Design and synthesis of 4-benzylpiperidine carboxamides as dual serotonin and norepinephrine reuptake inhibitors

Bioorg Med Chem. 2015 Oct 1;23(19):6418-26. doi: 10.1016/j.bmc.2015.08.022.

Suresh Paudel ¹, Yongkai Cao ¹, Shuohan Guo ¹, Byeongkwan An ², Kyeong-Man Kim ³, Seung Hoon Cheon ⁴

Affiliations

1 College of Pharmacy and Research Institute of Drug Development, Chonnam National University, Gwangju 61186, Republic of Korea.
2 Jeonnam Development Institute for Korean Traditional Medicine, 288, Udeuraendeu-gil, Anyang-myeon, Jangheung-gun, Jeollanam-do 59338, Republic of Korea.
3 College of Pharmacy and Research Institute of Drug Development, Chonnam National University, Gwangju 61186, Republic of Korea. Electronic address: [email protected].
4 College of Pharmacy and Research Institute of Drug Development, Chonnam National University, Gwangju 61186, Republic of Korea. Electronic address: [email protected].

PMID: 26337019 DOI: 10.1016/j.bmc.2015.08.022

Abstract

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.

Keywords

4-Benzylpiperidine carboxamide; Norepinephrine reuptake inhibitor; Serotonin reuptake inhibitor.

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