کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10594585 | 981836 | 2012 | 8 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
N-1-Alkyl-2-oxo-2-aryl amides as novel antagonists of the TRPA1 receptor
دانلود مقاله + سفارش ترجمه
دانلود مقاله ISI انگلیسی
رایگان برای ایرانیان
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: N-1-Alkyl-2-oxo-2-aryl amides as novel antagonists of the TRPA1 receptor N-1-Alkyl-2-oxo-2-aryl amides as novel antagonists of the TRPA1 receptor](/preview/png/10594585.png)
چکیده انگلیسی
A series of potent antagonists of the ion channel transient receptor potential A1 (TRPA1) was developed by modifying lead structure 16 that was discovered by high-throughput screening. Based on lead compound 16, a SAR was established, showing a narrow region at the nitro-aromatic R1 moiety and at the warhead, while the R2 side had a much wider scope including ureas and carbamates. Compound 16 inhibits Ca2+-activated TRPA1 currents reversibly in whole cell patch clamp experiments, indicating that under in vivo conditions, it does not react covalently, despite its potentially electrophilic ketone.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 17, 1 September 2012, Pages 5485-5492
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 17, 1 September 2012, Pages 5485-5492
نویسندگان
Karl S.A. Vallin, Karin J. Sterky, Eva Nyman, Jenny Bernström, Rebecka From, Christian Linde, Alexander B.E. Minidis, Andreas Nolting, Katja Närhi, Ellen M. Santangelo, Fernando W. Sehgelmeble, Daniel Sohn, Jennie Strindlund, Dirk Weigelt,