Nonpeptidic Inhibitors of Human Leukocyte Elastase. 2. Design, Synthesis, and in vitro Activity of a Series of 3-Amino-6-aryl-2-oxopyridyl Trifluoromethyl Ketones

1994 ◽  
Vol 37 (20) ◽  
pp. 3303-3312 ◽  
Author(s):  
James R. Damewood ◽  
Philip D. Edwards ◽  
Scott Feeney ◽  
Bruce C. Gomes ◽  
Gary B. Steelman ◽  
...  
Keyword(s):  
Human Leukocyte ◽  
Vitro Activity ◽  
In Vitro Activity ◽  
Leukocyte Elastase ◽  
Design Synthesis ◽  
Trifluoromethyl Ketones ◽  
Human Leukocyte Elastase

2α-Alkoxymethyl Cephalosporins: Reactions of exo-2-Methylene Cephalosporin Sulfones with Alcohols

1994 ◽  
Vol 59 (10) ◽  
pp. 2282-2292 ◽  
Author(s):  
Maxwell D. Cummings ◽  
David P. Czajkowski ◽  
John Brunstein ◽  
Narender A. V. Reddy ◽  
Oludotun A. Phillips ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Nucleophilic Addition ◽  
Human Leukocyte ◽  
Vitro Activity ◽  
In Vitro Activity ◽  
Leukocyte Elastase ◽  
Human Leukocyte Elastase

A series of 2α-alkoxymethyl cephem sulfones were prepared by nucleophilic addition of a variety of alcohols to exo-2-methylene cephem sulfones. The 2α-alkoxymethyl group was introduced with the aim of improving the inhibitory activity against human leukocyte elastase (HLE) over the unsubstituted compounds. However, against HLE the in vitro activity was still inferior to that shown by the C-2 unsubstituted cephem sulfones.

Non-peptidic inhibitors of human leukocyte elastase. 4. Design, synthesis, and in vitro and in vivo activity of a series of .beta.-carbolinone-containing trifluoromethyl ketones

1995 ◽  
Vol 38 (1) ◽  
pp. 86-97 ◽  
Author(s):  
Chris A. Veale ◽  
James R. Jr. Damewood ◽  
Gary B. Steelman ◽  
Craig Bryant ◽  
Bruce Gomes ◽  
...  
Keyword(s):  
Human Leukocyte ◽  
Leukocyte Elastase ◽  
Design Synthesis ◽  
Trifluoromethyl Ketones ◽  
Human Leukocyte Elastase ◽  
Peptidic Inhibitors

Design, synthesis, and in vitro evaluation of inhibitors of human leukocyte elastase based on a functionalized cyclic sulfamide scaffold

2004 ◽  
Vol 12 (3) ◽  
pp. 589-593 ◽  
Author(s):  
Jiaying Zhong ◽  
Xiangdong Gan ◽  
Kevin R Alliston ◽  
William C Groutas
Keyword(s):  
Human Leukocyte ◽  
Leukocyte Elastase ◽  
Design Synthesis ◽  
In Vitro Evaluation ◽  
Human Leukocyte Elastase

Design, synthesis, and in vitro inhibitory activity toward human leukocyte elastase, cathepsin G, and proteinase 3 of saccharin-derived sulfones and congeners

1996 ◽  
Vol 4 (9) ◽  
pp. 1393-1400 ◽  
Author(s):  
William C. Groutas ◽  
Jeffrey B. Epp ◽  
Radhika Venkataraman ◽  
Rongze Kuang ◽  
Tien My Truong ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Human Leukocyte ◽  
Cathepsin G ◽  
Proteinase 3 ◽  
Leukocyte Elastase ◽  
Design Synthesis ◽  
Human Leukocyte Elastase

Nonpeptidic inhibitors of human leukocyte elastase. 5. Design, synthesis, and x-ray crystallography of a series of orally active 5-aminopyrimidin-6-one-containing trifluoromethyl ketones

