selected publications
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academic article
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Chemoenzymatic Synthesis and Pharmacological Characterization of Functionalized Aspartate Analogues As Novel Excitatory Amino Acid Transporter Inhibitors..
Journal of Medicinal Chemistry.
61.
2018
Delineation of the functional properties and the mechanism of action of AA29504, an allosteric agonist and positive allosteric modulator of GABAA receptors..
Biochemical Pharmacology.
150.
2018
Functionalization of Oxazolo[4,5‐b]pyrazines by Deprotometallation.
European Journal of Organic Chemistry.
2018.
2018
Augmentation of Anticancer Drug Efficacy in Murine Hepatocellular Carcinoma Cells by a Peripherally Acting Competitive N-Methyl-d-aspartate (NMDA) Receptor Antagonist..
Journal of Medicinal Chemistry.
60.
2017
Design and Synthesis of a Series of l-trans-4-Substituted Prolines as Selective Antagonists for the Ionotropic Glutamate Receptors Including Functional and X-ray Crystallographic Studies of New Subtype Selective Kainic Acid Receptor Subtype 1 (GluK1) Antagonist (2S,4R)-4-(2-Carboxyphenoxy)pyrrolidine-2-carboxylic Acid..
Journal of Medicinal Chemistry.
60.
2017
Revisiting the Quinoxalinedione Scaffold in the Construction of New Ligands for the Ionotropic Glutamate Receptors..
ACS Chemical Neuroscience.
8.
2017
Tetrabutylammonium Fluoride as a Mild and Versatile Reagent for Cleaving Boroxazolidones to Their Corresponding Free α‐Amino Acids.
European Journal of Organic Chemistry.
2017.
2017
Bioavailability Studies and in vitro Profiling of the Selective Excitatory Amino Acid Transporter Subtype 1 (EAAT1) Inhibitor UCPH‐102.
ChemMedChem.
11.
2016
Identification of a New Class of Selective Excitatory Amino Acid Transporter Subtype 1 (EAAT1) Inhibitors Followed by a Structure-Activity Relationship Study..
Journal of Medicinal Chemistry.
59.
2016
New 4-Functionalized Glutamate Analogues Are Selective Agonists at Metabotropic Glutamate Receptor Subtype 2 or Selective Agonists at Metabotropic Glutamate Receptor Group III..
Journal of Medicinal Chemistry.
59.
2016
New Insight into the Structure–Activity Relationships of the Selective Excitatory Amino Acid Transporter Subtype 1 (EAAT1) Inhibitors UCPH‐101 and UCPH‐102.
ChemMedChem.
11.
2016
Synthesis and pharmacological characterization of the selective GluK1 radioligand ( S )-2-amino-3-(6-[ 3 H]-2,4-dioxo-3,4-dihydrothieno[3,2- d ]pyrimidin-1(2 H )-yl)propanoic acid ([ 3 H]-NF608).
MedChemComm.
7.
2016
β-Sulfonamido Functionalized Aspartate Analogues as Excitatory Amino Acid Transporter Inhibitors: Distinct Subtype Selectivity Profiles Arising from Subtle Structural Differences..
Journal of Medicinal Chemistry.
59.
2016
A Multifaceted GABAA Receptor Modulator: Functional Properties and Mechanism of Action of the Sedative-Hypnotic and Recreational Drug Methaqualone (Quaalude).
Molecular Pharmacology.
88.
2015
Benzoxazoles and oxazolopyridines in medicinal chemistry studies.
European Journal of Medicinal Chemistry.
97.
2015
Binding mode of an α-amino acid-linked quinoxaline-2,3-dione analogue at glutamate receptor subtype GluK1..
ACS Chemical Neuroscience.
6.
2015
Blood–Brain Barrier Permeability and Brain Uptake Mechanism of Kainic Acid and Dihydrokainic Acid.
Neurochemical Research.
40.
2015
ChemInform Abstract: Benzoxazoles and Oxazolopyridines in Medicinal Chemistry Studies.
ChemInform.
46.
2015
Excitatory amino acid transporters: recent insights into molecular mechanisms, novel modes of modulation and new therapeutic possibilities.
Current Opinion in Pharmacology.
20.
2015
Structure-Activity Relationship Study of Ionotropic Glutamate Receptor Antagonist (2S,3R)-3-(3-Carboxyphenyl)pyrrolidine-2-carboxylic Acid..
Journal of Medicinal Chemistry.
58.
2015
Synthesis and Selective Functionalization of [1,2,4]Triazolo-[4,3-a]pyrazines.
Synlett.
26.
