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9th April 2014 @ 02:40

GitHub Issue #174

The team are currently in the middle of synthesising the triazolopyrazines, both ether and amide linked compounds in the series. I (Jo Ubels) have been looking at the data from MMV on the ether linked series (example below).

I have synthesised the core triazolopyrazine rings (shown in black) with the benzonitrile group attached (pink) and am synthesising more with a chloro group in place of the nitrile. I have made one complete compound with phenethyl alcohol as the ether to test the reaction conditions. My question is, what alcohols (blue), amines or thiols should we buy to link to my compounds? Looking through the MMV data I have found that most of the alcohols already used are fluorinated so I searched for alcohols/amines/thiols with other ring substituents. A selection of alcohols that I have found can be seen in this table along with prices and shipping information.

Table of possible alcohols to buy.pdf

The alcohols that have already been tested can be found in this table, along with their potency data.

Alcohols-Amines that have been tested.pdf

Which compounds should we synthesise next based on the available alcohols? Are any of the possible alcohols particularly attractive/unattractive when paired with the nitrile or chloro group containing triazolopryazine ring cores? We need to be able to reatin potency and increase the solubility and metabolic stability of the compounds. If you can help us decide what to buy and synthesise next then we'd love to hear from you. The list of alcohols/amines/thiols is not exhaustive and I will try to add more suggestions in the next day or so.

To make suggestions you can post a comment below this blog, on GitHub, our G+ site, Twitter or last (and also least) by email to opensourcemalaria@gmail.com.

Thanks,

Jo & the OSM Team

Linked Posts
Attached Files
Table of possible alcohols to buy.pdf
Alcohols-Amines that have been tested.pdf
Representative series 4 ether.png