A Novel Benzazepinone Sodium Channel Blocker with Oral Efficacy in a Rat Model of Neuropathic Pain
Overview
Authors
Affiliations
A series of benzazepinones were synthesized and evaluated for block of Nav1.7 sodium channels. Compound 30 from this series displayed potent channel block, good selectivity versus other targets, and dose-dependent oral efficacy in a rat model of neuropathic pain.
CF-Cyclobutanes: Synthesis, Properties, and Evaluation as a Unique -Butyl Group Analogue.
Ahunovych V, Klipkov A, Bugera M, Tarasenko K, Trofymchuk S, Razhyk B JACS Au. 2024; 4(11):4507-4517.
PMID: 39610719 PMC: 11600199. DOI: 10.1021/jacsau.4c00864.
Inhibition of Na1.7: the possibility of ideal analgesics.
Kitano Y, Shinozuka T RSC Med Chem. 2022; 13(8):895-920.
PMID: 36092147 PMC: 9384491. DOI: 10.1039/d2md00081d.
Divergent synthesis of benzazepines and bridged polycycloalkanones via dearomative rearrangement.
Shi Q, Liao Z, Liu Z, Wen J, Li C, He J Nat Commun. 2022; 13(1):4402.
PMID: 35906217 PMC: 9338057. DOI: 10.1038/s41467-022-31920-1.
Fluorinated phenylalanines: synthesis and pharmaceutical applications.
Awad L, Ayoup M Beilstein J Org Chem. 2020; 16:1022-1050.
PMID: 32509033 PMC: 7237815. DOI: 10.3762/bjoc.16.91.
Nicolas S, Zoukimian C, Bosmans F, Montnach J, Diochot S, Cuypers E Toxins (Basel). 2019; 11(6).
PMID: 31234412 PMC: 6628435. DOI: 10.3390/toxins11060367.