A. Robichaud

发表

Highly potent, selective, and orally active phosphodiesterase 10A inhibitors.

U. Egerland, N. Hoefgen, M. Malamas, 2011, Journal of medicinal chemistry.

Allosteric Modalities for Membrane-Bound Receptors: Insights from Drug Hunting for Brain Diseases.

A. Robichaud, Quinn Coughlin, A. Hopper, 2019, Journal of medicinal chemistry.

Design and synthesis of 5,5'-disubstituted aminohydantoins as potent and selective human beta-secretase (BACE1) inhibitors.

Rajiv Chopra, Iwan Gunawan, Jim Turner, 2010, Journal of medicinal chemistry.

Neuropharmacological Profile of Novel and Selective 5-HT6 Receptor Agonists: WAY-181187 and WAY-208466

Derek Cole, Qin Shan, A. Robichaud, 2008, Neuropsychopharmacology.

Neuroactive Steroids. 1. Positive Allosteric Modulators of the (γ-Aminobutyric Acid)A Receptor: Structure-Activity Relationships of Heterocyclic Substitution at C-21.

Gabriel M. Belfort, F. Salituro, B. Harrison, 2015, Journal of medicinal chemistry.

Novel, highly potent, selective 5-HT2A/D2 receptor antagonists as potential atypical antipsychotics.

B. Largent, A. Robichaud, D. Robertson, 2003, Bioorganic & medicinal chemistry letters.

Benzimidazole- and indole-substituted 1,3'-bipyrrolidine benzamides as histamine H3 receptor antagonists.

T. Comery, A. Robichaud, J. Ellingboe, 2010, Bioorganic & medicinal chemistry letters.

Chapter 1. Promise and progress of central G-protein coupled receptor modulators for obesity treatments

B. Largent, A. Robichaud, K. Miller, 2002 .

A new method for determining levels of sedation in dogs: A pilot study with propofol and a novel neuroactive steroid anesthetic

Gabriel M. Belfort, F. Salituro, A. Robichaud, 2018, Journal of Neuroscience Methods.

Acylguanidine inhibitors of beta-secretase: optimization of the pyrrole ring substituents extending into the S1' substrate binding pocket.

M. Malamas, K. Fan, B. Harrison, 2008, Bioorganic & medicinal chemistry letters.

Approaches to Amyloid Therapies for the Treatment of Alzheimer's Disease

A. Robichaud, J. S. Jacobsen, Kim Ji-in, 2010 .

Novel pyrrolyl 2-aminopyridines as potent and selective human beta-secretase (BACE1) inhibitors.

Rajiv Chopra, Peter Reinhart, Jim Turner, 2010, Bioorganic & medicinal chemistry letters.

Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders.

G. Snyder, Qiang Zhang, A. Robichaud, 2014, Journal of medicinal chemistry.

The Major Brain Cholesterol Metabolite 24(S)-Hydroxycholesterol Is a Potent Allosteric Modulator of N-Methyl-d-Aspartate Receptors

Gabriel M. Belfort, S. Paul, A. Robichaud, 2013, The Journal of Neuroscience.

Mode of action of DL-norgestrel and ethinylestradiol combination in postcoital contraception.

A. Robichaud, S. C. Macleod, A. Robichaud, 1979, Fertility and sterility.

Di-substituted pyridinyl aminohydantoins as potent and highly selective human beta-secretase (BACE1) inhibitors.

Matthew S. Johnson, M. Malamas, K. Fan, 2010, Bioorganic & medicinal chemistry.

Effect of dehydration and hyperosmolal hydration on lignocaine and metabolites disposition in conscious rabbits

A. Robichaud, P. Souich, A. Lécrivain, 1994, British journal of pharmacology.

Preclinical characterization of zuranolone (SAGE-217), a selective neuroactive steroid GABAA receptor positive allosteric modulator

Gabriel M. Belfort, M. Quirk, F. Salituro, 2020, Neuropharmacology.

