کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1393241 | 1501195 | 2009 | 13 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Heterocyclic replacement of the central phenyl core of diamine-based histamine H3 receptor antagonists
دانلود مقاله + سفارش ترجمه
دانلود مقاله ISI انگلیسی
رایگان برای ایرانیان
کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Heterocyclic replacement of the central phenyl core of diamine-based histamine H3 receptor antagonists Heterocyclic replacement of the central phenyl core of diamine-based histamine H3 receptor antagonists](/preview/png/1393241.png)
چکیده انگلیسی
A series of small molecules consisting of a heterocyclic core flanked by two basic functionalities were synthesized and screened for in vitro affinity at the human histamine H3 receptor (hH3R). Nine of the twenty-eight compounds tested were found to possess a hH3R Ki of less than 5 nM and consisted of a diverse range of central hetero-aromatic linkers (pyridine, pyrazine, oxazole, isoxazole, thiazole, furan, thiophene, and pyrrole). One member of this series, (4-isopropyl-piperazin-1-yl)-(6-piperidin-1-ylmethyl-pyridin-3-yl)-methanone (37), was found to be a high affinity, selective antagonist that crosses the blood-brain barrier and occupies H3 receptors after oral administration in the rat.
Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Medicinal Chemistry - Volume 44, Issue 11, November 2009, Pages 4413–4425
Journal: European Journal of Medicinal Chemistry - Volume 44, Issue 11, November 2009, Pages 4413–4425
نویسندگان
Devin M. Swanson, Chandra R. Shah, Brian Lord, Kirsten Morton, Lisa K. Dvorak, Curt Mazur, Richard Apodaca, Wei Xiao, Jamin D. Boggs, Mark Feinstein, Sandy J. Wilson, Ann J. Barbier, Pascal Bonaventure, Timothy W. Lovenberg, Nicholas I. Carruthers,