کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1372918 | 981886 | 2011 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Phenyl isoxazole voltage-gated sodium channel blockers: Structure and activity relationship
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Phenyl isoxazole voltage-gated sodium channel blockers: Structure and activity relationship Phenyl isoxazole voltage-gated sodium channel blockers: Structure and activity relationship](/preview/png/1372918.png)
چکیده انگلیسی
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 NaV1.7 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.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 13, 1 July 2011, Pages 3871–3876
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 13, 1 July 2011, Pages 3871–3876
نویسندگان
Istvan Macsari, Lars Sandberg, Yevgeni Besidski, Ylva Gravenfors, Tobias Ginman, Johan Bylund, Tjerk Bueters, Anders B. Eriksson, Per-Eric Lund, Elisabet Venyike, Per I. Arvidsson,