H. Selnick

发表

Discovery of oxadiazoyl tertiary carbinamine inhibitors of beta-secretase (BACE-1).

Min Xu, Qian Huang, D. Hazuda, 2006, Journal of medicinal chemistry.

Beta-secretase (BACE-1) inhibitors: accounting for 10s loop flexibility using rigid active sites.

G. McGaughey, Hemaka A. Rajapakse, M. Lai, 2007, Bioorganic & medicinal chemistry letters.

Design and synthesis of potent, selective, and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen-activated protein kinase.

E. A. O'neill, J. Vacca, B. Frantz, 1999, Journal of Medicinal Chemistry.

Inhibition of cap (m7GpppXm)-dependent endonuclease of influenza virus by 4-substituted 2,4-dioxobutanoic acid compounds

D. Hazuda, W. Mcclements, J. Tomassini, 1994, Antimicrobial Agents and Chemotherapy.

Inhibition ofCap(m7GpppXm)-Dependent Endonuclease ofInfluenza Virus by4-Substituted 2,4-Dioxobutanoic AcidCompounds

D. Hazuda, W. Mcclements, J. Tomassini, 1994 .

Preparation of 3-amino-1,4-benzodiazepin-2-ones via direct azidation with trisyl azide

N. Liverton, A. Tebben, H. Selnick, 1996 .

Suppression of Lethal Ischemic Ventricular Arrhythmias by the Class III Agent E4031 in a Canine Model of Previous Myocardial Infarction

H. Selnick, R. Stein, J. Lynch, 1990, Journal of cardiovascular pharmacology.

Discovery of Isonicotinamide Derived β-Secretase Inhibitors: In Vivo Reduction of β-Amyloid

Alison R. Gregro, Amy S. Espeseth, Min Xu, 2007 .

Discovery of isonicotinamide derived beta-secretase inhibitors: in vivo reduction of beta-amyloid.

Alison R. Gregro, Amy S. Espeseth, Min Xu, 2007, Journal of medicinal chemistry.

A facile three-step synthesis of 1,2-amino alcohols using the Ellman homochiral tert-butylsulfinamide

J. Barrow, P. Nantermet, H. Selnick, 2001 .

Antiarrhythmic efficacy of selective blockade of the cardiac slowly activating delayed rectifier current, I(Ks), in canine models of malignant ischemic ventricular arrhythmia.

G. Billman, N. Liverton, A. Tebben, 1999, Circulation.

Design and synthesis of potent, selective, and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen-activated protein kinase.

E. A. O'neill, J. Vacca, B. Frantz, 1999, Journal of medicinal chemistry.

Pharmacological Properties of MK-3207, a Potent and Orally Active Calcitonin Gene-Related Peptide Receptor Antagonist

J. Vacca, C. Regan, Y. S. Tang, 2010, Journal of Pharmacology and Experimental Therapeutics.

Discovery of a nonpeptidic small molecule antagonist of the human platelet thrombin receptor (PAR-1).

J. Barrow, K. Rittle, R. Freidinger, 2002, Bioorganic & medicinal chemistry letters.

The synthesis of dihydrothieno[2,3-b]thiophenes by a metal-halogen exchange initiated intramolecular acylation

G. Ponticello, H. Selnick, E. M. Radzilowski, 1991 .

Selective alpha1a adrenergic receptor antagonists based on 4-aryl-3,4-dihydropyridine-2-ones.

J. Barrow, R. Freidinger, R. Chang, 2000, Bioorganic & medicinal chemistry letters.

Novel oxazolidinone calcitonin gene-related peptide (CGRP) receptor antagonists for the acute treatment of migraine.

H. Selnick, M. Fraley, D. Gauvreau, 2015, Bioorganic & medicinal chemistry letters.

Class III antiarrhythmic activity in vivo by selective blockade of the slowly activating cardiac delayed rectifier potassium current IKs by (R)-2-(2,4-trifluoromethyl)-N-[2-oxo-5-phenyl-1-(2,2,2-trifluoroethyl)- 2, 3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]acetamide.

J J Baldwin, M. Sanguinetti, R. Freidinger, 1997, Journal of medicinal chemistry.

