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Items: 1 to 50 of 56

1.

The Development Process for Discovery and Clinical Advancement of Modern Antimalarials.

Ashton TD, Devine SM, Möhrle JJ, Laleu B, Burrows JN, Charman SA, Creek DJ, Sleebs BE.

J Med Chem. 2019 Aug 20. doi: 10.1021/acs.jmedchem.9b00761. [Epub ahead of print]

PMID:
31385706
2.

Identification of Plasmodium falciparum Mitochondrial Malate: Quinone Oxidoreductase Inhibitors from the Pathogen Box.

Wang X, Miyazaki Y, Inaoka DK, Hartuti ED, Watanabe YI, Shiba T, Harada S, Saimoto H, Burrows JN, Benito FJG, Nozaki T, Kita K.

Genes (Basel). 2019 Jun 21;10(6). pii: E471. doi: 10.3390/genes10060471.

3.

Partnering to fight malaria in India: Past, present and future.

Samby K, Ramachandruni H, Banerji J, Burrows JN, Daumerie PG, Hooft van Huijsduijnen RAM, Duparc S, Wells TNC.

J Vector Borne Dis. 2019 Jan-Mar;56(1):15-24. doi: 10.4103/0972-9062.257769. Review.

4.

Cyclization-blocked proguanil as a strategy to improve the antimalarial activity of atovaquone.

Skinner-Adams TS, Fisher GM, Riches AG, Hutt OE, Jarvis KE, Wilson T, von Itzstein M, Chopra P, Antonova-Koch Y, Meister S, Winzeler EA, Clarke M, Fidock DA, Burrows JN, Ryan JH, Andrews KT.

Commun Biol. 2019 May 3;2:166. doi: 10.1038/s42003-019-0397-3. eCollection 2019.

5.

Injectable anti-malarials revisited: discovery and development of new agents to protect against malaria.

Macintyre F, Ramachandruni H, Burrows JN, Holm R, Thomas A, Möhrle JJ, Duparc S, Hooft van Huijsduijnen R, Greenwood B, Gutteridge WE, Wells TNC, Kaszubska W.

Malar J. 2018 Nov 1;17(1):402. doi: 10.1186/s12936-018-2549-1. Review.

6.

Target Validation and Identification of Novel Boronate Inhibitors of the Plasmodium falciparum Proteasome.

Xie SC, Gillett DL, Spillman NJ, Tsu C, Luth MR, Ottilie S, Duffy S, Gould AE, Hales P, Seager BA, Charron CL, Bruzzese F, Yang X, Zhao X, Huang SC, Hutton CA, Burrows JN, Winzeler EA, Avery VM, Dick LR, Tilley L.

J Med Chem. 2018 Nov 21;61(22):10053-10066. doi: 10.1021/acs.jmedchem.8b01161. Epub 2018 Nov 7.

7.

Isoxazolopyrimidine-Based Inhibitors of Plasmodium falciparum Dihydroorotate Dehydrogenase with Antimalarial Activity.

Kokkonda S, El Mazouni F, White KL, White J, Shackleford DM, Lafuente-Monasterio MJ, Rowland P, Manjalanagara K, Joseph JT, Garcia-Pérez A, Fernandez J, Gamo FJ, Waterson D, Burrows JN, Palmer MJ, Charman SA, Rathod PK, Phillips MA.

ACS Omega. 2018 Aug 31;3(8):9227-9240. doi: 10.1021/acsomega.8b01573. Epub 2018 Aug 15.

8.

Evaluation of Current and Emerging Antimalarial Medicines for Inhibition of Toxoplasma gondii Growth in Vitro.

Radke JB, Burrows JN, Goldberg DE, Sibley LD.

ACS Infect Dis. 2018 Aug 10;4(8):1264-1274. doi: 10.1021/acsinfecdis.8b00113. Epub 2018 Jul 25.

9.

Synthesis and Structure-Activity Relationships of the Novel Antimalarials 5-Pyridinyl-4(1 H)-Pyridones.

Bueno JM, Calderon F, Chicharro J, De la Rosa JC, Díaz B, Fernández J, Fiandor JM, Fraile MT, García M, Herreros E, García-Pérez A, Lorenzo M, Mallo A, Puente M, Saadeddin A, Ferrer S, Angulo-Barturen I, Burrows JN, León ML.