Anticonvulsant profile of the neuroactive steroid, SGE-516, in animal models

F. Salituro, A. Robichaud, J. Doherty, 2017, Epilepsy Research.

Neuroactive Steroids. 2. 3α-Hydroxy-3β-methyl-21-(4-cyano-1H-pyrazol-1'-yl)-19-nor-5β-pregnan-20-one (SAGE-217): A Clinical Next Generation Neuroactive Steroid Positive Allosteric Modulator of the (γ-Aminobutyric Acid)A Receptor.

Gabriel M. Belfort, F. Salituro, B. Harrison, 2017, Journal of medicinal chemistry.

SAM-531, N,N-dimethyl-3-{[3-(1-naphthylsulfonyl)-1H-indazol-5-yl]oxy} propan-1-amine, a novel serotonin-6 receptor antagonist with preclinical pro-cognitive efficacy

T. Comery, A. Robichaud, M. Pangalos, 2010, Alzheimer's & Dementia.

Muscarinic effect of atrial natriuretic peptide on rabbit airways

A. Robichaud, P. Souich, M. Michoud, 1993, British journal of pharmacology.

Negative chronotropic effect of the atrial natriuretic peptide in an anesthetized dog model.

A. Robichaud, C. Ribuot, C. Lambert, 1994, European journal of pharmacology.

Tricyclic thiazolopyrazole derivatives as metabotropic glutamate receptor 4 positive allosteric modulators.

A. Robichaud, D. Doller, M. Sabio, 2011, Journal of medicinal chemistry.

Effect of intravenous atrial natriuretic peptide on gas exchange in humans

A. Robichaud, P. Hamet, R. Amyot, 1994, Peptides.

Effect of atrial natriuretic peptide on bronchial tone in anesthetized rabbits

R. Peslin, C. Duvivier, A. Robichaud, 1993, Peptides.

Plasma atrial natriuretic peptide during spontaneous bronchoconstriction in asthmatics

A. Robichaud, P. Hamet, P. Souich, 1995, Peptides.

N-Aryl pyrrolidinonyl oxadiazoles as potent mGluR5 positive allosteric modulators.

A. Robichaud, A. D. White, R. Brodbeck, 2012, Bioorganic & medicinal chemistry letters.

Novel, highly potent, selective 5-HT2A/D2 receptor antagonists as potential atypical antipsychotics.

B. Largent, A. Robichaud, D. Robertson, 2003, Bioorganic & medicinal chemistry letters.

4-(2-Aminoethoxy)-N-(phenylsulfonyl)indoles as novel 5-HT6 receptor ligands.

B. Harrison, A. Robichaud, D. Huryn, 2005, Bioorganic & medicinal chemistry letters.

The synthesis of chiral α,β-unsaturated and aryl oxazolines from ketones and arols via their triflates and pd-catalyzed CO and amino alcohol coupling

A. Robichaud, A. Meyers, M. Mckennon, 1992 .

A REGIOSPECIFIC SYNTHESIS OF 3,3,6-TRIMETHYLINDAN-1-ONE

A. Robichaud, P. F. Vogt, B. F. Molino, 2001 .

One-pot synthesis of highly substituted indolines

A. Robichaud, Kevin G. Liu, L. Rebecca, 2010 .

Hunting the emesis and efficacy targets of PDE4 inhibitors: identification of the photoaffinity probe 8-(3-azidophenyl)-6- [(4-iodo-1H-1-imidazolyl)methyl]quinoline (APIIMQ).

A. Robichaud, H. Perrier, Z. Huang, 2000, Journal of medicinal chemistry.

Novel 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines are potent 5-HT(6) agonists.

B. Harrison, A. Robichaud, C. Beyer, 2009, Bioorganic & medicinal chemistry.

The synthesis and biological evaluation of quinolyl-piperazinyl piperidines as potent serotonin 5-HT1A antagonists.

M. Day, T. Comery, S. Grauer, 2010, Journal of medicinal chemistry.

5-Piperazinyl-3-sulfonylindazoles as potent and selective 5-hydroxytryptamine-6 antagonists.

T. Comery, A. Robichaud, Z. Hughes, 2010, Journal of medicinal chemistry.

The next generation of PDE4 inhibitors.

