Discovery of morpholine-based aryl sulfonamides as Nav1.7 inhibitors.
Bioorg Med Chem Lett
; 28(5): 958-962, 2018 03 01.
Article
em En
| MEDLINE
| ID: mdl-29439904
ABSTRACT
Replacement of the piperidine ring in the lead benzenesulfonamide Nav1.7 inhibitor 1 with a weakly basic morpholine core resulted in a significant reduction in Nav1.7 inhibitory activity, but the activity was restored by shortening the linkage from methyleneoxy to oxygen. These efforts led to a series of morpholine-based aryl sulfonamides as isoform-selective Nav1.7 inhibitors. This report describes the synthesis and SAR of these analogs.
Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Sulfonamidas
/
Morfolinas
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Canal de Sódio Disparado por Voltagem NAV1.7
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Bloqueadores do Canal de Sódio Disparado por Voltagem
Idioma:
En
Ano de publicação:
2018
Tipo de documento:
Article