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Structural Modifications that Alter the P-Glycoprotein Efflux Properties of Compounds

Journal of medicinal chemistry, 2012-06, Vol.55 (11), p.4877-4895

Hitchcock, Stephen A

2012

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Blood–brain barrier permeability considerations for CNS-targeted compound library design

Current opinion in chemical biology, 2008-06, Vol.12 (3), p.318-323

Hitchcock, Stephen A

2008

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From Fragment Screening to In Vivo Efficacy: Optimization of a Series of 2-Aminoquinolines as Potent Inhibitors of Beta-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1)

Journal of medicinal chemistry, 2011-08, Vol.54 (16), p.5836-5857

2011

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Enhanced histamine H2 excitation of striatal cholinergic interneurons in l -DOPA-induced dyskinesia

Neurobiology of disease, 2015-04, Vol.76, p.67-76

2015

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Structure−Brain Exposure Relationships

Journal of medicinal chemistry, 2006-12, Vol.49 (26), p.7559-7583

2006

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Rapid Identification of a Novel Small Molecule Phosphodiesterase 10A (PDE10A) Tracer

Journal of medicinal chemistry, 2012-05, Vol.55 (10), p.4776-4787

2012

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Discovery and Optimization of a Novel Series of N-Arylamide Oxadiazoles as Potent, Highly Selective and Orally Bioavailable Cannabinoid Receptor 2 (CB2) Agonists

Journal of medicinal chemistry, 2008-08, Vol.51 (16), p.5019-5034

2008

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Targeting cannabinoid agonists for inflammatory and neuropathic pain

Expert opinion on investigational drugs, 2007-07, Vol.16 (7), p.951-965

2007

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Design and Preparation of a Potent Series of Hydroxyethylamine Containing β-Secretase Inhibitors That Demonstrate Robust Reduction of Central β-Amyloid

Journal of medicinal chemistry, 2012-11, Vol.55 (21), p.9009-9024

2012

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Nonspecificity of Binding of γ-Secretase Modulators to the Amyloid Precursor Protein

Biochemistry (Easton), 2009-12, Vol.48 (50), p.11837-11839

2009

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Design and Synthesis of Potent, Orally Efficacious Hydroxyethylamine Derived β-Site Amyloid Precursor Protein Cleaving Enzyme (BACE1) Inhibitors

Journal of medicinal chemistry, 2012-11, Vol.55 (21), p.9025-9044

2012

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Use of structure based design to increase selectivity of pyridyl-cinnoline phosphodiesterase 10A (PDE10A) inhibitors against phosphodiesterase 3 (PDE3)

Bioorganic & medicinal chemistry letters, 2012-11, Vol.22 (22), p.6938-6942

2012

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Hydroxyethylamine-based inhibitors of BACE1: P1–P3 macrocyclization can improve potency, selectivity, and cell activity

Bioorganic & medicinal chemistry letters, 2013-08, Vol.23 (15), p.4459-4464

2013

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An Orally Available BACE1 Inhibitor That Affords Robust CNS Aβ Reduction without Cardiovascular Liabilities

ACS medicinal chemistry letters, 2015-02, Vol.6 (2), p.210-215

2015

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Establishing the relationship between in vitro potency, pharmacokinetic, and pharmacodynamic parameters in a series of orally available, hydroxyethylamine-derived β-secretase inhibitors

The Journal of pharmacology and experimental therapeutics, 2012-11, Vol.343 (2), p.460-467

2012

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Design and synthesis of N-[6-(Substituted Aminoethylideneamino)-2-Hydroxyindan-1-yl]arylamides as selective and potent muscarinic M1 agonists

Bioorganic & medicinal chemistry letters, 2015-10, Vol.25 (19), p.4158-4163

2015

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The First Total Synthesis of Bacterial Cell Wall Precursor UDP−N-Acetylmuramyl-Pentapeptide (Park Nucleotide)

Journal of the American Chemical Society, 1998-03, Vol.120 (8), p.1916-1917

1998

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Structure guided P1′ modifications of HEA derived β-secretase inhibitors for the treatment of Alzheimer’s disease

Bioorganic & medicinal chemistry letters, 2012-06, Vol.22 (11), p.3607-3611

2012

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Structural modifications of N-arylamide oxadiazoles : Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB2

