| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1378854 | Bioorganic & Medicinal Chemistry Letters | 2006 | 7 Pages |
Abstract
Several potent, functionally active MCHr1 antagonists derived from quinolin-2(1H)-ones and quinazoline-2(1H)-ones have been synthesized and evaluated. Pyridylmethyl substitution at the quinolone 1-position results in derivatives with low-nM binding potency and good selectivity with respect to hERG binding.
Graphical abstractSeveral potent, functionally active MCHr1 antagonists derived from quinolin-2(1H)-ones and quinazoline-2(1H)-ones have been synthesized and evaluated. Pyridylmethyl substitution at the quinolone 1-position results in derivatives with low-nM binding potency and good selectivity with respect to hERG binding.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Christopher Blackburn, Matthew J. LaMarche, James Brown, Jennifer Lee Che, Courtney A. Cullis, Sujen Lai, Martin Maguire, Thomas Marsilje, Bradley Geddes, Elizabeth Govek, Vivek Kadambi, Colleen Doherty, Brian Dayton, Sevan Brodjian, Kennan C. Marsh,