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Discovery of Potent Myeloid Cell Leukemia 1 (Mcl-1) Inhibitors Using Fragment-Based Methods and Structure-Based Design

Journal of medicinal chemistry, 2013-01, Vol.56 (1), p.15-30

2013

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Hypoglycemic and antihyperglycemic effect of Witheringia solanacea in normal and alloxan-induced hyperglycemic rats

Journal of ethnopharmacology, 2011-01, Vol.133 (2), p.907-910

2011

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Selective VPS34 Inhibitors: High Efficiency Design by Profiting from Small Structural Differences

Journal of medicinal chemistry, 2022-09, Vol.65 (17), p.11497-11499

Garcia-Barrantes, Pedro M.

2022

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Total Synthesis of Gombamide A

Organic letters, 2016-08, Vol.18 (15), p.3810-3813

2016

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Activation of the mGlu1 metabotropic glutamate receptor has antipsychotic-like effects and is required for efficacy of M4 muscarinic receptor allosteric modulators

Molecular psychiatry, 2020-11, Vol.25 (11), p.2786-2799

2020

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A Novel M 1 PAM VU0486846 Exerts Efficacy in Cognition Models without Displaying Agonist Activity or Cholinergic Toxicity

ACS chemical neuroscience, 2018-09, Vol.9 (9), p.2274-2285

2018

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The discovery of VU0486846: steep SAR from a series of M 1 PAMs based on a novel benzomorpholine core

Bioorganic & medicinal chemistry letters, 2018-07, Vol.28 (12), p.2175

2018

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Development of Novel, CNS Penetrant Positive Allosteric Modulators for the Metabotropic Glutamate Receptor Subtype 1 (mGlu1), Based on an N‑(3-Chloro-4-(1,3-dioxoisoindolin-2-yl)phenyl)-3-methylfuran-2-carboxamide Scaffold, That Potentiate Wild Type and Mutant mGlu1 Receptors Found in Schizophrenics

Journal of medicinal chemistry, 2015-10, Vol.58 (20), p.7959-7971

2015

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The discovery of VU0486846: steep SAR from a series of M1 PAMs based on a novel benzomorpholine core

Bioorganic & medicinal chemistry letters, 2018-07, Vol.28 (12), p.2175-2179

2018

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Chemical Modulation of Mutant mGlu1 Receptors Derived from Deleterious GRM1 Mutations Found in Schizophrenics

ACS chemical biology, 2014-10, Vol.9 (10), p.2334-2346

2014

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Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 1: SAR of modifications to the central aryl core

Bioorganic & medicinal chemistry letters, 2015-11, Vol.25 (22), p.5107-5110

2015

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Lead optimization of the VU0486321 series of mGlu(1) PAMs. Part 2: SAR of alternative 3-methyl heterocycles and progress towards an in vivo tool

Bioorganic & medicinal chemistry letters, 2016-02, Vol.26 (3), p.751-756

2016

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Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 3. Engineering plasma stability by discovery and optimization of isoindolinone analogs

Bioorganic & medicinal chemistry letters, 2016-04, Vol.26 (8), p.1869-1872

2016

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Re-exploration of the mGlu1 PAM Ro 07-11401 scaffold: Discovery of analogs with improved CNS penetration despite steep SAR

Bioorganic & medicinal chemistry letters, 2016-05, Vol.26 (9), p.2289-2292

2016

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Synthesis and biological evaluation of novel ferrocene–naphthoquinones as antiplasmodial agents

European journal of medicinal chemistry, 2013-12, Vol.70, p.548-557

2013

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Further optimization of the M1 PAM VU0453595: Discovery of novel heterobicyclic core motifs with improved CNS penetration

Bioorganic & medicinal chemistry letters, 2016-08, Vol.26 (15), p.3822-3825

2016

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Discovery of 3-aminopicolinamides as metabotropic glutamate receptor subtype 4 (mGlu4) positive allosteric modulator warheads engendering CNS exposure and in vivo efficacy

Bioorganic & medicinal chemistry letters, 2016-06, Vol.26 (12), p.2915-2919

2016

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A Novel M1 PAM VU0486846 Exerts Efficacy in Cognition Models without Displaying Agonist Activity or Cholinergic Toxicity

