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Items: 1 to 50 of 156

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.

Discovery of Benzoylsulfonohydrazides as Potent Inhibitors of the Histone Acetyltransferase KAT6A.

Leaver DJ, Cleary B, Nguyen N, Priebbenow DL, Lagiakos HR, Sanchez J, Xue L, Huang F, Sun Y, Mujumdar P, Mudududdla R, Varghese S, Teguh S, Charman SA, White KL, Katneni K, Cuellar M, Strasser JM, Dahlin JL, Walters MA, Street IP, Monahan BJ, Jarman KE, Sabroux HJ, Falk H, Chung MC, Hermans SJ, Parker MW, Thomas T, Baell JB.

J Med Chem. 2019 Aug 8;62(15):7146-7159. doi: 10.1021/acs.jmedchem.9b00665. Epub 2019 Jul 17.

PMID:
31256587
3.

Novel Human Aminopeptidase N Inhibitors: Discovery and Optimization of Subsite Binding Interactions.

Lee J, Vinh NB, Drinkwater N, Yang W, Kannan Sivaraman K, Schembri LS, Gazdik M, Grin PM, Butler GS, Overall CM, Charman SA, McGowan S, Scammells PJ.

J Med Chem. 2019 Aug 8;62(15):7185-7209. doi: 10.1021/acs.jmedchem.9b00757. Epub 2019 Jul 18.

PMID:
31251594
4.

Ozonide Antimalarial Activity in the Context of Artemisinin-Resistant Malaria.

Giannangelo C, Fowkes FJI, Simpson JA, Charman SA, Creek DJ.

Trends Parasitol. 2019 Jul;35(7):529-543. doi: 10.1016/j.pt.2019.05.002. Epub 2019 Jun 5. Review.

5.

Falcipain Inhibitors Based on the Natural Product Gallinamide A Are Potent in Vitro and in Vivo Antimalarials.

Stoye A, Juillard A, Tang AH, Legac J, Gut J, White KL, Charman SA, Rosenthal PJ, Grau GER, Hunt NH, Payne RJ.

J Med Chem. 2019 Jun 13;62(11):5562-5578. doi: 10.1021/acs.jmedchem.9b00504. Epub 2019 May 22.

PMID:
31062592
6.

3,3'-Disubstituted 5,5'-Bi(1,2,4-triazine) Derivatives with Potent in Vitro and in Vivo Antimalarial Activity.

Xue L, Shi DH, Harjani JR, Huang F, Beveridge JG, Dingjan T, Ban K, Diab S, Duffy S, Lucantoni L, Fletcher S, Chiu FCK, Blundell S, Ellis K, Ralph SA, Wirjanata G, Teguh S, Noviyanti R, Chavchich M, Creek D, Price RN, Marfurt J, Charman SA, Cuellar ME, Strasser JM, Dahlin JL, Walters MA, Edstein MD, Avery VM, Baell JB.

J Med Chem. 2019 Mar 14;62(5):2485-2498. doi: 10.1021/acs.jmedchem.8b01799. Epub 2019 Mar 5.

PMID:
30715882
7.

Evaluation of 4-Amino 2-Anilinoquinazolines against Plasmodium and Other Apicomplexan Parasites In Vitro and in a P. falciparum Humanized NOD-scid IL2Rγnull Mouse Model of Malaria.

Gilson PR, Nguyen W, Poole WA, Teixeira JE, Thompson JK, Guo K, Stewart RJ, Ashton TD, White KL, Sanz LM, Gamo FJ, Charman SA, Wittlin S, Duffy J, Tonkin CJ, Tham WH, Crabb BS, Cooke BM, Huston CD, Cowman AF, Sleebs BE.

Antimicrob Agents Chemother. 2019 Feb 26;63(3). pii: e01804-18. doi: 10.1128/AAC.01804-18. Print 2019 Mar.

8.

Derivatives of a benzoquinone acyl hydrazone with activity against Toxoplasma gondii.

Sanford AG, Schulze TT, Potluri LP, Watson GF, Darner EB, Zach SJ, Hemsley RM, Wallick AI, Warner RC, Charman SA, Wang X, Vennerstrom JL, Davis PH.

Int J Parasitol Drugs Drug Resist. 2018 Dec;8(3):488-492. doi: 10.1016/j.ijpddr.2018.11.001. Epub 2018 Nov 10.

9.

SAR of a new antischistosomal urea carboxylic acid.

Wu J, Wang C, Häberli C, White KL, Shackleford DM, Chen G, Dong Y, Charman SA, Keiser J, Vennerstrom JL.

