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Enzyme Research

Reports outline enzyme research study findings from University of Lisboa

Published in Pharma Law Weekly, May 13th, 2008

Research findings, 'Azetidine-2,4-diones (4-oxo-beta-lactams) as scaffolds for designing elastase inhibitors,' are discussed in a new report. "A new class of inhibitors 4-oxo-beta-lactams (azetidine-2,4-diones), containing the required structural elements for molecular recognition, inhibit porcine pancreatic elastase (PPE) but show a dramatically lower reactivity toward hydroxide compared with the analogous inhibitors 3-oxo-beta-sultams. Inhibition is the result of acylation of the active site serine and electron-withdrawing substituents at the N-(4-aryl) position in 3,3-diethyl-N-aryl derivatives increasing the rate of enzyme acylation and generating a Hammett rho-value of 0.65,"...

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