Results 111 to 120 of about 629 (164)

Interaction of Arylpiperazines With the Dopamine Receptor D2 Binding Site [PDF]

open access: yesArzneimittelforschung, 2005
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]

open access: yesSynthetic Communications, 2007
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

Synthesis and Structure–Activity Relationships of Novel Arylpiperazines as Potent Antagonists of α1-Adrenoceptor

open access: yesEuropean Journal of Medicinal Chemistry, 2016
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]

open access: yesSynthetic Communications, 2007
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

Asymmetric synthesis of 2-arylpiperazines

Bioorganic & Medicinal Chemistry Letters, 2014
An 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

Synthesis and crystal structures of arylpiperazine compounds (“synthesis crystal structures arylpiperazine” for short)

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
openaire   +2 more sources

Progress in arylpiperazine synthesis by the catalytic amination reaction

Bioorganic & Medicinal Chemistry, 2002
Careful 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
openaire   +2 more sources

In-vivo metabolism of 4-substituted arylpiperazines to pharmacologically active 1-arylpiperazines.

Bollettino chimico farmaceutico, 1991
A 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
openaire   +2 more sources

Arylpiperazine Derivatives Acting at 5-HT1A Receptors

Current Medicinal Chemistry, 2002
Serotonin (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
openaire   +2 more sources

Soluble polymer-supported synthesis of arylpiperazines

Tetrahedron Letters, 1998
Abstract 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
openaire   +1 more source

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