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

A Arcadi; C Asti; L Brandolini; G Caselli; F Marinelli; V Ruggieri

doi:10.1016/s0960-894x(99)00168-7

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

Bioorg Med Chem Lett. 1999 May 3;9(9):1291-4. doi: 10.1016/s0960-894x(99)00168-7.

Authors

A Arcadi¹, C Asti, L Brandolini, G Caselli, F Marinelli, V Ruggieri

Affiliation

¹ Dipartimento di Chimica, Ingegneria Chimica e Materiali, Università degli Studi di L'Aquila, Italy. arcadi@aquila.infn.it

PMID: 10340616
DOI: 10.1016/s0960-894x(99)00168-7

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Benzoxazines
Dose-Response Relationship, Drug
Humans
Inhibitory Concentration 50
Kinetics
Leukocyte Elastase / antagonists & inhibitors*
Lung / drug effects
Mice
Oxazines / chemical synthesis*
Oxazines / pharmacology*
Sputum / enzymology

Substances

2-(6'-methoxy-3',4'-dihydro-1'-naphthyl)-4H-3,1-benzoxazin-4-one
Benzoxazines
Oxazines
Leukocyte Elastase