A novel series of potent and selective small molecule inhibitors of the complement component C1s

…, F Ali, CR Illig, MJ Rudolph, S Klein, E Khalil…

Index: Subasinghe, Nalin L.; Ali, Farah; Illig, Carl R.; Rudolph, M. Jonathan; Klein, Scott; Khalil, Ehab; Soll, Richard M.; Bone, Roger F.; Spurlino, John C.; DesJarlais, Renee L.; Crysler, Carl S.; Cummings, Maxwell D.; Morris Jr., Philip E.; Kilpatrick, John M.; Babu, Y. Sudhakara Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 12 p. 3043 - 3047

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Citation Number: 17

Abstract

Activation of the classical pathway of complement has been implicated in disease states such as hereditary angioedema, ischemia-reperfusion injury and acute transplant rejection. The trypsin-like serine protease C1s represents a pivotal upstream point of control in the classical pathway of complement activation and is therefore likely to be a useful target in the therapeutic intervention of these disease states. A series of thiopheneamidine-based ...