Biological Results for Third Set of Compounds

Published by MatTodd on 15 December 2012 - 6:57am

Subject 

Results

A summary of the biological activities obtained for the third set of compounds in 2012 - those arising from the consultation for which synthetic and commercial compounds that were most wanted. See also some links for analysis of trends in the data.

First set (Oct 19th) Data, and these were discussed briefly in an online meeting.

Second set (Nov 8th) Data, and discussion

Third set (Dec 10) Data (essentially inactive, aside from mild activity for OSM-S-103

 

Previous discussion of these data, highlighting trends.

Importance of primary amide side chain.

Impact of replacing ester with amides and amines. And impact on the two original GSK compounds.

Dramatic impact of methylation of the hit compound.

Low efficacy of pyrazoles.

Prodrug hypothesis II and III

Reminder of the efficacy of the near neighbour thiazolidinones.

Suggestion of next compounds, including hybrids, and the WANTED! compounds.