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Synthesis and Evaluation of Novel α-Aminoamides Containing Benzoheterocyclic Moiety for the Treatment of Pain
- Source :
- Molecules, Molecules, Vol 26, Iss 1716, p 1716 (2021), Volume 26, Issue 6
- Publication Year :
- 2021
- Publisher :
- MDPI, 2021.
-
Abstract
- Novel α-aminoamide derivatives containing different benzoheterocyclics moiety were synthesized and evaluated as voltage-gated sodium ion channels blocks the treatment of pain. Compounds 6a, 6e, and 6f containing the benzofuran group displayed more potent in vivo analgesic activity than ralfinamide in both the formalin test and the writhing assay. Interestingly, they also exhibited potent in vitro anti-Nav1.7 and anti-Nav1.8 activity in the patch-clamp electrophysiology assay. Therefore, compounds 6a, 6e, and 6f, which have inhibitory potency for two pain-related Nav targets, could serve as new leads for the development of analgesic medicines.
- Subjects :
- α-aminoamides
Male
sodium channel blocker
Analgesic
Pharmaceutical Science
Pain
Pharmacology
Nav1.7
Nav1.8
Article
Analytical Chemistry
lcsh:QD241-441
NAV1.8 Voltage-Gated Sodium Channel
03 medical and health sciences
chemistry.chemical_compound
Mice
0302 clinical medicine
Sodium channel blocker
lcsh:Organic chemistry
In vivo
Drug Discovery
Moiety
Animals
Physical and Theoretical Chemistry
Benzofuran
030304 developmental biology
0303 health sciences
Analgesics
Chemistry
Sodium channel
Ralfinamide
Organic Chemistry
NAV1.7 Voltage-Gated Sodium Channel
Amides
In vitro
dual channel inhibitors
Chemistry (miscellaneous)
Molecular Medicine
Drug Evaluation
030217 neurology & neurosurgery
Sodium Channel Blockers
Subjects
Details
- Language :
- English
- ISSN :
- 14203049
- Volume :
- 26
- Issue :
- 6
- Database :
- OpenAIRE
- Journal :
- Molecules
- Accession number :
- edsair.doi.dedup.....b7668d78f9efe365608cc2c8ee926c45