Bioorganic and Medicinal Chemistry Letters p. 2779 - 2782 (2001)
Update date:2022-08-05
Topics: Acylation Hydrogenation Molecular docking Lithium aluminum hydride Diphenyl ether Sulfonamide Diazonium salt Sulfonyl chloride Weinreb amide Tert-butyl ester X-ray crystal structure Ligand Design Lead Optimization Virtual Screening Structural Analysis Protein Structure Determination Synthesis and Testing Iterative Optimization Pharmacokinetic and Toxicological Studies Animal and Clinical Trials
Shahripour, Aurash B
Plummer, Mark S
Lunney, Elizabeth A
Sawyer, Tomi K
Stankovic, Charles J
Connolly, Michael K
Rubin, John R
Walker, Nigel P.C
Brady, Kenneth D
Allen, Hamish J
Talanian, Robert V
Wong, Winnie W
Humblet, Christine
A series of compounds was designed and prepared as inhibitors of interleukin-1β converting enzyme (ICE), also known as caspase-1. These inhibitors, which employ a diphenyl ether sulfonamide, were designed to improve potency by forming favorable interactions between the diphenyl ether rings and the prime side hydrophobic region. An X-ray crystal structure of a representative member of the diphenyl ether sulfonamide series bound to the active site of caspase-1 was obtained.
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