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Discovery of a Novel Class of Orally Active Antifungal β-1,3-d-Glucan Synthase Inhibitors

Antimicrobial Agents and Chemotherapy, 2011-11, Vol.55 (11), p.5099-5106

2011

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Discovery of oxazole-based PDE4 inhibitors with picomolar potency

Bioorganic & medicinal chemistry letters, 2012-04, Vol.22 (7), p.2594-2597

2012

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SAR studies of pyridazinone derivatives as novel glucan synthase inhibitors

Bioorganic & medicinal chemistry letters, 2011-05, Vol.21 (10), p.2890-2893

2011

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The synthesis and structure–activity relationship of pyridazinones as glucan synthase inhibitors

Bioorganic & medicinal chemistry letters, 2011-03, Vol.21 (6), p.1819-1822

2011

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Lead optimization of a sulfonylurea-based piperazine pyridazinone series of glucan synthase inhibitors

Bioorganic & medicinal chemistry letters, 2012-07, Vol.22 (14), p.4896-4899

2012

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The optimization of pyridazinone series of glucan synthase inhibitors

Bioorganic & medicinal chemistry letters, 2012-08, Vol.22 (16), p.5268-5271

2012

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Effects of structure on inhibitory activity in a series of mechanism-based inhibitors of human neutrophil elastase

Bioorganic & medicinal chemistry, 2010-09, Vol.18 (18), p.6646-6650

2010

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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 inhibition of serine proteases by heterocyclic sulfide derivatives of 1,2,5-thiadiazolidin-3-one 1,1 dioxide

Bioorganic & medicinal chemistry, 2000-07, Vol.8 (7), p.1713-1717

2000

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Inhibition of serine proteases by functionalized sulfonamides coupled to the 1,2,5-thiadiazolidin-3-one 1,1 dioxide scaffold

Bioorganic & medicinal chemistry, 2001-06, Vol.9 (6), p.1543-1548

2001

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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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Discovery of aminoquinazoline derivatives as human A(2A) adenosine receptor antagonists

Bioorganic & medicinal chemistry letters, 2016-02, Vol.26 (4), p.1348-1354

2016

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Discovery of aminoquinazoline derivatives as human A2A adenosine receptor antagonists

Bioorganic & medicinal chemistry letters, 2016-02, Vol.26 (4), p.1348-1354

2016

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Inhibition of Escherichia coli by dimethyl fumarate

International journal of food microbiology, 2001-04, Vol.65 (1), p.125-130

2001

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Use of the 1,2,5-thiadiazolidin-3-one 1,1 dioxide and isothiazolidin-3-one 1,1 dioxide scaffolds in the design of potent inhibitors of serine proteinases

Bioorganic & medicinal chemistry letters, 1998-03, Vol.8 (5), p.539-544

1998

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Discovery of aminoquinazoline derivatives as human A sub(2A) adenosine receptor antagonists

Bioorganic & medicinal chemistry letters, 2016-02, Vol.26 (4), p.1348-1354

2016

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Discovery of oral and inhaled PDE4 inhibitors

Bioorganic & medicinal chemistry letters, 2013-10, Vol.23 (20), p.5528-5532

2013

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Substituted 3-oxo-1,2,5-Thiadiazolidine 1,1-Dioxides: A New Class of Potential Mechanism-Based Inhibitors of Human Leukocyte Elastase and Cathepsin G

Biochemical and biophysical research communications, 1994-01, Vol.198 (1), p.341-349

1994

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Discovery of a highly potent series of oxazole-based phosphodiesterase 4 inhibitors

Bioorganic & medicinal chemistry letters, 2007-09, Vol.17 (18), p.5150-5154

2007

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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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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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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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Enantioselective syntheses of carbocyclic ribavirin and its analogs: linear versus convergent approaches

Tetrahedron letters, 2000, Vol.41 (49), p.9575-9579

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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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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Discovery of a Novel Class of Orally Active Antifungal β-1,3-d-Glucan Synthase Inhibitors

Discovery of oxazole-based PDE4 inhibitors with picomolar potency

SAR studies of pyridazinone derivatives as novel glucan synthase inhibitors

The synthesis and structure–activity relationship of pyridazinones as glucan synthase inhibitors

Lead optimization of a sulfonylurea-based piperazine pyridazinone series of glucan synthase inhibitors

The optimization of pyridazinone series of glucan synthase inhibitors

Effects of structure on inhibitory activity in a series of mechanism-based inhibitors of human neutrophil elastase

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

Potent inhibition of serine proteases by heterocyclic sulfide derivatives of 1,2,5-thiadiazolidin-3-one 1,1 dioxide

Inhibition of serine proteases by functionalized sulfonamides coupled to the 1,2,5-thiadiazolidin-3-one 1,1 dioxide scaffold

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

Discovery of aminoquinazoline derivatives as human A(2A) adenosine receptor antagonists

Discovery of aminoquinazoline derivatives as human A2A adenosine receptor antagonists

Inhibition of Escherichia coli by dimethyl fumarate

Use of the 1,2,5-thiadiazolidin-3-one 1,1 dioxide and isothiazolidin-3-one 1,1 dioxide scaffolds in the design of potent inhibitors of serine proteinases

Discovery of aminoquinazoline derivatives as human A sub(2A) adenosine receptor antagonists

Discovery of oral and inhaled PDE4 inhibitors

Substituted 3-oxo-1,2,5-Thiadiazolidine 1,1-Dioxides: A New Class of Potential Mechanism-Based Inhibitors of Human Leukocyte Elastase and Cathepsin G

Discovery of a highly potent series of oxazole-based phosphodiesterase 4 inhibitors

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

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

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

Enantioselective syntheses of carbocyclic ribavirin and its analogs: linear versus convergent approaches

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

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

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