A. Robichaud, Z. Huang, Y. Ducharme, 2001, Current opinion in chemical biology.

Azetidinyl oxadiazoles as potent mGluR5 positive allosteric modulators.

A. Robichaud, A. D. White, R. Brodbeck, 2012, Bioorganic & medicinal chemistry letters.

5‐HT6 antagonists as potential treatment for cognitive dysfunction

A. Robichaud, Kevin G. Liu, 2009 .

Dual acting norepinephrine reuptake inhibitors and 5-HT(2A) receptor antagonists: Identification, synthesis and activity of novel 4-aminoethyl-3-(phenylsulfonyl)-1H-indoles.

A. Robichaud, R. Winneker, E. Koury, 2009, Bioorganic & medicinal chemistry.

Novel 1-(azacyclyl)-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines as 5-HT6 agonists and antagonists.

A. Robichaud, R. Magolda, H. Elokdah, 2007, Bioorganic & medicinal chemistry.

Synthesis of 3,3-disubstituted oxindoles

A. Robichaud, Kevin G. Liu, 2007 .

Identification of a series of benzoxazoles as potent 5-HT6 ligands.

T. Comery, A. Robichaud, L. Di, 2009, Bioorganic & medicinal chemistry letters.

A general and convenient synthesis of N-aryl piperazines

A. Robichaud, Kevin G. Liu, 2005 .

Recent progress on the identification of metabotropic glutamate 4 receptor ligands and their potential utility as CNS therapeutics.

A. Robichaud, C. Lindsley, C. Hopkins, 2011, ACS chemical neuroscience.

Asymmetric additions to chiral naphthyloxazolines. An entry into tetracyclic terpene ring systems related to aphidicolin, scopadulcic acid, and kauranes

A. Robichaud, A. Meyers, 1991 .

Substituted furans as inhibitors of the PDE4 enzyme.

C. Bayly, A. Robichaud, H. Perrier, 1999, Bioorganic & medicinal chemistry letters.

Use of aza-Cope rearrangement-Mannich cyclization reactions to achieve a general entry to Melodinus and Aspidosperma alkaloids. Stereocontrolled total syntheses of (.+-.)-deoxoapodine, (.+-.)-meloscine, and (.+-.)-epimeloscine and a formal synthesis of (.+-.)-1-acetylaspidoalbidine

L. Overman, A. Robichaud, G. Robertson, 1991 .

SAGE-718: A First-in-Class N-Methyl-d-Aspartate Receptor Positive Allosteric Modulator for the Potential Treatment of Cognitive Impairment.

M. D. Hill, M. Quirk, F. Salituro, 2022, Journal of medicinal chemistry.

Neuroactive Steroid N-Methyl-D-aspartate Receptor (NMDAR) Positive Allosteric Modulators: Synthesis, SAR and Pharmacological Activity.

M. Quirk, F. Salituro, B. Harrison, 2019, Journal of medicinal chemistry.

Possible role of valvular serotonin 5-HT(2B) receptors in the cardiopathy associated with fenfluramine.

B. Largent, A. Robichaud, D. Robertson, 2000, Molecular pharmacology.

A General and Convenient Synthesis of N‐Aryl Piperazines.

A. Robichaud, Kevin G. Liu, 2006 .

Asymmetric Synthesis of the Squalene Synthase Inhibitor Zaragozic Acid C

A. Robichaud, J. Barrow, Davidr . Evans, 1994 .

The metabolic disposition of aprepitant, a substance P receptor antagonist, in rats and dogs.

A. Robichaud, T. Baillie, R. Anari, 2004, Drug metabolism and disposition: the biological fate of chemicals.

Novel neuroactive steroids as positive allosteric modulators of NMDA receptors: mechanism, site of action, and rescue pharmacology on GRIN variants associated with neurological conditions

M. Quirk, A. Robichaud, S. Traynelis, 2023, Cellular and Molecular Life Sciences.

Chapter 2. Recent advances in selective serotonin receptor modulation

B. Largent, A. Robichaud, 2000 .

2-(Pyrrolidin-1-yl)ethyl-3,4-dihydroisoquinolin-1(2H)-one derivatives as potent and selective histamine-3 receptor antagonists.

