blogs

26 Jan

near neighbours sythesis

Published by ZoeH

I've been working for six weeks now with the Todd Research Group at Sydney University as part of an undergraduate summer research program. The aim of my project is to synthesise analogues of this group of hits from the  antimalarial dataset released by GSK.

23 Jan

Bronsted Acid catalysed PS reaction update

Published by m.robertson

January 2012, Here's a quick update on where we are regards the Bronsted Acid catalysed Pictet-Spengler reaction.
 

20 Jan

Update:- January 2012

Published by m.robertson

It's been too long since I've updated the progress of this project on here but here's a brief summary of where we are and what's planned for the near future.  From late November we've had a summer student, Kat Badiola, working on the project.  She started with preparing pure, racemic samples of the 3

19 Jan

Reacting to the first set of biological results

Published by pylioja

Subject 

Request for Help

We have received encouraging biological results for the analogues we sent for testing before Christmas. Mat has discussed this here on TSL and on G+. Our best hit came from the "near-neighbour" compound and the original GSK hits came out slightly less active than in their original high throughput screen.

27 Dec

Puzzled over MS

Published by KatB

Subject 

Rants, Miscellaneous

Background
Relevant experiment.  Basically, the Pictet-Spengler to form 3 PZQ analogues and PZQ itself.
The mass spec is of a by-product of the acid mediated PS cyclisation of MNR10-1 to form KAB8-1, aka the dimethoxy N-benzoyl PZQ analogue.

02 Dec

Two weeks in the PZQ lab

Published by KatB

Subject 

Rants, Miscellaneous

 
I've now reached the end of my second week in the lab working on the Pictet-Spengler route to praziquantel.
 

04 Nov

TCMDC-123812 and 123794 and intermediates sent to GSK Tres Cantos

Published by pylioja

 I have just packaged up TCMDC-123794 (PMY 11-2) and -123812 (PMY 10-2) along with the parent acid (PMY 8-2), ester (PMY 6-1), aldehyde (PMY 2-4), near neighbour analogue (PMY 14-1) and also the acylurea by-product (P

02 Nov

A range of compounds are ready for testing with more coming.

Published by pylioja

Subject 

Request for Help

I'm now happy with the data for TCMDC-123812 and TCMDC-123794. A bit of usual practical annoynce with TCMDC-123794 caused some trivial issues, namely a bit of repurification and acetone in the final spectra. These have now been taken care of and the compounds are ready for testing!

17 Oct

Where Else Have the Aryl Pyrroles been Evaluated?

Published by MatTodd

Subject 

Miscellaneous

Last week I was talking with Lei Liu from Tsinghua University, who was visiting Sydney to give a talk on his synthetic methodology research. I showed him the compounds that are the starting point of the open source drug discovery project for malaria, the arylpyrrole set.

09 Oct

TCMDC-123812 and 123794, pending purification.

Published by pylioja

Subject 

Request for Help

I'm now fairly confident that I've made TCMDC-123794 and TCMDC-123812. By fairly confident I mean that I've got a reasonable looking but crude 1H NMR and low res. mass spec of both of the compounds. They are not clean by NMR after a column and the yield of the reaction was pretty bad (~20%). Still this isn't too bad for a first go, using a quick and dirty acid chloride. Most of the mass seems to go toward turning the acid into the anhydride.

Pages