Inhibition of human leukocyte elastase. 2. Inhibition by substituted cephalosporin esters and amides.
J Med Chem
; 33(9): 2522-8, 1990 Sep.
Article
en En
| MEDLINE
| ID: mdl-2391692
A variety of 7 alpha-methoxycephalosporin ester and amide sulfones were prepared and tested to determine the structure-activity relations for inhibition of human leukocyte elastase (HLE), a serine protease which has been implicated in several degenerative lung and tissue diseases. The most potent IC50 values were obtained with neutral, lipophilic derivatives, with the esters being more active than the amides. However, the best time-dependent inhibition in this series was observed with the p- and m-carboxybenzyl esters 7b and 7c. These results are discussed in terms of the proposed mechanism of inhibition as well as a molecular modeling study using the recently solved X-ray crystal structure of HLE.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Ácidos Carboxílicos
/
Elastasa Pancreática
/
Cefalosporinas
/
Ésteres
/
Amidas
Límite:
Humans
Idioma:
En
Revista:
J Med Chem
Asunto de la revista:
QUIMICA
Año:
1990
Tipo del documento:
Article
Pais de publicación:
Estados Unidos