Effects of New and Potent Methanesulfonanilide Class III Antiarrhythmic Agents on Myocardial Refractoriness and Contractility in Isolated Cardiac Muscle

H. Selnick, J. Lynch, D. Claremon, 1991, Journal of cardiovascular pharmacology.

Cardiac Electrophysiologic and Inotropic Actions of New and Potent Methanesulfonanilide Class III Antiarrhythmic Agents in Anesthetized Dogs

H. Selnick, J. Lynch, D. Claremon, 1991, Journal of cardiovascular pharmacology.

Insights into activity and inhibition from the crystal structure of human O-GlcNAcase.

Sujata Sharma, D. Klein, D. Hall, 2017, Nature chemical biology.

Anti-influenza virus activities of 4-substituted 2,4-dioxobutanoic acid inhibitors

J. Tomassini, H. Selnick, J. Hastings, 1996, Antimicrobial agents and chemotherapy.

Synthesis and evaluation of imidazole acetic acid inhibitors of activated thrombin-activatable fibrinolysis inhibitor as novel antithrombotics.

J. Barrow, J. Vacca, S. Stauffer, 2003, Journal of medicinal chemistry.

[(11)C]MK-4232: The First Positron Emission Tomography Tracer for the Calcitonin Gene-Related Peptide Receptor.

Sandra M. Sanabria-Bohórquez, L. Gantert, E. Hostetler, 2013, ACS medicinal chemistry letters.

MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.

J. Vacca, H. Selnick, S. Graham, 2012, Bioorganic & medicinal chemistry letters.

Potent thrombin inhibitors via a 20-membered ring olefin metathesis macrocyclization

P. Nantermet, H. Selnick, 2003 .

P2 pyridine N-oxide thrombin inhibitors: a novel peptidomimetic scaffold.

Youwei Yan, L. Kuo, J. Vacca, 2005, Bioorganic & medicinal chemistry letters.

Design and synthesis of potent and selective macrocyclic thrombin inhibitors.

Youwei Yan, J. Barrow, L. Kuo, 2003, Bioorganic & medicinal chemistry letters.

Pharmacokinetic optimization of 3-amino-6-chloropyrazinone acetamide thrombin inhibitors. Implementation of P3 pyridine N-oxides to deliver an orally bioavailable series containing P1 N-benzylamides.

Youwei Yan, L. Kuo, J. Vacca, 2003, Bioorganic & medicinal chemistry letters.

Unexpected enhancement of thrombin inhibitor potency with o-aminoalkylbenzylamides in the P1 position.

Lawrence C Kuo, Daniel R McMasters, James C Barrow, 2003, Bioorganic & medicinal chemistry letters.

Imidazole acetic acid TAFIa inhibitors: SAR studies centered around the basic P(1)(') group.

J. Barrow, J. Vacca, D. Colussi, 2004, Bioorganic & medicinal chemistry letters.

The total synthesis of avermectin A1a

R. Hungate, S. Danishefsky, H. Selnick, 1989 .

Novel CGRP receptor antagonists from central amide replacements causing a reversal of preferred chirality.

J. Vacca, H. Selnick, R. Bednar, 2010, Bioorganic & medicinal chemistry letters.

Inhibition of O-GlcNAcase leads to elevation of O-GlcNAc tau and reduction of tauopathy and cerebrospinal fluid tau in rTg4510 mice

N. Hastings, B. Butts, R. Hargreaves, 2017, Molecular Neurodegeneration.

Discovery and evaluation of potent P1 aryl heterocycle-based thrombin inhibitors.

Lawrence C Kuo, Daniel R McMasters, James C Barrow, 2004, Journal of medicinal chemistry.

Design and Synthesis of 2,3,5‐Substituted Imidazolidin‐4‐one Inhibitors of BACE‐1

Amy S. Espeseth, Qian Huang, A. Espeseth, 2007, ChemMedChem.

Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors.

D. Hazuda, A. Simon, G. McGaughey, 2007, Bioorganic & medicinal chemistry letters.

The total synthesis of the aglycon of avermectin A1a

R. Hungate, S. Danishefsky, H. Selnick, 1987 .

Orally bioavailable imidazoazepanes as calcitonin gene-related peptide (CGRP) receptor antagonists: discovery of MK-2918.