J Med Chem. 2018 Apr 26;61(8):3422-3435. doi: 10.1021/acs.jmedchem.7b01256. Epub 2018 Apr 5.

PMID:
29589932
10.

Design and Synthesis of Orally Bioavailable Piperazine Substituted 4(1H)-Quinolones with Potent Antimalarial Activity: Structure-Activity and Structure-Property Relationship Studies.

Neelarapu R, Maignan JR, Lichorowic CL, Monastyrskyi A, Mutka TS, LaCrue AN, Blake LD, Casandra D, Mashkouri S, Burrows JN, Willis PA, Kyle DE, Manetsch R.

J Med Chem. 2018 Feb 22;61(4):1450-1473. doi: 10.1021/acs.jmedchem.7b00738. Epub 2018 Feb 9.

11.

Malaria.

Phillips MA, Burrows JN, Manyando C, van Huijsduijnen RH, Van Voorhis WC, Wells TNC.

Nat Rev Dis Primers. 2017 Aug 3;3:17050. doi: 10.1038/nrdp.2017.50. Review.

PMID:
28770814
12.

Assessing the anthelmintic activity of pyrazole-5-carboxamide derivatives against Haemonchus contortus.

Jiao Y, Preston S, Song H, Jabbar A, Liu Y, Baell J, Hofmann A, Hutchinson D, Wang T, Koehler AV, Fisher GM, Andrews KT, Laleu B, Palmer MJ, Burrows JN, Wells TNC, Wang Q, Gasser RB.

Parasit Vectors. 2017 May 31;10(1):272. doi: 10.1186/s13071-017-2191-8.

13.

Erratum to: New developments in anti-malarial target candidate and product profiles.

Burrows JN, Duparc S, Gutteridge WE, van Huijsduijnen RH, Kaszubska W, Macintyre F, Mazzuri S, Möhrle JJ, Wells TNC.

Malar J. 2017 Apr 18;16(1):151. doi: 10.1186/s12936-017-1809-9. No abstract available.

14.

Antimalarial Pyrido[1,2-a]benzimidazoles: Lead Optimization, Parasite Life Cycle Stage Profile, Mechanistic Evaluation, Killing Kinetics, and in Vivo Oral Efficacy in a Mouse Model.

Singh K, Okombo J, Brunschwig C, Ndubi F, Barnard L, Wilkinson C, Njogu PM, Njoroge M, Laing L, Machado M, Prudêncio M, Reader J, Botha M, Nondaba S, Birkholtz LM, Lauterbach S, Churchyard A, Coetzer TL, Burrows JN, Yeates C, Denti P, Wiesner L, Egan TJ, Wittlin S, Chibale K.

J Med Chem. 2017 Feb 23;60(4):1432-1448. doi: 10.1021/acs.jmedchem.6b01641. Epub 2017 Feb 7.

PMID:
28094524
15.

New developments in anti-malarial target candidate and product profiles.

Burrows JN, Duparc S, Gutteridge WE, Hooft van Huijsduijnen R, Kaszubska W, Macintyre F, Mazzuri S, Möhrle JJ, Wells TNC.

Malar J. 2017 Jan 13;16(1):26. doi: 10.1186/s12936-016-1675-x. Review. Erratum in: Malar J. 2017 Apr 18;16(1):151.

16.

Open Source Drug Discovery: Highly Potent Antimalarial Compounds Derived from the Tres Cantos Arylpyrroles.

Williamson AE, Ylioja PM, Robertson MN, Antonova-Koch Y, Avery V, Baell JB, Batchu H, Batra S, Burrows JN, Bhattacharyya S, Calderon F, Charman SA, Clark J, Crespo B, Dean M, Debbert SL, Delves M, Dennis AS, Deroose F, Duffy S, Fletcher S, Giaever G, Hallyburton I, Gamo FJ, Gebbia M, Guy RK, Hungerford Z, Kirk K, Lafuente-Monasterio MJ, Lee A, Meister S, Nislow C, Overington JP, Papadatos G, Patiny L, Pham J, Ralph SA, Ruecker A, Ryan E, Southan C, Srivastava K, Swain C, Tarnowski MJ, Thomson P, Turner P, Wallace IM, Wells TN, White K, White L, Willis P, Winzeler EA, Wittlin S, Todd MH.

