| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1364148 | Bioorganic & Medicinal Chemistry Letters | 2009 | 5 Pages |
Abstract
We have been exploring the potential of 5-HT2B antagonists as a therapy for chronic heart failure. To assess the potential of this therapeutic approach, we sought compounds possessing the following attributes: (a) potent and selective antagonism of the 5-HT2B receptor, (b) low impact of serum proteins on potency, and (c) desirable pharmacokinetic properties. This Letter describes our investigation of a biphenyl benzimidazole class of compounds that resulted in 5-HT2B antagonists possessing the above attributes. Improving potency in a human serum albumin shift assay proved to be the most significant SAR discovery.
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Neil Moss, Younggi Choi, Derek Cogan, Adam Flegg, Andreas Kahrs, Pui Loke, Orietta Meyn, Raj Nagaraja, Spencer Napier, Ashley Parker, J. Thomas Peterson, Philip Ramsden, Christopher Sarko, Donna Skow, Josh Tomlinson, Heather Tye, Mark Whitaker,