4-苄基哌啶羧酰胺作为5-羟色胺和去甲肾上腺素双重再摄取抑制剂的设计与合成
Design and synthesis of 4-benzylpiperidine carboxamides as dual serotonin and norepinephrine reuptake inhibitors.
作者信息
Paudel Suresh, Cao Yongkai, Guo Shuohan, An Byeongkwan, Kim Kyeong-Man, Cheon Seung Hoon
机构信息
College of Pharmacy and Research Institute of Drug Development, Chonnam National University, Gwangju 61186, Republic of Korea.
Jeonnam Development Institute for Korean Traditional Medicine, 288, Udeuraendeu-gil, Anyang-myeon, Jangheung-gun, Jeollanam-do 59338, Republic of Korea.
出版信息
Bioorg Med Chem. 2015 Oct 1;23(19):6418-26. doi: 10.1016/j.bmc.2015.08.022. Epub 2015 Aug 20.
A series of 4-benzylpiperidine carboxamides were designed and synthesized, and tested for their dual (serotonin and norepinephrine) reuptake inhibition. The synthesis of 4-benzylpiperidine carboxamides involved two main steps: amidation and substitution. Derivatives with 3 carbon linker displayed better activity than with 2 carbon linker. 4-Biphenyl- and 2-naphthyl-substituted derivatives 7e and 7j showed greater dual reuptake inhibition than standard drug venlafaxine HCl.
设计并合成了一系列4-苄基哌啶甲酰胺，并对其双重（5-羟色胺和去甲肾上腺素）再摄取抑制作用进行了测试。4-苄基哌啶甲酰胺的合成涉及两个主要步骤：酰胺化和取代反应。具有3个碳原子连接基的衍生物比具有2个碳原子连接基的衍生物表现出更好的活性。4-联苯基和2-萘基取代的衍生物7e和7j比标准药物盐酸文拉法辛表现出更强的双重再摄取抑制作用。
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