title: Design, synthesis and stability of N-acyloxymethyl- and N-aminocarbonyloxymethyl-2-azetidinones as human leukocyte elastase inhibitors.
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.
authors.affiliation: INETI, Dep. Biotecnologia, Estrada das Palmeiras, Lisboa, Portugal.
authors.forename: A
authors.initials: A
authors.lastname: Clemente
authors.forename: A
authors.initials: A
authors.lastname: Domingos
authors.forename: A P
authors.initials: AP
authors.lastname: Grancho
authors.forename: J
authors.initials: J
authors.lastname: Iley
authors.forename: R
authors.initials: R
authors.lastname: Moreira
authors.forename: J
authors.initials: J
authors.lastname: Neres
authors.forename: N
authors.initials: N
authors.lastname: Palma
authors.forename: A B
authors.initials: AB
authors.lastname: Santana
authors.forename: E
authors.initials: E
authors.lastname: Valente
mesh_terms: D001384:Azetidines / Q000138:chemical synthesis / Q000494:pharmacology; D015195:Drug Design; D004355:Drug Stability; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D019272:Leukocyte Elastase / Q000037:antagonists & inhibitors*; D008958:Models, Molecular; D012680:Sensitivity and Specificity
chemical_list: C116379:2-azetidinone; D001384:Azetidines; D004791:Enzyme Inhibitors; D019272:Leukocyte Elastase