Discovery and Synthesis of Drugs
Desinfarma
José Manuel
Brea Floriani
Senior university lecturer
Publications by the researcher in collaboration with José Manuel Brea Floriani (46)
2024
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Exploring Biginelli-based scaffolds as A2B adenosine receptor antagonists: Unveiling novel structure-activity relationship trends, lead compounds, and potent colorectal anticancer agents
Biomedicine and Pharmacotherapy, Vol. 173
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N-Adamantyl-1-alkyl-4-oxo-1,4-dihydroquinoline-3-carboxamide Derivatives as Fluorescent Probes to Detect Microglia Activation through the Imaging of Cannabinoid Receptor Subtype 2 (CB2R)
Journal of Medicinal Chemistry, Vol. 67, Núm. 13, pp. 11003-11023
2023
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A Robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery
Molecules, Vol. 28, Núm. 24
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Development of N-(1-Adamantyl)benzamides as Novel Anti-Inflammatory Multitarget Agents Acting as Dual Modulators of the Cannabinoid CB2 Receptor and Fatty Acid Amide Hydrolase
Journal of Medicinal Chemistry, Vol. 66, Núm. 1, pp. 235-250
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Exploring the Effect of Halogenation in a Series of Potent and Selective A2BAdenosine Receptor Antagonists
Journal of Medicinal Chemistry, Vol. 66, Núm. 1, pp. 890-912
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Fluorescence based HTS-compatible ligand binding assays for dopamine D3 receptors in baculovirus preparations and live cells
Frontiers in Molecular Biosciences, Vol. 10
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N-adamantyl-anthranil amide derivatives: New selective ligands for the cannabinoid receptor subtype 2 (CB2R)
European Journal of Medicinal Chemistry, Vol. 248
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Pharmacological insights emerging from the characterization of a large collection of synthetic cannabinoid receptor agonists designer drugs
Biomedicine and Pharmacotherapy, Vol. 164
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Stapling Amantadine to Melanostatin Neuropeptide: Discovery of Potent Positive Allosteric Modulators of the D2 Receptors
ACS Medicinal Chemistry Letters, Vol. 14, Núm. 12, pp. 1656-1663
2022
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A 2B adenosine receptor antagonists rescue lymphocyte activity in adenosine-producing patient-derived cancer models
Journal for ImmunoTherapy of Cancer, Vol. 10, Núm. 5
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Exploring Non-orthosteric Interactions with a Series of Potent and Selective A3Antagonists
ACS Medicinal Chemistry Letters, Vol. 13, Núm. 2, pp. 243-249
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Identification of A2BAR as a potential target in colorectal cancer using novel fluorescent GPCR ligands
Biomedicine and Pharmacotherapy, Vol. 153
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Optimization of 2-Amino-4,6-diarylpyrimidine-5-carbonitriles as Potent and Selective A1Antagonists
Journal of Medicinal Chemistry, Vol. 65, Núm. 3, pp. 2091-2106
2021
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3,4-Dihydropyrimidin-2(1H)-ones as Antagonists of the Human A2B Adenosine Receptor: Optimization, Structure-Activity Relationship Studies, and Enantiospecific Recognition
Journal of medicinal chemistry, Vol. 64, Núm. 1, pp. 458-480
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Discovery of New Potent Positive Allosteric Modulators of Dopamine D2Receptors: Insights into the Bioisosteric Replacement of Proline to 3-Furoic Acid in the Melanostatin Neuropeptide
Journal of Medicinal Chemistry, Vol. 64, Núm. 9, pp. 6209-6220
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Synthesis, Pharmacological, and Biological Evaluation of 2-Furoyl-Based MIF-1 Peptidomimetics and the Development of a General-Purpose Model for Allosteric Modulators (ALLOPTML)
ACS Chemical Neuroscience, Vol. 12, Núm. 1, pp. 203-215
2020
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Nitrogen-Walk Approach to Explore Bioisosteric Replacements in a Series of Potent A2B Adenosine Receptor Antagonists
Journal of medicinal chemistry, Vol. 63, Núm. 14, pp. 7721-7739
2019
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Synthesis, Pharmacological, and Biological Evaluation of MIF-1 Picolinoyl Peptidomimetics as Positive Allosteric Modulators of D2R
ACS Chemical Neuroscience, Vol. 10, Núm. 8, pp. 3690-3702
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Trifluorinated Pyrimidine-Based A2B Antagonists: Optimization and Evidence of Stereospecific Recognition
Journal of Medicinal Chemistry, Vol. 62, Núm. 20, pp. 9315-9330
2018
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Clinical validation of blood/brain glutamate grabbing in acute ischemic stroke
Annals of Neurology, Vol. 84, Núm. 2, pp. 260-273