ACS Cent Sci. 2016 Oct 26;2(10):687-701. Epub 2016 Sep 14.

17.

A Triazolopyrimidine-Based Dihydroorotate Dehydrogenase Inhibitor with Improved Drug-like Properties for Treatment and Prevention of Malaria.

Phillips MA, White KL, Kokkonda S, Deng X, White J, El Mazouni F, Marsh K, Tomchick DR, Manjalanagara K, Rudra KR, Wirjanata G, Noviyanti R, Price RN, Marfurt J, Shackleford DM, Chiu FC, Campbell M, Jimenez-Diaz MB, Bazaga SF, Angulo-Barturen I, Martinez MS, Lafuente-Monasterio M, Kaminsky W, Silue K, Zeeman AM, Kocken C, Leroy D, Blasco B, Rossignol E, Rueckle T, Matthews D, Burrows JN, Waterson D, Palmer MJ, Rathod PK, Charman SA.

ACS Infect Dis. 2016 Dec 9;2(12):945-957. Epub 2016 Oct 4.

18.

Open data in drug discovery and development: lessons from malaria.

Wells TN, Willis P, Burrows JN, Hooft van Huijsduijnen R.

Nat Rev Drug Discov. 2016 Oct;15(10):661-2. doi: 10.1038/nrd.2016.154. Epub 2016 Aug 12.

PMID:
27516171
19.

ICI 56,780 Optimization: Structure-Activity Relationship Studies of 7-(2-Phenoxyethoxy)-4(1H)-quinolones with Antimalarial Activity.

Maignan JR, Lichorowic CL, Giarrusso J, Blake LD, Casandra D, Mutka TS, LaCrue AN, Burrows JN, Willis PA, Kyle DE, Manetsch R.

J Med Chem. 2016 Jul 28;59(14):6943-60. doi: 10.1021/acs.jmedchem.6b00759. Epub 2016 Jul 12.

PMID:
27291102
20.

Tetrahydro-2-naphthyl and 2-Indanyl Triazolopyrimidines Targeting Plasmodium falciparum Dihydroorotate Dehydrogenase Display Potent and Selective Antimalarial Activity.

Kokkonda S, Deng X, White KL, Coteron JM, Marco M, de Las Heras L, White J, El Mazouni F, Tomchick DR, Manjalanagara K, Rudra KR, Chen G, Morizzi J, Ryan E, Kaminsky W, Leroy D, Martínez-Martínez MS, Jimenez-Diaz MB, Bazaga SF, Angulo-Barturen I, Waterson D, Burrows JN, Matthews D, Charman SA, Phillips MA, Rathod PK.

J Med Chem. 2016 Jun 9;59(11):5416-31. doi: 10.1021/acs.jmedchem.6b00275. Epub 2016 May 21.

21.

Hit and lead criteria in drug discovery for infectious diseases of the developing world.

Katsuno K, Burrows JN, Duncan K, Hooft van Huijsduijnen R, Kaneko T, Kita K, Mowbray CE, Schmatz D, Warner P, Slingsby BT.

Nat Rev Drug Discov. 2015 Nov;14(11):751-8. doi: 10.1038/nrd4683. Epub 2015 Oct 5. Review.

PMID:
26435527
22.

A long-duration dihydroorotate dehydrogenase inhibitor (DSM265) for prevention and treatment of malaria.

Phillips MA, Lotharius J, Marsh K, White J, Dayan A, White KL, Njoroge JW, El Mazouni F, Lao Y, Kokkonda S, Tomchick DR, Deng X, Laird T, Bhatia SN, March S, Ng CL, Fidock DA, Wittlin S, Lafuente-Monasterio M, Benito FJ, Alonso LM, Martinez MS, Jimenez-Diaz MB, Bazaga SF, Angulo-Barturen I, Haselden JN, Louttit J, Cui Y, Sridhar A, Zeeman AM, Kocken C, Sauerwein R, Dechering K, Avery VM, Duffy S, Delves M, Sinden R, Ruecker A, Wickham KS, Rochford R, Gahagen J, Iyer L, Riccio E, Mirsalis J, Bathhurst I, Rueckle T, Ding X, Campo B, Leroy D, Rogers MJ, Rathod PK, Burrows JN, Charman SA.

