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Biological Results for First Set of Compounds

MatTodd — Tue, 10 Jan 2012 18:12:30 -0600

near neighbours sythesis

ZoeH — Wed, 25 Jan 2012 18:29:00 -0600

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. They are referred to here as 'near neighbours' because they share the arylpyrrole moiety present in the two hits (TCMDC 123812 and 123794) Paul has been working on, but have a thiazolodinone side chain. The major components of my project are:

Bronsted Acid catalysed PS reaction update

m.robertson — Sun, 22 Jan 2012 23:08:54 -0600

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

Reacting to the first set of biological results

pylioja — Thu, 19 Jan 2012 17:47:11 -0600

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. However, Paul Willis at MMV rates TCMDC-123794 as a better lead than PMY 14-1 (TSL post).

Update:- January 2012

m.robertson — Thu, 19 Jan 2012 18:32:45 -0600

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 PZQ analogues shown below (compounds 6-8) via the Pictet-Spengler cyc

Stop SOPA

gtaylor — Tue, 17 Jan 2012 22:58:03 -0600

Alternative synthesis of PZQ using Phenylglycine

M_Lilley1985 — Thu, 12 Jan 2012 05:43:46 -0600

I was looking at all the difficulty that is occuring with finding a cheap source of chiral catalyst for the Pictet-Splenger and mused about using Phenylglycine, as this avoids the issue due to it being part of the chiral pool.
Anyway here is my attempt at getting the key ring system together for the system. Don't think anything I used is particularly expensive. Sorry about the conditions being vague, was just a quick thought that I came up with.

Open Source Drug Discovery for Malaria

MatTodd — Mon, 25 Jul 2011 06:39:15 -0500