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Items: 14

1.

Rational Design, Synthesis, and Biological Evaluation of Heterocyclic Quinolones Targeting the Respiratory Chain of Mycobacterium tuberculosis.

Hong WD, Gibbons PD, Leung SC, Amewu R, Stocks PA, Stachulski A, Horta P, Cristiano MLS, Shone AE, Moss D, Ardrey A, Sharma R, Warman AJ, Bedingfield PTP, Fisher NE, Aljayyoussi G, Mead S, Caws M, Berry NG, Ward SA, Biagini GA, O'Neill PM, Nixon GL.

J Med Chem. 2017 May 11;60(9):3703-3726. doi: 10.1021/acs.jmedchem.6b01718. Epub 2017 Apr 25.

2.

Targeting the mitochondrial electron transport chain of Plasmodium falciparum: new strategies towards the development of improved antimalarials for the elimination era.

Nixon GL, Pidathala C, Shone AE, Antoine T, Fisher N, O'Neill PM, Ward SA, Biagini GA.

Future Med Chem. 2013 Sep;5(13):1573-91. doi: 10.4155/fmc.13.121. Erratum in: Future Med Chem. 2013 Oct;5(16):2010.

3.

Antimalarial pharmacology and therapeutics of atovaquone.

Nixon GL, Moss DM, Shone AE, Lalloo DG, Fisher N, O'Neill PM, Ward SA, Biagini GA.

J Antimicrob Chemother. 2013 May;68(5):977-85. doi: 10.1093/jac/dks504. Epub 2013 Jan 4. Review.

4.

Generation of quinolone antimalarials targeting the Plasmodium falciparum mitochondrial respiratory chain for the treatment and prophylaxis of malaria.

Biagini GA, Fisher N, Shone AE, Mubaraki MA, Srivastava A, Hill A, Antoine T, Warman AJ, Davies J, Pidathala C, Amewu RK, Leung SC, Sharma R, Gibbons P, Hong DW, Pacorel B, Lawrenson AS, Charoensutthivarakul S, Taylor L, Berger O, Mbekeani A, Stocks PA, Nixon GL, Chadwick J, Hemingway J, Delves MJ, Sinden RE, Zeeman AM, Kocken CH, Berry NG, O'Neill PM, Ward SA.

Proc Natl Acad Sci U S A. 2012 May 22;109(21):8298-303. doi: 10.1073/pnas.1205651109. Epub 2012 May 7.

5.

Identification of novel antimalarial chemotypes via chemoinformatic compound selection methods for a high-throughput screening program against the novel malarial target, PfNDH2: increasing hit rate via virtual screening methods.

Sharma R, Lawrenson AS, Fisher NE, Warman AJ, Shone AE, Hill A, Mbekeani A, Pidathala C, Amewu RK, Leung S, Gibbons P, Hong DW, Stocks P, Nixon GL, Chadwick J, Shearer J, Gowers I, Cronk D, Parel SP, O'Neill PM, Ward SA, Biagini GA, Berry NG.

J Med Chem. 2012 Apr 12;55(7):3144-54. doi: 10.1021/jm3001482. Epub 2012 Mar 22.

6.

Identification, design and biological evaluation of heterocyclic quinolones targeting Plasmodium falciparum type II NADH:quinone oxidoreductase (PfNDH2).

Leung SC, Gibbons P, Amewu R, Nixon GL, Pidathala C, Hong WD, Pacorel B, Berry NG, Sharma R, Stocks PA, Srivastava A, Shone AE, Charoensutthivarakul S, Taylor L, Berger O, Mbekeani A, Hill A, Fisher NE, Warman AJ, Biagini GA, Ward SA, O'Neill PM.

J Med Chem. 2012 Mar 8;55(5):1844-57. doi: 10.1021/jm201184h. Epub 2012 Feb 24.

7.

Identification, design and biological evaluation of bisaryl quinolones targeting Plasmodium falciparum type II NADH:quinone oxidoreductase (PfNDH2).

Pidathala C, Amewu R, Pacorel B, Nixon GL, Gibbons P, Hong WD, Leung SC, Berry NG, Sharma R, Stocks PA, Srivastava A, Shone AE, Charoensutthivarakul S, Taylor L, Berger O, Mbekeani A, Hill A, Fisher NE, Warman AJ, Biagini GA, Ward SA, O'Neill PM.

