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Molecules 2016, 21(7), 793; doi:10.3390/molecules21070793

Synthesis and Evaluation of Novel α-Aminoamides Containing an Indole Moiety for the Treatment of Neuropathic Pain

Beijing Institute of Pharmacology & Toxicology, 27 Tai-Ping Road, Beijing 100850, China
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Authors to whom correspondence should be addressed.
Academic Editor: Diego Muñoz-Torrero
Received: 28 April 2016 / Revised: 13 June 2016 / Accepted: 14 June 2016 / Published: 23 June 2016
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [1215 KB, uploaded 23 June 2016]   |  

Abstract

The α-aminoamide family of sodium ion channel blockers have exhibited analgesic effects on neuropathic pain. Here, a series of novel α-aminoamides containing an indole ring were designed and synthesized. These compounds were evaluated in mice using a formalin test and they exhibited significant anti-allodynia activities. However, the analgesic mechanism of these compounds remains unclear; a subset of the synthesized compounds can only moderately inhibit the sodium ion channel, Nav1.7, in a whole-cell patch clamp assay. Overall, these results suggest that introduction of an indole moiety to α-aminoamide derivatives can significantly improve their bioactivity and further study is warranted. View Full-Text
Keywords: neuropathic pain; α-aminoamide derivatives; voltage-gated sodium channel blockers neuropathic pain; α-aminoamide derivatives; voltage-gated sodium channel blockers
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Li, H.; Fan, S.; Cheng, J.; Zhang, P.; Zhong, B.; Shi, W. Synthesis and Evaluation of Novel α-Aminoamides Containing an Indole Moiety for the Treatment of Neuropathic Pain. Molecules 2016, 21, 793.

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