کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1374151 | 981914 | 2009 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Identification of novel and orally active spiroindoline NPY Y5 receptor antagonists
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Identification of novel and orally active spiroindoline NPY Y5 receptor antagonists Identification of novel and orally active spiroindoline NPY Y5 receptor antagonists](/preview/png/1374151.png)
چکیده انگلیسی
A series of spiroindoline-3,4′-piperidine derivatives were synthesized and evaluated for their binding affinities and antagonistic activities at Y5 receptors. Potent Y5 antagonists were tested for their oral bioavailabilities and brain penetration in rats. Some of the antagonists showed good oral bioavailability and/or good brain penetration. In particular, compound 6e was orally bioavailable and brain penetrant, and oral administration of 6e inhibited bPP-induced food intake in rats with a minimum effective dose of 10 mg/kg.
A series of potent and orally active spiroindoline-3,4′-piperidine derivatives NPY Y5 receptor antagonists are described.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 6, 15 March 2009, Pages 1564–1568
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 6, 15 March 2009, Pages 1564–1568
نویسندگان
Toshihiro Sakamoto, Minoru Moriya, Yuji Haga, Toshiyuki Takahashi, Takunobu Shibata, Osamu Okamoto, Katsumasa Nonoshita, Hidefumi Kitazawa, Masayasu Hidaka, Akira Gomori, Hisashi Iwaasa, Akane Ishihara, Akio Kanatani, Takehiro Fukami, Ying-Duo Gao,