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Items: 27

1.

Substituted Aminoacetamides as Novel Leads for Malaria Treatment.

Norcross NR, Wilson C, Baragaña B, Hallyburton I, Osuna-Cabello M, Norval S, Riley J, Fletcher D, Sinden R, Delves M, Ruecker A, Duffy S, Meister S, Antonova-Koch Y, Crespo B, de Cózar C, Sanz LM, Gamo FJ, Avery VM, Frearson JA, Gray DW, Fairlamb AH, Winzeler EA, Waterson D, Campbell SF, Willis PA, Read KD, Gilbert IH.

ChemMedChem. 2019 Jul 17;14(14):1329-1335. doi: 10.1002/cmdc.201900329. Epub 2019 Jul 3.

PMID:
31188540
2.

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.

J Med Chem. 2019 Feb 14;62(3):1180-1202. doi: 10.1021/acs.jmedchem.8b01218. Epub 2018 Dec 20.

3.

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.

J Med Chem. 2018 Sep 27;61(18):8374-8389. doi: 10.1021/acs.jmedchem.8b00884. Epub 2018 Sep 12.

4.

A role for trypanosomatid aldo-keto reductases in methylglyoxal, prostaglandin and isoprostane metabolism.

Roberts AJ, Dunne J, Scullion P, Norval S, Fairlamb AH.

Biochem J. 2018 Aug 30;475(16):2593-2610. doi: 10.1042/BCJ20180232.

5.

Antitrypanosomal 8-Hydroxy-Naphthyridines Are Chelators of Divalent Transition Metals.

Wall RJ, Moniz S, Thomas MG, Norval S, Ko EJ, Marco M, Miles TJ, Gilbert IH, Horn D, Fairlamb AH, Wyllie S.

Antimicrob Agents Chemother. 2018 Jul 27;62(8). pii: e00235-18. doi: 10.1128/AAC.00235-18. Print 2018 Aug.

6.

Design and Synthesis of Brain Penetrant Trypanocidal N-Myristoyltransferase Inhibitors.

Bayliss T, Robinson DA, Smith VC, Brand S, McElroy SP, Torrie LS, Mpamhanga C, Norval S, Stojanovski L, Brenk R, Frearson JA, Read KD, Gilbert IH, Wyatt PG.

J Med Chem. 2017 Dec 14;60(23):9790-9806. doi: 10.1021/acs.jmedchem.7b01255. Epub 2017 Nov 22.

7.

Development of a Novel Lead that Targets M. tuberculosis Polyketide Synthase 13.

Aggarwal A, Parai MK, Shetty N, Wallis D, Woolhiser L, Hastings C, Dutta NK, Galaviz S, Dhakal RC, Shrestha R, Wakabayashi S, Walpole C, Matthews D, Floyd D, Scullion P, Riley J, Epemolu O, Norval S, Snavely T, Robertson GT, Rubin EJ, Ioerger TR, Sirgel FA, van der Merwe R, van Helden PD, Keller P, Böttger EC, Karakousis PC, Lenaerts AJ, Sacchettini JC.

Cell. 2017 Jul 13;170(2):249-259.e25. doi: 10.1016/j.cell.2017.06.025. Epub 2017 Jun 29.

8.

Activation of Bicyclic Nitro-drugs by a Novel Nitroreductase (NTR2) in Leishmania.

Wyllie S, Roberts AJ, Norval S, Patterson S, Foth BJ, Berriman M, Read KD, Fairlamb AH.

PLoS Pathog. 2016 Nov 3;12(11):e1005971. doi: 10.1371/journal.ppat.1005971. eCollection 2016 Nov.

9.

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.

J Med Chem. 2016 Nov 10;59(21):9672-9685. Epub 2016 Sep 10.

10.

Trisubstituted Pyrimidines as Efficacious and Fast-Acting Antimalarials.

Norcross NR, Baragaña B, Wilson C, Hallyburton I, Osuna-Cabello M, Norval S, Riley J, Stojanovski L, Simeons FR, Porzelle A, Grimaldi R, Wittlin S, Duffy S, Avery VM, Meister S, Sanz L, Jiménez-Díaz B, Angulo-Barturen I, Ferrer S, Martínez MS, Gamo FJ, Frearson JA, Gray DW, Fairlamb AH, Winzeler EA, Waterson D, Campbell SF, Willis P, Read KD, Gilbert IH.

