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.

Ionic Inhibitors of Human Leukocyte Elastase: Pyridinium and Phenyl Carboxylate Derivatives of 3-Alkyl-N-Hydroxysuccinimide

1990 ◽  
Vol 79 (10) ◽  
pp. 886-888 ◽  
Author(s):  
W.C. Groutas ◽  
M.A. Stanga ◽  
J.C. Castrisos ◽  
E.J. Schatz ◽  
M.J. Brubaker
Keyword(s):  
Human Leukocyte ◽  
Leukocyte Elastase ◽  
Human Leukocyte Elastase ◽  
Derivatives Of
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