Bioorg Med Chem Lett. 2018 Dec 15;28(23-24):3648-3651. doi: 10.1016/j.bmcl.2018.10.039. Epub 2018 Oct 25.

PMID:
30389288
10.

Inhibition of Cytomegalovirus Replication with Extended-Half-Life Synthetic Ozonides.

Wang Y, Mukhopadhyay R, Roy S, Kapoor A, Su YP, Charman SA, Chen G, Wu J, Wang X, Vennerstrom JL, Arav-Boger R.

Antimicrob Agents Chemother. 2018 Dec 21;63(1). pii: e01735-18. doi: 10.1128/AAC.01735-18. Print 2019 Jan.

11.

Erratum for Brunschwig et al., "UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria".

Brunschwig C, Lawrence N, Taylor D, Abay E, Njoroge M, Basarab GS, Le Manach C, Paquet T, Gonzàlez Cabrera D, Nchinda AT, de Kock C, Wiesner L, Denti P, Waterson D, Blasco B, Leroy D, Witty MJ, Donini C, Duffy J, Wittlin S, White KL, Charman SA, Jiménez-Díaz MB, Angulo-Barturen I, Herreros E, Gamo FJ, Rochford R, Mancama D, Coetzer TL, van der Watt ME, Reader J, Birkholtz LM, Marsh KC, Solapure SM, Burke JE, McPhail JA, Vanaerschot M, Fidock DA, Fish PV, Siegl P, Smith DA, Wirjanata G, Noviyanti R, Price RN, Marfurt J, Silue KD, Street LJ, Chibale K.

Antimicrob Agents Chemother. 2018 Oct 24;62(11). pii: e01941-18. doi: 10.1128/AAC.01941-18. Print 2018 Nov. No abstract available.

12.

Using Human Plasma as an Assay Medium in Caco-2 Studies Improves Mass Balance for Lipophilic Compounds.

Katneni K, Pham T, Saunders J, Chen G, Patil R, White KL, Abla N, Chiu FCK, Shackleford DM, Charman SA.

Pharm Res. 2018 Sep 17;35(11):210. doi: 10.1007/s11095-018-2493-3.

13.

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.

14.

Inhibitors of histone acetyltransferases KAT6A/B induce senescence and arrest tumour growth.

Baell JB, Leaver DJ, Hermans SJ, Kelly GL, Brennan MS, Downer NL, Nguyen N, Wichmann J, McRae HM, Yang Y, Cleary B, Lagiakos HR, Mieruszynski S, Pacini G, Vanyai HK, Bergamasco MI, May RE, Davey BK, Morgan KJ, Sealey AJ, Wang B, Zamudio N, Wilcox S, Garnham AL, Sheikh BN, Aubrey BJ, Doggett K, Chung MC, de Silva M, Bentley J, Pilling P, Hattarki M, Dolezal O, Dennis ML, Falk H, Ren B, Charman SA, White KL, Rautela J, Newbold A, Hawkins ED, Johnstone RW, Huntington ND, Peat TS, Heath JK, Strasser A, Parker MW, Smyth GK, Street IP, Monahan BJ, Voss AK, Thomas T.

Nature. 2018 Aug;560(7717):253-257. doi: 10.1038/s41586-018-0387-5. Epub 2018 Aug 1.

PMID:
30069049
15.

UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria.

Brunschwig C, Lawrence N, Taylor D, Abay E, Njoroge M, Basarab GS, Le Manach C, Paquet T, Cabrera DG, Nchinda AT, de Kock C, Wiesner L, Denti P, Waterson D, Blasco B, Leroy D, Witty MJ, Donini C, Duffy J, Wittlin S, White KL, Charman SA, Jiménez-Díaz MB, Angulo-Barturen I, Herreros E, Gamo FJ, Rochford R, Mancama D, Coetzer TL, van der Watt ME, Reader J, Birkholtz LM, Marsh KC, Solapure SM, Burke JE, McPhail JA, Vanaerschot M, Fidock DA, Fish PV, Siegl P, Smith DA, Wirjanata G, Noviyanti R, Price RN, Marfurt J, Silue KD, Street LJ, Chibale K.

Antimicrob Agents Chemother. 2018 Aug 27;62(9). pii: e00012-18. doi: 10.1128/AAC.00012-18. Print 2018 Sep. Erratum in: Antimicrob Agents Chemother. 2018 Oct 24;62(11):.

16.

