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Optimizing a Weakly Binding Fragment into a Potent RORγt Inverse Agonist with Efficacy in an in Vivo Inflammation Model

Journal of medicinal chemistry, 2018-08, Vol.61 (15), p.6724-6735

2018

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Synthesis and Biological Evaluation of New Triazolo- and Imidazolopyridine RORγt Inverse Agonists

ChemMedChem, 2016-12, Vol.11 (24), p.2640-2648

2016

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Total Synthesis of (±)-Jiadifenin and Studies Directed to Understanding Its SAR: Probing Mechanistic and Stereochemical Issues in Palladium-Mediated Allylation of Enolate-Like Structures

Journal of the American Chemical Society, 2006-01, Vol.128 (3), p.1016-1022

2006

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Discovery of 1H-pyrrolo[2,3-c]pyridine-7-carboxamides as novel, allosteric mGluR5 antagonists

Bioorganic & medicinal chemistry letters, 2012-10, Vol.22 (20), p.6454-6459

2012

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Quinazolinedione sulfonamides: A novel class of competitive AMPA receptor antagonists with oral activity

Bioorganic & medicinal chemistry letters, 2011-06, Vol.21 (11), p.3358-3361

2011

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Design and Synthesis of Selurampanel, a Novel Orally Active and Competitive AMPA Receptor Antagonist

ChemMedChem, 2017-02, Vol.12 (3), p.197-201

2017

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6-Amino quinazolinedione sulfonamides as orally active competitive AMPA receptor antagonists

Bioorganic & medicinal chemistry letters, 2012-01, Vol.22 (2), p.996-999

2012

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Total Synthesis of (±)-Jiadifenin, a Non-peptidyl Neurotrophic Modulator

Journal of the American Chemical Society, 2004-11, Vol.126 (44), p.14358-14359

2004

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The Synthesis and Preliminary Biological Evaluation of a Novel Steroid with Neurotrophic Activity: NGA0187

Journal of organic chemistry, 2005-11, Vol.70 (24), p.9849-9856

2005

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De Novo Design, Synthesis, and In Vitro Evaluation of a New Class of Nonpeptidic Inhibitors of the Malarial Enzyme Plasmepsin II

Chembiochem : a European journal of chemical biology, 2002-11, Vol.3 (11), p.1137-1141

2002

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Development of a New Class of Inhibitors for the Malarial Aspartic Protease Plasmepsin II Based on a Central 7-Azabicyclo[2.2.1]heptane Scaffold

Helvetica chimica acta, 2003-06, Vol.86 (6), p.2173-2191

2003

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Radical Couplings as Key Steps for the Preparation of Derivatives of Nonactic Acid

Monatshefte für Chemie, 2007-02, Vol.138 (2), p.121-129

2007

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A New Class of Inhibitors for the Malarial Aspartic Protease Plasmepsin II Based on a Central 11-Azatricyclo[6.2.1.02,7]undeca-2,4,6-triene Scaffold

Helvetica chimica acta, 2003-06, Vol.86 (6), p.2192-2209

2003

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Compound Property Optimization in Drug Discovery Using Quantitative Surface Sampling Micro Liquid Chromatography with Tandem Mass Spectrometry

Analytical chemistry (Washington), 2016-12, Vol.88 (23), p.11813-11820

2016

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α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Antagonists: From Bench to Bedside

Journal of medicinal chemistry, 2010-08, Vol.53 (15), p.5367-5382

2010

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Metabolism and disposition of the metabotropic glutamate receptor 5 antagonist (mGluR5) mavoglurant (AFQ056) in healthy subjects

Drug metabolism and disposition, 2013-09, Vol.41 (9), p.1626-1641

2013

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Cover Picture: Design and Synthesis of Selurampanel, a Novel Orally Active and Competitive AMPA Receptor Antagonist (ChemMedChem 3/2017)

ChemMedChem, 2017-02, Vol.12 (3), p.196-196

2017

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Synthesis and Biological Evaluation of New Triazolo- and Imidazolopyridine ROR[gamma]t Inverse Agonists

ChemMedChem, 2016-12, Vol.11 (24), p.2640-2648

2016

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Discovery of 1H-pyrrolo[2,3-c]pyridine-7-carboxamides as novel, allosteric mGluRS antagonists

Bioorganic & medicinal chemistry letters, 2012, Vol.22 (20), p.6454-6459

2012

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Benzimidazoles as Potent and Orally Active mGlu5 Receptor Antagonists with an Improved PK Profile

