LECTURE EIGHT

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Synthetic Chemistry

© Jem Stach - Material intended solely for students enrolled @ Newcastle University - MSc Industrial and Commercial Biotechnology. jem.stach@newcastle.ac.uk

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Directed reading

Lecture covers semi-synthetic antibiotics, medicinal chemistry, SAR studies, target orientated antimicrobial design, Lipinski’s rule-of-five

Haydon DJ et al. An inhibitor of FtsZ with potent and selective anti-staphylococcal activity. Science. 2008 Sep 19;321(5896):1673-5. doi: 10.1126/science.1159961.

Hackbarth CJ et al. N-alkyl urea hydroxamic acids as a new class of peptide deformylase inhibitors with antibacterial activity. Antimicrob Agents Chemother. 2002 Sep;46(9):2752-64.

Clements JM et al. Antibiotic activity and characterization of BB-3497, a novel peptide deformylase inhibitor. Antimicrob Agents Chemother. 2001 Feb;45(2):563-70.

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Czaplewski LG et al. Antibacterial alkoxybenzamide inhibitors of the essential bacterial cell division protein FtsZ. Bioorg Med Chem Lett. 2009 Jan 15;19(2):524-7. doi: 10.1016/j.bmcl.2008.11.021. Epub 2008 Nov 13.

Lipinski C. Chris Lipinski discusses life and chemistry after the Rule of Five. Drug Discov Today. 2003 Jan 1;8(1):12-6.

Baker SJ et al. Therapeutic potential of boron-containing compounds. Future Med Chem. 2009 Oct;1(7):1275-88. doi: 10.4155/fmc.09.71.

Extra material associated with this lecture can be found in the Reading section