کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1371980 | 981863 | 2009 | 7 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Discovery of novel diarylketoxime derivatives as selective and orally active melanin-concentrating hormone 1 receptor antagonists
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله

چکیده انگلیسی
Optimization of the lead 2a led to the identification of a novel diarylketoxime class of melanin-concentrating hormone 1 receptor (MCH-1R) antagonists. Our focus was directed toward improvement of hERG activity and metabolic stability. The representative derivative 4b showed potent and dose-dependent body weight reduction in diet-induced obese (DIO) C57BL/6J mice after oral administration. The synthesis and structure–activity relationships of the novel diarylketoxime MCH-1R antagonists are described.
The identification of selective and orally active MCH-1R antagonist 4b is reported.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 18, 15 September 2009, Pages 5339–5345
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 18, 15 September 2009, Pages 5339–5345
نویسندگان
Takao Suzuki, Minoru Kameda, Makoto Ando, Hiroshi Miyazoe, Etsuko Sekino, Satoru Ito, Kouta Masutani, Kaori Kamijo, Akihiro Takezawa, Minoru Moriya, Masahiko Ito, Junko Ito, Kazuho Nakase, Hiroko Matsushita, Akane Ishihara, Norihiro Takenaga,