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First Set of Biological Results from the Third Round of Compounds
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The team set about synthesising targets SA - SJ and ordered the commercial compounds chosen at the consultation in July. In late September, the commercial compounds, plus some of the synthetic targets (and analogues) were sent away for biological evaluation.
The results of the assay (performed in Vicky Avery's lab) showed that the molecules submitted were either inactive or displayed low activity. However, the results have certainly given the team some food for thought. Of particular interest was the inactive compound OSM-S-92, which possesses a pyrazole core in place of the 2,5-dimethyl pyrrole core of the original hit (OSM-S-5, 404 nM). All pyrazoles tested to date have been inactive in this assay. The team also noted the activity seen (albeit micro- rather than nanomolar) of 'reductive amination' compounds OSM-S-88 and OSM-S-95. Previously, compounds possessing a secondary amine appended to the pyrrole ring, were shown to be in active in the biological evaluation.
The next set of synthetic compounds have been submitted, so hopefully this data will be posted towards the end of next week.