Literature DB >> 14741295

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

William G Harter1, Hans Albrect, Kenneth Brady, Bradley Caprathe, James Dunbar, John Gilmore, Sheryl Hays, Catherine R Kostlan, Beth Lunney, Nigel Walker.   

Abstract

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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Year:  2004        PMID: 14741295     DOI: 10.1016/j.bmcl.2003.10.065

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  4 in total

Review 1.  Small Molecule Active Site Directed Tools for Studying Human Caspases.

Authors:  Marcin Poreba; Aleksandra Szalek; Paulina Kasperkiewicz; Wioletta Rut; Guy S Salvesen; Marcin Drag
Journal:  Chem Rev       Date:  2015-11-09       Impact factor: 60.622

2.  Design, synthesis, and biological evaluation of beta-ketosulfonamide adenylation inhibitors as potential antitubercular agents.

Authors:  Jagadeshwar Vannada; Eric M Bennett; Daniel J Wilson; Helena I Boshoff; Clifton E Barry; Courtney C Aldrich
Journal:  Org Lett       Date:  2006-10-12       Impact factor: 6.005

3.  Room temperature synthesis and antibacterial activity of new sulfonamides containing n,n-diethyl-substituted amido moieties.

Authors:  Olayinka O Ajani; Oluwole B Familoni; Feipeng Wu; Johnbull O Echeme; Zheng Sujiang
Journal:  Int J Med Chem       Date:  2012-10-17

4.  Identification and Structure-Activity Relationship of Recovered Phenolics with Antioxidant and Antihyperglycemic Potential from Sugarcane Molasses Vinasse.

Authors:  Zhe Huang; Yinning Chen; Riming Huang; Zhengang Zhao
Journal:  Foods       Date:  2022-10-08
  4 in total

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