T. Comery, J. Brennan, A. Robichaud, 2012, Journal of medicinal chemistry.

An asymmetric synthesis of the takano lactone. A formal synthesis of 9-(-)-eburnamine

A. Robichaud, A. Meyers, J. Romine, 1990 .

New pyrazolyl and thienyl aminohydantoins as potent BACE1 inhibitors: exploring the S2' region.

Matthew S. Johnson, M. Malamas, J. Erdei, 2011, Bioorganic & medicinal chemistry letters.

The synthetic neuroactive steroid SGE-516 reduces status epilepticus and neuronal cell death in a rat model of soman intoxication

A. Robichaud, J. Doherty, J. McDonough, 2017, Epilepsy & Behavior.

5-HT6 medicinal chemistry.

A. Robichaud, Kevin G. Liu, 2010, International review of neurobiology.

The Synthesis of Chiral α,β-Unsaturated and Aryloxazolines from Ketones and Arols via Their Triflates and Pd-Catalyzed CO and Amino Alcohol Coupling.

A. Robichaud, A. Meyers, M. McKennon, 1992 .

Rearrangement of 3,3-disubstituted indolenines and synthesis of 2,3-substituted indoles.

James F. Mattes, A. Robichaud, Kevin G. Liu, 2006, Organic letters.

Radiosynthesis of 123I-labelled benzimidazoles as novel single-photon emission computed tomography tracers for the histamine H3 receptor

S. Pimlott, A. Robichaud, J. Gross, 2011 .

3,4-Dihydropyrimido(1,2-a)indol-10(2H)-ones as potent non-peptidic inhibitors of caspase-3.

B. Harrison, A. Robichaud, L. Mosyak, 2009, Bioorganic & medicinal chemistry.

5-Cyclic amine-3-arylsulfonylindazoles as novel 5-HT6 receptor antagonists.

T. Comery, Radka Graf, A. Robichaud, 2010, Journal of Medicinal Chemistry.

Identification of a novel series of 3-piperidinyl-5-sulfonylindazoles as potent 5-HT6 ligands.

T. Comery, A. Robichaud, L. Di, 2009, Bioorganic & medicinal chemistry letters.

Identification of 3-sulfonylindazole derivatives as potent and selective 5-HT(6) antagonists.

T. Comery, A. Robichaud, L. Di, 2011, Bioorganic & medicinal chemistry.

Enhanced clearance of Aβ in brain by sustaining the plasmin proteolysis cascade

T. Comery, A. Robichaud, M. Pangalos, 2008, Proceedings of the National Academy of Sciences.

Tetrahydrocarbazole-based serotonin reuptake inhibitor/dopamine D2 partial agonists for the potential treatment of schizophrenia.

K. Marquis, S. Grauer, J. Brennan, 2009, Bioorganic & medicinal chemistry letters.

3-(Arylsulfonyl)-1-(azacyclyl)-1H-indoles are 5-HT(6) receptor modulators.

B. Harrison, A. Robichaud, S. Antane, 2010, Bioorganic & medicinal chemistry letters.

1-(2-Aminoethyl)-3-(arylsulfonyl)-1H-pyrrolopyridines are 5-HT(6) receptor ligands.

B. Harrison, A. Robichaud, S. Antane, 2009, Bioorganic & medicinal chemistry letters.

Approaches to palliative therapies for Alzheimer's disease.

A. Robichaud, 2006, Current Topics in Medicinal Chemistry.

1-Sulfonylindazoles as potent and selective 5-HT6 ligands.

Li Di, Edward H Kerns, Guo Ming Zhang, 2009, Bioorganic & medicinal chemistry letters.

Aminoimidazoles as potent and selective human beta-secretase (BACE1) inhibitors.

Matthew S. Johnson, M. Malamas, J. Erdei, 2009, Journal of medicinal chemistry.

