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

Rui Moreira; Ana Bela Santana; Jim Iley; João Neres; Kenneth T. Douglas; Peter N. Horton; Michael B. Hursthouse

doi:10.1021/jm0501331

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

Journal of Medicinal Chemistry ◽

10.1021/jm0501331 ◽

2005 ◽

Vol 48 (15) ◽

pp. 4861-4870 ◽

Cited By ~ 25

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

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

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/s0960-894x(01)00131-7 ◽

2001 ◽

Vol 11 (8) ◽

pp. 1065-1068 ◽

Cited By ~ 38

Author(s):

A Clemente ◽

A Domingos ◽

A.P Grancho ◽

J Iley ◽

R Moreira ◽

...

Keyword(s):

Human Leukocyte ◽

Leukocyte Elastase ◽

Design Synthesis ◽

Human Leukocyte Elastase

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

Bioorganic & Medicinal Chemistry ◽

10.1016/j.bmc.2003.10.059 ◽

2004 ◽

Vol 12 (3) ◽

pp. 589-593 ◽

Cited By ~ 23

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

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

Bioorganic & Medicinal Chemistry ◽

10.1016/0968-0896(96)00133-2 ◽

1996 ◽

Vol 4 (9) ◽

pp. 1393-1400 ◽

Cited By ~ 30

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

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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

Journal of Medicinal Chemistry ◽

10.1021/jm00001a014 ◽

1995 ◽

Vol 38 (1) ◽

pp. 86-97 ◽

Cited By ~ 41

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

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The Gabriel-Colman rearrangement in biological systems: design, synthesis and biological evaluation of phthalimide and saccharin derivatives as potential mechanism-based inhibitors of human leukocyte elastase, cathepsin G and proteinase 3

Bioorganic & Medicinal Chemistry ◽

10.1016/0968-0896(95)00013-7 ◽

1995 ◽

Vol 3 (2) ◽

pp. 187-193 ◽

Cited By ~ 10

Author(s):

William C. Groutas ◽

Lee S. Chong ◽

Radhika Venkataraman ◽

Jeffrey B. Epp ◽

Rongze Kuang ◽

...

Keyword(s):

Systems Design ◽

Human Leukocyte ◽

Biological Evaluation ◽

Cathepsin G ◽

Proteinase 3 ◽

Potential Mechanism ◽

Leukocyte Elastase ◽

Design Synthesis ◽

Human Leukocyte Elastase ◽

Synthesis And Biological Evaluation

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Nonpeptidic Inhibitors of Human Leukocyte Elastase. 3. Design, Synthesis, X-ray Crystallographic Analysis, and Structure-Activity Relationships for a Series of Orally Active 3-Amino-6-phenyl-2-pyridinyl Trifluoromethyl Ketones

Journal of Medicinal Chemistry ◽

10.1021/jm00046a016 ◽

1994 ◽

Vol 37 (20) ◽

pp. 3313-3326 ◽

Cited By ~ 27

Author(s):

Peter R. Bernstein ◽

Don Andisik ◽

Prudence K. Bradley ◽

Craig B. Bryant ◽

Christopher Ceccarelli ◽

...

Keyword(s):

Human Leukocyte ◽

Crystallographic Analysis ◽

Leukocyte Elastase ◽

Design Synthesis ◽

X Ray ◽

Structure Activity Relationships ◽

Trifluoromethyl Ketones ◽

Structure Activity ◽

Human Leukocyte Elastase ◽

Orally Active

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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

Journal of Medicinal Chemistry ◽

10.1021/jm00001a015 ◽

1995 ◽

Vol 38 (1) ◽

pp. 98-108 ◽

Cited By ~ 44

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

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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

Journal of Medicinal Chemistry ◽

10.1021/jm00046a015 ◽

1994 ◽

Vol 37 (20) ◽

pp. 3303-3312 ◽

Cited By ~ 20

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

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

ChemInform ◽

10.1002/chin.200133119 ◽

2010 ◽

Vol 32 (33) ◽

pp. no-no

Author(s):

A. Clemente ◽

A. Domingos ◽

A. P. Grancho ◽

J. Iley ◽

R. Moreira ◽

...

Keyword(s):

Human Leukocyte ◽

Leukocyte Elastase ◽

Design Synthesis ◽

Human Leukocyte Elastase

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Design, synthesis and biological evaluation of succinimide derivatives as potential mechanism-based inhibitors of human leukocyte elastase, cathepsin G and proteinase 3

Bioorganic & Medicinal Chemistry ◽

10.1016/0968-0896(95)00024-b ◽

1995 ◽

Vol 3 (4) ◽

pp. 375-381 ◽

Cited By ~ 14

Author(s):

William C. Groutas ◽

Michael J. Brubaker ◽

Lee S. Chong ◽

Radhika Venkataraman ◽

He Huang ◽

...

Keyword(s):

Human Leukocyte ◽

Biological Evaluation ◽

Cathepsin G ◽

Proteinase 3 ◽

Potential Mechanism ◽

Leukocyte Elastase ◽

Design Synthesis ◽

Human Leukocyte Elastase ◽

Synthesis And Biological Evaluation

Download Full-text