Citation: Hao-Tian Li, Shi-Yong Fan, Zhi-Ping Li, Fang-Lin Yu, Xiao-Qin Hu, Jing-Chao Cheng, Ping Zhang, Bo-Hua Zhong, Wei-Guo Shi. Synthesis and evaluation of novel α-aminoamides with substituted benzene scaffold for the treatment of neuropathic pain[J]. Chinese Chemical Letters, ;2016, 27(10): 1630-1634. doi: 10.1016/j.cclet.2016.06.034 shu

Synthesis and evaluation of novel α-aminoamides with substituted benzene scaffold for the treatment of neuropathic pain

Beijing Institute of Pharmacology & Toxicology, Beijing 100850, China

Corresponding author: Bo-Hua Zhong, bohuazhong@yahoo.com Wei-Guo Shi, shiwg1988@126.com
Received Date: 6 May 2016
Revised Date: 16 June 2016
Accepted Date: 23 June 2016
Available Online: 1 October 2016

Figures(4)

Small molecule sodium ion channel blockers with a pharmacophore of α-aminoamide have exhibited anti-allodynia effects on neuropathic pain. A library of new α-aminoamide derivatives containing a scaffold of substituted benzene were designed and synthesized. These compounds were evaluated in mice formalin model and they exhibited significant analgesic activities. However, the anti-allodynia mechanism of these compounds remains unclear; some of the target compounds can only moderately inhibit the sodium ion channel, Nav1.7, in a whole-cell patch clamp assay. These results suggest that introduction of the moiety of substituted benzene to α-aminoamide derivatives can improve their bioactivity and further study is warranted.
- Neuropathic pain,
- α-Aminoamide derivatives,
- Voltage-gated sodium channel blockers,
- Theory of bioisosterism
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