设计、合成及 4-芳基哌嗪甲酰胺类单胺类神经递质再摄取抑制剂的对接研究。
Design, synthesis and docking study of 4-arylpiperazine carboxamides as monoamine neurotransmitters reuptake inhibitors.
机构信息
College of Pharmacy and Research Institute of Drug Development, Chonnam National University, Gwangju 61186, Republic of Korea.
College of Pharmacy and Natural Medicine Research Institute, Mokpo National University, Jeonnam 58554, Republic of Korea.
出版信息
Bioorg Med Chem. 2018 Aug 7;26(14):4127-4135. doi: 10.1016/j.bmc.2018.06.043. Epub 2018 Jul 2.
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.
合理药物设计方法已被用于生成 4-芳基哌嗪甲酰胺，以开发更安全、更有效和更有效的单胺神经递质再摄取抑制剂。在所合成的 27 种化合物中，化合物 9 对转染 hSERT 或 hNET 的 HEK 细胞表现出强烈的单胺神经递质再摄取抑制活性。还研究了 9 的 Surflex-Dock 对接模型。
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