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10th September 2013 @ 10:02

The OSM team are ready to tackle the synthesis and evaluation of a new triazolopyrazine series.

In late June, Paul Willis shared a summary document from a CRO who had been working on the synthesis of some triazolopyrazine analogues (funded by MMV) following the discovery of a hit molecule. The OSM team now plan to design and evaluate further analogues based on the triazolopyrazine core.

The summary document is here

MMV Briefing Document for OSM_Triazolopyrazines.docx
MMV Briefing Document for OSM_Triazolopyrazines.pdf
and the abstract is below:

'We have made compounds in this series down to 16nM potency. The series also seems to have good in vitro HLM and hHEP stability Clint < 8.1 is compatible with 10nM potency. However, RLM remains stubbornly high, particularly for the more potent analogues translating to short half-lives in rat PK. The series also appears to have little polypharmacology or cytotoxicity. The project has so far not challenged the hypothesis that rat metabolism may not be a great model for human metabolism for this series.'

A consultation on the next molecules to be synthesised by the OSM team will be held in the next fortnight. We are currently waiting for the raw data, which will be posted here on receipt. For more information on the triazolopyrazines, please take a look at the project wiki

For the structures of all the inherited compounds together with their potencies, see: Updated Data on Amounts Remaining in MMV Stock of Series 4

Linked Posts
Attached Files
MMV Briefing Document for OSM_Triazolopyrazines.pdf
MMV Briefing Document for OSM_Triazolopyrazines.docx