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

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.

Design, Synthesis, and Enzymatic Evaluation ofN1-Acyloxyalkyl- andN1-Oxazolidin-2,4-dion-5-yl-Substituted β-lactams as Novel Inhibitors of Human Leukocyte Elastase

2005 ◽  
Vol 48 (15) ◽  
pp. 4861-4870 ◽  
Author(s):  
Rui Moreira ◽  
Ana Bela Santana ◽  
Jim Iley ◽  
João Neres ◽  
Kenneth T. Douglas ◽  
...  
Keyword(s):  
Human Leukocyte ◽  
Leukocyte Elastase ◽  
Design Synthesis ◽  
Human Leukocyte Elastase

ChemInform Abstract: FR901451, a Novel Inhibitor of Human Leukocyte Elastase from Flexibacter sp. Part 2. Pharmacological Effect of FR901451.

ChemInform ◽  
2010 ◽  
Vol 26 (23) ◽  
pp. no-no
Author(s):  
T. FUJITA ◽  
Y. SHINGUH ◽  
A. YAMAZAKI ◽  
K. NAKAHARA ◽  
M. OKAMOTO ◽  
...  
Keyword(s):  
Human Leukocyte ◽  
Pharmacological Effect ◽  
Leukocyte Elastase ◽  
Human Leukocyte Elastase

Heterocyclic inhibitors of human leukocyte elastase: 3-Hydroxypyridazopyrimidine, 3-hydroxypyridopyrimidine and 3-hydroxyquinazoline-2,4-1H,3H0dione derivatives

1993 ◽  
Vol 3 (6) ◽  
pp. 1163-1168 ◽  
Author(s):  
William C. Groutas ◽  
James C. Castrisos ◽  
Michael A. Stanga ◽  
Rong-ze Kuang ◽  
Radhika Venkataraman ◽  
...  
Keyword(s):  
Human Leukocyte ◽  
Leukocyte Elastase ◽  
Human Leukocyte Elastase

Mechanism of inhibition of human leukocyte elastase by two cephalosporin derivatives

Biochemistry ◽  
1992 ◽  
Vol 31 (21) ◽  
pp. 4980-4986 ◽  
Author(s):  
W. B. Knight ◽  
A. L. Maycock ◽  
B. G. Green ◽  
B. M. Ashe ◽  
P. Gale ◽  
...  
Keyword(s):  
Human Leukocyte ◽  
Leukocyte Elastase ◽  
Mechanism Of Inhibition ◽  
Human Leukocyte Elastase

Pulmonary Hemorrhage Induced by Intratracheal Administration of Human Leukocyte Elastase in Hamsters

1991 ◽  
Vol 624 (1) ◽  
pp. 331-333 ◽  
Author(s):  
ROBERT J. GORDON ◽  
EDWARD FERGUSON ◽  
RICHARD DUNLAP ◽  
CATHERINE FRANKE ◽  
PAUL J. SILVER
Keyword(s):  
Pulmonary Hemorrhage ◽  
Human Leukocyte ◽  
Leukocyte Elastase ◽  
Intratracheal Administration ◽  
Human Leukocyte Elastase
Sign in / Sign up

Export Citation Format

Share Document