J Med Chem. 2012 Mar 8;55(5):1831-43. doi: 10.1021/jm201179h. Epub 2012 Feb 24.

8.

Endoperoxide carbonyl falcipain 2/3 inhibitor hybrids: toward combination chemotherapy of malaria through a single chemical entity.

Gibbons P, Verissimo E, Araujo NC, Barton V, Nixon GL, Amewu RK, Chadwick J, Stocks PA, Biagini GA, Srivastava A, Rosenthal PJ, Gut J, Guedes RC, Moreira R, Sharma R, Berry N, Cristiano ML, Shone AE, Ward SA, O'Neill PM.

J Med Chem. 2010 Nov 25;53(22):8202-6. doi: 10.1021/jm1009567. Epub 2010 Oct 27.

PMID:
20979352
9.

Identification of a 1,2,4,5-tetraoxane antimalarial drug-development candidate (RKA 182) with superior properties to the semisynthetic artemisinins.

O'Neill PM, Amewu RK, Nixon GL, Bousejra ElGarah F, Mungthin M, Chadwick J, Shone AE, Vivas L, Lander H, Barton V, Muangnoicharoen S, Bray PG, Davies J, Park BK, Wittlin S, Brun R, Preschel M, Zhang K, Ward SA.

Angew Chem Int Ed Engl. 2010 Aug 2;49(33):5693-7. doi: 10.1002/anie.201001026. No abstract available.

PMID:
20629058
10.

Discovery of potent small-molecule inhibitors of multidrug-resistant Plasmodium falciparum using a novel miniaturized high-throughput luciferase-based assay.

Lucumi E, Darling C, Jo H, Napper AD, Chandramohanadas R, Fisher N, Shone AE, Jing H, Ward SA, Biagini GA, DeGrado WF, Diamond SL, Greenbaum DC.

Antimicrob Agents Chemother. 2010 Sep;54(9):3597-604. doi: 10.1128/AAC.00431-10. Epub 2010 Jun 14.

11.

Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.

O'Neill PM, Shone AE, Stanford D, Nixon G, Asadollahy E, Park BK, Maggs JL, Roberts P, Stocks PA, Biagini G, Bray PG, Davies J, Berry N, Hall C, Rimmer K, Winstanley PA, Hindley S, Bambal RB, Davis CB, Bates M, Gresham SL, Brigandi RA, Gomez-de-Las-Heras FM, Gargallo DV, Parapini S, Vivas L, Lander H, Taramelli D, Ward SA.

J Med Chem. 2009 Apr 9;52(7):1828-44. doi: 10.1021/jm8012757.

12.

Semi-synthetic and synthetic 1,2,4-trioxaquines and 1,2,4-trioxolaquines: synthesis, preliminary SAR and comparison with acridine endoperoxide conjugates.

Ara├║jo NC, Barton V, Jones M, Stocks PA, Ward SA, Davies J, Bray PG, Shone AE, Cristiano ML, O'Neill PM.

Bioorg Med Chem Lett. 2009 Apr 1;19(7):2038-43. doi: 10.1016/j.bmcl.2009.02.013. Epub 2009 Feb 8.

PMID:
19251414
13.

Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century.

O'Neill PM, Park BK, Shone AE, Maggs JL, Roberts P, Stocks PA, Biagini GA, Bray PG, Gibbons P, Berry N, Winstanley PA, Mukhtar A, Bonar-Law R, Hindley S, Bambal RB, Davis CB, Bates M, Hart TK, Gresham SL, Lawrence RM, Brigandi RA, Gomez-delas-Heras FM, Gargallo DV, Ward SA.

J Med Chem. 2009 Mar 12;52(5):1408-15. doi: 10.1021/jm8012618.

PMID:
19222165
14.

Comparative preclinical drug metabolism and pharmacokinetic evaluation of novel 4-aminoquinoline anti-malarials.

Davis CB, Bambal R, Moorthy GS, Hugger E, Xiang H, Park BK, Shone AE, O'Neill PM, Ward SA.

J Pharm Sci. 2009 Jan;98(1):362-77. doi: 10.1002/jps.21469.

PMID:
18563832

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