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Discovery of morpholine-based aryl sulfonamides as Nav1.7 inhibitors.
Wu, Yong-Jin; Guernon, Jason; McClure, Andrea; Venables, Brian; Rajamani, Ramkumar; Robbins, Kevin J; Knox, Ronald J; Matchett, Michele; Pieschl, Rick L; Herrington, James; Bristow, Linda J; Meanwell, Nicholas A; Olson, Richard; Thompson, Lorin A; Dzierba, Carolyn.
Afiliação
  • Wu YJ; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492-7660, USA. Electronic address: yong-jin.wu@bms.com.
  • Guernon J; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492-7660, USA.
  • McClure A; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492-7660, USA.
  • Venables B; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492-7660, USA.
  • Rajamani R; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492-7660, USA.
  • Robbins KJ; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492-7660, USA.
  • Knox RJ; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492-7660, USA.
  • Matchett M; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492-7660, USA.
  • Pieschl RL; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492-7660, USA.
  • Herrington J; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492-7660, USA.
  • Bristow LJ; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492-7660, USA.
  • Meanwell NA; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492-7660, USA.
  • Olson R; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492-7660, USA.
  • Thompson LA; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492-7660, USA.
  • Dzierba C; Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492-7660, USA.
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.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Sulfonamidas / Morfolinas / Canal de Sódio Disparado por Voltagem NAV1.7 / Bloqueadores do Canal de Sódio Disparado por Voltagem Idioma: En Ano de publicação: 2018 Tipo de documento: Article
Texto completo
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PubMed Links
Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Sulfonamidas / Morfolinas / Canal de Sódio Disparado por Voltagem NAV1.7 / Bloqueadores do Canal de Sódio Disparado por Voltagem Idioma: En Ano de publicação: 2018 Tipo de documento: Article