Synthesis and profiling of benzylmorpholine 1,2,4,5-tetraoxane analogue N205: Towards tetraoxane scaffolds with potential for single dose cure of malaria.

O' Neill PM, Stocks PA, Sabbani S, Roberts NL, Amewu RK, Shore ER, Aljayyoussi G, Angulo-Barturén I, Belén M, Jiménez-Díaz, Bazaga SF, Martínez MS, Campo B, Sharma R, Charman SA, Ryan E, Chen G, Shackleford DM, Davies J, Nixon GL, Biagini GA, Ward SA.

Bioorg Med Chem. 2018 Jul 15;26(11):2996-3005. doi: 10.1016/j.bmc.2018.05.006. Epub 2018 May 17.

PMID:
29779669
17.

Assessing drug efficacy against Plasmodium falciparum liver stages in vivo.

Flannery EL, Foquet L, Chuenchob V, Fishbaugher M, Billman Z, Navarro MJ, Betz W, Olsen TM, Lee J, Camargo N, Nguyen T, Schafer C, Sack BK, Wilson EM, Saunders J, Bial J, Campo B, Charman SA, Murphy SC, Phillips MA, Kappe SH, Mikolajczak SA.

JCI Insight. 2018 Jan 11;3(1). pii: 92587. doi: 10.1172/jci.insight.92587. eCollection 2018 Jan 11.

18.

Progress in antischistosomal N,N'-diaryl urea SAR.

Wu J, Wang C, Leas D, Vargas M, White KL, Shackleford DM, Chen G, Sanford AG, Hemsley RM, Davis PH, Dong Y, Charman SA, Keiser J, Vennerstrom JL.

Bioorg Med Chem Lett. 2018 Feb 1;28(3):244-248. doi: 10.1016/j.bmcl.2017.12.064. Epub 2017 Dec 29.

19.

Parasite-Mediated Degradation of Synthetic Ozonide Antimalarials Impacts In Vitro Antimalarial Activity.

Giannangelo C, Stingelin L, Yang T, Tilley L, Charman SA, Creek DJ.

Antimicrob Agents Chemother. 2018 Feb 23;62(3). pii: e01566-17. doi: 10.1128/AAC.01566-17. Print 2018 Mar.

20.

Long-Lasting and Fast-Acting in Vivo Efficacious Antiplasmodial Azepanylcarbazole Amino Alcohol.

Abla N, Bashyam S, Charman SA, Greco B, Hewitt P, Jiménez-Díaz MB, Katneni K, Kubas H, Picard D, Sambandan Y, Sanz L, Smith D, Wang T, Willis P, Wittlin S, Spangenberg T.

ACS Med Chem Lett. 2017 Nov 28;8(12):1304-1308. doi: 10.1021/acsmedchemlett.7b00391. eCollection 2017 Dec 14.

21.

Novel Toxoplasma gondii inhibitor chemotypes.

Sanford AG, Schulze TT, Potluri LP, Hemsley RM, Larson JJ, Judge AK, Zach SJ, Wang X, Charman SA, Vennerstrom JL, Davis PH.

Parasitol Int. 2018 Apr;67(2):107-111. doi: 10.1016/j.parint.2017.10.010. Epub 2018 Jan 4.

22.

The novel compound PBT434 prevents iron mediated neurodegeneration and alpha-synuclein toxicity in multiple models of Parkinson's disease.

Finkelstein DI, Billings JL, Adlard PA, Ayton S, Sedjahtera A, Masters CL, Wilkins S, Shackleford DM, Charman SA, Bal W, Zawisza IA, Kurowska E, Gundlach AL, Ma S, Bush AI, Hare DJ, Doble PA, Crawford S, Gautier EC, Parsons J, Huggins P, Barnham KJ, Cherny RA.

Acta Neuropathol Commun. 2017 Jun 28;5(1):53. doi: 10.1186/s40478-017-0456-2.

23.

Antimalarial Inhibitors Targeting Serine Hydroxymethyltransferase (SHMT) with in Vivo Efficacy and Analysis of their Binding Mode Based on X-ray Cocrystal Structures.

Schwertz G, Witschel MC, Rottmann M, Bonnert R, Leartsakulpanich U, Chitnumsub P, Jaruwat A, Ittarat W, Schäfer A, Aponte RA, Charman SA, White KL, Kundu A, Sadhukhan S, Lloyd M, Freiberg GM, Srikumaran M, Siggel M, Zwyssig A, Chaiyen P, Diederich F.