Bioorganic & medicinal chemistry letters, 2008-08, Vol.18 (15), p.4267-4274

2008

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Discovery of α-amidosulfones as potent and selective agonists of CB2 : Synthesis, SAR, and pharmacokinetic properties

Bioorganic & medicinal chemistry letters, 2009, Vol.19 (1), p.31-35

2009

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Radiolabeling of a high potency cannabinoid subtype-1 receptor ligand, N-(4-fluoro-benzyl)-4-(3-(piperidin-1-yl)-indole-1-sulfonyl)benzamide (PipISB), with carbon-11 or fluorine-18

Journal of labelled compounds & radiopharmaceuticals, 2008-03, Vol.51 (3), p.146-152

2008

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A tandem radical macrocyclisation - radical transannulation strategy to the taxane ring system

Tetrahedron letters, 1992-08, Vol.33 (33), p.4843-4846

1992

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A Remarkable Glycosidation Reaction: The Total Synthesis of Calicheamicin .gamma.1I

Journal of the American Chemical Society, 1995-05, Vol.117 (21), p.5750-5756

1995

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Synthesis and conformational analysis of α,α-difluoroalkyl heteroaryl ethers

Tetrahedron letters, 2009-09, Vol.50 (39), p.5452-5455

2009

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Structural Modifications that Alter the P-Glycoprotein Efflux Properties of Compounds

Blood–brain barrier permeability considerations for CNS-targeted compound library design

From Fragment Screening to In Vivo Efficacy: Optimization of a Series of 2-Aminoquinolines as Potent Inhibitors of Beta-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1)

Enhanced histamine H2 excitation of striatal cholinergic interneurons in l -DOPA-induced dyskinesia

Structure−Brain Exposure Relationships

Rapid Identification of a Novel Small Molecule Phosphodiesterase 10A (PDE10A) Tracer

Discovery and Optimization of a Novel Series of N-Arylamide Oxadiazoles as Potent, Highly Selective and Orally Bioavailable Cannabinoid Receptor 2 (CB2) Agonists

Targeting cannabinoid agonists for inflammatory and neuropathic pain

Design and Preparation of a Potent Series of Hydroxyethylamine Containing β-Secretase Inhibitors That Demonstrate Robust Reduction of Central β-Amyloid

Nonspecificity of Binding of γ-Secretase Modulators to the Amyloid Precursor Protein

Development of 2-aminooxazoline 3-azaxanthenes as orally efficacious β-secretase inhibitors for the potential treatment of Alzheimer’s disease

Design and Synthesis of Potent, Orally Efficacious Hydroxyethylamine Derived β-Site Amyloid Precursor Protein Cleaving Enzyme (BACE1) Inhibitors

Use of structure based design to increase selectivity of pyridyl-cinnoline phosphodiesterase 10A (PDE10A) inhibitors against phosphodiesterase 3 (PDE3)

Hydroxyethylamine-based inhibitors of BACE1: P1–P3 macrocyclization can improve potency, selectivity, and cell activity

An Orally Available BACE1 Inhibitor That Affords Robust CNS Aβ Reduction without Cardiovascular Liabilities

Establishing the relationship between in vitro potency, pharmacokinetic, and pharmacodynamic parameters in a series of orally available, hydroxyethylamine-derived β-secretase inhibitors

Design and synthesis of N-[6-(Substituted Aminoethylideneamino)-2-Hydroxyindan-1-yl]arylamides as selective and potent muscarinic M1 agonists

The First Total Synthesis of Bacterial Cell Wall Precursor UDP−N-Acetylmuramyl-Pentapeptide (Park Nucleotide)

Structure guided P1′ modifications of HEA derived β-secretase inhibitors for the treatment of Alzheimer’s disease

Structural modifications of N-arylamide oxadiazoles : Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB2

Discovery of α-amidosulfones as potent and selective agonists of CB2 : Synthesis, SAR, and pharmacokinetic properties

Radiolabeling of a high potency cannabinoid subtype-1 receptor ligand, N-(4-fluoro-benzyl)-4-(3-(piperidin-1-yl)-indole-1-sulfonyl)benzamide (PipISB), with carbon-11 or fluorine-18

A tandem radical macrocyclisation - radical transannulation strategy to the taxane ring system

A Remarkable Glycosidation Reaction: The Total Synthesis of Calicheamicin .gamma.1I

Synthesis and conformational analysis of α,α-difluoroalkyl heteroaryl ethers

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