• Title/Summary/Keyword: Arylpiperazine

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Rapid Synthesis of Arylpiperazine Derivatives for Imaging 5-HT1A Receptor under Microwave Irradiation

  • Park, Sang-Hyun;Gwon, Hui-Jeong;Lee, Hyo-Sun;Park, Kyung-Bae
    • Bulletin of the Korean Chemical Society
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    • v.26 no.11
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    • pp.1701-1705
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    • 2005
  • We have established an efficient method for the synthesis of the arylpiperazine derivatives in which the acylation of 2-aminopyridine, the coupling reaction of the acyl compound with piperazines, and reduction of the arylpiperazines were performed under a microwave irradiation (300 W) to afford the corresponding target compounds in quantitative yields. In all cases, the reaction times were remarkably reduced when compared with those of the conventional method.

Synthesis and Biological Activities of (4-Arylpiperazinyl)piperidines as Nonpeptide BACE 1 Inhibitors

  • Boja, Poojary;Won, Sun-Woo;Suh, Dong-Hoon;Chu, Jeong-Hyun;Park, Woo-Kyu;Lim, Hee-Jong
    • Bulletin of the Korean Chemical Society
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    • v.32 no.4
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    • pp.1249-1252
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    • 2011
  • Inhibition of BACE 1 activity is considered as a promising therapeutic target for Alzheimer's Disease (AD). Synthesis and inhibitory activities of (4-arylpiperazinyl)piperidines by bioisosteric replacement of a biaryl group with an arylpiperazine as BACE 1 inhibitors are described. The resulting (4-arylpiperazinyl)piperidines represent novel nonpeptide BACE 1 inhibitors with improved in vitro potency.

99mTc(CO)3-Labeled Histidine-Arylpiperazines as Potential Radiotracers for a Neuroreceptor Targeting

  • Choi, Kang-hyuk;Hong, Young-Don;Choi, Ok-Ja;Choi, Sun-Ju
    • Bulletin of the Korean Chemical Society
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    • v.27 no.8
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    • pp.1189-1193
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    • 2006
  • In order to develop radiopharmaceuticals for targeting a serotonin receptor such as $5-HT_{1A}$, histidine-$C_n$-arylpiperazines (AP) (C = alkyl, n = 2, 3, 4) were prepared in five steps with yields of 25%, 37% and 51%, respectively, and radiolabeled with the $[^{99m}Tc(CO)_3(H_2O)+3]^+$. The $^{99m}Tc(CO)_3$-Histidine-Cn-APs were prepared with a high yield (>99%) and characterized as a tridentate complex with a neutral charge to pass through the blood-brain barrier (BBB). The rhenium complexes with $Re(CO)_3$ were also synthesised and comparative experiments were achieved to evaluate the nature of the $^{99m}Tc$ complexes.