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19th May 2015 @ 11:42

Compounds synthesised by Tom Foley and Jamie Scott, masters research students in Edinburgh, from November 2014 - March 2015.

 

EDIreport07052015.pdf

 

 

Lot 4 series 3.png

Lot 4 series 4.png
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10th December 2014 @ 14:10

Biological activities of OSM-S-106 and PT-22-C1 performed at the Dundee Drug Discovery Unit by Irene Hallyburton.

OSM-S-106 was resynthesised in Edinburgh (PT-23-C1) and found to have an activity of 150 nM, consistent with that reported as TCMDC 135294 but a little lower than the Avery results. Adding a methyl group to improve solubility by introducing an axial twist gave PT-22-C1, which was inactive.

 

 

 

 

OSM-S-106 and PT-22-C1.pdf
Attached Files
11th July 2013 @ 10:13

Biological evaluation of OSM-E-4 through 8 performed at the Dundee Drug Discovery Unit by Irene Hallyburton.

Unfortunately all five compounds tested were inactive, possibly with some low activity at maximum doses (0.05 mM) although this may be an artifact of the fitting.

OSM-E-4 was dosed according to concentrations calculated with a molecular weight of 240 rather than 314 due to inconsistent mass specta available when samples were sent to Dundee.

Given that OSM-E-4 is inactive, I do not recommend that this sample is rerun: Tthe consequence of this miscalculation is that the lower limit of activity is even higher than normal and this compound is extra-specially inactive.

 

 

OSM-E-4 through OSM-E-8.pdf

 

Synthetic procedures: OSM-E-4 through 7 were synthesised in one experiment: Synthesis of PT-1-14 and OSM-E-8 was synthesised here: Amidation of PT-1-14C3 (PT-1-15)

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9th May 2013 @ 12:44

Biological evaluation of OSM-E-1 through 3 performed at the Dundee Drug Discovery Unit by Irene Hallyburton.

Unfortunately all three compounds tested were inactive, possibly with activity ~60,000 nM for OSM-E-2 although this may be an artifact of the fitting.

 

 

OSM-E-1 through OSM-E-3 - corrected protocol.pdf

 

Synthetic procedures: 

OSM-E-1: Amidation of PT-1-9A (PT-1-10)

OSM-E-2: Amidation of PT-1-11 (PT-1-12)

OSM-E-3: amidation of PT-1-3C (PT-1-5)

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