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Bioorg Med Chem Lett. 2018 Mar 1;28(5):958-962. doi: 10.1016/j.bmcl.2018.01.035. Epub 2018 Feb 1.

Discovery of morpholine-based aryl sulfonamides as Nav1.7 inhibitors.

Author information

1
Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492-7660, USA. Electronic address: yong-jin.wu@bms.com.
2
Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492-7660, USA.

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.

KEYWORDS:

Aryl sulfonamides; Morpholine-based; Na(v)1.7 inhibitor; Pain

PMID:
29439904
DOI:
10.1016/j.bmcl.2018.01.035
[Indexed for MEDLINE]

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