کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10583794 | 981310 | 2014 | 18 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Design, synthesis, and structure-activity relationships of a series of novel N-aryl-2-phenylcyclopropanecarboxamide that are potent and orally active orexin receptor antagonists
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کلمات کلیدی
DMFNMPOX1ROrexin receptor antagonistOX2Rtetra-n-butylammonium fluorideTBAFDCMN-methyl-2-pyrrolidoneTHFTBDPSDMSO - DMSON,N-dimethylformamide - N، N-dimethylformamideN,N-diisopropylethylamine - N، N-دییزوپروپیلتیلامینSleep disorder - اختلال خوابElectroencephalogram - الکتروانسفالوگرافیEMG - الکترومیوگرافیelectromyogram - الکترومیوگرافیBenzyl - بنزیلInsomnia - بی خوابیTetrahydrofuran - تتراهیدروفورانtert-butyldiphenylsilyl - ترت بوتیل دی فینیل سیلیلtriethylamine - تری اتیلامینDIAD - دیادDichloromethane - دیکلورمتانDiisopropyl azodicarboxylate - دییزوپروپیل azodicarboxylateDimethyl sulfoxide - دیمتیل سولفواکسیدDIPEA - نخودEEG - نوار مغزیHATU - هاتوHypocretin - هیپوکراتینTEA - چایOrexin 1 receptor - گیرنده اورکسین 1Orexin 2 receptor - گیرنده اورکسین 2
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Design, synthesis, and structure-activity relationships of a series of novel N-aryl-2-phenylcyclopropanecarboxamide that are potent and orally active orexin receptor antagonists Design, synthesis, and structure-activity relationships of a series of novel N-aryl-2-phenylcyclopropanecarboxamide that are potent and orally active orexin receptor antagonists](/preview/png/10583794.png)
چکیده انگلیسی
Herein we describe the design, synthesis, and structure-activity relationships (SARs) of a novel phenylcyclopropane series represented by 7 and 33b as antagonists of orexin 1 and orexin 2 receptors. With 4 serving as the initial lead for the development of orexin antagonists, exploration of SAR resulted in improved binding affinity for orexin 1 and orexin 2 receptors. Among the synthesized compounds, 33b ((â)-N-(5-cyanopyridin-2-yl)-2-[(3,4-dimethoxyphenyl)oxymethyl]-2-phenylcyclopropanecarboxamide) exhibited potent in vitro activity and oral efficacy in animal sleep measurement experiments. The results of our study suggest that compound 33b may serve as a valuable template for the development of new orexin receptor antagonists.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 22, Issue 21, 1 November 2014, Pages 6071-6088
Journal: Bioorganic & Medicinal Chemistry - Volume 22, Issue 21, 1 November 2014, Pages 6071-6088
نویسندگان
Yu Yoshida, Taro Terauchi, Yoshimitsu Naoe, Yuji Kazuta, Fumihiro Ozaki, Carsten T. Beuckmann, Makoto Nakagawa, Michiyuki Suzuki, Ikuo Kushida, Osamu Takenaka, Takashi Ueno, Masahiro Yonaga,