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.
Cristovao Beata +2 more
exaly +7 more sources
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
exaly +6 more sources
Synthesis, Computational Studies and Preliminary Pharmacological Evaluation of New Arylpiperazines [PDF]
Journal of Chemistry, 2011 A series of novel arylpiperazines were synthesized and the target compounds evaluated for atypical antipsychotic activity in apomorphine induced climbing behavior (D2 antagonism), 5-HTP induced head twitches (5-HT2A antagonism) and catalepsy studies in ...
Sushil Kumar
exaly +4 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
doaj +5 more sources
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
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
doaj +2 more sources
Integrated Structural, Physicochemical, Pharmacokinetic and Pharmacodynamic Evaluation of Substituted Phenylcarbonyloxypiperazinopropanols as Antimycobacterial Agents [PDF]
LifeThis research aimed to evaluate structural, physicochemical and pharmacokinetic characteristics of racemic 2-hydroxy-3-(4-phenylpiperazin-1-yl)propyl 4-[(alkoxycarbonyl)amino]benzoates (Ib)–(IVb) and 2-hydroxy-3-[4-(R-substituted phenyl)piperazin-1-yl ...
Dominika Nádaská +9 more
doaj +2 more sources
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
doaj +2 more sources
Solution phase combinatorial synthesis of arylpiperazines
Tetrahedron Letters, 1997 A solution phase combinatorial synthesis of aryl piperazines 1 and 2 is described based on the S(N)Ar reaction and Schotten-Baumann acylation. The use of excess reagent is allowed and pure arylpiperazines 1 and 2 were obtained by simple acid/base washing.
Neuville, Luc, Zhu, Jieping
openaire +2 more sources
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
doaj +2 more sources