J Med Chem. 2016 Jul 14;59(13):6101-20. doi: 10.1021/acs.jmedchem.6b00028. Epub 2016 Jun 17.

11.

Corrigendum: A novel multiple-stage antimalarial agent that inhibits protein synthesis.

Baragaña B, Hallyburton I, Lee MC, Norcross NR, Grimaldi R, Otto TD, Proto WR, Blagborough AM, Meister S, Wirjanata G, Ruecker A, Upton LM, Abraham TS, Almeida MJ, Pradhan A, Porzelle A, Martínez MS, Bolscher JM, Woodland A, Luksch T, Norval S, Zuccotto F, Thomas J, Simeons F, Stojanovski L, Osuna-Cabello M, Brock PM, Churcher TS, Sala KA, Zakutansky SE, Jiménez-Díaz MB, Sanz LM, Riley J, Basak R, Campbell M, Avery VM, Sauerwein RW, Dechering KJ, Noviyanti R, Campo B, Frearson JA, Angulo-Barturen I, Ferrer-Bazaga S, Gamo FJ, Wyatt PG, Leroy D, Siegl P, Delves MJ, Kyle DE, Wittlin S, Marfurt J, Price RN, Sinden RE, Winzeler EA, Charman SA, Bebrevska L, Gray DW, Campbell S, Fairlamb AH, Willis PA, Rayner JC, Fidock DA, Read KD, Gilbert IH.

Nature. 2016 Sep 1;537(7618):122. doi: 10.1038/nature18280. Epub 2016 May 25. No abstract available.

12.

The anti-tubercular drug delamanid as a potential oral treatment for visceral leishmaniasis.

Patterson S, Wyllie S, Norval S, Stojanovski L, Simeons FR, Auer JL, Osuna-Cabello M, Read KD, Fairlamb AH.

Elife. 2016 May 24;5. pii: e09744. doi: 10.7554/eLife.09744.

13.

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.

J Med Chem. 2015 Oct 8;58(19):7695-706. doi: 10.1021/acs.jmedchem.5b00596. Epub 2015 Sep 29.

14.

Development of Small-Molecule Trypanosoma brucei N-Myristoyltransferase Inhibitors: Discovery and Optimisation of a Novel Binding Mode.

Spinks D, Smith V, Thompson S, Robinson DA, Luksch T, Smith A, Torrie LS, McElroy S, Stojanovski L, Norval S, Collie IT, Hallyburton I, Rao B, Brand S, Brenk R, Frearson JA, Read KD, Wyatt PG, Gilbert IH.

ChemMedChem. 2015 Nov;10(11):1821-36. doi: 10.1002/cmdc.201500301. Epub 2015 Sep 23.

15.

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.

ChemMedChem. 2015 Nov;10(11):1809-20. doi: 10.1002/cmdc.201500300. Epub 2015 Sep 18.

16.

A novel multiple-stage antimalarial agent that inhibits protein synthesis.

Baragaña B, Hallyburton I, Lee MC, Norcross NR, Grimaldi R, Otto TD, Proto WR, Blagborough AM, Meister S, Wirjanata G, Ruecker A, Upton LM, Abraham TS, Almeida MJ, Pradhan A, Porzelle A, Luksch T, Martínez MS, Luksch T, Bolscher JM, Woodland A, Norval S, Zuccotto F, Thomas J, Simeons F, Stojanovski L, Osuna-Cabello M, Brock PM, Churcher TS, Sala KA, Zakutansky SE, Jiménez-Díaz MB, Sanz LM, Riley J, Basak R, Campbell M, Avery VM, Sauerwein RW, Dechering KJ, Noviyanti R, Campo B, Frearson JA, Angulo-Barturen I, Ferrer-Bazaga S, Gamo FJ, Wyatt PG, Leroy D, Siegl P, Delves MJ, Kyle DE, Wittlin S, Marfurt J, Price RN, Sinden RE, Winzeler EA, Charman SA, Bebrevska L, Gray DW, Campbell S, Fairlamb AH, Willis PA, Rayner JC, Fidock DA, Read KD, Gilbert IH.

