کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1362989 | 981500 | 2010 | 5 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Identification of a new biaryl scaffold generating potent renin inhibitors Identification of a new biaryl scaffold generating potent renin inhibitors](/preview/png/1362989.png)
The discovery and SAR of a series of potent renin inhibitors possessing a novel biaryl scaffold are described herein. Molecular modeling revealed that the cyclopropylamide spacer present in 1 can be replaced by a simple, substituted aromatic ring such as a toluene in 2. The resulting compounds exhibit subnanomolar renin IC50 and good oral bioavailability in rats.
The discovery and SAR of a series of potent renin inhibitors possessing a novel biaryl scaffold are described herein. Molecular modeling revealed that the cyclopropylamide spacer present in our lead compound can be replaced by a simple, substituted aromatic ring such as a toluene. The resulting compounds exhibit subnanomolar renin IC50 and good oral bioavailability in rats.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 19, 1 October 2010, Pages 5822–5826