The bioisosteric replacement of the indole core of CRTH2 antagonists using thienopyrroles was investigated, resulting in potent antagonists with good selectivity over DP1. Early ADME/PK assessment of this chemotype demonstrated bioavailability in mice.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1016/j.bmcl.2011.01.008 | DOI Listing |
J Med Chem
April 2012
Oxagen Ltd., 91 Milton Park, Abingdon, Oxon OX14 4RY, UK.
Bioorg Med Chem Lett
March 2011
Abbott Laboratories, Worcester, MA 01605, USA.
The bioisosteric replacement of the indole core of CRTH2 antagonists using thienopyrroles was investigated, resulting in potent antagonists with good selectivity over DP1. Early ADME/PK assessment of this chemotype demonstrated bioavailability in mice.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!