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Bioorg Med Chem Lett. 2006 Apr 15;16(8):2200-4. Epub 2006 Feb 3.

A novel series of arylsulfonylthiophene-2-carboxamidine inhibitors of the complement component C1s.

Author information

1
Johnson & Johnson Pharmaceutical Research and Development, L.L.C., 665 Stockton Drive, Exton, PA 19341, USA. nsubasin@prdus.jnj.com

Abstract

Inhibiting the classical pathway of complement activation by attenuating the proteolytic activity of the serine protease C1s is a potential strategy for the therapeutic intervention in disease states such as hereditary angioedema, ischemia-reperfusion injury, and acute transplant rejection. A series of arylsulfonylthiophene-2-carboxamidine inhibitors of C1s were synthesized and evaluated for C1s inhibitory activity. The most potent compound had a Ki of 10nM and >1000-fold selectivity over uPA, tPA, FX(a), thrombin, and plasmin.

PMID:
16460935
DOI:
10.1016/j.bmcl.2006.01.036
[Indexed for MEDLINE]

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