Phenyl isoxazole voltage-gated sodium channel blockers: structure and activity relationship
2011 (English)In: Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, E-ISSN 1464-3405, Vol. 21, no 13, 3871-3876 p.Article in journal (Refereed) Published
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.
Place, publisher, year, edition, pages
2011. Vol. 21, no 13, 3871-3876 p.
Sodium channel blockers, Na(V)1.7 blocker, Neuropathic pain, Phenyl isoxazoles, Voltage-gated channel
IdentifiersURN: urn:nbn:se:uu:diva-155602DOI: 10.1016/j.bmcl.2011.05.041ISI: 000291474300004OAI: oai:DiVA.org:uu-155602DiVA: diva2:426849