کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1397841 | 1501191 | 2010 | 7 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Discovery of benzhydrylpiperazine derivatives as CB1 receptor inverse agonists via privileged structure-based approach Discovery of benzhydrylpiperazine derivatives as CB1 receptor inverse agonists via privileged structure-based approach](/preview/png/1397841.png)
The present study describes the identification via privileged structure-based approach of the benzhydrylpiperazine moiety as a potential scaffold to develop novel CB1 receptor modulators. Efficient structural optimization of the initial four hit compounds led to a high quality lead series, represented by compound 6c. Compound 6c is a highly potent and selective CB1 receptor inverse agonist that is able to reduce body weight in diet-induced obese Sprague–Dawley rats. The preparation of privileged structure-based library, the progression from hit to lead, the structure–activity relationships in the lead series and in vitro and in vivo activity of compound 6c are discussed.
A series of benzhydrylpiperazine derivatives was identified as a novel class of CB1 receptor inverse agonists utilizing privileged structure approach.Figure optionsDownload as PowerPoint slide
Journal: European Journal of Medicinal Chemistry - Volume 45, Issue 3, March 2010, Pages 1133–1139