کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10588283 | 981450 | 2011 | 8 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and evaluation of hermitamides A and B as human voltage-gated sodium channel blockers
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
Hermitamides A and B are lipopeptides isolated from a Papau New Guinea collection of the marine cyanobacterium Lyngbya majuscula. We hypothesized that the hermitamides are ligands for the human voltage-gated sodium channel (hNaV) based on their structural similarity to the jamaicamides. Herein, we describe the nonracemic total synthesis of hermitamides A and B and their epimers. We report the ability of the hermitamides to displace [3H]-BTX at 10 μM more potently than phenytoin, a clinically used sodium channel blocker. We also present a potential binding mode for (S)-hermitamide B in the BTX-binding site and electrophysiology showing that these compounds are potent blockers of the hNav1.2 voltage-gated sodium channel.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 19, Issue 14, 15 July 2011, Pages 4322-4329
Journal: Bioorganic & Medicinal Chemistry - Volume 19, Issue 14, 15 July 2011, Pages 4322-4329
نویسندگان
Eliseu O. De Oliveira, Kristin M. Graf, Manoj K. Patel, Aparna Baheti, Hye-Sik Kong, Linda H. MacArthur, Sivanesan Dakshanamurthy, Kan Wang, Milton L. Brown, Mikell Paige,