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Calixarenes and Tuberculosis Therapies
We are investigating the synthesis and biological activity of a series of calixarenes and novel small molecule analogues with anti-TB activities. To date, we have established efficient synthetic methodologies to prepare a range of novel calix[8]arenes with PEG moieties attached at the lower rim via ether linkages. Testing in vivoestablished preliminary structure–activity relationships, with some compounds exhibiting significant anti-mycobacterial activity. The calixarenes appear to act via a novel host macrophage mediated mechanism, involving the up-regulation of arginase and functioning iNOS . Further studies are underway using labelled calixarenes to probe this novel mechanism of action through a collaboration with Prof. D. Young (NIMR, Mill Hill).
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University College London - Gower Street - London - WC1E 6BT Tel:+44 (0)20 7679 2000

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