کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1374779 | 981924 | 2008 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Novel 2-imidazoles as potent, selective and CNS penetrant α1A adrenoceptor partial agonists
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Novel 2-imidazoles as potent, selective and CNS penetrant α1A adrenoceptor partial agonists Novel 2-imidazoles as potent, selective and CNS penetrant α1A adrenoceptor partial agonists](/preview/png/1374779.png)
چکیده انگلیسی
A novel series of central nervous system (CNS) penetrant indane 2-imidazoles have been identified as potent, partial agonists of the α1A adrenergic receptor, having good selectivity over the α1B, α1D and α2 sub-types. A key structural motif to impart selectivity is a methylene spacer between the indane and a pendant substituent, which includes heterocycles, sulphones and ethers. Introduction of an ortho-halogen to this group led to a lowering of intrinsic efficacy (Emax).
A series of novel 2-imidazoles is described, which combine potent and selective α1A partial agonist pharmacology with good CNS penetration.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 24, 15 December 2008, Pages 6437–6440
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 24, 15 December 2008, Pages 6437–6440
نویسندگان
Lee R. Roberts, Justin Bryans, Kelly Conlon, Gordon McMurray, Alan Stobie, Gavin A. Whitlock,