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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. 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. 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.
Identification of GSK3186899/DDD853651 as a Preclinical Development Candidate for the Treatment of Visceral Leishmaniasis.
Thomas MG, De Rycker M, Ajakane M, Albrecht S, Álvarez-Pedraglio AI, Boesche M, Brand S, Campbell L, Cantizani-Perez J, Cleghorn LAT, Copley RCB, Crouch SD, Daugan A, Drewes G, Ferrer S, Ghidelli-Disse S, Gonzalez S, Gresham SL, Hill AP, Hindley SJ, Lowe RM, MacKenzie CJ, MacLean L, Manthri S, Martin F, Miguel-Siles J, Nguyen VL, Norval S, Osuna-Cabello M, Woodland A, Patterson S, Pena I, Quesada-Campos MT, Reid IH, Revill C, Riley J, Ruiz-Gomez JR, Shishikura Y, Simeons FRC, Smith A, Smith VC, Spinks D, Stojanovski L, Thomas J, Thompson S, Underwood T, Gray DW, Fiandor JM, Gilbert IH, Wyatt PG, Read KD, Miles TJ. Thomas MG, et al. Among authors: cleghorn lat. J Med Chem. 2019 Feb 14;62(3):1180-1202. doi: 10.1021/acs.jmedchem.8b01218. Epub 2018 Dec 20. J Med Chem. 2019. PMID: 30570265 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. ChemMedChem. 2011 Oct 4;6(10):1832-40. doi: 10.1002/cmdc.201100278. Epub 2011 Aug 10. ChemMedChem. 2011. PMID: 21834094 Free PMC article.
Identification of inhibitors of the Leishmania cdc2-related protein kinase CRK3.
Cleghorn LA, Woodland A, Collie IT, Torrie LS, Norcross N, Luksch T, Mpamhanga C, Walker RG, Mottram JC, Brenk R, Frearson JA, Gilbert IH, Wyatt PG. Cleghorn LA, et al. ChemMedChem. 2011 Dec 9;6(12):2214-24. doi: 10.1002/cmdc.201100344. Epub 2011 Sep 13. ChemMedChem. 2011. PMID: 21913331 Free PMC article.
From on-target to off-target activity: identification and optimisation of Trypanosoma brucei GSK3 inhibitors and their characterisation as anti-Trypanosoma brucei drug discovery lead molecules.
Woodland A, Grimaldi R, Luksch T, Cleghorn LA, Ojo KK, Van Voorhis WC, Brenk R, Frearson JA, Gilbert IH, Wyatt PG. Woodland A, et al. ChemMedChem. 2013 Jul;8(7):1127-37. doi: 10.1002/cmdc.201300072. Epub 2013 Jun 14. ChemMedChem. 2013. PMID: 23776181 Free PMC article.
Identification of Morpholino Thiophenes as Novel Mycobacterium tuberculosis Inhibitors, Targeting QcrB.
Cleghorn LAT, Ray PC, Odingo J, Kumar A, Wescott H, Korkegian A, Masquelin T, Lopez Moure A, Wilson C, Davis S, Huggett M, Turner P, Smith A, Epemolu O, Zuccotto F, Riley J, Scullion P, Shishikura Y, Ferguson L, Rullas J, Guijarro L, Read KD, Green SR, Hipskind P, Parish T, Wyatt PG. Cleghorn LAT, et al. J Med Chem. 2018 Aug 9;61(15):6592-6608. doi: 10.1021/acs.jmedchem.8b00172. Epub 2018 Jul 26. J Med Chem. 2018. PMID: 29944372 Free PMC article.
18 results