ACS chemical neuroscience, 2018-09, Vol.9 (9), p.2274-2285

2018

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Diverse Effects on M 1 Signaling and Adverse Effect Liability within a Series of M 1 Ago-PAMs

ACS chemical neuroscience, 2017-04, Vol.8 (4), p.866-883

2017

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Physicochemical and chromatographic method of characterization of Matricaria recutita tinctures

Journal of pharmacy & pharmacognosy research, 2016-01, Vol.4 (1), p.18-24

2016

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Total synthesis of actinophenanthroline A

Tetrahedron letters, 2016-05, Vol.57 (20), p.2194-2196

2016

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Activation of the mGlu.sub.1 metabotropic glutamate receptor has antipsychotic-like effects and is required for efficacy of M.sub.4 muscarinic receptor allosteric modulators

Molecular psychiatry, 2020-11, Vol.25 (11), p.2786

2020

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One pot synthesis of unsymmetrical ketones from carboxylic and boronic acids via PyClU-mediated acylative Suzuki coupling

Tetrahedron letters, 2017-03, Vol.58 (9), p.898-901

2017

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Discovery of Potent Myeloid Cell Leukemia 1 (Mcl-1) Inhibitors Using Fragment-Based Methods and Structure-Based Design

Hypoglycemic and antihyperglycemic effect of Witheringia solanacea in normal and alloxan-induced hyperglycemic rats

Selective VPS34 Inhibitors: High Efficiency Design by Profiting from Small Structural Differences

Total Synthesis of Gombamide A

Activation of the mGlu1 metabotropic glutamate receptor has antipsychotic-like effects and is required for efficacy of M4 muscarinic receptor allosteric modulators

A Novel M 1 PAM VU0486846 Exerts Efficacy in Cognition Models without Displaying Agonist Activity or Cholinergic Toxicity

The discovery of VU0486846: steep SAR from a series of M 1 PAMs based on a novel benzomorpholine core

The discovery of VU0486846: steep SAR from a series of M1 PAMs based on a novel benzomorpholine core

Chemical Modulation of Mutant mGlu1 Receptors Derived from Deleterious GRM1 Mutations Found in Schizophrenics

Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 1: SAR of modifications to the central aryl core

Lead optimization of the VU0486321 series of mGlu(1) PAMs. Part 2: SAR of alternative 3-methyl heterocycles and progress towards an in vivo tool

Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 3. Engineering plasma stability by discovery and optimization of isoindolinone analogs

Discovery, Synthesis, and Preclinical Characterization of N‑(3-Chloro-4-fluorophenyl)‑1H‑pyrazolo[4,3‑b]pyridin-3-amine (VU0418506), a Novel Positive Allosteric Modulator of the Metabotropic Glutamate Receptor 4 (mGlu4)

Re-exploration of the mGlu1 PAM Ro 07-11401 scaffold: Discovery of analogs with improved CNS penetration despite steep SAR

Discovery of VU0409551/JNJ-46778212: An mGlu5 Positive Allosteric Modulator Clinical Candidate Targeting Schizophrenia

Synthesis and biological evaluation of novel ferrocene–naphthoquinones as antiplasmodial agents

Further optimization of the M1 PAM VU0453595: Discovery of novel heterobicyclic core motifs with improved CNS penetration

Discovery of 3-aminopicolinamides as metabotropic glutamate receptor subtype 4 (mGlu4) positive allosteric modulator warheads engendering CNS exposure and in vivo efficacy

A Novel M1 PAM VU0486846 Exerts Efficacy in Cognition Models without Displaying Agonist Activity or Cholinergic Toxicity

Diverse Effects on M 1 Signaling and Adverse Effect Liability within a Series of M 1 Ago-PAMs

Physicochemical and chromatographic method of characterization of Matricaria recutita tinctures

Total synthesis of actinophenanthroline A

Activation of the mGlu.sub.1 metabotropic glutamate receptor has antipsychotic-like effects and is required for efficacy of M.sub.4 muscarinic receptor allosteric modulators

One pot synthesis of unsymmetrical ketones from carboxylic and boronic acids via PyClU-mediated acylative Suzuki coupling

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