ACS medicinal chemistry letters, 2011-01, Vol.2 (1), p.58-62

2011

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Malonylation/Decarbalkoxylation of Furan Derivatives as Key Steps for the Preparation of Nonactic Acid Derivatives. Part I [1]

Monatshefte für Chemie, 2007-02, Vol.138 (2), p.131-139

2007

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Malonylation/Decarbalkoxylation of Furan Derivatives as Key Steps for the Preparation of Nonactic Acid Derivatives. Part II [1]

Monatshefte für Chemie, 2007-02, Vol.138 (2), p.141-147

2007

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De novo design, synthesis and in vitro evaluation of new non-peptidic inhibitors of the malarial enzymeplasmepsin II

Carcache, David A

2002

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The Synthesis and Preliminary Biological Evaluation of a Novel Steroid with Neurotrophic Activity: NGA0187

ChemInform, 2006-04, Vol.37 (15), p.no-no

2006

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Total Synthesis of (.+-.)-Jiadifenin and Studies Directed to Understanding Its SAR: Probing Mechanistic and Stereochemical Issues in Palladium-Mediated Allylation of Enolate-Like Structures

ChemInform, 2006-06, Vol.37 (24), p.no-no

2006

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Optimizing a Weakly Binding Fragment into a Potent RORγt Inverse Agonist with Efficacy in an in Vivo Inflammation Model

Synthesis and Biological Evaluation of New Triazolo- and Imidazolopyridine RORγt Inverse Agonists

Total Synthesis of (±)-Jiadifenin and Studies Directed to Understanding Its SAR: Probing Mechanistic and Stereochemical Issues in Palladium-Mediated Allylation of Enolate-Like Structures

Discovery of 1H-pyrrolo[2,3-c]pyridine-7-carboxamides as novel, allosteric mGluR5 antagonists

Quinazolinedione sulfonamides: A novel class of competitive AMPA receptor antagonists with oral activity

Design and Synthesis of Selurampanel, a Novel Orally Active and Competitive AMPA Receptor Antagonist

6-Amino quinazolinedione sulfonamides as orally active competitive AMPA receptor antagonists

Total Synthesis of (±)-Jiadifenin, a Non-peptidyl Neurotrophic Modulator

The Synthesis and Preliminary Biological Evaluation of a Novel Steroid with Neurotrophic Activity: NGA0187

De Novo Design, Synthesis, and In Vitro Evaluation of a New Class of Nonpeptidic Inhibitors of the Malarial Enzyme Plasmepsin II

Development of a New Class of Inhibitors for the Malarial Aspartic Protease Plasmepsin II Based on a Central 7-Azabicyclo[2.2.1]heptane Scaffold

Radical Couplings as Key Steps for the Preparation of Derivatives of Nonactic Acid

A New Class of Inhibitors for the Malarial Aspartic Protease Plasmepsin II Based on a Central 11-Azatricyclo[6.2.1.02,7]undeca-2,4,6-triene Scaffold

Compound Property Optimization in Drug Discovery Using Quantitative Surface Sampling Micro Liquid Chromatography with Tandem Mass Spectrometry

α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Antagonists: From Bench to Bedside

Metabolism and disposition of the metabotropic glutamate receptor 5 antagonist (mGluR5) mavoglurant (AFQ056) in healthy subjects

Cover Picture: Design and Synthesis of Selurampanel, a Novel Orally Active and Competitive AMPA Receptor Antagonist (ChemMedChem 3/2017)

Synthesis and Biological Evaluation of New Triazolo- and Imidazolopyridine ROR[gamma]t Inverse Agonists

Discovery of 1H-pyrrolo[2,3-c]pyridine-7-carboxamides as novel, allosteric mGluRS antagonists

Benzimidazoles as Potent and Orally Active mGlu5 Receptor Antagonists with an Improved PK Profile

Malonylation/Decarbalkoxylation of Furan Derivatives as Key Steps for the Preparation of Nonactic Acid Derivatives. Part I [1]

Malonylation/Decarbalkoxylation of Furan Derivatives as Key Steps for the Preparation of Nonactic Acid Derivatives. Part II [1]

De novo design, synthesis and in vitro evaluation of new non-peptidic inhibitors of the malarial enzymeplasmepsin II

The Synthesis and Preliminary Biological Evaluation of a Novel Steroid with Neurotrophic Activity: NGA0187

Total Synthesis of (.+-.)-Jiadifenin and Studies Directed to Understanding Its SAR: Probing Mechanistic and Stereochemical Issues in Palladium-Mediated Allylation of Enolate-Like Structures

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