The complement cascade is a major component of the innate immune system in mammals and other vertebrate species.  It plays a major role in the destruction of invading microorganisms and the clearance of immune complexes. However, unregulated complement activation leading to acute inflammation and tissue damage has been implicated in the pathology of many disease states. Here we describe the synthesis, in vitro potency, and in vivo pharmacokinetic properties of pegylated arylsulfonylthiophene-2-carboxamidine inhibitors (1 ) of the complement component C1s.                                                                  

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

244th National Meeting (2012)

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