A. W. Shaw, J. Vacca, H. Selnick, 2011, Bioorganic & medicinal chemistry letters.

In Vitro and in Vivo Evaluation of Dihydropyrimidinone C-5 Amides as Potent and Selective α1A Receptor Antagonists for the Treatment of Benign Prostatic Hyperplasia

J. Barrow, K. Rittle, R. Freidinger, 2000 .

The total synthesis of zincophorin

S. Danishefsky, H. Selnick, M. Deninno, 1987 .

9-hydroxyazafluorenes and their use in thrombin inhibitors.

Youwei Yan, B. Wong, P. Nantermet, 2005, Journal of medicinal chemistry.

Preparation and evaluation of 1,3-diaminocyclopentane-linked dihydropyrimidinone derivatives as selective α1a-receptor antagonists

J. Barrow, R. Freidinger, R. Chang, 2000 .

Total synthesis of (±)-gnididione and (±)-isognididione

H. Selnick, P. Jacobi, 1990 .

Discovery and initial structure-activity relationships of trisubstituted ureas as thrombin receptor (PAR-1) antagonists.

J. Barrow, R. Freidinger, P. Nantermet, 2001, Bioorganic & medicinal chemistry letters.

Methyl-substitution of an iminohydantoin spiropiperidine β-secretase (BACE-1) inhibitor has a profound effect on its potency.

A. Simon, G. McGaughey, J. Barrow, 2015, Bioorganic & medicinal chemistry letters.

A novel degradation in the avermectin series: A stereospecific osmylation reaction

S. Danishefsky, H. Selnick, 1987 .

The Total Synthesis of the Aglycon of Avermectin A1a.

R. Hungate, S. Danishefsky, H. Selnick, 1988 .

Enynones in organic synthesis. I: Spiroannulation by tandem oxy-Cope rearrangement-electrocyclic ring closure

M. Martinelli, H. Selnick, P. Jacobi, 1988 .

The total synthesis of avermectin A1a. New protocols for the synthesis of novel 2-deoxypyranose systems and their axial glycosides

S. Danishefsky, H. Selnick, D. Armistead, 1987 .

A systematic degradation of zincophorin: a stereoselective synthesis of the C17-C25 fragment

S. Danishefsky, H. Selnick, M. Deninno, 1986 .

First Demonstration of Cerebrospinal Fluid and Plasma Aβ Lowering with Oral Administration of a β-Site Amyloid Precursor Protein-Cleaving Enzyme 1 Inhibitor in Nonhuman Primates

Alison R. Gregro, Amy S. Espeseth, Min Xu, 2009, Journal of Pharmacology and Experimental Therapeutics.

First Demonstration of Cerebrospinal Fluid and Plasma A (cid:1) Lowering with Oral Administration of a (cid:1) -Site Amyloid Precursor Protein-Cleaving Enzyme 1 Inhibitor in Nonhuman Primates □ S

Alison R. Gregro, Amy S. Espeseth, Min Xu, 2008 .

Discovery of 6-(Fluoro-(18)F)-3-(1H-pyrrolo[2,3-c]pyridin-1-yl)isoquinolin-5-amine ([(18)F]-MK-6240): A Positron Emission Tomography (PET) Imaging Agent for Quantification of Neurofibrillary Tangles (NFTs).

Talakad G. Lohith, S. Melquist, L. Gantert, 2016, Journal of medicinal chemistry.

Antiarrhythmic efficacy of combined I(Ks) and beta-adrenergic receptor blockade.

N. Liverton, H. Selnick, J. Lynch, 2002, The Journal of pharmacology and experimental therapeutics.

In Vivo Quantification of Calcitonin Gene-Related Peptide Receptor Occupancy by Telcagepant in Rhesus Monkey and Human Brain Using the Positron Emission Tomography Tracer [11C]MK-4232

Sandra M. Sanabria-Bohórquez, G. Bormans, L. Gantert, 2013, The Journal of Pharmacology and Experimental Therapeutics.

Bis-heteroannulation. 16. A synthetic approach to geigerin

H. Selnick, P. Jacobi, K. M. Touchette, 1992 .

The synthesis of dihydrofurano[2,3-b]thiopyrans, thiepins and thiophenes

H. Selnick, L. M. Brookes, 1989 .

SAR of tertiary carbinamine derived BACE1 inhibitors: role of aspartate ligand amine pKa in enzyme inhibition.

