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

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 16, 2012, Pages 5303-5307

  Subasinghe, Nalin L ^a   Khalil, Ehab ^a   Travins, Jeremy M ^a   Ali, Farah ^a   Ballentine, Shelley K ^a   Hufnagel, Heather R ^a   Pan, Wenxi ^a   Leonard, Kristi ^a   Bone, Roger F ^a   Soll, Richard M ^a   Crysler, Carl S ^a   Ninan, Nisha ^a   Kirkpatrick, Jennifer ^a   Kolpak, Michael X ^a   Diloreto, Karen A ^a   Eisennagel, Stephen H ^a   Huebert, Norman D ^a   Molloy, Christopher J ^a   Tomczuk, Bruce E ^a   Gaul, Michael D ^a  

^a JANSSEN RESEARCH AND DEVELOPMENT   (Belgium)

Author keywords

C1s inhibitors; Complement inhibitors; Pegylated molecule pharmacokinetics; Pegylated molecule PK; Pegylated small molecule; Pegylation; Pharmacokinetics; Polyethylene glycol modified; Polyethylene glycol modified small molecule

Indexed keywords

BIPHENYLSULFONYL THIOPHENE CARBOXAMIDINE INHIBITOR; COMPLEMENT COMPONENT C1; COMPLEMENT COMPONENT C1S INHIBITOR; MACROGOL; UNCLASSIFIED DRUG;

ADULT RESPIRATORY DISTRESS SYNDROME; ARTICLE; CHEMICAL STRUCTURE; COMPLEMENT CLASSICAL PATHWAY; DRUG CONFORMATION; DRUG DESIGN; DRUG POTENCY; DRUG SYNTHESIS; GRAFT REJECTION; IN VIVO STUDY; PHARMACOKINETICS; REPERFUSION INJURY; STRUCTURE ACTIVITY RELATION;

AMIDES; ANIMALS; COMPLEMENT C1S; DRUG DESIGN; HALF-LIFE; POLYETHYLENE GLYCOLS; PROTEASE INHIBITORS; RATS; THIOPHENES;

EID: 84864414397     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2012.06.030     Document Type: Article

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