Structural Aspects of Arylpiperazines as Aminergic GPCR Ligands [PDF]
MoleculesArylpiperazines are considered a “privileged scaffold” in medical chemistry due to their versatility and modular structure, enabling modifications towards diverse molecular targets with desired potency, selectivity, and pharmacokinetic properties.
Beata Cristovao, Agnieszka Anna Kaczor
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Design, Synthesis and Biological Evaluation of Novel N-Arylpiperazines Containing a 4,5-Dihydrothiazole Ring [PDF]
Pharmaceuticals, 2023 Arylpiperazines represent one of the most important classes of 5-HT1AR ligands and have attracted considerable interests for their versatile properties in chemistry and pharmacology, leading to the research of new derivatives that has been focused on the
Ferdinando Fiorino +2 more
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Photocatalysis and Kinetic Resolution by Lithiation to Give Enantioenriched 2-Arylpiperazines. [PDF]
Org Lett, 2023 Piperazines are important heterocycles in drug compounds. We report the asymmetric synthesis of arylpiperazines by photocatalytic decarboxylative arylation (metallaphotoredox catalysis) then kinetic resolution using n-BuLi/(+)-sparteine. This gave a range of piperazines with very high enantioselectivities.
Das A, Choi A, Coldham I.
europepmc +6 more sources
Arylpiperazine Derivatives and Cancer: A New Challenge in Medicinal Chemistry [PDF]
PharmaceuticalsBackground: In recent decades, there has been a startling rise in the number of cancer patients worldwide, which has led to an amazing upsurge in the development of novel anticancer treatment candidates.
Giorgia Andreozzi +8 more
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Synthesis, Docking Studies and Pharmacological Evaluation of Serotoninergic Ligands Containing a 5-Norbornene-2-Carboxamide Nucleus [PDF]
Molecules, 2022 A new series of 5-norbornene-2-carboxamide derivatives was prepared and their affinities to the 5-HT1A, 5-HT2A, and 5-HT2C receptors were evaluated and compared to a previously synthesized series of derivatives characterized by exo-N-hydroxy-5-norbornene-
Rosa Sparaco +20 more
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Synthesis, in vitro and in vivo evaluation of 11C-O-methylated arylpiperazines as potential serotonin 1A (5-HT1A) receptor antagonist radiotracers [PDF]
EJNMMI Radiopharmacy and Chemistry, 2020 Background Serotonin 1A (5-HT1A) receptors are implicated in the pathogenesis of several psychiatric and neurodegenerative disorders motivating the development of suitable radiotracers for in vivo positron emission tomography (PET) neuroimaging. The gold
Vidya Narayanaswami +12 more
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New N-Arylpiperazine-Based Compounds as Potential Inhibitors of Purinergic P2X7-Associated Signaling [PDF]
LifeThis research paper focused on the synthesis of 1-[2-hydroxy-3-(phenylcarbamoyloxy)propyl]-4-(R1, R2-substituted phenyl)piperazin-1-ium chlorides (I)–(III), containing R1, R2 = H, Cl and/or OCH3, and the evaluation of some of their physicochemical ...
Gabriela Greifová +8 more
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Coumarin-piperazine derivatives as biologically active compounds [PDF]
Saudi Pharmaceutical Journal, 2020 A number of psychiatric disorders, including anxiety, schizophrenia, Parkinson’s disease, depression and others CNS diseases are known to induce defects in the function of neural pathways sustained by the neurotransmitters, like dopamine and serotonin. N-
Kinga Ostrowska
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Molecules, 2017 Novel 1-(2-{3-/4-[(alkoxycarbonyl)amino]phenyl}-2-hydroxyethyl)-4-(2-fluorophenyl)-piperazin-1-ium chlorides (alkoxy = methoxy to butoxy; 8a–h) have been designed and synthesized through multistep reactions as a part of on-going research programme ...
Peter Mikus +2 more
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The Structure–Antimicrobial Activity Relationships of a Promising Class of the Compounds Containing the N-Arylpiperazine Scaffold [PDF]
Molecules, 2016 This research was focused on in silico characterization and in vitro biological testing of the series of the compounds carrying a N-arylpiperazine moiety.
Ivan Malík +9 more
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