Christopher J. Helal

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Stereoselective synthesis of spiropiperidines as BACE-1 aspartyl protease inhibitors via late stage N-arylation of a 1,8-diazaspiro[4.5]dec-3-en-2-one pharmacophore.

S. Sakya, Kevin Ogilvie, Jason K. Dutra, 2013, The Journal of organic chemistry.

A platform for automated nanomole-scale reaction screening and micromole-scale synthesis in flow

Paul Richardson, Christopher J Helal, William Farrell, 2018, Science.

Reduction of Carbonyl Compounds with Chiral Oxazaborolidine Catalysts: A New Paradigm for Enantioselective Catalysis and a Powerful New Synthetic Method.

E. Corey, Christopher J. Helal, 1998, Angewandte Chemie.

Late-Stage Microsomal Oxidation Reduces Drug–Drug Interaction and Identifies Phosphodiesterase 2A Inhibitor PF-06815189

Michael De Vivo, Stephen Jenkinson, R. Scott Obach, 2018, ACS medicinal chemistry letters.

Novel electronic effects of remote substituents on the oxazaborolidine-catalyzed enantioselective reduction of ketones

E. Corey, Christopher J. Helal, 1995 .

Potent and cellularly active 4-aminoimidazole inhibitors of cyclin-dependent kinase 5/p25 for the treatment of Alzheimer's disease.

J. Pandit, F. Menniti, M. Ahlijanian, 2009, Bioorganic & medicinal chemistry letters.

Ru/Ni Dual Catalytic Desulfinative Photoredox Csp2-Csp3 Cross-Coupling of Alkyl Sulfinate Salts and Aryl Halides.

N. Sach, R. Chandrasekaran, J. Chen, 2017, Organic letters.

Discovery of the Potent and Selective M1 PAM-Agonist N-[(3R,4S)-3-Hydroxytetrahydro-2H-pyran-4-yl]-5-methyl-4-[4-(1,3-thiazol-4-yl)benzyl]pyridine-2-carboxamide (PF-06767832): Evaluation of Efficacy and Cholinergic Side Effects.

Gregory W. Kauffman, J. Edgerton, S. Steyn, 2016, Journal of medicinal chemistry.

Design and selection parameters to accelerate the discovery of novel central nervous system positron emission tomography (PET) ligands and their application in the development of a novel phosphodiesterase 2A PET ligand.

L. Chen, K. Zasadny, P. Verhoest, 2013, Journal of medicinal chemistry.

Asymmetric synthesis of (S)-carbinoxamine. New aspects of oxazaborolidine-catalyzed enantioselective carbonyl reduction

E. Corey, Christopher J. Helal, E. J. Corey, 1996 .

Discovery of cyclopropyl chromane-derived pyridopyrazine-1,6-dione γ-secretase modulators with robust central efficacy.

Gregory W. Kauffman, David S. Ramirez, L. Pustilnik, 2017, MedChemComm.

Discovery of Trifluoromethyl Glycol Carbamates as Potent and Selective Covalent Monoacylglycerol Lipase (MAGL) Inhibitors for Treatment of Neuroinflammation.

Timothy L. Foley, J. Pandit, J. Cianfrogna, 2018, Journal of medicinal chemistry.

Discovery and Lead Optimization of Atropisomer D1 Agonists with Reduced Desensitization.

R. Kozak, David L. Gray, B. Rai, 2018, Journal of medicinal chemistry.

A concise and regioselective synthesis of 1-alkyl-4-imidazolecarboxylates.

Christopher J. Helal, John C. Lucas, 2002, Organic letters.

Direct Catalytic Enantioselective Reduction of Achiral α,β-Ynones. Strong Remote Steric Effects Across the C−C Triple Bond

E. Corey, Christopher J. Helal, P. A. Magriotis, 1996 .

The Corey–Bakshi–Shibata Reduction: Mechanistic and Synthetic Considerations – Bifunctional Lewis Base Catalysis with Dual Activation

M. P. Meyer, Christopher J. Helal, 2016 .

Use of structure-based design to discover a potent, selective, in vivo active phosphodiesterase 10A inhibitor lead series for the treatment of schizophrenia.

K. Fennell, J. Pandit, F. Menniti, 2011, Journal of medicinal chemistry.

Introduction of a Crystalline, Shelf-Stable Reagent for the Synthesis of Sulfur(VI) Fluorides.

Jeffrey B. Sperry, Hua Zhou, L. R. Hoth, 2018, Organic letters.

Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disorders.

F. Menniti, F. Nelson, C. Proulx-Lafrance, 2012, Journal of medicinal chemistry.

Parallel Synthesis of 1H-Pyrazolo[3,4-d]pyrimidines via Condensation of N-Pyrazolylamides and Nitriles.

Christopher J. Helal, Akshay A Shah, L. Chenard, 2017, ACS combinatorial science.

Catalytic enantioselective synthesis of the second generation histamine antagonist cetirizine hydrochloride

E. Corey, Christopher J. Helal, 1996 .

Reduction of Carbonyl Compounds with Chiral Oxazaborolidine Catalysts: A New Paradigm for Enantioselective Catalysis and a Powerful New Synthetic Method

E. Corey, Christopher J. Helal, 1998 .

Discovery and SAR of 2-aminothiazole inhibitors of cyclin-dependent kinase 5/p25 as a potential treatment for Alzheimer's disease.

Christopher B. Cooper, F. Menniti, M. Ahlijanian, 2004, Bioorganic & medicinal chemistry letters.

A catalytic enantioselective synthesis of chiral monosubstituted oxiranes

E. Corey, Christopher J. Helal, 1993 .

High-Throughput Ligand Screening Enables the Enantioselective Conjugate Borylation of Cyclobutenones to Access Synthetically Versatile Tertiary Cyclobutylboronates.

Rory M. McDonald, N. Sach, D. Hall, 2019, Angewandte Chemie.

Synthetic Approaches to the New Drugs Approved During 2018.

C. J. O’Donnell, C. Leverett, Hong X. Ding, 2020, Journal of medicinal chemistry.

High‐Throughput Ligand Screening Enables the Enantioselective Conjugate Borylation of Cyclobutenones to Access Synthetically Versatile Tertiary Cyclobutylboronates

N. Sach, D. Hall, W. Farrell, 2019, Angewandte Chemie.

An Efficient Catalytic Stereoselective Route to a Key Intermediate for the Synthesis of the Long-Lived PGI2 Analog ZK 96480 (CicaprostTM)

E. Corey, Christopher J. Helal, 1997 .

Direct Catalytic Enantioselective Reduction of Achiral α,β- Ynones. Strong Remote Steric Effects Across the C-C Triple Bond.

E. Corey, Christopher J. Helal, P. A. Magriotis, 1997 .

Synthetic Approaches to the New Drugs Approved During 2017.

Emma McInturff, Carolyn A Leverett, Christopher J Helal, 2019, Journal of medicinal chemistry.

Glycogen Synthase Kinase-3 (GSK-3): A Kinase with Exceptional Therapeutic Potential

Travis T Wager, D. Kung, Christopher J. Helal, 2005 .

Selective Mechanism-Based Inactivation of CYP3A4 by CYP3cide (PF-04981517) and Its Utility as an In Vitro Tool for Delineating the Relative Roles of CYP3A4 versus CYP3A5 in the Metabolism of Drugs

G. S. Walker, R. Obach, R. Walsky, 2012, Drug Metabolism and Disposition.

Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor.

Laura McDowell, Scot Mente, Mihaly Hajos, 2017, Journal of medicinal chemistry.

Phosphodiesterase 9A Regulates Central cGMP and Modulates Responses to Cholinergic and Monoaminergic Perturbation In Vivo

Anne W. Schmidt, F. Menniti, M. Hajós, 2012, Journal of Pharmacology and Experimental Therapeutics.

Preclinical Evaluation of 18F-PF-05270430, a Novel PET Radioligand for the Phosphodiesterase 2A Enzyme

Yiyun Huang, R. Carson, J. Ropchan, 2016, The Journal of Nuclear Medicine.

Preclinical Evaluation of 18 FPF-05270430 , a Novel PET Radioligand for the Phosphodiesterase 2 A Enzyme

Yiyun Huang, R. Carson, J. Ropchan, 2016 .

Quick Building Blocks (QBB): An Innovative and Efficient Business Model To Speed Medicinal Chemistry Analog Synthesis.

Jacquelyn Klug-McLeod, Christopher J Helal, Chakrapani Subramanyam, 2019, ACS medicinal chemistry letters.

Photoaffinity Labeling and Quantitative Chemical Proteomics Identify LXRβ as the Functional Target of Enhancers of Astrocytic apoE.

P. Verhoest, C. Steppan, Travis T Wager, 2020, Cell chemical biology.

Selective Brain Penetrant PDE 9 A Inhibitor for the Treatment of Cognitive Disorders

Ey, F. Menniti, F. Nelson, 2012 .

