کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1376632 | 981962 | 2008 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
5-Aryluracils as potent GnRH antagonists—Characterization of atropisomers
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
Optimization of a series of uracils bearing a 2-fluoro- or 2-chloro-3-methoxyphenyl group at the 5-position resulted in compounds such as 3d and 3f with subnanomolar binding affinity at the human GnRH receptor. While the 2-fluoro-3-methoxyphenyl compound 3a was characterized as a mixture of interchangeable atropisomers, the diastereoisomers of 2-chloro-3-methoxyphenyl analogs were separated. It was found that the aR-atropisomer was much more potent than the aS-isomer based on the X-ray crystal structure of 3h-II.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 11, 1 June 2008, Pages 3344–3349
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 11, 1 June 2008, Pages 3344–3349
نویسندگان
Liren Zhao, Zhiqiang Guo, Yongsheng Chen, Tao Hu, Dongpei Wu, Yun-Fei Zhu, Martin Rowbottom, Timothy D. Gross, Fabio C. Tucci, R. Scott Struthers, Qiu Xie, Chen Chen,