Excavating Precursors from Herb Pairs <i>Polygala tenuifolia</i> and <i>Acori tatarinowii</i>: Synthesis and Anticonvulsant Activity Evaluation of 3,4,5-Trimethoxycinnamic Acid (TMCA) Piperazine Amide Derivatives. [PDF]
Zhao Z, Lei M, Wang Y, Bai Y, Qiao H.
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Rhodanine-Piperazine Hybrids as Potential VEGFR, EGFR, and HER2 Targeting Anti-Breast Cancer Agents. [PDF]
Szczepański J +6 more
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A Series of Novel 1-H-isoindole-1,3(2H)-dione Derivatives as Acetylcholinesterase and Butyrylcholinesterase Inhibitors: In Silico, Synthesis and In Vitro Studies. [PDF]
Krzyżak E +5 more
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The medicinal chemistry of arylpiperazines with potential antidepressant efficacy
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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
Harsha G. Jaisinghani +2 more
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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
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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
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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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Arylpiperazines with Affinity Toward a1-Adrenergic Receptors
Current Medicinal Chemistry, 2002In 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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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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