Open Source TB

Finding new drugs to treat TB following open-source principles - join us!

Sister projects at @OSantibiotics, @MycetOS and @O_S_M.

[Open Source TB @OpenSourceTB]

The Open Source TB account has been a little quiet of late but what a great post to make our comeback with! Carlota is working on the diversity-oriented synthesis portion of #OSTBSeries4, which you can read more about here: https://t.co/3xkie4Jg7H

[Klementine Burrell-Sander @Klemistry]

So excited to have a new honours student join the Rutledge group - Carlota has just started working on the @OpenSourceTB project with me!

[Open Source TB @OpenSourceTB]

Thanks for the shoutout! Our most recent work is now up on @GitHub at https://t.co/GtW4DfybDK.

Or you can check out the #OpenSourceTB or #OpenSourceDrugDiscovery hashtags to find out more!

[The Neuro @TheNeuro_MNI]

#OAWeek shoutout to The Open Source Tuberculosis Consortium (@OpenSourceTB), which is trying a different approach to curing #Tuberculosis. Guided by #opensource principles, everything is open and anyone can contribute. Check them out here: https://t.co/BveOFBF28t

[Open Source TB @OpenSourceTB]

And hopefully we'll be back at it soon, just with a bit of extra PPE 😷 👩‍🔬

[Open Source TB @OpenSourceTB]

COVID-19 restrictions have kept us out of the lab, so unfortunately we don't have any more current synthetic work to discuss right now. But that doesn't stop you from getting involved - #OpenSourceDrugDiscovery projects are larger than a single lab!

[Open Source TB @OpenSourceTB]

@Inorganick_ We're already using lots of base (like 5 equivalents per amine!) but will definitely try heating it up and see how that goes

[Open Source TB @OpenSourceTB]

#OpenSourceTB's diversity oriented synthesis also includes a double allylation of boc-protected linear polyamine (analogous to the propargylation we mentioned last week).

Theoretically, this will help us install other functionalities...

[Open Source TB @OpenSourceTB]

We’ve tried THF instead of DMF, + different bases (KOH and NaOH) but our yields are still low..,we think we’re getting the mono-allylated side product, which complicates purification.

Any ideas? We’d love suggestions!

#ChemTwitter #RealTimeChem #MedChem #OpenSourceTB

[Open Source TB @OpenSourceTB]

..but we had way more trouble with this one than expected - read about our trials and tribulations on @GitHub: https://t.co/c9YuEbJfQh

#OpenSourceTB #OpenSourceDrugDiscovery #OpenScience

[Open Source TB @OpenSourceTB]

This fab illustration of the 6 laws of #OpenSourceDrugDiscovery features our sister project @O_S_M but the same principles apply to our work, too!

If you're curious about them, read the paper here: https://t.co/gttU2HgC3k

#OpenScience

[#UniteHealth Social Media Awards @socmed4good]

A vision in orange, #Malaria #Innovator @MatToddChem as envisioned by @_dangerouscake https://t.co/nEL2ZDxYin

[Open Source TB @OpenSourceTB]

…but we struggled to purify the product of the Michaelis-Arbuzov reaction. We tried a column (DCM:MeOH with 10% NH4) + trituration with toluene, then lockdown interfered.

Have you got any ideas for purifying this? We’d love to hear!

#ChemTwitter #RealTimeChem #MedChem

[Open Source TB @OpenSourceTB]

Series 4 of #OpenSourceTB has a focus on diversity-oriented synthesis. Here’s one of the routes we planned to install a non-activated alkene. Our first reaction (acylation) had great yields…

#MedChem #ChemTwitter #OpenSourceDrugDiscovery #OpenScience

[Open Source TB @OpenSourceTB]

#OpenSourceTB uses @GitHub to easily share our data & experimental methods and collaborate with others - check it out here! https://t.co/GtW4DfybDK

#OpenSourceDrugDiscovery #OpenScience

[Klementine Burrell-Sander @Klemistry]

So good to be able to work on our paper about using @GitHub as an ELN *in person* with @krscroggie 😊

[Nature Medicine @NatureMedicine]

The Tuberculosis Drug Accelerator, an experiment designed to facilitate collaboration in drug discovery, has reached a 10-year landmark.

Carl Nathan @WeillCornell and colleagues review the consortium’s achievements, advantages and limitations. #TB

https://t.co/uZWiA8AeIU

[Open Source TB @OpenSourceTB]

We're also not the only ones trying to make #DrugDiscovery more open!

Read about Huntington's disease reasearcher Dr Rachel Harding's experiences with #OpenScience here:

https://t.co/drtwUqaRQb | @PLOSBiology

#OpenSourceDrugDiscovery

[Open Source TB @OpenSourceTB]

Curious about what success #OpenSourceDrugDiscovery has had so far?

Well, the easiest one to point to is the identification of a new resolution approach for #Praziquantel (used to treat schistosomiasis).

https://t.co/uyr8HMc8GB | @MatToddChem @PLOSNTDs

[Open Source TB @OpenSourceTB]

#OpenSourceDrugDiscovery aims to accelerate that process by sharing ideas and data openly, and encouraging collaboration.

We're hopeful that these #OpenScience principles will help us finding new drugs to treat #Tuberculosis and thus save millions of lives!

[Open Source TB @OpenSourceTB]

Did you know that 1.4 million people died from #Tuberculosis in 2019? (Ref - @WHO)

The UN has a goal to #EndTB by 2030 - only 9 years from now. But typical #DrugDiscovery pipelines take 10+ years...

[Open Source TB @OpenSourceTB]

Some interesting #DrugDiscovery work that could potentially impact how we approach future series of #OpenSourceTB!

#Tuberculosis

[Genetic Engineering & Biotechnology News @GENbio]

Tuberculosis Essential Gene Index of Vulnerability Points to Promising, Underexplored Targets

Researchers say the ability to identify and prioritize vulnerable essential genes provides a roadmap to reinvigorate target-based drug discovery in TB. Read more:https://t.co/VwOfriZmSi

[Open Source TB @OpenSourceTB]

**EDIT - this reaction scheme has a rather important component missing - we've been using NaH + dry DMF, with the propargyl bromide (based on a previous student's work with allylation).

[Open Source TB @OpenSourceTB]

We started trying to use boc-protection to make some bis-functionalised linear polyamines - the plan was to propargylate the protected amine then use a naphthyl-azide coupling partner for a click reaction.

#RealTimeChem #OpenSourceTB #ChemTwitter #MedChem #DrugDiscovery

[Open Source TB @OpenSourceTB]

We're struggling to isolate pure product - we think partially bc the reaction mixture contains both mono- and bis-propargylated amine. Read about our attempts (and make suggestions!) here: https://t.co/JAMn3vxWQb

Any ideas #ChemTwitter?

#RealTimeChem #MedChem #OpenSourceTB

[Open Source TB @OpenSourceTB]

@Inorganick_ Omg - just realised that I've forgotten to include NaH on the reaction. I've tried using it but had no luck with it, possibly bc the tin we have is pretty old. Will definitely try cesium carbonate though!