Papers 2014

Lead Optimization of a Pyrazole Sulfonamide Series of Trypanosoma brucei N-Myristoyltransferase Inhibitors: Idenification and Evaluation of CNS Penetrant Compounds as Potential Treatments for Stage 2 Human African Trypanosomiasis. Brand, S.; Norcorss, N. R.; Thompson, S.; Harrison, J. R.; Smith, V. C.; Robinson, D. A.; Torrie, L. S.; McElroy, S. P.; Hallyburton, I.; Norval, S.; Scullion, P.; Stojanovski, L.; Simeons, F. R. C.; van Aalten, D.; Frearson, J. A.; Fairlamb, A. H.; Ferguson, M. A. J.; Wyatt, P. G.; Gilbert, I. H.; Read, K. D. J. Med. Chem., 2014, 57, 9855-9869.

Characterisation of a melamino nitroheterocycle as a potential lead for the treatment of human African trypanosomiasis. Giordani, F.; Buschini, A.; Baliani, A.; Kaiser, M.; Brun, R.; Barrett, M. P.; Pellacani, C.; Poli, P.; Gilbert, I. H. Antimicrob. Agents Chemother. 2014, 58, 5747-5757. link to journal abstract in pubmed

Fragment screening reveals salicylci hydroxamic acid as an inhibitor of Trypanosoma brucei GPI GlcNAc-PI deN-acetylase. Urbaniak, M. D.; Capes, A. S.; Crossman, A.; O’Neill, S.; Thompson, S.; Gilbert, I. H.; Ferguson, M. A. J. Carbohydr. Res., 2014, 387, 54-58. link to journal abstract in pubmed

Probing the substrate specificity of Trypanosoma brucei GlcNAc-PI de-N-acetylase with synthetic substrate analogues. Capes, A. S.; Crossman, A.; Urbaniak, M. D.; Gilbert, S. H.; Ferguson, M. A.; Gilbert, I. H. Org. Biomol. Chem., 2014, 12, 1919-1934. link to journal abstract in pubmed

Target-based drug discovery for human African trypanosomiasis: selection of molecular target and chemical matter. Gilbert, I. H. Parasitology, 2014, 141, 28-36. link to journal abstract in pubmed