Adam J. Simon, Georgia B. McGaughey, Philippe G. Nantermet, 2010, Bioorganic & medicinal chemistry letters.

Preparation and trapping of 3-lithium-O-lithiophenoxide

H. Selnick, M. Bourgeois, J. W. Butcher, 1993 .

In vitro and in vivo evaluation of dihydropyrimidinone C-5 amides as potent and selective alpha(1A) receptor antagonists for the treatment of benign prostatic hyperplasia.

J. Barrow, K. Rittle, R. Freidinger, 2000, Journal of medicinal chemistry.

MK-8719, a Novel and Selective O-GlcNAcase Inhibitor That Reduces the Formation of Pathological Tau and Ameliorates Neurodegeneration in a Mouse Model of Tauopathy

Lynn A. Hyde, E. Hostetler, J. Uslaner, 2020, The Journal of Pharmacology and Experimental Therapeutics.

Discovery of MK-8719, A Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies.

D. Klein, J. Hess, D. Vocadlo, 2019, Journal of medicinal chemistry.

An Improved Procedure for the Cyanation of Aryl Triflates: A Convenient Synthesis of 6-Cyano-1,2,3,4-Tetrahydroisoquinoline

G. R. Smith, A. Tebben, H. Selnick, 1995 .

An Improved Procedure for the Cyanation of Aryl Triflates: A Convenient Synthesis of 6-Cyano-1,2,3,4-tetrahydroisoquinoline.

G. R. Smith, A. Tebben, H. Selnick, 1995 .

4-Oxospiro[benzopyran-2,4'-piperidines] as class III antiarrhythmic agents. Pharmacological studies on 3,4-dihydro-1'-[2-(benzofurazan-5-yl)- ethyl]-6-methanesulfonamidospiro[(2H)-1-benzopyran-2,4'-piperidin]-4-on e (L-691,121).

B. T. Phillips, J. Baldwin, C. N. Habecker, 1992, Journal of medicinal chemistry.

Inhibition of O-GlcNAcase leads to elevation of O-GlcNAc tau and reduction of tauopathy and cerebrospinal fluid tau in rTg4510 mice

Lynn A. Hyde, N. Hastings, B. Butts, 2017, Molecular Neurodegeneration.

In Vivo Canine Cardiac Electrophysiologic Profile of 1,4‐Benzodiazepine Iks Blockers

A. Tebben, H. Selnick, J. Lynch, 2003, Journal of cardiovascular pharmacology.

A short radiosynthesis of 6-[C3H3]-dorzolamide at very high specific activity and optical purity

H. Burns, G. Ponticello, H. Selnick, 1996 .

Novel CGRP receptor antagonists through a design strategy of target simplification with addition of molecular flexibility.

J. Vacca, H. Selnick, I. M. Bell, 2009, Bioorganic & medicinal chemistry letters.

Discovery and SAR of isonicotinamide BACE-1 inhibitors that bind beta-secretase in a N-terminal 10s-loop down conformation.

Alison R. Gregro, Georgia B McGaughey, M Katharine Holloway, 2007, Bioorganic & medicinal chemistry letters.

Identification of potent, highly constrained CGRP receptor antagonists.

Steven S. Sharik, Cory R. Theberge, J. Vacca, 2010, Bioorganic & medicinal chemistry letters.

Discovery of MK-3207: A Highly Potent, Orally Bioavailable CGRP Receptor Antagonist.

J. Vacca, C. Regan, T. Prueksaritanont, 2010, ACS medicinal chemistry letters.

Evolution of Tertiary Carbinamine BACE‐1 Inhibitors: Aβ Reduction in Rhesus CSF upon Oral Dosing

Alison R. Gregro, A. Simon, G. McGaughey, 2009, ChemMedChem.

EARLY CLINICAL RESULTS AND PRECLINICAL VALIDATION OF THE O-GLCNACASE (OGA) INHIBITOR MK-8719 AS A NOVEL THERAPEUTIC FOR THE TREATMENT OF TAUOPATHIES

Dawn M. Toolan, Joseph James Duffy, J. Renger, 2016, Alzheimer's & Dementia.