کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1360276 | 981432 | 2009 | 9 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Novel and potent small-molecule urotensin II receptor agonists
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Novel and potent small-molecule urotensin II receptor agonists Novel and potent small-molecule urotensin II receptor agonists](/preview/png/1360276.png)
چکیده انگلیسی
A series of analogs of the non-peptidic urotensin II receptor agonist N-[1-(4-chlorophenyl)-3-(dimethylamino)propyl]-4-phenylbenzamide (FL104) has been synthesized and evaluated pharmacologically. The enantiomers of the two most potent racemic analogues were obtained from the corresponding diastereomeric mandelic amides. In agreement with previously observed SAR, most of the agonist potency resided in the (S) enantiomers. The most potent UII receptor agonist in the new series was (S)-N-[3-dimethylamino-1-(2-naphthyl)propyl]-4-(4-chlorophenyl)benzamide (EC50 = 23 nM at the urotensin II receptor).
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 17, Issue 13, 1 July 2009, Pages 4657–4665
Journal: Bioorganic & Medicinal Chemistry - Volume 17, Issue 13, 1 July 2009, Pages 4657–4665
نویسندگان
Fredrik Lehmann, Erika A. Currier, Bryan Clemons, Lars K. Hansen, Roger Olsson, Uli Hacksell, Kristina Luthman,