Literature DB >> 26337019

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

Suresh Paudel1, Yongkai Cao1, Shuohan Guo1, Byeongkwan An2, Kyeong-Man Kim3, Seung Hoon Cheon4.   

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.
Copyright © 2015 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  4-Benzylpiperidine carboxamide; Norepinephrine reuptake inhibitor; Serotonin reuptake inhibitor

Mesh:

Substances:

Year:  2015        PMID: 26337019     DOI: 10.1016/j.bmc.2015.08.022

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  3 in total

1.  Visible-Light Photoredox-Catalyzed Amidation of Benzylic Alcohols.

Authors:  Silvia Gaspa; Andrea Farina; Mariella Tilocca; Andrea Porcheddu; Luisa Pisano; Massimo Carraro; Ugo Azzena; Lidia De Luca
Journal:  J Org Chem       Date:  2020-07-23       Impact factor: 4.354

2.  Design, Synthesis, and Functional Evaluation of 1, 5-Disubstituted Tetrazoles as Monoamine Neurotransmitter Reuptake Inhibitors.

Authors:  Suresh Paudel; Shuji Wang; Eunae Kim; Dooti Kundu; Xiao Min; Chan Young Shin; Kyeong-Man Kim
Journal:  Biomol Ther (Seoul)       Date:  2022-03-01       Impact factor: 4.634

3.  Structural Requirements for Modulating 4-Benzylpiperidine Carboxamides from Serotonin/Norepinephrine Reuptake Inhibitors to Triple Reuptake Inhibitors.

Authors:  Suresh Paudel; Eunae Kim; Anlin Zhu; Srijan Acharya; Xiao Min; Seung Hoon Cheon; Kyeong-Man Kim
Journal:  Biomol Ther (Seoul)       Date:  2021-07-01       Impact factor: 4.634

  3 in total

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