Design, synthesis and stability of N-acyloxymethyl- and N-aminocarbonyloxymethyl-2-azetidinones as human leukocyte elastase inhibitors

Clemente, A.; Domingos, A.; Grancho, A. P.; Iley, James; Moreira, R.; Neres, J.; Palma, N.; Santana, A. B. and Valente, E. (2001). Design, synthesis and stability of N-acyloxymethyl- and N-aminocarbonyloxymethyl-2-azetidinones as human leukocyte elastase inhibitors. Bioorganic and Medicinal Chemistry Letters, 11(8) pp. 1065–1068.

DOI: https://doi.org/10.1016/S0960-894X(01)00131-7

Abstract

A series of N-acyloxymethyl- and N-aminocarbonyloxymethyl derivatives of 2-azetidinones, 3, with different substituent patterns at the beta-lactam C-3 and C-4 positions, were designed as potential mechanism-based inhibitors for human leukocyte elastase and found to exhibit inhibitory potency and selectivity for the enzyme.

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