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1.
Activation of the mGlu1 metabotropic glutamate receptor has antipsychotic-like effects and is required for efficacy of M4 muscarinic receptor allosteric modulators.
Mol Psychiatry
; 25(11): 2786-2799, 2020 11.
Artículo
en Inglés
| MEDLINE | ID: mdl-30116027
2.
The discovery of VU0486846: steep SAR from a series of M1 PAMs based on a novel benzomorpholine core.
Bioorg Med Chem Lett
; 28(12): 2175-2179, 2018 07 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-29754948
3.
Re-exploration of the mGlu1 PAM Ro 07-11401 scaffold: Discovery of analogs with improved CNS penetration despite steep SAR.
Bioorg Med Chem Lett
; 26(9): 2289-92, 2016 May 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-27013388
4.
Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 3. Engineering plasma stability by discovery and optimization of isoindolinone analogs.
Bioorg Med Chem Lett
; 26(8): 1869-72, 2016 Apr 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-26988302
5.
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.
Bioorg Med Chem Lett
; 26(3): 751-756, 2016 Feb 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-26778256
6.
Further optimization of the M1 PAM VU0453595: Discovery of novel heterobicyclic core motifs with improved CNS penetration.
Bioorg Med Chem Lett
; 26(15): 3822-5, 2016 08 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-27173801
7.
Discovery of 3-aminopicolinamides as metabotropic glutamate receptor subtype 4 (mGlu4) positive allosteric modulator warheads engendering CNS exposure and in vivo efficacy.
Bioorg Med Chem Lett
; 26(12): 2915-2919, 2016 06 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-27131990
8.
Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 1: SAR of modifications to the central aryl core.
Bioorg Med Chem Lett
; 25(22): 5107-10, 2015 Nov 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-26476971
9.
Selective VPS34 Inhibitors: High Efficiency Design by Profiting from Small Structural Differences.
J Med Chem
; 65(17): 11497-11499, 2022 09 08.
Artículo
en Inglés
| MEDLINE | ID: mdl-35998347
10.
A Novel M1 PAM VU0486846 Exerts Efficacy in Cognition Models without Displaying Agonist Activity or Cholinergic Toxicity.
ACS Chem Neurosci
; 9(9): 2274-2285, 2018 09 19.
Artículo
en Inglés
| MEDLINE | ID: mdl-29701957
11.
Diverse Effects on M1 Signaling and Adverse Effect Liability within a Series of M1 Ago-PAMs.
ACS Chem Neurosci
; 8(4): 866-883, 2017 04 19.
Artículo
en Inglés
| MEDLINE | ID: mdl-28001356
12.
Total Synthesis of Gombamide A.
Org Lett
; 18(15): 3810-3, 2016 08 05.
Artículo
en Inglés
| MEDLINE | ID: mdl-27442228
13.
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).
ACS Chem Neurosci
; 7(9): 1192-200, 2016 09 21.
Artículo
en Inglés
| MEDLINE | ID: mdl-27075300
14.
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.
J Med Chem
; 58(20): 7959-71, 2015 Oct 22.
Artículo
en Inglés
| MEDLINE | ID: mdl-26426481
15.
Discovery of VU0409551/JNJ-46778212: An mGlu5 Positive Allosteric Modulator Clinical Candidate Targeting Schizophrenia.
ACS Med Chem Lett
; 6(6): 716-20, 2015 Jun 11.
Artículo
en Inglés
| MEDLINE | ID: mdl-26157544
16.
Chemical modulation of mutant mGlu1 receptors derived from deleterious GRM1 mutations found in schizophrenics.
ACS Chem Biol
; 9(10): 2334-46, 2014 Oct 17.
Artículo
en Inglés
| MEDLINE | ID: mdl-25137254
17.
Synthesis and biological evaluation of novel ferrocene-naphthoquinones as antiplasmodial agents.
Eur J Med Chem
; 70: 548-57, 2013.
Artículo
en Inglés
| MEDLINE | ID: mdl-24211630
18.
Discovery of potent myeloid cell leukemia 1 (Mcl-1) inhibitors using fragment-based methods and structure-based design.
J Med Chem
; 56(1): 15-30, 2013 Jan 10.
Artículo
en Inglés
| MEDLINE | ID: mdl-23244564
19.
Hypoglycemic and antihyperglycemic effect of Witheringia solanacea in normal and alloxan-induced hyperglycemic rats.
J Ethnopharmacol
; 133(2): 907-10, 2011 Jan 27.
Artículo
en Inglés
| MEDLINE | ID: mdl-20937373
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