Results 1 to 10 of about 310 (140)

Structural Aspects of Arylpiperazines as Aminergic GPCR Ligands [PDF]

Molecules
Arylpiperazines 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.
Agata Bartyzel, Beata Cristovao, Agnieszka A Kaczor   +2 more
exaly   +6 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
Beatrice Severino, Angela Corvino, Rosa Sparaco   +2 more
exaly   +4 more sources

Arylpiperazine Derivatives and Cancer: A New Challenge in Medicinal Chemistry [PDF]

Pharmaceuticals
Background: 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, Angela Corvino, Beatrice Severino, Elisa Magli, Elisa Perissutti, Francesco Frecentese, Vincenzo Santagada, Giuseppe Caliendo, Ferdinando Fiorino   +8 more
doaj   +5 more sources

Synthesis and In Vitro Antimycobacterial Activity of Novel N-Arylpiperazines Containing an Ethane-1,2-diyl Connecting Chain [PDF]

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 ...
Tomáš GONĚC, Ivan Malik, Józef Csöllei   +2 more
exaly   +4 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, Ewa Kędzierska, Agnieszka A. Kaczor, Anna Bielenica, Elisa Magli, Beatrice Severino, Angela Corvino, Ewa Gibuła-Tarłowska, Jolanta H. Kotlińska, Giorgia Andreozzi, Paolo Luciano, Elisa Perissutti, Francesco Frecentese, Marcello Casertano, Anna Leśniak, Magdalena Bujalska-Zadrożny, Małgorzata Oziębło, Raffaele Capasso, Vincenzo Santagada, Giuseppe Caliendo, Ferdinando Fiorino   +20 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, Junchao Tong, Ferdinando Fiorino, Beatrice Severino, Rosa Sparaco, Elisa Magli, Flavia Giordano, Peter M. Bloomfield, Jaya Prabhakaran, J. John Mann, Neil Vasdev, Kenneth Dahl, J. S. Dileep Kumar   +12 more
doaj   +2 more sources

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
doaj   +2 more sources

Prediction of overall in vitro microsomal stability of drug candidates based on molecular modeling and support vector machines. Case study of novel arylpiperazines derivatives. [PDF]

PLoS ONE, 2015
Other than efficacy of interaction with the molecular target, metabolic stability is the primary factor responsible for the failure or success of a compound in the drug development pipeline.
Szymon Ulenberg, Mariusz Belka, Marek Król, Franciszek Herold, Weronika Hewelt-Belka, Agata Kot-Wasik, Tomasz Bączek   +6 more
doaj   +2 more sources

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, Jozef Csöllei, Josef Jampílek, Lukáš Stanzel, Iveta Zadražilová, Jan Hošek, Šárka Pospíšilová, Alois Čížek, Aidan Coffey, Jim O’Mahony   +9 more
doaj   +2 more sources

Biologically Active 1-Arylpiperazines. Synthesis of New N-(4-Aryl-1-piperazinyl)alkyl Derivatives of Quinazolidin-4(3H)-one, 2,3-Dihydrophthalazine-1,4-dione and 1,2-Dihydropyridazine-3,6-dione as Potential Serotonin Receptor Ligands

Molecules, 2001
The synthesis of a series of new n-propyl and n-butyl chain containing 1-arylpiperazine derivatives of quinazolidin-4(3H)-one (7) 2-phenyl-2,3-dihydrophthalazine-1,4-dione (8) and 1-phenyl-1,2-dihydropyridazine-3,6-dione (9) as potential serotonin ...
Piotr Kowalski, TERESA Kowalska, Andrzej J Bojarski   +2 more
exaly   +3 more sources