کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1359699 | 981410 | 2011 | 11 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Discovery of novel phenylpyridone derivatives as potent and selective MCH1R antagonists
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Discovery of novel phenylpyridone derivatives as potent and selective MCH1R antagonists Discovery of novel phenylpyridone derivatives as potent and selective MCH1R antagonists](/preview/png/1359699.png)
چکیده انگلیسی
The design, synthesis and structure–activity relationships of a novel class of N-phenylpyridone MCH1R antagonists are described. The core part of the N-phenylpyridone structure was newly designed and the side chain moieties that were attached to the core part were extensively explored. As a result of optimization of the N-phenylpyridone leads, we successfully developed the orally available, and brain-penetrable MCH1R selective antagonist 7c, exhibiting excellent anti-obese effect in diet-induced obese (DIO) mice.
The synthesis and evaluation of a series of phenylpyridone derivatives as MCH1R antagonists are described.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 19, Issue 2, 15 January 2011, Pages 883–893
Journal: Bioorganic & Medicinal Chemistry - Volume 19, Issue 2, 15 January 2011, Pages 883–893
نویسندگان
Yuji Haga, Sayaka Mizutani, Akira Naya, Hiroyuki Kishino, Hisashi Iwaasa, Masahiko Ito, Junko Ito, Minoru Moriya, Nagaaki Sato, Norihiro Takenaga, Akane Ishihara, Shigeru Tokita, Akio Kanatani, Norikazu Ohtake,