Sci Transl Med. 2015 Jul 15;7(296):296ra111. doi: 10.1126/scitranslmed.aaa6645.

23.

ELQ-300 prodrugs for enhanced delivery and single-dose cure of malaria.

Miley GP, Pou S, Winter R, Nilsen A, Li Y, Kelly JX, Stickles AM, Mather MW, Forquer IP, Pershing AM, White K, Shackleford D, Saunders J, Chen G, Ting LM, Kim K, Zakharov LN, Donini C, Burrows JN, Vaidya AB, Charman SA, Riscoe MK.

Antimicrob Agents Chemother. 2015 Sep;59(9):5555-60. doi: 10.1128/AAC.01183-15. Epub 2015 Jun 29.

24.

Killing the hypnozoite--drug discovery approaches to prevent relapse in Plasmodium vivax.

Campo B, Vandal O, Wesche DL, Burrows JN.

Pathog Glob Health. 2015 May;109(3):107-22. doi: 10.1179/2047773215Y.0000000013. Epub 2015 Apr 18. Review.

25.

Subtle changes in endochin-like quinolone structure alter the site of inhibition within the cytochrome bc1 complex of Plasmodium falciparum.

Stickles AM, de Almeida MJ, Morrisey JM, Sheridan KA, Forquer IP, Nilsen A, Winter RW, Burrows JN, Fidock DA, Vaidya AB, Riscoe MK.

Antimicrob Agents Chemother. 2015 Apr;59(4):1977-82. doi: 10.1128/AAC.04149-14. Epub 2015 Jan 20.

26.

Orally bioavailable 6-chloro-7-methoxy-4(1H)-quinolones efficacious against multiple stages of Plasmodium.

Cross RM, Flanigan DL, Monastyrskyi A, LaCrue AN, Sáenz FE, Maignan JR, Mutka TS, White KL, Shackleford DM, Bathurst I, Fronczek FR, Wojtas L, Guida WC, Charman SA, Burrows JN, Kyle DE, Manetsch R.

J Med Chem. 2014 Nov 13;57(21):8860-79. doi: 10.1021/jm500942v. Epub 2014 Oct 22.

27.

Defining the biology component of the drug discovery strategy for malaria eradication.

Leroy D, Campo B, Ding XC, Burrows JN, Cherbuin S.

Trends Parasitol. 2014 Oct;30(10):478-90. doi: 10.1016/j.pt.2014.07.004. Epub 2014 Aug 15. Review.

PMID:
25131411
28.

Screening and hit evaluation of a chemical library against blood-stage Plasmodium falciparum.

Avery VM, Bashyam S, Burrows JN, Duffy S, Papadatos G, Puthukkuti S, Sambandan Y, Singh S, Spangenberg T, Waterson D, Willis P.

Malar J. 2014 May 27;13:190. doi: 10.1186/1475-2875-13-190.

29.

Fluorine modulates species selectivity in the triazolopyrimidine class of Plasmodium falciparum dihydroorotate dehydrogenase inhibitors.

Deng X, Kokkonda S, El Mazouni F, White J, Burrows JN, Kaminsky W, Charman SA, Matthews D, Rathod PK, Phillips MA.

J Med Chem. 2014 Jun 26;57(12):5381-94. doi: 10.1021/jm500481t. Epub 2014 Jun 13.

30.

Discovery, synthesis, and optimization of antimalarial 4(1H)-quinolone-3-diarylethers.

Nilsen A, Miley GP, Forquer IP, Mather MW, Katneni K, Li Y, Pou S, Pershing AM, Stickles AM, Ryan E, Kelly JX, Doggett JS, White KL, Hinrichs DJ, Winter RW, Charman SA, Zakharov LN, Bathurst I, Burrows JN, Vaidya AB, Riscoe MK.

