High school synthesis workshop 2022

[kym834]

We are running a workshop with high school students in late May/early June who will work on the synthesis of a few more compounds for this series. They will be looking at changing up the aniline used in the synthesis to explore different aromatic groups attached to the amine of the 2-aminothiazoles (R in the image below).

@wwjvdsande - as these compounds are not well known, we are wondering if you have resources or capacity to run a tox screen of the hit? Or maybe know of someone who could do it on our behalf? We'd love to check that these compounds aren't crazy toxic before we set off trying to make them with students.

@OpenSourceMycetoma/corecontrib - If anyone has any other ideas about how we could investigate the safety, love to hear it too!

[wwjvdsande]

@kym834 for us we typically only test if the compounds are toxic to the larvae. Since the larvae can stand higher concentrations of certain toxic compounds than humans can I don't think this is a good solution for you.

[kym834]

Here are the compounds we are intending to make in this round of synthesis. @mattodd @AndyBishopSevenoaks

[kym834]

@wwjvdsande and @MA-Jjingyi we've prepared 6 of these compounds we made with students for shipment with FedEx. They'll be picked up on Monday (AU time) and are estimated to arrive Thursday (Ntherlands time).

Also, I'm presenting at a conference on the 6th of July. Do you think we'd have the in vitro results by then? Love to present this 🙂

[MA-Jjingyi]

@wwjvdsande and @MA-Jjingyi we've prepared 6 of these compounds we made with students for shipment with FedEx. They'll be picked up on Monday (AU time) and are estimated to arrive Thursday (Ntherlands time).

Also, I'm presenting at a conference on the 6th of July. Do you think we'd have the in vitro results by then? Love to present this 🙂

@kym834 Hi, kymberley. thanks for your delivery. when we get the package, we will let you know. but it is a pity we cann't finish the in vitro test before your presentation.

[mattodd]

This is really great. @kym834 are the compounds in the Master List with the relevant MyOS codes, and could they please make an appearance here?

[wwjvdsande]

@kym834 we have added the six compounds to our screening plate, three extra compounds arrived. Where they also from this group?

[kym834]

@wwjvdsande these three compounds are ones I made myself. They are 2-aminothiazoles. I'll post the structure and add them to the master list tomorrow.

[wwjvdsande]

@kym834 great we will add them to the screening plate

[kym834]

The workshops we ran in May/June of 2022 resulted in 6 new compounds to be added to the series 2 library. The compounds that were synthesised, characterised and shipped to Wendy and Co. are shown below.

These compounds were all made following the general synthesis route. The other 4 compounds that we had planned to make were not synthesised as there were issues with generating the thiourea starting materials.

[wwjvdsande]

@kym834 the compounds are tested and the results are added to spreadsheet MYOS_00315 and MYOS_00317 seemed most active out of this set.

[kym834]

Summary of the in vitro activities below:

Couple of points:

• Modification at 4 position seems to be tolerated and give similar activity to hit compound.
• 3 position less tolerant of modification.