemistry)
  • Protease Inhibitors (chemical synthesis, chemistry, pharmacokinetics)
  • Rats
  • Thiophenes (chemistry)

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