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Utilization of the 1,2,5-thiadiazolidin-3-one 1,1 dioxide scaffold in the design of potent inhibitors of serine proteases: SAR studies using carboxylates

Bioorganic & medicinal chemistry, 2000-05, Vol.8 (5), p.1005-1016

2000

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1,2,5-Thiadiazolidin-3-one 1,1 Dioxide: A Powerful Scaffold for Probing the S′ Subsites of (Chymo)trypsin-Like Serine Proteases

Archives of biochemistry and biophysics, 2001-01, Vol.385 (1), p.162-169

2001

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Efficient inhibition of human leukocyte elastase and cathepsin G by saccharin derivatives

Journal of medicinal chemistry, 1993-10, Vol.36 (21), p.3178-3181

1993

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Structure-Based Design of a General Class of Mechanism-Based Inhibitors of the Serine Proteinases Employing a Novel Amino Acid-Derived Heterocyclic Scaffold

Biochemistry (Easton), 1997-04, Vol.36 (16), p.4739-4750

1997

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Potent and Specific Inhibition of Human Leukocyte Elastase, Cathepsin G and Proteinase 3 by Sulfone Derivatives Employing the 1,2,5-Thiadiazolidin-3-one 1,1 Dioxide Scaffold

Bioorganic & medicinal chemistry, 1998-06, Vol.6 (6), p.661-671

1998

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Facile Preparation of Nucleoside-5‘-carboxylic Acids

Journal of organic chemistry, 1999-01, Vol.64 (1), p.293-295

1999

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Inhibitors of human neutrophil cathepsin G: Structural and biochemical studies

Archives of biochemistry and biophysics, 1992-04, Vol.294 (1), p.144-146

1992

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Mechanism-Based Inhibitors of Serine Proteinases Based on the Gabriel-Colman Rearrangement

Biochemical and biophysical research communications, 1993-08, Vol.194 (3), p.1491-1499

1993

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Exploiting Polymerase Promiscuity: A Simple Colorimetric RNA Polymerase Assay

Virology (New York, N.Y.), 2000-09, Vol.274 (2), p.429-437

2000

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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, 1996-09, Vol.4 (9), p.1393-1400

1996

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Isoxazoline derivatives as potential inhibitors of the proteolytic enzymes human leukocyte elastase, cathepsin G and proteinase 3: a structure-activity relationship study

Bioorganic & medicinal chemistry, 1995-02, Vol.3 (2), p.125-128

1995

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Amino Acid-Derived Phthalimide and Saccharin Derivatives as Inhibitors of Human Leukocyte Elastase, Cathepsin G, and Proteinase 3

Archives of biochemistry and biophysics, 1996-08, Vol.332 (2), p.335-340

1996

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Derivatives of 3-alkyl-N-hydroxysuccinimide: probing the effect of structure on bioactivity toward human leukocyte elastase

Drug design and discovery, 1994-02, Vol.11 (2), p.149

1994

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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, 1995-04, Vol.3 (4), p.375-381

1995

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3-(alkylthio)-N-hydroxysuccinimide derivatives : potent inhibitors of human leukocyte elastase

Biochimica et biophysica acta, 1993-08, Vol.1164 (3), p.283-288

1993

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Mechanism-based inhibition of human leukocyte elastase and cathepsin G by substituted dihydrouracils

Biochimica et biophysica acta, 1994-11, Vol.1227 (3), p.130

1994

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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, 1995-02, Vol.3 (2), p.187-193

1995

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A general approach toward the design of mechanism-based inactivators of serine proteinases: inactivation of human leukocyte elastase by a phthalimide derivative

Bioorganic & medicinal chemistry letters, 1993-12, Vol.3 (12), p.2745-2750

1993

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A General Inhibitor Scaffold for Serine Proteases with a (Chymo)trypsin-Like Fold: Solution-Phase Construction and Evaluation of the First Series of Libraries of Mechanism-Based Inhibitors

Journal of the American Chemical Society, 1999-09, Vol.121 (35), p.8128-8129

1999

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Mechanism-based inactivation of human leukocyte elastase via an enzyme-induced sulfonamide fragmentation process