J Med Chem. 2017 Jun 22;60(12):4840-4860. doi: 10.1021/acs.jmedchem.7b00008. Epub 2017 Jun 13.

PMID:
28537728
24.

A tetraoxane-based antimalarial drug candidate that overcomes PfK13-C580Y dependent artemisinin resistance.

O'Neill PM, Amewu RK, Charman SA, Sabbani S, Gnädig NF, Straimer J, Fidock DA, Shore ER, Roberts NL, Wong MH, Hong WD, Pidathala C, Riley C, Murphy B, Aljayyoussi G, Gamo FJ, Sanz L, Rodrigues J, Cortes CG, Herreros E, Angulo-Barturén I, Jiménez-Díaz MB, Bazaga SF, Martínez-Martínez MS, Campo B, Sharma R, Ryan E, Shackleford DM, Campbell S, Smith DA, Wirjanata G, Noviyanti R, Price RN, Marfurt J, Palmer MJ, Copple IM, Mercer AE, Ruecker A, Delves MJ, Sinden RE, Siegl P, Davies J, Rochford R, Kocken CHM, Zeeman AM, Nixon GL, Biagini GA, Ward SA.

Nat Commun. 2017 May 24;8:15159. doi: 10.1038/ncomms15159.

25.

Antimalarial efficacy of MMV390048, an inhibitor of Plasmodium phosphatidylinositol 4-kinase.

Paquet T, Le Manach C, Cabrera DG, Younis Y, Henrich PP, Abraham TS, Lee MCS, Basak R, Ghidelli-Disse S, Lafuente-Monasterio MJ, Bantscheff M, Ruecker A, Blagborough AM, Zakutansky SE, Zeeman AM, White KL, Shackleford DM, Mannila J, Morizzi J, Scheurer C, Angulo-Barturen I, Martínez MS, Ferrer S, Sanz LM, Gamo FJ, Reader J, Botha M, Dechering KJ, Sauerwein RW, Tungtaeng A, Vanachayangkul P, Lim CS, Burrows J, Witty MJ, Marsh KC, Bodenreider C, Rochford R, Solapure SM, Jiménez-Díaz MB, Wittlin S, Charman SA, Donini C, Campo B, Birkholtz LM, Hanson KK, Drewes G, Kocken CHM, Delves MJ, Leroy D, Fidock DA, Waterson D, Street LJ, Chibale K.

Sci Transl Med. 2017 Apr 26;9(387). pii: eaad9735. doi: 10.1126/scitranslmed.aad9735.

26.

Sansanmycin natural product analogues as potent and selective anti-mycobacterials that inhibit lipid I biosynthesis.

Tran AT, Watson EE, Pujari V, Conroy T, Dowman LJ, Giltrap AM, Pang A, Wong WR, Linington RG, Mahapatra S, Saunders J, Charman SA, West NP, Bugg TD, Tod J, Dowson CG, Roper DI, Crick DC, Britton WJ, Payne RJ.

Nat Commun. 2017 Mar 1;8:14414. doi: 10.1038/ncomms14414.

27.

Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).

Dong Y, Wang X, Kamaraj S, Bulbule VJ, Chiu FC, Chollet J, Dhanasekaran M, Hein CD, Papastogiannidis P, Morizzi J, Shackleford DM, Barker H, Ryan E, Scheurer C, Tang Y, Zhao Q, Zhou L, White KL, Urwyler H, Charman WN, Matile H, Wittlin S, Charman SA, Vennerstrom JL.

J Med Chem. 2017 Apr 13;60(7):2654-2668. doi: 10.1021/acs.jmedchem.6b01586. Epub 2017 Jan 18.

PMID:
28052200
28.

Novel inhibitors of Plasmodium falciparum based on 2,5-disubstituted furans.

Krake SH, Martinez PDG, McLaren J, Ryan E, Chen G, White K, Charman SA, Campbell S, Willis P, Dias LC.

Eur J Med Chem. 2017 Jan 27;126:929-936. doi: 10.1016/j.ejmech.2016.12.024. Epub 2016 Dec 11.

PMID:
28002775
29.

Revisiting the SAR of the Antischistosomal Aryl Hydantoin (Ro 13-3978).

Wang C, Zhao Q, Vargas M, Jones JO, White KL, Shackleford DM, Chen G, Saunders J, Ng AC, Chiu FC, Dong Y, Charman SA, Keiser J, Vennerstrom JL.

J Med Chem. 2016 Dec 8;59(23):10705-10718. Epub 2016 Nov 28.

30.

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.

31.

