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9th October 2013 @ 21:54

A month ago today, the team announced a new series that were presented by MMV for further investigation. As previously discussed, one advantage of this series is that a lot of data is already available both the CRO who MMV sponsored to undertake some synthesis.

This blog aims to tie this data together and serve as a platform for discussion about the next series. 

Some synthesis has been started already, based on some experimental data from the CRO, although new ideas for the route are also welcome.

Important, at the moment some raw data from the CRO is not available and so some of these points are conjecture and may be edited at a later date (of course the original post will remain but with additional information).

This is a pictorial summary of the MMV briefing document:

Taken together with the some other data from big pharma, here are some thoughts for the next things to explore:

Resynthesis of MMV670652 to confirm potency and possible enantioselective synthesis

Synthesis of p-bromophenyl analog and possible extention of the aryl chain with heterocycles

Exploring the nature of substitution of the phenethyl aryl group. Different combinations of di-fluoro?

Lots of fluorine in these molecules..could incorporating a CF2H group on the pyrazine ring be beneficial?

Different core? Different Nitrogen subtitution?

Introduction of basic centres without reducing potency - how can we do this?

 

Attached Files
Series 4 Summary.cdx
Series 4 Summary.png
MMV Briefing Document for OSM_Triazolopyrazines.pdf
MMV670652.png
Bromo.png