4-Oxo-β-lactams (azetidine-2, 4-diones) are potent and selective inhibitors of human leukocyte elastase

J Mulchande, R Oliveira, M Carrasco…

Index: Mulchande, Jalmira; Oliveira, Rudi; Carrasco, Marta; Gouveia, Luis; Guedes, Rita C.; Iley, Jim; Moreira, Rui Journal of Medicinal Chemistry, 2010 , vol. 53, # 1 p. 241 - 253

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Citation Number: 30

Abstract

Human leukocyte elastase (HLE) is a serine protease stored in and secreted from neutrophils that plays a determinant role in the pathogenesis of several lung diseases. 4- Oxo-β-lactams, previously reported as acylating agents of porcine pancreatic elastase, were found to be selective and potent inhibitors of HLE. Structure− activity relationship analysis showed that inhibitory activity is very sensitive to the nature of C-3 substituents, with small ...