J Med Chem. 2014 May 8;57(9):3818-34. doi: 10.1021/jm500147k. Epub 2014 Apr 18.

31.

In vitro and in vivo characterization of the antimalarial lead compound SSJ-183 in Plasmodium models.

Schleiferböck S, Scheurer C, Ihara M, Itoh I, Bathurst I, Burrows JN, Fantauzzi P, Lotharius J, Charman SA, Morizzi J, Shackleford DM, White KL, Brun R, Wittlin S.

Drug Des Devel Ther. 2013 Nov 15;7:1377-84. doi: 10.2147/DDDT.S51298. eCollection 2013.

32.

Antimalarial drug discovery - the path towards eradication.

Burrows JN, Burlot E, Campo B, Cherbuin S, Jeanneret S, Leroy D, Spangenberg T, Waterson D, Wells TN, Willis P.

Parasitology. 2014 Jan;141(1):128-39. doi: 10.1017/S0031182013000826. Epub 2013 Jul 17. Review.

33.

The open access malaria box: a drug discovery catalyst for neglected diseases.

Spangenberg T, Burrows JN, Kowalczyk P, McDonald S, Wells TN, Willis P.

PLoS One. 2013 Jun 17;8(6):e62906. doi: 10.1371/journal.pone.0062906. Print 2013.

34.

Designing the next generation of medicines for malaria control and eradication.

Burrows JN, van Huijsduijnen RH, Möhrle JJ, Oeuvray C, Wells TN.

Malar J. 2013 Jun 6;12:187. doi: 10.1186/1475-2875-12-187. Review.

35.

Quinolone-3-diarylethers: a new class of antimalarial drug.

Nilsen A, LaCrue AN, White KL, Forquer IP, Cross RM, Marfurt J, Mather MW, Delves MJ, Shackleford DM, Saenz FE, Morrisey JM, Steuten J, Mutka T, Li Y, Wirjanata G, Ryan E, Duffy S, Kelly JX, Sebayang BF, Zeeman AM, Noviyanti R, Sinden RE, Kocken CHM, Price RN, Avery VM, Angulo-Barturen I, Jiménez-Díaz MB, Ferrer S, Herreros E, Sanz LM, Gamo FJ, Bathurst I, Burrows JN, Siegl P, Guy RK, Winter RW, Vaidya AB, Charman SA, Kyle DE, Manetsch R, Riscoe MK.

Sci Transl Med. 2013 Mar 20;5(177):177ra37. doi: 10.1126/scitranslmed.3005029.

36.

Antimalarial drug discovery: where next?

Burrows JN.

Future Med Chem. 2012 Dec;4(18):2233-5. doi: 10.4155/fmc.12.189. No abstract available.

37.

Endochin-like quinolones are highly efficacious against acute and latent experimental toxoplasmosis.

Doggett JS, Nilsen A, Forquer I, Wegmann KW, Jones-Brando L, Yolken RH, Bordón C, Charman SA, Katneni K, Schultz T, Burrows JN, Hinrichs DJ, Meunier B, Carruthers VB, Riscoe MK.

Proc Natl Acad Sci U S A. 2012 Sep 25;109(39):15936-41. Epub 2012 Sep 10.

38.

The global pipeline of new medicines for the control and elimination of malaria.

Anthony MP, Burrows JN, Duparc S, Moehrle JJ, Wells TN.

Malar J. 2012 Sep 7;11:316. doi: 10.1186/1475-2875-11-316. Review.

39.

P. falciparum in vitro killing rates allow to discriminate between different antimalarial mode-of-action.

Sanz LM, Crespo B, De-Cózar C, Ding XC, Llergo JL, Burrows JN, García-Bustos JF, Gamo FJ.

PLoS One. 2012;7(2):e30949. doi: 10.1371/journal.pone.0030949. Epub 2012 Feb 23.

40.

Cyclopropyl carboxamides, a chemically novel class of antimalarial agents identified in a phenotypic screen.

Sanz LM, Jiménez-Díaz MB, Crespo B, De-Cozar C, Almela MJ, Angulo-Barturen I, Castañeda P, Ibañez J, Fernández EP, Ferrer S, Herreros E, Lozano S, Martínez MS, Rueda L, Burrows JN, García-Bustos JF, Gamo FJ.

