کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1367328 | 981625 | 2006 | 5 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Discovery and synthesis of tetrahydroindolone derived semicarbazones as selective Kv1.5 blockers Discovery and synthesis of tetrahydroindolone derived semicarbazones as selective Kv1.5 blockers](/preview/png/1367328.png)
A novel class of tetrahydroindolone-derived semicarbazones has been discovered as potent Kv1.5 blockers. In in vitro studies, several compounds exhibited very good potency for blockade of Kv1.5. Compound 8i showed good selectivity for blockade of Kv1.5 vs hERG and L-type calcium channels. In an anesthetized pig model, compounds 8i and 10c increased atrial ERP about 28%, 18%, respectively, in the right atrium without affecting ventricular ERP.
A novel class of tetrahydroindolone-derived semicarbazones has been discovered as potent Kv1.5 blockers. In in vitro studies, several compounds exhibited very good potency for blockade of Kv1.5. Compound 8i showed good selectivity for blockade of Kv1.5 vs hERG and L-type calcium channels. In an anesthetized pig model, compounds 8i and 10c increased atrial ERP by 17–26% in the right atrium without affecting ventricular ERP.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 22, 15 November 2006, Pages 5859–5863