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  • Macsari, Istvan (author)

Phenyl isoxazole voltage-gated sodium channel blockers : structure and activity relationship

  • Article/chapterEnglish2011

Publisher, publication year, extent ...

  • Elsevier BV,2011
  • printrdacarrier

Numbers

  • LIBRIS-ID:oai:DiVA.org:uu-155602
  • https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-155602URI
  • https://doi.org/10.1016/j.bmcl.2011.05.041DOI

Supplementary language notes

  • Language:English
  • Summary in:English

Part of subdatabase

Classification

  • Subject category:ref swepub-contenttype
  • Subject category:art swepub-publicationtype

Notes

  • Blocking of certain sodium channels is considered to be an attractive mechanism to treat chronic pain conditions. Phenyl isoxazole carbamate 1 was identified as a potent and selective Na(V)1.7 blocker. Structural analogues of 1, both carbamates, ureas and amides, were proven to be useful in establishing the structure-activity relationship and improving ADME related properties. Amide 24 showed a good overall in vitro profile, that translated well to rat in vivo PK.

Subject headings and genre

Added entries (persons, corporate bodies, meetings, titles ...)

  • Sandberg, Lars (author)
  • Besidski, Yevgeni (author)
  • Gravenfors, Ylva (author)
  • Ginman, Tobias (author)
  • Bylund, Johan (author)
  • Bueters, Tjerk (author)
  • Eriksson, Anders B. (author)
  • Lund, Per-Eric (author)
  • Venyike, Elisabet (author)
  • Arvidsson, Per I.Uppsala universitet,Avdelningen för organisk farmaceutisk kemi(Swepub:uu)pearv049 (author)
  • Uppsala universitetAvdelningen för organisk farmaceutisk kemi (creator_code:org_t)

Related titles

  • In:Bioorganic & Medicinal Chemistry Letters: Elsevier BV21:13, s. 3871-38760960-894X1464-3405

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