| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1371762 | Bioorganic & Medicinal Chemistry Letters | 2012 | 5 Pages |
Abstract
A new series of epiminocyclohepta[b]indoles with potent 5-HT6 antagonist activity were discovered and optimized using in vitro protocols. One compound from this series was progressed to advanced pharmacokinetic (PK) studies followed by 5-HT6 receptor occupancy studies. The compound was found to have excellent oral absorption, a highly favorable PK profile and demonstrated pharmacodynamic interaction with the 5-HT6 receptor as shown by ex vivo autoradiography.
Graphical abstractThe synthesis and SAR of epiminocyclohepta[b]indole analogs as 5-HT6 antagonists are described.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
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Authors
Alan J. Henderson, Peter R. Guzzo, Animesh Ghosh, Jagjit Kaur, Jia-Man Koo, Kassoum Nacro, Shailaja Panduga, Rashmi Pathak, Bharat Shimpukade, Valentina Tan, Kai Xiang, Jonathan D. Wierschke, Matthew L. Isherwood,