Results 111 to 120 of about 629 (164)
Interaction of Arylpiperazines With the Dopamine Receptor D2 Binding Site [PDF]
The docking of several 1-benzyl-4-arylpiperazines to the dopamine receptor (DAR) D-2 was examined. The results demonstrated that the interaction of protonated NI of the piperazine ring with Asp 86 (III.32) and edge-to-face interactions of the aromatic ...
Vladimir Sukalovic +2 more
exaly +5 more sources
Synthesis of 2‐Benzothienyl Carbonyl 4‐Arylpiperazines as Novel Delavirdine Analogs [PDF]
A novel series of 2-benzothienyl carbonyl arylpiperazines (6a-f) was synthesized as potential HIV nonnucleoside reverse transcriptase inhibitors (NNRTIs).
Ramiro Araya-Maturana +1 more
exaly +1 more source
Arylpiperazines 2–11 were synthesized, and their biological profiles at α1-adrenergic receptors (α1-ARs) assessed by binding assays in CHO cells expressing human cloned subtypes and by functional experiments in isolated rat vas deferens (α1A), spleen ...
Andressa Souza de Oliveira +2 more
exaly +3 more sources
Synthesis of Benzo[b]Thiophene Carboxamides Connected to 4‐Arylpiperazines Through a Benzylic Spacer: Potential Ligands With 5‐HT1A Binding Affinity [PDF]
New benzothiophene arylpiperazine derivatives 8 (a-f) were synthesized as potential serotoninergic agents with 5-HT1A receptor affinity. Preparation of the derivatives was performed by treating N-[2-(chloromethyl)phenyl]-4,7-dimethoxybenzo[b]thiophene-2 ...
Roberto Acevedo +2 more
exaly +1 more source
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Asymmetric synthesis of 2-arylpiperazines
Bioorganic & Medicinal Chemistry Letters, 2014An asymmetric synthesis of 2-arylpiperazines starting from phenacyl bromides, a variety of which are easily available, has been established. The synthesis features a CBS reduction of phenacyl bromide to provide optically enriched compounds, an SN2 reaction of 1,2,3-oxathiazolidine 2-oxides with an azide anion with invert of configuration, and ...
Satoshi, Yokoshima +4 more
openaire +2 more sources
Molecular Crystals and Liquid Crystals, 2017
Arylpiperazine derivatives referred in this article possessed antitumor activity, which were synthesized and crystallized through the gradual evaporation process.
Zhou, Jinhui +4 more
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Arylpiperazine derivatives referred in this article possessed antitumor activity, which were synthesized and crystallized through the gradual evaporation process.
Zhou, Jinhui +4 more
openaire +2 more sources
Progress in arylpiperazine synthesis by the catalytic amination reaction
Bioorganic & Medicinal Chemistry, 2002Careful base and solvent optimization for catalytic amination is described. A Pd-catalyzed amination between some arylbromide and unprotected piperazine (1equiv) was efficiently carried out with Pd/BINAP catalyst in a toluene-DBU solvent system, which is useful for the one-pot preparation of unsymmetrical piperazine through amination and in-situ N ...
Yasuhiro, Torisawa +2 more
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In-vivo metabolism of 4-substituted arylpiperazines to pharmacologically active 1-arylpiperazines.
Bollettino chimico farmaceutico, 1991A common metabolic process of 4-substituted arylpiperazine pharmacological agents is cleavage of the side-chain to yield 1-arylpiperazines. These metabolites are a well-known class of centrally active compounds and their formation may therefore be a pharmacologically significant pathway, at least in certain species, for derivates that undergo extensive
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Arylpiperazine Derivatives Acting at 5-HT1A Receptors
Current Medicinal Chemistry, 2002Serotonin (5-hydroxytryptamine, 5-HT) is one of the most attractive targets for medicinal chemists. Among 5-HTRs, the 5-HT(1A) subtype is the best studied and it is generally accepted that it is involved in psychiatric disorders such as anxiety and depression. Several structurally different compounds are known to bind 5-HT(1A)R sites.
M L, López-Rodríguez +4 more
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Soluble polymer-supported synthesis of arylpiperazines
Tetrahedron Letters, 1998Abstract A method for soluble, inexpensive polymer-supported synthesis of piperazine and piperidine libraries on the basis of nucleophilic aryl substitution (S n Ar) and N-acylation is reported. Asymmetric N, N′-disubstituted piperazine and piperidine derivatives, that are potential drug candidates, can be synthesized in quantitative yields and ...
Pi-Chi Pan, Chung-Ming Sun
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