1995 ◽  
Vol 38 (1) ◽  
pp. 98-108 ◽  
Author(s):  
Chris A. Veale ◽  
Peter R. Bernstein ◽  
Craig Bryant ◽  
Christopher Ceccarelli ◽  
James R. Jr. Damewood ◽  
...  
Keyword(s):  
Human Leukocyte ◽  
Leukocyte Elastase ◽  
Design Synthesis ◽  
X Ray ◽  
X Ray Crystallography ◽  
Trifluoromethyl Ketones ◽  
Human Leukocyte Elastase ◽  
Orally Active

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

DEVELOPMENT OF A SPECIFIC RADIODMMUNOASSAY FOR DETERMINATION OF PEPTIDES DERIVED FROM HUMAN LEUKOCYTE ELASTASE DEGRADATION OF HUMAN FIBRIN (OGEN)

1987 ◽  
Author(s):  
R Wallin ◽  
T Saldeen
Keyword(s):  
Human Leukocyte ◽  
In Vitro Study ◽  
Molecular Size ◽  
Molar Ratio ◽  
Leukocyte Elastase ◽  
Severe Renal Failure ◽  
Human Leukocyte Elastase ◽  
Edta Plasma

This paper describes a RIA for determination of the vasoactive peptide BB 30-43 and related peptides derived from leukocyte elastase degradaticn of human fibrin(ogen). The peptide was synthesized and could easily be labelled with 125I.Rabbits were iirmunized with BB 30-43 conjugated to bovine albumin. The antibody was found to bind about 5C% of the tracer in absence of BB 30-43 in a ˜1/800 diluticn. The RIA can detect peptide concentrations between 50 - 25000 pmol/L. The crossreaction with fibrinogen is very low (<0.001%) and with plas-min derived fibrin(ogen) peptides Bβ 1-42 and BB 15-42 also low (<0.2%). Plasma samples can be analyzed without any pretreatment. In an in vitro study fibrin and fibrincgen was degraded with plasmin or leukocyte elastase. Plasmin degradaticn of fibrin and fibrincgen did not release peptides which cross-reacted with our antibody, whereas leukocyte elastase degradation released peptides from both fibrin and fibrinogen which crossreact whith the antibody.The imnunolqgical activity was not changed after degrading peptide Bβ 30-43 with a) trypsin, b) plasmin, c) batraxobin, d) thrombin, e) elastase, at +37°,1 h, in a molar ratio of 1:100. Even degradaticn by elastase (1:3.5) +37°, 1 h, did not destroy the iirmunological activity.The imriunolcgical stability of peptide B< 30-43 in EDTA-plasma (+37°) seems to be very good. In citrated and heparinized plasma the activity of this peptide seems to vanish quite fast. In spite of these results we have detected high levels of iirmunolcgical activitiy in citrated or heparinized patient plasma. The molecular distribution of the peptides detected in plasma by our RIA corresponded to a fragnent containing about 25 amino acids. This fragnent seemes to be rather stable in plasma. When this fragnent was degraded with elastase in vitro a peptide with a molecular size resembling BB 30-43 was obtained. Over 300 patient samples have been studied. About 20 per cent were positive and the highest levels were found in patients with ARDS, septicaemia, severe renal failure, pulmonary embolism, pneumonia and pulmonary congestion.

Design, Synthesis and Stability of N-Acyloxymethyl- and N-Aminocarbonyloxymethyl-2-azetidinones as Human Leukocyte Elastase Inhibitors

2001 ◽  
Vol 11 (8) ◽  
pp. 1065-1068 ◽  
Author(s):  
A Clemente ◽  
A Domingos ◽  
A.P Grancho ◽  
J Iley ◽  
R Moreira ◽  
...  
Keyword(s):  
Human Leukocyte ◽  
Leukocyte Elastase ◽  
Design Synthesis ◽  
Human Leukocyte Elastase

scholarly journals Human Leukocyte Elastase Induces Keratinocyte Proliferation In Vitro and In Vivo

2002 ◽  
Vol 118 (1) ◽  
pp. 49-54 ◽  
Author(s):  
Christina Rogalski ◽  
Ulf Meyer-Hoffert ◽  
Ehrhardt Proksch ◽  
Oliver Wiedow
Keyword(s):  
Human Leukocyte ◽  
Leukocyte Elastase ◽  
Keratinocyte Proliferation ◽  
Human Leukocyte Elastase ◽  
Proliferation In Vitro
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