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Group-Based Optimization of Potent and Cell-Active Inhibitors of the von Hippel–Lindau (VHL) E3 Ubiquitin Ligase: Structure–Activity Relationships Leading to the Chemical Probe (2S,4R)‑1-((S)‑2-(1-Cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxy‑N‑(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (VH298)

Journal of medicinal chemistry, 2018-01, Vol.61 (2), p.599-618

2018

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Structural Insights into Electrophile Irritant Sensing by the Human TRPA1 Channel

Neuron (Cambridge, Mass.), 2020-03, Vol.105 (5), p.882-894.e5

2020

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Thiazole-Based Thiosemicarbazones: Synthesis, Cytotoxicity Evaluation and Molecular Docking Study

Drug design, development and therapy, 2021, Vol.15, p.659-677

2021

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SIRT1 activators suppress inflammatory responses through promotion of p65 deacetylation and inhibition of NF-κB activity

PloS one, 2012-09, Vol.7 (9), p.e46364

2012

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Structure-activity relationship studies in substituted sulfamoyl benzamidothiazoles that prolong NF-κB activation

Bioorganic & medicinal chemistry, 2021-08, Vol.43, p.116242-116242, Article 116242

2021

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Discovery of 7‑(Prolinol‑N‑yl)-2-phenylamino-thiazolo[5,4‑d]pyrimidines as Novel Non-Nucleoside Partial Agonists for the A2A Adenosine Receptor: Prediction from Molecular Modeling

Journal of medicinal chemistry, 2016-06, Vol.59 (12), p.5922-5928

2016

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A retinoic acid receptor β2 agonist attenuates transcriptome and metabolome changes underlying nonalcohol-associated fatty liver disease

The Journal of biological chemistry, 2021-12, Vol.297 (6), p.101331, Article 101331

2021

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Engagement of the GABA to KCC2 signaling pathway contributes to the analgesic effects of A3AR agonists in neuropathic pain

The Journal of neuroscience, 2015-04, Vol.35 (15), p.6057-6067

2015

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Discovery of aryl aminothiazole γ-secretase modulators with novel effects on amyloid β-peptide production

Bioorganic & medicinal chemistry letters, 2021-12, Vol.54, p.128446-128446, Article 128446

2021

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New Antitumor Imidazo[2,1-b]thiazole Guanylhydrazones and Analogues

Journal of medicinal chemistry, 2008-02, Vol.51 (4), p.809-816

2008

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Involvement of β3-adrenoceptors in the inhibitory control of cholinergic activity in human bladder: Direct evidence by [3H]-acetylcholine release experiments in the isolated detrusor

European journal of pharmacology, 2015-07, Vol.758, p.115-122

2015

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Alkoxyphenylthiazoles with broad-spectrum activity against multidrug-resistant gram-positive bacterial pathogens

European journal of medicinal chemistry, 2018-05, Vol.152, p.318-328

2018

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Novel 2-(5-Aryl-4,5-Dihydropyrazol-1-yl)thiazol-4-One as EGFR Inhibitors: Synthesis, Biological Assessment and Molecular Docking Insights

Drug design, development and therapy, 2022, Vol.16, p.1457-1471

2022

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A Retinoic Acid Receptor β 2 Agonist Improves Cardiac Function in a Heart Failure Model

The Journal of pharmacology and experimental therapeutics, 2021-11, Vol.379 (2), p.182-190

2021

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Synthesis and anticancer activity of new thiazolo[3,2-a]pyrimidines: DNA binding and molecular modeling study

Bioorganic chemistry, 2017-10, Vol.74, p.41-52

2017

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New series of hydrazinyl thiazole derivatives of piperidin-4-one: Synthesis, structural elucidation, analgesic activity and comparative structure activity relationship

Pakistan journal of pharmaceutical sciences, 2021-07, Vol.34 (4), p.1415-1420

2021

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New bithiazolyl hydrazones: Novel synthesis, characterization and antitubercular evaluation

Bioorganic & medicinal chemistry letters, 2017-01, Vol.27 (2), p.288-294

2017

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Design, synthesis, biological evaluation, and docking study of novel dual-acting thiazole-pyridiniums inhibiting acetylcholinesterase and β-amyloid aggregation for Alzheimer’s disease

Bioorganic chemistry, 2020-10, Vol.103, p.104186, Article 104186

2020

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Development of Masitinib Derivatives with Enhanced M pro Ligand Efficiency and Reduced Cytotoxicity

Molecules (Basel, Switzerland), 2023-09, Vol.28 (18)

2023

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Review on Synthetic Chemistry and Antibacterial Importance of Thiazole Derivatives

