5 documents found, page 1 of 1
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...
Synthesis, stability and in vitro dermal evaluation of aminocarbonyloxymethyl e...
Mendes, E; Furtado, T; Neres, J; Iley, J; Jarvinen, T; Rautio, J; Moreira, RAminocarbonyloxymethyl esters 3 based on (S)-amino acid carriers were synthesised and evaluated as potential prodrugs of carboxylic acid agents. In addition, the compounds were evaluated as topical prodrugs with the aim of improving the dermal delivery of two non-steroidal anti-inflammatory agents: naproxen and flufenamic acid. The lipophilicities of these compounds were determined and their hydrolyses in aqueo...
Estéres Aminocarboniloximetílicos como potenciais pró-fármacos de ácidos carbox...
Furtado, T; Iley, J; Jarvinen, T; Mendes, E; Moreira, R; Neres, J; Rautio,J
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