Inhibition of human leukocyte elastase by derivatives of N-hydroxysuccinimide. A structure-activity-relationship study

1989 ◽  
Vol 32 (7) ◽  
pp. 1607-1611 ◽  
Author(s):  
W. C. Groutas ◽  
M. J. Brubaker ◽  
M. A. Stanga ◽  
J. C. Castrisos ◽  
J. P. Crowley ◽  
...  
Keyword(s):  
Human Leukocyte ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Leukocyte Elastase ◽  
Structure Activity ◽  
Human Leukocyte Elastase ◽  
Relationship Study ◽  
Derivatives Of

Prejunctional effect of quaternary derivatives of l-hyoscyamine at the rat neuromuscular junction. A structure-activity relationship study

1994 ◽  
Vol 25 (7) ◽  
pp. 1397-1404 ◽  
Author(s):  
Caden Souccar ◽  
Janete Do Carmo Soldera ◽  
Roberta Monterazzo Cysneiros ◽  
Maria Do Carmo Gonçalo ◽  
Antonio José Lapa
Keyword(s):  
Neuromuscular Junction ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structure Activity ◽  
Relationship Study ◽  
Derivatives Of

Synthesis and evaluation of novel β-lactam inhibitors of human leukocyte elastase

2001 ◽  
Vol 79 (4) ◽  
pp. 377-387 ◽  
Author(s):  
K P Koteva ◽  
André M Cantin ◽  
W A Neugebauer ◽  
E Escher
Keyword(s):  
Serine Protease ◽  
Protease Inhibitors ◽  
Neutrophil Elastase ◽  
Human Leukocyte ◽  
Leukocyte Elastase ◽  
Piperazine Derivatives ◽  
Structure Activity ◽  
Human Leukocyte Elastase ◽  
Benzhydryl Piperazine ◽  
Derivatives Of

A series of β-lactam derivatives were synthesized and tested to determine the structure-activity relationship for inhibition of human leukocyte elastase (HLE), a serine protease involved in several degenerative lung and tissue diseases. The most potent IC50 values were obtained with neutral hydrophobic 7α-methoxy cephalosporanic acid derivatives. Tryptophanyl-9-fluorenylmethyl ester and N-benzhydryl piperazine derivatives of 7α-methoxy cephalosporanic acid represent two novel HLE inhibitors, with length of action persisting beyond 24 h.Key words: β-lactams, neutrophil elastase, protease inhibitors, peptides.

scholarly journals New ether oxime derivatives of erythromycin A. A structure-activity relationship study.

1991 ◽  
Vol 44 (3) ◽  
pp. 313-330 ◽  
Author(s):  
JEAN-CLAUDE GASC ◽  
SOLANGE GOUIN D''AMBRIERES ◽  
ANDRÉ LUTZ ◽  
JEAN-FRANÇOIS CHANTOT
Keyword(s):  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structure Activity ◽  
Relationship Study ◽  
Oxime Derivatives ◽  
Erythromycin A ◽  
Derivatives Of
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