Antimicrob Agents Chemother. 2011 Dec;55(12):5740-5. doi: 10.1128/AAC.05188-11. Epub 2011 Oct 3.

41.

Novel orally active antimalarial thiazoles.

González Cabrera D, Douelle F, Feng TS, Nchinda AT, Younis Y, White KL, Wu Q, Ryan E, Burrows JN, Waterson D, Witty MJ, Wittlin S, Charman SA, Chibale K.

J Med Chem. 2011 Nov 10;54(21):7713-9. doi: 10.1021/jm201108k. Epub 2011 Oct 11.

PMID:
21966980
42.

Challenges in antimalarial drug discovery.

Burrows JN, Leroy D, Lotharius J, Waterson D.

Future Med Chem. 2011 Sep;3(11):1401-12. doi: 10.4155/fmc.11.91. Review.

PMID:
21879844
43.

Structure-guided lead optimization of triazolopyrimidine-ring substituents identifies potent Plasmodium falciparum dihydroorotate dehydrogenase inhibitors with clinical candidate potential.

Coteron JM, Marco M, Esquivias J, Deng X, White KL, White J, Koltun M, El Mazouni F, Kokkonda S, Katneni K, Bhamidipati R, Shackleford DM, Angulo-Barturen I, Ferrer SB, Jiménez-Díaz MB, Gamo FJ, Goldsmith EJ, Charman WN, Bathurst I, Floyd D, Matthews D, Burrows JN, Rathod PK, Charman SA, Phillips MA.

J Med Chem. 2011 Aug 11;54(15):5540-61. doi: 10.1021/jm200592f. Epub 2011 Jul 14.

44.

The state of the art in anti-malarial drug discovery and development.

Burrows JN, Chibale K, Wells TN.

Curr Top Med Chem. 2011;11(10):1226-54. Review.

PMID:
21401508
45.

The design and synthesis of novel N-hydroxyformamide inhibitors of ADAM-TS4 for the treatment of osteoarthritis.

De Savi C, Pape A, Cumming JG, Ting A, Smith PD, Burrows JN, Mills M, Davies C, Lamont S, Milne D, Cook C, Moore P, Sawyer Y, Gerhardt S.

Bioorg Med Chem Lett. 2011 Mar 1;21(5):1376-81. doi: 10.1016/j.bmcl.2011.01.036. Epub 2011 Jan 18.

PMID:
21300546
46.

Endochin optimization: structure-activity and structure-property relationship studies of 3-substituted 2-methyl-4(1H)-quinolones with antimalarial activity.

Cross RM, Monastyrskyi A, Mutka TS, Burrows JN, Kyle DE, Manetsch R.

J Med Chem. 2010 Oct 14;53(19):7076-94. doi: 10.1021/jm1007903.

PMID:
20828199
47.

Targeting the hypnozoite reservoir of Plasmodium vivax: the hidden obstacle to malaria elimination.

Wells TN, Burrows JN, Baird JK.

Trends Parasitol. 2010 Mar;26(3):145-51. doi: 10.1016/j.pt.2009.12.005. Epub 2010 Feb 3. Review.

PMID:
20133198
48.

ProSAR: a new methodology for combinatorial library design.

Chen H, Börjesson U, Engkvist O, Kogej T, Svensson MA, Blomberg N, Weigelt D, Burrows JN, Lange T.

J Chem Inf Model. 2009 Mar;49(3):603-14.

PMID:
19434898
49.

An integrated approach to fragment-based lead generation: philosophy, strategy and case studies from AstraZeneca's drug discovery programmes.

Albert JS, Blomberg N, Breeze AL, Brown AJ, Burrows JN, Edwards PD, Folmer RH, Geschwindner S, Griffen EJ, Kenny PW, Nowak T, Olsson LL, Sanganee H, Shapiro AB.

Curr Top Med Chem. 2007;7(16):1600-29. Review.

PMID:
17979771
50.

Fragment screening: an introduction.

Leach AR, Hann MM, Burrows JN, Griffen EJ.

Mol Biosyst. 2006 Sep;2(9):430-46.

PMID:
17153140

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