Synthesis and in vitro and in vivo evaluation of the 2-(6'methoxy-3',4'-dihydro-1'-naphtyl)-4H-3,1-benzoxazin-4- one as a new potent substrate inhibitor of human leukocyte elastase.
The title 2-vinyl-4H-3,1-benzoxazin-4-one has been synthesised and tested for inhibitory activity against human leukocyte elastase. The compound has shown activity both in vitro towards human sputum elastase and in vivo in an hemorrhagic assay.
Arcadi
A
A
Dipartimento di Chimica, Ingegneria Chimica e Materiali, Università degli Studi di L'Aquila, Italy. arcadi@aquila.infn.it
Asti
C
C
Brandolini
L
L
Caselli
G
G
Marinelli
F
F
Ruggieri
V
V
D000818:Animals; D048588:Benzoxazines; D004305:Dose-Response Relationship, Drug; D006801:Humans; D020128:Inhibitory Concentration 50; D007700:Kinetics; D019272:Leukocyte Elastase / Q000037:antagonists & inhibitors*; D008168:Lung / Q000187:drug effects; D051379:Mice; D010078:Oxazines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013183:Sputum / Q000201:enzymology
C120630:2-(6'-methoxy-3',4'-dihydro-1'-naphthyl)-4H-3,1-benzoxazin-4-one; D048588:Benzoxazines; D010078:Oxazines; D019272:Leukocyte Elastase