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
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 ...
Andrzej Bojarski +2 more
exaly +3 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 +9 more
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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 +6 more
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Bioactive conformation of 1-arylpiperazines at central serotonin receptors
Journal of Medicinal Chemistry, 1985 A number of 1-arylpiperazines have been characterized as direct-acting serotonin agonists. Conformational parameters of this class that may affect receptor recognition and binding have been examined through the analysis of X-ray data and synthesis of rigid analogues.
J R, Huff +5 more
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Arylpiperazines with Affinity Toward a1-Adrenergic Receptors
Current Medicinal Chemistry, 2002 In the last years, alpha(1) adrenoceptors (alpha(1)-AR) have been the subject of intense research, in part because receptor-binding studies and molecular biology have opened up new aspects of understanding but also because of the potential to find new drugs possibly acting toward pathophysiological processes where alpha(1)-AR are involved, such as ...
MANETTI F. +3 more
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Pharmacological evaluation of selected arylpiperazines with atypical antipsychotic potential
Bioorganic & Medicinal Chemistry Letters, 2004 Six active compounds, among previously synthesized and screened arylpiperazines, were selected and evaluated for the binding affinity to rat dopamine, serotonin and alpha(1) receptors. Two compounds with benztriazole group had a 5-HT(2A)/D(2) binding ratio characteristic for atypical neuroleptics (>1, pK(i) values).
Tomić, Mirko +7 more
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6-[2-(4-arylpiperazin-1-yl)ethyl]-4-halo-1,3-dihydro-2h-benzimidazole-2-thiones: Synthesis and pharmacological evaluation [PDF]
Journal of the Serbian Chemical Society, 2007 Eight new compounds with halogen atom introduced into the benzimidazole- 2-thione dopaminergic pharmacophore of 5-[2-(4-arylpiperazin-1-yl)ethyl]-1,3-dihydro- 2H-benzimidazole-2-thiones with the arylpiperazine part of the molecule being selected ...
Andrić Deana +5 more
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Synthesis and pharmacological evaluation of N-{4-[2-(4-arylpiperazin-1- yl)ethyl]phenyl} arylamides [PDF]
, 2019 Serotonin 5HT1a receptor belongs to a class of G-protein coupled receptors. It serves as a potential target for neurological disorders such as depression, anxiety etc.
Dukic-Stefanovic, Sladjana +5 more
core +6 more sources
Antimalarials based on the arylpiperazine privileged substructure [PDF]
, 2005 Based on a previous study, arylpiperazines (2-chlorophenylpiperazine, 2-ethoxyphenylpiperazine and phenylpiperazine) were found to be significantly more potent against the chloroquine-resistant (K1) strain than against the chloroquine-sensitive(DIO) strain.
Molyneaux, Carrie-Anne
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