کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1392891 | 1501163 | 2012 | 13 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Discovery, design and synthesis of Y-shaped peroxisome proliferator-activated receptor δ agonists as potent anti-obesity agents in vivo
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Discovery, design and synthesis of Y-shaped peroxisome proliferator-activated receptor δ agonists as potent anti-obesity agents in vivo Discovery, design and synthesis of Y-shaped peroxisome proliferator-activated receptor δ agonists as potent anti-obesity agents in vivo](/preview/png/1392891.png)
چکیده انگلیسی
We have discovered and demonstrated the in vitro and in vivo PPARδ-selective activity of novel Y-shaped agonists. These compounds activated hPPARδ with EC50 values between 1 and 523 nM. Surprisingly, compounds 10a, 11d, 11e and 11f were the most potent and most selective hPPARδ agonists with 104-fold selectivity over the other two subtypes, namely, hPPARα and hPPARγ. The PPARδ ligands 10a, 11e and 11f showed good bioavailability and in vivo efficacy.
Figure optionsDownload as PowerPoint slideHighlights
► We synthesized a series of Y-shaped analogs with alkyl and arylalkyl substituents.
► Compounds 10a, 11d, 11e and 11f displayed excellent selectivity and potency.
► Selective PPARδ agonists showed good bioavailability and in vivo efficacy.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Medicinal Chemistry - Volume 53, July 2012, Pages 190–202
Journal: European Journal of Medicinal Chemistry - Volume 53, July 2012, Pages 190–202
نویسندگان
Jungyeob Ham, Hoosang Hwang, Euno Kim, Jeong-ah Kim, Sung Jin Cho, Jaeyoung Ko, Woojin Lee, Jaehwan Lee, Harish Holla, Joydeep Banerjee, Seokho Kim, Inho Yang, Hyun Joo Lee, Kyoungjin Shin, Hyukjae Choi, Sang-Jip Nam, Jungae Tak, Dongyup Hahn,