کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1397536 | 1501177 | 2011 | 5 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Discovery of novel SCD1 inhibitors: 5-Alkyl-4,5-dihydro-3H-spiro[1,5-benzoxazepine-2,4′-piperidine] analogs Discovery of novel SCD1 inhibitors: 5-Alkyl-4,5-dihydro-3H-spiro[1,5-benzoxazepine-2,4′-piperidine] analogs](/preview/png/1397536.png)
Expansion of the 6-membered ring and subsequent fine-tuning of the newly obtained 7-membered spiropiperidine structure resulted in the discovery of a series of novel and potent SCD1 inhibitors. Preliminary SAR was explored by modifying an alkyl chain on the azepine nitrogen and resulted in the identification of a highly potent SCD1 inhibitor: 6-[5-(cyclopropylmethyl)-4,5-dihydro-1′H,3H-spiro[1,5-benzoxazepine-2,4′-piperidin]-1′-yl]-N-(2-hydroxy-2-pyridin-3-ylethyl)pyridazine-3-carboxamide (9). Compound 9 exhibited an IC50 value of 0.01 μM against human SCD1.
Expansion of the 6-membered ring and subsequent fine-tuning of the newly obtained 7-membered spiropiperidine structure resulted in the discovery of novel and potent SCD1 inhibitors.Figure optionsDownload as PowerPoint slideHighlights
► Expansion of the 6-membered ring resulted in the discovery of novel SCD1 inhibitors.
► Preliminary SAR resulted in the identification of a highly potent SCD1 inhibitor.
► Compound 9 exhibited an IC50 value of 0.01 μM against human SCD1.
Journal: European Journal of Medicinal Chemistry - Volume 46, Issue 5, May 2011, Pages 1892–1896