Recent Advances in Selective Serotonergic Agents

A. Robichaud, W. Childers, 2005 .

WS-50030 [7-{4-[3-(1H-inden-3-yl)propyl]piperazin-1-yl}-1,3-benzoxazol-2(3H)-one]: A Novel Dopamine D2 Receptor Partial Agonist/Serotonin Reuptake Inhibitor with Preclinical Antipsychotic-Like and Antidepressant-Like Activity

K. Marquis, S. Grauer, J. Brennan, 2010, Journal of Pharmacology and Experimental Therapeutics.

Design and synthesis of aminohydantoins as potent and selective human β-secretase (BACE1) inhibitors with enhanced brain permeability.

M. Malamas, J. Erdei, K. Fan, 2010, Bioorganic & medicinal chemistry letters.

TheMajorBrainCholesterolMetabolite 24(S)-HydroxycholesterolIsaPotentAllosteric ModulatorofN-Methyl-D-AspartateReceptors

A. Robichaud, B. Chow, G. Belfort, 2013 .

Thiophene substituted acylguanidines as BACE1 inhibitors.

M. Malamas, A. Robichaud, R. Chopra, 2007, Bioorganic & medicinal chemistry letters.

Fused thiazolyl alkynes as potent mGlu5 receptor positive allosteric modulators.

A. Robichaud, M. Grenon, A. Hopper, 2013, Bioorganic & medicinal chemistry letters.

Novel triazines as potent and selective phosphodiesterase 10A inhibitors.

U. Egerland, N. Hoefgen, M. Malamas, 2012, Bioorganic & medicinal chemistry letters.

Rescue of deficient amygdala tonic γ‐aminobutyric acidergic currents in the Fmr–/y mouse model of fragile X syndrome by a novel γ‐aminobutyric acid type A receptor‐positive allosteric modulator

F. Salituro, A. Robichaud, M. Huntsman, 2016, Journal of neuroscience research.

Novel alpha-7 nicotinic acetylcholine receptor agonists containing a urea moiety: identification and characterization of the potent, selective, and orally efficacious agonist 1-[6-(4-fluorophenyl)pyridin-3-yl]-3-(4-piperidin-1-ylbutyl) urea (SEN34625/WYE-103914).

T. Comery, K. Marquis, S. Grauer, 2010, Journal of medicinal chemistry.

Discovery and initial optimization of 5,5'-disubstituted aminohydantoins as potent beta-secretase (BACE1) inhibitors.

M. Malamas, K. Fan, A. Robichaud, 2010, Bioorganic & medicinal chemistry letters.

Alzheimer's disease: a light at the end of the tunnel?

A. Robichaud, Albert J. Robichaud, David P. Rotella, 2009 .

A regiospecific synthesis of a series of 1-sulfonyl azepinoindoles as potent 5-HT6 ligands.

T. Comery, A. Robichaud, L. Di, 2008, Bioorganic & medicinal chemistry letters.

Aminoimidazoles as potent and selective human beta-secretase (BACE1) inhibitors.

Matthew S. Johnson, M. Malamas, J. Erdei, 2009, Journal of medicinal chemistry.

The Major Brain Cholesterol Metabolite 24(S)-Hydroxycholesterol Is a Potent Allosteric Modulator of N-Methyl-d-Aspartate Receptors

Gabriel M. Belfort, S. Paul, A. Robichaud, 2013, The Journal of Neuroscience.

Novel triazines as potent and selective phosphodiesterase 10A inhibitors.

U. Egerland, N. Hoefgen, M. Malamas, 2012, Bioorganic & medicinal chemistry letters.

Acylguanidine inhibitors of β-secretase: Optimization of the pyrrole ring substituents extending into the S1 and S3 substrate binding pockets

M. Malamas, K. Fan, B. Harrison, 2008 .

Design and synthesis of squalene synthase inhibitors - acylic mimics of the zaragazic acids

A. Robichaud, J. Bergstrom, G. D. Berger, 1994 .

T. Comery, K. Marquis, S. Grauer, 2010, Journal of medicinal chemistry.