Archives of biochemistry and biophysics, 2004-09, Vol.429 (1), p.60-70

2004

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Dual-action inhibitors of proteolytic enzymes: potential therapeutic agents for cystic fibrosis and related ailments

Bioorganic & medicinal chemistry, 1993-10, Vol.1 (4), p.273-277

1993

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A ONE-STEP PROTOCOL FOR THE N-CHLOROMETHYLATION OF HETEROCYCLIC IMIDES

Synthetic communications, 2001-01, Vol.31 (20), p.3055-3058

2001

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A general approach toward the design of inhibitors of serine proteinases: inhibition of human leukocyte elastase by substituted dihydrouracils

Bioorganic & medicinal chemistry letters, 1992-12, Vol.2 (12), p.1565-1570

1992

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Potential mechanism-based inhibitors of proteolytic enzymes

Bioorganic & medicinal chemistry letters, 1992, Vol.2 (2), p.175-180

1992

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Inhibition of human leukocyte elastase and cathepsin G by isoxazoline derivatives

Bioorganic & medicinal chemistry letters, 1992-12, Vol.2 (12), p.1571-1574

1992

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Utilization of the 1,2,5-thiadiazolidin-3-one 1,1 dioxide scaffold in the design of potent inhibitors of serine proteases: SAR studies using carboxylates

1,2,5-Thiadiazolidin-3-one 1,1 Dioxide: A Powerful Scaffold for Probing the S′ Subsites of (Chymo)trypsin-Like Serine Proteases

Efficient inhibition of human leukocyte elastase and cathepsin G by saccharin derivatives

Structure-Based Design of a General Class of Mechanism-Based Inhibitors of the Serine Proteinases Employing a Novel Amino Acid-Derived Heterocyclic Scaffold

Potent and Specific Inhibition of Human Leukocyte Elastase, Cathepsin G and Proteinase 3 by Sulfone Derivatives Employing the 1,2,5-Thiadiazolidin-3-one 1,1 Dioxide Scaffold

Facile Preparation of Nucleoside-5‘-carboxylic Acids

Inhibitors of human neutrophil cathepsin G: Structural and biochemical studies

Mechanism-Based Inhibitors of Serine Proteinases Based on the Gabriel-Colman Rearrangement

Exploiting Polymerase Promiscuity: A Simple Colorimetric RNA Polymerase Assay

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

Isoxazoline derivatives as potential inhibitors of the proteolytic enzymes human leukocyte elastase, cathepsin G and proteinase 3: a structure-activity relationship study

Amino Acid-Derived Phthalimide and Saccharin Derivatives as Inhibitors of Human Leukocyte Elastase, Cathepsin G, and Proteinase 3

Derivatives of 3-alkyl-N-hydroxysuccinimide: probing the effect of structure on bioactivity toward human leukocyte elastase

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

3-(alkylthio)-N-hydroxysuccinimide derivatives : potent inhibitors of human leukocyte elastase

Mechanism-based inhibition of human leukocyte elastase and cathepsin G by substituted dihydrouracils

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

A general approach toward the design of mechanism-based inactivators of serine proteinases: inactivation of human leukocyte elastase by a phthalimide derivative

A General Inhibitor Scaffold for Serine Proteases with a (Chymo)trypsin-Like Fold: Solution-Phase Construction and Evaluation of the First Series of Libraries of Mechanism-Based Inhibitors

Mechanism-based inactivation of human leukocyte elastase via an enzyme-induced sulfonamide fragmentation process

Dual-action inhibitors of proteolytic enzymes: potential therapeutic agents for cystic fibrosis and related ailments

A ONE-STEP PROTOCOL FOR THE N-CHLOROMETHYLATION OF HETEROCYCLIC IMIDES

A general approach toward the design of inhibitors of serine proteinases: inhibition of human leukocyte elastase by substituted dihydrouracils

Potential mechanism-based inhibitors of proteolytic enzymes

Inhibition of human leukocyte elastase and cathepsin G by isoxazoline derivatives

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