A facile synthesis of 2,3-azaisoindoline

S. Sakya, C. J. O’Donnell, Kees Pouwer, 2010 .

Discovery of a series of efficient, centrally efficacious BACE1 inhibitors through structure-based drug design.

K. Parris, K. Atchison, D. Riddell, 2015, Journal of medicinal chemistry.

Identification of a Potent, Highly Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor Clinical Candidate.

J. Pandit, W. Hoffman, M. Hajós, 2018, Journal of medicinal chemistry.

Catalytic Enantioselective Synthesis of a cis-β-Boronyl Cyclobutylcarboxyester Scaffold and Its Highly Diastereoselective Nickel/Photoredox Dual-Catalyzed Csp3–Csp2 Cross-Coupling to Access Elusive trans-β-Aryl/Heteroaryl Cyclobutylcarboxyesters

N. Sach, D. Hall, W. Farrell, 2020, ACS Catalysis.

Correction to “Catalytic Enantioselective Synthesis of a cis-β-Boronyl Cyclobutylcarboxyester Scaffold and Its Highly Diastereoselective Nickel/Photoredox Dual-Catalyzed Csp3–Csp2 Cross-Coupling to Access Elusive trans-β-Aryl/Heteroaryl Cyclobutylcarboxyesters”

N. Sach, D. Hall, M. Reese, 2021, ACS Catalysis.

PDEs as CNS Targets: PDE9 Inhibitors for Cognitive Deficit Diseases

Xinjun Hou, Christopher J. Helal, M. M. Claffey, 2014 .

Current landscape of phosphodiesterase 10A (PDE10A) inhibition.

Christopher J Helal, Xinjun Hou, Xinjun Hou, 2012, Journal of medicinal chemistry.

Identification of a brain penetrant PDE9A inhibitor utilizing prospective design and chemical enablement as a rapid lead optimization strategy.

Anne W. Schmidt, F. Menniti, F. Nelson, 2009, Journal of medicinal chemistry.

Application of structure-based drug design and parallel chemistry to identify selective, brain penetrant, in vivo active phosphodiesterase 9A inhibitors.

Laura McDowell, Spiros Liras, Mihaly Hajos, 2012, Journal of medicinal chemistry.

The Discovery of a Novel Phosphodiesterase (PDE) 4B-Preferring Radioligand for Positron Emission Tomography (PET) Imaging.

R. J. Mather, L. Chen, K. Zasadny, 2017, Journal of medicinal chemistry.

Aminomethyl-Derived Beta Secretase (BACE1) Inhibitors: Engaging Gly230 without an Anilide Functionality

K. Parris, Eric F. Johnson, K. Atchison, 2016, Journal of medicinal chemistry.

Discovery and SAR of 2‐Aminothiazole Inhibitors of Cyclin‐Dependent Kinase 5/p25 as a Potential Treatment for Alzheimer′s Disease.

Christopher J. Helal, 2005 .

Late-Stage Microsomal Oxidation Reduces Drug–Drug Interaction and Identifies Phosphodiesterase 2A Inhibitor PF-06815189

G. S. Walker, A. Stepan, R. Obach, 2018, ACS Medicinal Chemistry Letters.

Increased building block access through collaboration.

Angel Guzman-Perez, Christopher J Helal, Alessandra Bartolozzi, 2018, Drug discovery today.

The Discovery of a Novel Phosphodiesterase (PDE) 4B-Preferring Radioligand for Positron Emission Tomography (PET) Imaging.

R. J. Mather, L. Chen, K. Zasadny, 2017, Journal of medicinal chemistry.

Discovery of Clinical Candidate PF-06648671: A Potent γ-Secretase Modulator for the Treatment of Alzheimer's Disease.

Gregory W. Kauffman, L. Pustilnik, É. Hajós‐Korcsok, 2024, Journal of medicinal chemistry.

Discovery and Preclinical Characterization of BIIB129, a Covalent, Selective, and Brain-Penetrant BTK Inhibitor for the Treatment of Multiple Sclerosis

R. Prince, M. Hoemberger, Christopher J. Helal, 2024, Journal of medicinal chemistry.

Discovery of cyclopropyl chromane-derived pyridopyrazine-1,6-dione γ-secretase modulators with robust central efficacy.

Gregory W. Kauffman, David S. Ramirez, L. Pustilnik, 2017, MedChemComm.