Top Tweets for #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
#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...
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
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
Despite our adventures with cyclam, #OpenSourceTB series 4 is really about the linear polyamine analogues we've been exploring. Our first series of compounds had some promising results but we need to make more to establish some SAR...
#DrugDiscovery #Tuberculosis #OpenScience
Right before lockdown got in the way, #OpenSourceTB were working towards this cyclam derivative with #ferrocene pendant groups:
#OpenSourceDrugDiscovery #DrugDiscovery #ChemTwitter #Tuberculosis #MedChem
As mentioned, we wanted to try #adamantane as a hydrophobic pendant group on cyclam. Our proposed route was a click-coupling reaction between the bis-propargylated cyclam and azide-functionalised adamantane.
#OpenSourceDrugDiscovery #OpenSourceTB #DrugDiscovery #ChemTwitter
@Klemistry: I’m a @SydneyChemistry honours student looking at #MedChem and #SciComm and this year I’ve been trying to synthesise new molecules for #OpenSourceTB series 4 - more on exactly what I've gotten up to on that front later!
So now we want to look at some SAR! Series 4A fo #OpenSourceTB will be “filling in the blanks” of the incomplete set already synthesised to examine the effect of chain length, number of amines and number of pendant groups.
#MedChem #Tuberculosis #DrugDiscovery 2/
The focus of #OpenSourceTB series 4 is open cyclams – linear polyamines with the same 1-napthalimide pendant groups that showed good activity on the macrocycle have shown some promising results! Those compounds (made by Jamie Batten) can be found here: https://t.co/WUjDwqNQyy 1/
So what's #OpenSourceTB working now? Well,Series 4 started a bit differently – the Rutledge and @mattoddchem groups had been looking at cyclam + its derivatives as fluorescent probes for metal ions, as described here: https://t.co/9bVDjbfmHm
#DrugDiscovery #Tuberculosis 1/
If you're interested in any of our #OpenSourceTB work so far, it's all available here on
@github - you can find data on compounds, synthetic routes and all our publications in one spot!
https://t.co/GtW4DfybDK
#OpenSourceDrugDiscovery #DrugDiscovery #OpenScience #MedChem
Next up...the @GSK library furnished yet another lead compound for #OpenSourceTB Series 3. In 2015, OSTBS83 was identified by the Nathan lab (@WeillCornell) as a potent + selective Mtb inhibitor with low HepG2 toxicity.
#Tuberculosis #DrugDiscovery #OpenSourceDrugDiscovery 1/
#OpenSourceTB series 2 centred around another hit from the @GSK screen. Lead compound TCMDC-14693 had a micromolar min. inhibitory concentration against the H37Rv #Tuberculosis cell line, and relatively low toxicity against HepG2 (a human carcinoma cell line). #DrugDiscovery 1/
Unfortunately, the compounds had less than desirable in vivo tolerability (see paper) and research into this series ultimately came to an end. But there were still plenty of hits for #OpenSourceTB to follow up on...
https://t.co/gm4a8XKvYS
#OpenScience #MedChem 4/4
So where does #OpenSourceTB fit into things? Well, #OpenSourceDrugDiscovery pioneer @MatToddChem oversaw the beginnings of this project back in 2013, when 177 lead compounds from the @GSK compound library were placed in the public domain... https://t.co/1rNUXnuXu6 #MedChem 1/
We think it's time for a refresher on what this project is all about!
#OpenSourceTB is an #OpenSourceDrugDiscovery project, which is in turn part of the larger movement of #OpenScience. So – what does all that actually mean?
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