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Page 1
Development of a 2,4-Diaminothiazole Series for the Treatment of Human African Trypanosomiasis Highlights the Importance of Static-Cidal Screening of Analogues.
Cleghorn LAT, Wall RJ, Albrecht S, MacGowan SA, Norval S, De Rycker M, Woodland A, Spinks D, Thompson S, Patterson S, Corpas Lopez V, Dey G, Collie IT, Hallyburton I, Kime R, Simeons FRC, Stojanovski L, Frearson JA, Wyatt PG, Read KD, Gilbert IH, Wyllie S. Cleghorn LAT, et al. Among authors: hallyburton i. J Med Chem. 2023 Jul 13;66(13):8896-8916. doi: 10.1021/acs.jmedchem.3c00509. Epub 2023 Jun 21. J Med Chem. 2023. PMID: 37343180 Free PMC article.
Discovery of a novel class of orally active trypanocidal N-myristoyltransferase inhibitors.
Brand S, Cleghorn LA, McElroy SP, Robinson DA, Smith VC, Hallyburton I, Harrison JR, Norcross NR, Spinks D, Bayliss T, Norval S, Stojanovski L, Torrie LS, Frearson JA, Brenk R, Fairlamb AH, Ferguson MA, Read KD, Wyatt PG, Gilbert IH. Brand S, et al. Among authors: hallyburton i. J Med Chem. 2012 Jan 12;55(1):140-52. doi: 10.1021/jm201091t. Epub 2011 Dec 7. J Med Chem. 2012. PMID: 22148754 Free PMC article.
Quinol derivatives as potential trypanocidal agents.
Capes A, Patterson S, Wyllie S, Hallyburton I, Collie IT, McCarroll AJ, Stevens MF, Frearson JA, Wyatt PG, Fairlamb AH, Gilbert IH. Capes A, et al. Among authors: hallyburton i. Bioorg Med Chem. 2012 Feb 15;20(4):1607-15. doi: 10.1016/j.bmc.2011.12.018. Epub 2011 Dec 27. Bioorg Med Chem. 2012. PMID: 22264753 Free PMC article.
Lead optimization of a pyrazole sulfonamide series of Trypanosoma brucei N-myristoyltransferase inhibitors: identification and evaluation of CNS penetrant compounds as potential treatments for stage 2 human African trypanosomiasis.
Brand S, Norcross NR, Thompson S, Harrison JR, Smith VC, Robinson DA, Torrie LS, McElroy SP, Hallyburton I, Norval S, Scullion P, Stojanovski L, Simeons FR, van Aalten D, Frearson JA, Brenk R, Fairlamb AH, Ferguson MA, Wyatt PG, Gilbert IH, Read KD. Brand S, et al. Among authors: hallyburton i. J Med Chem. 2014 Dec 11;57(23):9855-69. doi: 10.1021/jm500809c. Epub 2014 Nov 20. J Med Chem. 2014. PMID: 25412409 Free PMC article.
Discovery of Indoline-2-carboxamide Derivatives as a New Class of Brain-Penetrant Inhibitors of Trypanosoma brucei.
Cleghorn LA, Albrecht S, Stojanovski L, Simeons FR, Norval S, Kime R, Collie IT, De Rycker M, Campbell L, Hallyburton I, Frearson JA, Wyatt PG, Read KD, Gilbert IH. Cleghorn LA, et al. Among authors: hallyburton i. J Med Chem. 2015 Oct 8;58(19):7695-706. doi: 10.1021/acs.jmedchem.5b00596. Epub 2015 Sep 29. J Med Chem. 2015. PMID: 26418485 Free PMC article.
Discovery of a Quinoline-4-carboxamide Derivative with a Novel Mechanism of Action, Multistage Antimalarial Activity, and Potent in Vivo Efficacy.
Baragaña B, Norcross NR, Wilson C, Porzelle A, Hallyburton I, Grimaldi R, Osuna-Cabello M, Norval S, Riley J, Stojanovski L, Simeons FR, Wyatt PG, Delves MJ, Meister S, Duffy S, Avery VM, Winzeler EA, Sinden RE, Wittlin S, Frearson JA, Gray DW, Fairlamb AH, Waterson D, Campbell SF, Willis P, Read KD, Gilbert IH. Baragaña B, et al. Among authors: hallyburton i. J Med Chem. 2016 Nov 10;59(21):9672-9685. doi: 10.1021/acs.jmedchem.6b00723. Epub 2016 Sep 10. J Med Chem. 2016. PMID: 27631715 Free PMC article.
A Molecular Hybridization Approach for the Design of Potent, Highly Selective, and Brain-Penetrant N-Myristoyltransferase Inhibitors.
Harrison JR, Brand S, Smith V, Robinson DA, Thompson S, Smith A, Davies K, Mok N, Torrie LS, Collie I, Hallyburton I, Norval S, Simeons FRC, Stojanovski L, Frearson JA, Brenk R, Wyatt PG, Gilbert IH, Read KD. Harrison JR, et al. Among authors: hallyburton i. J Med Chem. 2018 Sep 27;61(18):8374-8389. doi: 10.1021/acs.jmedchem.8b00884. Epub 2018 Sep 12. J Med Chem. 2018. PMID: 30207721 Free PMC article.
Optimisation of the anti-Trypanosoma brucei activity of the opioid agonist U50488.
Smith VC, Cleghorn LA, Woodland A, Spinks D, Hallyburton I, Collie IT, Mok NY, Norval S, Brenk R, Fairlamb AH, Frearson JA, Read KD, Gilbert IH, Wyatt PG. Smith VC, et al. Among authors: hallyburton i. ChemMedChem. 2011 Oct 4;6(10):1832-40. doi: 10.1002/cmdc.201100278. Epub 2011 Aug 10. ChemMedChem. 2011. PMID: 21834094 Free PMC article.
Discovery of Inhibitors of Trypanosoma brucei by Phenotypic Screening of a Focused Protein Kinase Library.
Woodland A, Thompson S, Cleghorn LA, Norcross N, De Rycker M, Grimaldi R, Hallyburton I, Rao B, Norval S, Stojanovski L, Brun R, Kaiser M, Frearson JA, Gray DW, Wyatt PG, Read KD, Gilbert IH. Woodland A, et al. Among authors: hallyburton i. ChemMedChem. 2015 Nov;10(11):1809-20. doi: 10.1002/cmdc.201500300. Epub 2015 Sep 18. ChemMedChem. 2015. PMID: 26381210 Free PMC article.
35 results