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28th March 2014 @ 00:48

GitHub Tag #168

Introduction

In September 2013, the OSM team announced a new series, the triazolopyrazines. The team looked at the data provided by MMV (from Big Pharma and the CRO) and started to plan the next amides to synthesise. Currently, the OSM lab in Sydney are targetting ether and amide compounds based on actives from the original set. Several amides were made as part of the original pre-OSM campaign.

The amides

Two amide compounds (AEW 120-2 GitHub Tag #156 and TM 9-1 GitHub Tag #152) have been successfull synthesised and now the team need to choose some further amides to synthesise.

Inga perfomed a search of commercially available primary and secondary anilines and benzylamines and the team ordered some representative compounds. There is also the opportunity to introduce different aryl groups on the right hand side of the molecule through the use of different aldehyde in the synthesis. The figure below indicates compounds that can be accessed in Sydney with the materials currently available.

CLogP Data has been calculated for some of these compounds and can be found in the ChemDraw or PNG files.

Possible amides CLogP.cdxml
Possible amides CLogP.png

Consultation

Which compounds should be synthesised based on the starting materals currently in the lab? Do any of the compounds above look particularly attractive/unattractive. If you can help the team to decide on further amine or aldehyde (to introduce Ar) starting materials then we'd love to hear your thoughts. Commercially available compounds are preferrable but of course we can make some amines/aldehydes if they look interesting.

Ideas/suggestions can be posted as comments below this blog, on GitHub, our G+ site, Twitter or last (and also least) by email to opensourcemalaria@gmail.com.

Thanks

The OSM Team

(Originally authored by Alice Williamson, then tweaked by Mat Todd)

Linked Posts
Attached Files
Blog on Amides.png
Blog on Amides2.png
Possible amides CLogP.cdxml
Possible amides CLogP.png