Modeling key interactions between dopamine D2 receptor second extracellular loop and arylpiperazine ligands [PDF]
Journal of the Serbian Chemical Society, 2012 Second extracellular loop (ecl2) of dopamine (DA) D2 receptor is an essential part of dopaminergic ligands binding pocket. To form a part of the ligand binding surface it has to fold down into the transmembrane domain of the DA receptor.
Šukalović Vladimir +4 more
doaj +3 more sources
Modulating Properties of Piroxicam, Meloxicam and Oxicam Analogues against Macrophage-Associated Chemokines in Colorectal Cancer [PDF]
Molecules, 2021 The mechanisms underlying the antineoplastic effects of oxicams have not been fully elucidated. We aimed to assess the effect of classic and novel oxicams on the expression/secretion of macrophage-associated chemokines (RTqPCR/Luminex xMAP) in colorectal
Paulina Lewandowska +8 more
doaj +2 more sources
Novel Arylpiperazine Derivatives of Salicylamide with α1-Adrenolytic Properties Showed Antiarrhythmic and Hypotensive Properties in Rats. [PDF]
Int J Mol Sci, 2022 Cardiovascular diseases remain one of the leading causes of death worldwide. Unfortunately, the available pharmacotherapeutic options have limited effectiveness. Therefore, developing new drug candidates remains very important.
Żmudzka E +8 more
europepmc +2 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 +4 more sources
New Oxicam Derivatives—Studies of Membrane Interactions, Cytotoxicity, Cyclooxygenase Inhibition and Molecular Docking [PDF]
MembranesOxicam derivatives, a class of nonsteroidal anti-inflammatory drugs (NSAIDs), are important scaffolds for developing biologically active compounds. In this study, arylpiperazine oxicam derivatives (PR24–PR50) were examined for membrane interactions ...
Jadwiga Maniewska +4 more
doaj +2 more sources
New, Eco-Friendly Method for Synthesis of 3-Chlorophenyl and 1,1′-Biphenyl Piperazinylhexyl Trazodone Analogues with Dual 5-HT1A/5-HT7 Affinity and Its Antidepressant-like Activity [PDF]
Molecules, 2022 Serotonin 5-HT1A and 5-HT7 receptors play an important role in the pathogenesis and pharmacotherapy of depression. Previously identified N-hexyl trazodone derivatives, 2-(6-(4-(3-chlorophenyl)piperazin-1-yl)hexyl)-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one ...
Przemysław Zaręba +5 more
doaj +2 more sources
Potential Anti-Amnesic Activity of a Novel Multimodal Derivative of Salicylamide, JJGW08, in Mice [PDF]
Pharmaceuticals, 2023 Memory impairments constitute a significant problem worldwide, and the COVID-19 pandemic dramatically increased the prevalence of cognitive deficits. Patients with cognitive deficits, specifically memory disturbances, have underlying comorbid conditions ...
Elżbieta Żmudzka +7 more
doaj +2 more sources
The Structural Determinants for α1-Adrenergic/Serotonin Receptors Activity among Phenylpiperazine-Hydantoin Derivatives [PDF]
Molecules, 2021 Several studies confirmed the reciprocal interactions between adrenergic and serotoninergic systems and the influence of these phenomena on the pathogenesis of anxiety.
Katarzyna Kucwaj-Brysz +8 more
doaj +2 more sources
Synthesis of Some New Thiazole Derivatives and Their Biological Activity Evaluation
Journal of Chemistry, 2015 New 2-(4-arylpiperazine-1-yl)-N-[4-(2-(4-substituted phenyl)thiazol-4-yl)phenyl]acetamide derivatives were synthesized and evaluated for their antimicrobial and anticholinesterase activities.
Leyla Yurttaş +3 more
doaj +2 more sources
Arylpiperazine Derivative NAF19 Inhibits Prostate Cancer Activity and Its Molecular Mechanisms [PDF]
Drugs in R&DBackground and Objectives Androgen deprivation therapy (ADT) remains the primary treatment for advanced prostate cancer. However, most patients relapse within 18–24 months, progressing to castration-resistant prostate cancer (CRPC) which is currently ...
Hua Jiang +3 more
doaj +2 more sources