2015
The glutamate transport inhibitor DL-Threo-β-Benzyloxyaspartic acid (DL-TBOA) differentially affects SN38- and oxaliplatin-induced death of drug-resistant colorectal cancer cells.
BMC Cancer.
15.
2015
ChemInform Abstract: New Palladium‐Catalyzed Domino Reaction with Intramolecular Ring Closure of an N‐(2‐Chloro‐3‐heteroaryl)arylamide: First Synthesis of Oxazolo[4,5‐b]pyrazines..
ChemInform.
45.
2014
Molecular Recognition of Two 2,4‐syn‐Functionalized (S)‐Glutamate Analogues by the Kainate Receptor GluK3 Ligand Binding Domain.
ChemMedChem.
9.
2014
New Palladium‐Catalyzed Domino Reaction with Intramolecular Ring Closure of an N‐(2‐Chloro‐3‐heteroaryl)arylamide: First Synthesis of Oxazolo[4,5‐b]pyrazines.
Advanced Synthesis & Catalysis.
356.
2014
Probing for Improved Potency and In Vivo Bioavailability of Excitatory Amino Acid Transporter Subtype 1 Inhibitors UCPH-101 and UCPH-102: Design, Synthesis and Pharmacological Evaluation of Substituted 7-Biphenyl Analogs.
Neurochemical Research.
39.
2014
Profiling substrate specificity of two series of phenethylamine analogs at monoamine oxidase A and B.
Organic & Biomolecular Chemistry.
12.
2014
Study of Oxidative Cyclization Using PhI(OAc)2 in the Formation of Benzo[4,5]thiazolo[2,3-c][1,2,4]triazoles and Related Heterocycles – Scope and Limitations.
Synlett.
25.
2014
Synthesis of (3-hydroxy-pyrazolin-5-yl)glycine based ligands interacting with ionotropic glutamate receptors.
European Journal of Medicinal Chemistry.
75.
2014
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dataset
-
Chemoenzymatic
Synthesis and Pharmacological Characterization
of Functionalized Aspartate Analogues As Novel Excitatory Amino Acid
Transporter Inhibitors.
american-chemical-society.
2018
Augmentation of
Anticancer Drug Efficacy in Murine
Hepatocellular Carcinoma Cells by a Peripherally Acting Competitive N‑Methyl‑d‑aspartate (NMDA)
Receptor Antagonist.
american-chemical-society.
2017
Identification
of a New Class of Selective Excitatory
Amino Acid Transporter Subtype 1 (EAAT1) Inhibitors Followed by a
Structure–Activity Relationship Study.
american-chemical-society.
2016
New 4‑Functionalized
Glutamate Analogues Are
Selective Agonists at Metabotropic Glutamate Receptor Subtype 2 or
Selective Agonists at Metabotropic Glutamate Receptor Group III.
american-chemical-society.
2016
β‑Sulfonamido
Functionalized Aspartate
Analogues as Excitatory Amino Acid Transporter Inhibitors: Distinct
Subtype Selectivity Profiles Arising from Subtle Structural Differences.
american-chemical-society.
2016
β‑Sulfonamido
Functionalized Aspartate
Analogues as Excitatory Amino Acid Transporter Inhibitors: Distinct
Subtype Selectivity Profiles Arising from Subtle Structural Differences.
american-chemical-society.
2016
Structure–Activity
Relationship Study of Ionotropic Glutamate Receptor Antagonist (2S,3R)‑3-(3-Carboxyphenyl)pyrrolidine-2-carboxylic Acid.
american-chemical-society.
2015
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Allosteric Modulation of an Excitatory Amino Acid Transporter: The Subtype-Selective Inhibitor UCPH-101 Exerts Sustained Inhibition of EAAT1 through an Intramonomeric Site in the Trimerization Domain.
Journal of Neuroscience.
2013
Chemoenzymatic synthesis of new 2,4-syn-functionalized (S)-glutamate analogues and structure-activity relationship studies at ionotropic glutamate receptors and excitatory amino acid transporters..
Journal of Medicinal Chemistry.
2013
Heterocycles as Nonclassical Bioisosteres of α‐Amino Acids.
ChemMedChem.
2013
Structure-activity-relationship study of N-acyl-N-phenylpiperazines as potential inhibitors of the Excitatory Amino Acid Transporters (EAATs): improving the potency of a micromolar screening Hit is not truism.
SpringerPlus.
2013
Stereoselective Chemoenzymatic Synthesis of the Four Stereoisomers of
l-2-(2-Carboxycyclobutyl)glycine and Pharmacological Characterization at Human Excitatory
Amino Acid Transporter Subtypes 1, 2, and 3.
american-chemical-society.
2006
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