131230-67-6Relevant articles and documents
Inhibition of human leukocyte elastase by functionalized N-aryl azetidin-2-ones: Substituent effects at C-3 and benzylic positions
Vergely,Boggetto,Okochi,Golpayegani,Reboud-Ravaux,Kobaiter,Joyeau,Wakselman
, p. 199 - 208 (2007/10/02)
A series of functionalized N-aryl azetidin-2-ones with a latent alkylating group was prepared by a flexible four-step synthesis, They met criteria expected for a suicide-type inactivation of human leukocyte elastase (HLE) and porcine pancreatic elastase (
N-ARYL-AZETIDINONES, THEIR PREPARATION PROCESS AND THEIR USE AS ELASTASE INHIBITORS
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, (2008/06/13)
The invention relates to N-aryl-azetidinones, their preparation process and their use as active serine elastase inhibitors. The N-aryl-azetidinones are in accordance with formula: STR1 in which R. sup.1 and R 2 can be a halogen atom or an organic radical, R. sup.3 represents a halogen atom or another good starting group and R 4 represents H or an organic radical. The compounds with R 3 =Cl or OSO 2 CH 3, R 4 =H and R 1 =R. sup.2 =F or R 1 =F and R 2 =Br are irreversible and selective elastase inhibitors.
