13078-14-3Relevant articles and documents
Design, synthesis and docking study of 4-arylpiperazine carboxamides as monoamine neurotransmitters reuptake inhibitors
Paudel, Suresh,Sun, Ningning,Khadka, Daulat Bikram,Yoon, Goon,Kim, Kyeong-Man,Cheon, Seung Hoon
, p. 4127 - 4135 (2018/07/21)
Rational drug design method has been used to generate 4-arylpiperazine carboxamides in an effort to develop safer, more potent and effective monoamine neurotransmitters reuptake inhibitors. Out of twenty-seven synthesized compounds, compound 9 displayed potent monoamine neurotransmitter reuptake inhibitory activity against HEK cells transfected with hSERT or hNET. A Surflex-Dock docking model of 9 was also studied.
Exploration of substituted arylpiperazine–tetrazoles as promising dual norepinephrine and dopamine reuptake inhibitors
Paudel, Suresh,Acharya, Srijan,Yoon, Goo,Kim, Kyeong-Man,Cheon, Seung Hoon
, p. 5546 - 5555 (2016/10/22)
In the search for potent dual norepinephrine and dopamine reuptake inhibitors, several substituted arylpiperazine–tetrazoles were designed, synthesized and evaluated for their neurotransmitter reuptake inhibitory activities. Various derivatives exhibited selective and strong neurotransmitter reuptake inhibitory activity. In particular, compounds with a three-carbon linker displayed selective and stronger potency than those with two-carbon and four-carbon linkers. Interestingly, six compounds, 9b, 9c, 9d, 9o, 9q and 9u displayed more effective activity than the standard drug, bupropion. The provided SAR data and potent biological activity can offer useful guidelines for designing dual norepinephrine and dopamine reuptake inhibitors as effective therapeutic agents for treatment of several central nervous system diseases.
Synthesis and biological evaluation of novel N-[3-(4-phenylpip-erazin-1-yl) -propyl]-carboxamide derivatives
Weng, Zhiyong,Gao, Yanping,Zhang, Jiankang,Dong, Xiaowu,Liu, Tao
experimental part, p. 43 - 46 (2011/05/04)
A series of novel N-[3-(4-phenylpiperazin-1-yl)-propyl]-carboxamide derivatives were synthesised and studied for the potential treatment of HIV. These compounds were obtained through the efficient synthetic route that involved microwave assisted synthesis. These new compounds have been characterised by IR,1H NMR, MS and elemental analysis. The cell-cell fusion inhibitory activities of the compounds have also been evaluated.