4 documents found, page 1 of 1
Medicinal Chemistry
Moreira, R; Carreiras, MC; Lopes, F; Rocha, MJP; Mendes, E; LConstantino, Dias,; Santos, MM; Lavrado, J; Capela, R; Santana, AB; Valente, E
Design, synthesis, and enzymatic evaluation of N-1-acyloxyalkyl- and N-1-oxazol...
Moreira, R; Santana, AB; Iley, J; Neres, J; Douglas, KT; Horton, PN; Hursthouse, MBHuman leukocyte elastase (HLE) is a serine protease that very efficiently degrades various tissue matrix proteins such as elastin. The imbalance between HLE and its endogenous inhibitors leads to excessive elastin proteolysis and is considered to be responsible for the onset of chronic obstructive pulmonary disease (COPD). A novel series of C-3-, C-4-, and N-1-substituted azetidin-2-ones were prepared as potent...
Design, synthesis and stability of N-acyloxymethyl- and N-aminocarbonyloxymethy...
Clemente, A; Domingos, A; Grancho, AP; Iley, J; Moreira, R; Neres, J; Palma, N; Santana, AB; Valente, EA 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, (C) 2001 Elsevier Science Ltd. All rights reserved.
N-Acyloxymethyl-2-azetidinones as Human Leukocyte Elastase Inhibitors
Santana, AB; Valente, E; Neres, J; Moreira, R; Palma, N; Grancho, AP; Domingos, A; Clemente, A; Iley, J