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

Bioorganic and Medicinal Chemistry Letters

Volumn 9, Issue 9, 1999, Pages 1291-1294

  Arcadi, Antonio ^a   Asti, Cinzia ^b   Brandolini, Laura ^b   Caselli, Gianfranco ^b   Marinelli, Fabio ^a   Ruggieri, Viviana ^b  

^a UNIVERSITY OF L'AQUILA   (Italy)

^b Chemistry Section   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

2 (6' METHOXY 3',4' DIHYDRO 1' NAPHTHYL) 4H 3,1 BENZOXAZIN 4 ONE; ELASTASE; ENZYME INHIBITOR; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; DRUG MECHANISM; DRUG POTENCY; DRUG SCREENING; DRUG STABILITY; DRUG SYNTHESIS; ENZYME INHIBITION; LEUKOCYTE; NONHUMAN; ORAL DRUG ADMINISTRATION;

ANIMALS; DOSE-RESPONSE RELATIONSHIP, DRUG; HUMANS; INHIBITORY CONCENTRATION 50; KINETICS; LEUKOCYTE ELASTASE; LUNG; MICE; OXAZINES; SPUTUM;

EID: 0033519309     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(99)00168-7     Document Type: Article

References (13)

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10. 405nm ( Doherty, J.B.; Ashe, B.M.; Argenbright, L.W.; Baker, P.L.; Bonney, R.J.; Chandler, G.O.; Dahlgren, M.E.; Dorn, C.P. Jr.; Finke, P.E.; Firestone, R.A.; Fletcher, D.; Hagman, W.K.; Mumford, R.; O'Grady, L.; Maycock, A.L.; Pisano, J.M.; Shah, S.K.; Thompson, K.R.; Zimmerman, M. Nature 1986, 322, 192 ).
11. 405nm ( Doherty, J.B.; Ashe, B.M.; Argenbright, L.W.; Baker, P.L.; Bonney, R.J.; Chandler, G.O.; Dahlgren, M.E.; Dorn, C.P. Jr.; Finke, P.E.; Firestone, R.A.; Fletcher, D.; Hagman, W.K.; Mumford, R.; O'Grady, L.; Maycock, A.L.; Pisano, J.M.; Shah, S.K.; Thompson, K.R.; Zimmerman, M. Nature 1986, 322, 192 ).
12. 3): δ 159.1, 156.6, 146.7, 138.7, 137.2, 136.5, 130.0, 128.4, 128.3, 127.8, 127.3, 126.9, 123.5, 117.2, 113.7, 111.1, 55.3, 28.1, 23.7.
13. 3 2% w/v. The haemorrhage was expressed as μl equivalents of blood in 2 ml of BALF. The protective effect of the compound was calculated as a percentage of inhibition of lung haemorrhage in treated versus control animals. The basal value (vehicle) was subtracted from each treatment group.