| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1366985 | Bioorganic & Medicinal Chemistry Letters | 2007 | 5 Pages |
Abstract
A series of novel mGluR1 antagonists have been prepared. Incorporation of fragments derived from weak lead matter into a library led to enhanced potency in a new chemical series. A chemistry driven second library iteration, covering a greatly enhanced area of chemical space, maintained good potency and introduced metabolic stability.
Graphical abstractWeakly active (4) was converted into low molecular weight, high activity (29) using library chemistry.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Dafydd R. Owen, Peter G. Dodd, Simon Gayton, Ben S. Greener, Gareth W. Harbottle, Simon J. Mantell, Graham N. Maw, Simon A. Osborne, Huw Rees, Tracy J. Ringer, Margarita Rodriguez-Lens, Graham F. Smith,