Current drug discovery technologies, 2018, Vol.15 (3), p.214-228

2018

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Synthesis, Evaluation, and Radiolabeling of New Potent Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 2 as Potential Tracers for Positron Emission Tomography Imaging

Journal of medicinal chemistry, 2012-10, Vol.55 (20), p.8685-8699

2012

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Disrupting the CD95-PLCγ1 interaction prevents Th17-driven inflammation

Nature chemical biology, 2018-12, Vol.14 (12), p.1079-1089

2018

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Substituted 7‑Amino-5-thio-thiazolo[4,5‑d]pyrimidines as Potent and Selective Antagonists of the Fractalkine Receptor (CX3CR1)

Journal of medicinal chemistry, 2013-04, Vol.56 (8), p.3177-3190

2013

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A retinoic acid receptor β2 agonist reduces hepatic stellate cell activation in nonalcoholic fatty liver disease

Journal of molecular medicine (Berlin, Germany), 2016-10, Vol.94 (10), p.1143-1151

2016

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In Silico Analysis of the Ga 3+ /Fe 3+ Competition for Binding the Iron-Scavenging Siderophores of P. aeruginosa -Implementation of Three Gallium-Based Complexes in the "Trojan Horse" Antibacterial Strategy

Biomolecules (Basel, Switzerland), 2024-04, Vol.14 (4)

2024

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Structural Insights into Electrophile Irritant Sensing by the Human TRPA1 Channel

Thiazole-Based Thiosemicarbazones: Synthesis, Cytotoxicity Evaluation and Molecular Docking Study

SIRT1 activators suppress inflammatory responses through promotion of p65 deacetylation and inhibition of NF-κB activity

Structure-activity relationship studies in substituted sulfamoyl benzamidothiazoles that prolong NF-κB activation

Discovery of 7‑(Prolinol‑N‑yl)-2-phenylamino-thiazolo[5,4‑d]pyrimidines as Novel Non-Nucleoside Partial Agonists for the A2A Adenosine Receptor: Prediction from Molecular Modeling

A retinoic acid receptor β2 agonist attenuates transcriptome and metabolome changes underlying nonalcohol-associated fatty liver disease

Engagement of the GABA to KCC2 signaling pathway contributes to the analgesic effects of A3AR agonists in neuropathic pain

Discovery of aryl aminothiazole γ-secretase modulators with novel effects on amyloid β-peptide production

New Antitumor Imidazo[2,1-b]thiazole Guanylhydrazones and Analogues

Involvement of β3-adrenoceptors in the inhibitory control of cholinergic activity in human bladder: Direct evidence by [3H]-acetylcholine release experiments in the isolated detrusor

Alkoxyphenylthiazoles with broad-spectrum activity against multidrug-resistant gram-positive bacterial pathogens

Novel 2-(5-Aryl-4,5-Dihydropyrazol-1-yl)thiazol-4-One as EGFR Inhibitors: Synthesis, Biological Assessment and Molecular Docking Insights

A Retinoic Acid Receptor β 2 Agonist Improves Cardiac Function in a Heart Failure Model

Synthesis and anticancer activity of new thiazolo[3,2-a]pyrimidines: DNA binding and molecular modeling study

New series of hydrazinyl thiazole derivatives of piperidin-4-one: Synthesis, structural elucidation, analgesic activity and comparative structure activity relationship

New bithiazolyl hydrazones: Novel synthesis, characterization and antitubercular evaluation

Design, synthesis, biological evaluation, and docking study of novel dual-acting thiazole-pyridiniums inhibiting acetylcholinesterase and β-amyloid aggregation for Alzheimer’s disease

Development of Masitinib Derivatives with Enhanced M pro Ligand Efficiency and Reduced Cytotoxicity

Review on Synthetic Chemistry and Antibacterial Importance of Thiazole Derivatives

Synthesis, Evaluation, and Radiolabeling of New Potent Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 2 as Potential Tracers for Positron Emission Tomography Imaging

Disrupting the CD95-PLCγ1 interaction prevents Th17-driven inflammation

Substituted 7‑Amino-5-thio-thiazolo[4,5‑d]pyrimidines as Potent and Selective Antagonists of the Fractalkine Receptor (CX3CR1)

A retinoic acid receptor β2 agonist reduces hepatic stellate cell activation in nonalcoholic fatty liver disease

In Silico Analysis of the Ga 3+ /Fe 3+ Competition for Binding the Iron-Scavenging Siderophores of P. aeruginosa -Implementation of Three Gallium-Based Complexes in the "Trojan Horse" Antibacterial Strategy

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