Nature. 2015 Jun 18;522(7556):315-20. doi: 10.1038/nature14451. Erratum in: Nature. 2016 Sep 1;537(7618):122.

17.

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.

J Med Chem. 2014 Dec 11;57(23):9855-69. doi: 10.1021/jm500809c. Epub 2014 Nov 20.

18.

Structure-activity relationship studies of pyrrolone antimalarial agents.

Murugesan D, Kaiser M, White KL, Norval S, Riley J, Wyatt PG, Charman SA, Read KD, Yeates C, Gilbert IH.

ChemMedChem. 2013 Sep;8(9):1537-44. doi: 10.1002/cmdc.201300177. Epub 2013 Aug 5.

19.

The R enantiomer of the antitubercular drug PA-824 as a potential oral treatment for visceral Leishmaniasis.

Patterson S, Wyllie S, Stojanovski L, Perry MR, Simeons FR, Norval S, Osuna-Cabello M, De Rycker M, Read KD, Fairlamb AH.

Antimicrob Agents Chemother. 2013 Oct;57(10):4699-706. doi: 10.1128/AAC.00722-13. Epub 2013 Jul 15.

20.

Automated design of ligands to polypharmacological profiles.

Besnard J, Ruda GF, Setola V, Abecassis K, Rodriguiz RM, Huang XP, Norval S, Sassano MF, Shin AI, Webster LA, Simeons FR, Stojanovski L, Prat A, Seidah NG, Constam DB, Bickerton GR, Read KD, Wetsel WC, Gilbert IH, Roth BL, Hopkins AL.

Nature. 2012 Dec 13;492(7428):215-20. doi: 10.1038/nature11691.

21.

Skin-targeted inhibition of PPAR β/δ by selective antagonists to treat PPAR β/δ-mediated psoriasis-like skin disease in vivo.

Hack K, Reilly L, Palmer C, Read KD, Norval S, Kime R, Booth K, Foerster J.

PLoS One. 2012;7(5):e37097. doi: 10.1371/journal.pone.0037097. Epub 2012 May 14.

22.

The anti-trypanosome drug fexinidazole shows potential for treating visceral leishmaniasis.

Wyllie S, Patterson S, Stojanovski L, Simeons FR, Norval S, Kime R, Read KD, Fairlamb AH.

Sci Transl Med. 2012 Feb 1;4(119):119re1. doi: 10.1126/scitranslmed.3003326.

23.

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.

J Med Chem. 2012 Jan 12;55(1):140-52. doi: 10.1021/jm201091t. Epub 2011 Dec 7.

24.

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.

ChemMedChem. 2011 Oct 4;6(10):1832-40. doi: 10.1002/cmdc.201100278. Epub 2011 Aug 10.

25.

Characterization of in vivo metabolites of WR319691, a novel compound with activity against Plasmodium falciparum.

Milner E, Sousa J, Pybus B, Melendez V, Gardner S, Grauer K, Moon J, Carroll D, Auschwitz J, Gettayacamin M, Lee P, Leed S, McCalmont W, Norval S, Tungtaeng A, Zeng Q, Kozar M, Read KD, Li Q, Dow G.

Eur J Drug Metab Pharmacokinet. 2011 Sep;36(3):151-8. doi: 10.1007/s13318-011-0047-8. Epub 2011 Jul 13.

PMID:
21751074
26.

Central nervous system exposure of next generation quinoline methanols is reduced relative to mefloquine after intravenous dosing in mice.

Dow GS, Milner E, Bathurst I, Bhonsle J, Caridha D, Gardner S, Gerena L, Kozar M, Lanteri C, Mannila A, McCalmont W, Moon J, Read KD, Norval S, Roncal N, Shackleford DM, Sousa J, Steuten J, White KL, Zeng Q, Charman SA.

Malar J. 2011 Jun 6;10:150. doi: 10.1186/1475-2875-10-150.

27.

Aryl phosphoramidates of 5-phospho erythronohydroxamic acid, a new class of potent trypanocidal compounds.

Ruda GF, Wong PE, Alibu VP, Norval S, Read KD, Barrett MP, Gilbert IH.

J Med Chem. 2010 Aug 26;53(16):6071-8. doi: 10.1021/jm1004754.

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