B. Macchia et al., Synthesis, inhibitory activity towards human leukocyte elastase and molecular modelling studies of 1-carbamoyl-4-methyleneaminoxyazetidinones, EUR J MED C, 35(1), 2000, pp. 53-67
Some monocyclic beta-lactam derivatives of type 3 (MAOAs) in which the leav
ing group (LG) on the C(4) is a methyleneaminoxy moiety, were synthesised a
nd tested in vitro and in vivo for their inhibitory activity towards human
leukocyte elastase (HLE). Some compounds showed an appreciable in vitro inh
ibitory activity against this enzyme. Effects on the anti-HLE activity due
to the nature of the substituents R and R-1 present on their LG were observ
ed and rationalised by means of molecular modelling techniques. The results
of in vivo pharmacological tests indicated that MAOAs, while showing an in
hibitory activity on the haemorrhage induced by HLE, did not exhibit any ef
fects due to the R and R-1 substituents. (C) 2000 Editions scientifiques et
medicales Elsevier SAS.