Metabolic Studies on a Set of Arylpyrroles

Published by MatTodd on 7 May 2012 - 12:54pm

Subject 

Results

Eight compounds - two GSK originals and 6 promising-looking compounds made during this project were examined by Sue Charman's lab at Monash for metabolic degradation in vivo. In human terms that means they were tested (on a simplistic level) to see whether the compounds would last long in the blood or whether they would likely be metabolised. As part of these studies the solubilities of the compounds were evaluated.

Compounds were as follows. Note the use of the new "OSM-S" notation which we're introducing to give a compound a unique ID tag, independent of source, though there will probably always be trailing synthetic-prep tags.

The results are posted here.

As is often the case low degradation rates (good) come at the cost of low solubility. We kind of expected this based on the high logP values for some of these compounds. Presumably analogous compounds could be re-examined when more soluble.

Comments

The plasma stability results are in for OSM-S-5 (http://malaria.ourexperiment.org/uri/115). Basically it's stable in human plasma but metabolised quite quickly in mouse plasma. Good to know and it could be another reason for the in vivo fail.