The design and synthesis of sulfonamides as caspase-1 inhibitors.

Bioorg Med Chem Lett

Chemistry Department, Pfizer Global Research and Development, 2800 Plymouth Rd, Ann Arbor, MI 48105, USA.

Published: February 2004

A series of sulfonamides (1) has been prepared as inhibitors of interleukin-1beta converting enzyme (ICE), also known as caspase 1. These compounds were designed to improve potency by rigidifying the enzyme bound molecule through an intramolecular hydrogen bond. An X-ray crystal structure of a representative member of this series bound to the active site of ICE, confirms the presence of the hydrogen bonding interaction.

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http://dx.doi.org/10.1016/j.bmcl.2003.10.065DOI Listing

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