Identification of a Potential Antimalarial Drug Candidate from a Series of 2-Aminopyrazines by Optimization of Aqueous Solubility and Potency across the Parasite Life Cycle.

Le Manach C, Nchinda AT, Paquet T, Gonzàlez Cabrera D, Younis Y, Han Z, Bashyam S, Zabiulla M, Taylor D, Lawrence N, White KL, Charman SA, Waterson D, Witty MJ, Wittlin S, Botha ME, Nondaba SH, Reader J, Birkholtz LM, Jiménez-Díaz MB, Martínez MS, Ferrer S, Angulo-Barturen I, Meister S, Antonova-Koch Y, Winzeler EA, Street LJ, Chibale K.

J Med Chem. 2016 Nov 10;59(21):9890-9905. Epub 2016 Oct 26.

PMID:
27748596
32.

Nitroheterocyclic drugs cure experimental Trypanosoma cruzi infections more effectively in the chronic stage than in the acute stage.

Francisco AF, Jayawardhana S, Lewis MD, White KL, Shackleford DM, Chen G, Saunders J, Osuna-Cabello M, Read KD, Charman SA, Chatelain E, Kelly JM.

Sci Rep. 2016 Oct 17;6:35351. doi: 10.1038/srep35351.

33.

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.

34.

Hit-to-Lead Optimization of a Novel Class of Potent, Broad-Spectrum Trypanosomacides.

Russell S, Rahmani R, Jones AJ, Newson HL, Neilde K, Cotillo I, Rahmani Khajouei M, Ferrins L, Qureishi S, Nguyen N, Martinez-Martinez MS, Weaver DF, Kaiser M, Riley J, Thomas J, De Rycker M, Read KD, Flematti GR, Ryan E, Tanghe S, Rodriguez A, Charman SA, Kessler A, Avery VM, Baell JB, Piggott MJ.

J Med Chem. 2016 Nov 10;59(21):9686-9720. Epub 2016 Sep 19.

35.

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.

36.

Comparison of the Exposure Time Dependence of the Activities of Synthetic Ozonide Antimalarials and Dihydroartemisinin against K13 Wild-Type and Mutant Plasmodium falciparum Strains.

Yang T, Xie SC, Cao P, Giannangelo C, McCaw J, Creek DJ, Charman SA, Klonis N, Tilley L.

Antimicrob Agents Chemother. 2016 Jul 22;60(8):4501-10. doi: 10.1128/AAC.00574-16. Print 2016 Aug.

37.

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.

38.

Potent dual inhibitors of Plasmodium falciparum M1 and M17 aminopeptidases through optimization of S1 pocket interactions.

Drinkwater N, Vinh NB, Mistry SN, Bamert RS, Ruggeri C, Holleran JP, Loganathan S, Paiardini A, Charman SA, Powell AK, Avery VM, McGowan S, Scammells PJ.

Eur J Med Chem. 2016 Mar 3;110:43-64. doi: 10.1016/j.ejmech.2016.01.015. Epub 2016 Jan 13.

PMID:
26807544
39.

Trioxolane-Mediated Delivery of Mefloquine Limits Brain Exposure in a Mouse Model of Malaria.

Lauterwasser EM, Fontaine SD, Li H, Gut J, Katneni K, Charman SA, Rosenthal PJ, Bogyo M, Renslo AR.

ACS Med Chem Lett. 2015 Oct 2;6(11):1145-9. doi: 10.1021/acsmedchemlett.5b00296. eCollection 2015 Nov 12.

40.

Evidence for the in vitro bioactivation of aminopyrazole derivatives: trapping reactive aminopyrazole intermediates using glutathione ethyl ester in human liver microsomes.

Ryan E, Morrow BJ, Hemley CF, Pinson JA, Charman SA, Chiu FC, Foitzik RC.

Chem Res Toxicol. 2015 Sep 21;28(9):1747-52. doi: 10.1021/acs.chemrestox.5b00202. Epub 2015 Sep 8.

PMID:
26317231
41.

6-Arylpyrazine-2-carboxamides: A New Core for Trypanosoma brucei Inhibitors.

Rahmani R, Ban K, Jones AJ, Ferrins L, Ganame D, Sykes ML, Avery VM, White KL, Ryan E, Kaiser M, Charman SA, Baell JB.

J Med Chem. 2015 Sep 10;58(17):6753-65. doi: 10.1021/acs.jmedchem.5b00438. Epub 2015 Aug 30.

PMID:
26247439
42.

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.

43.

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.

44.

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

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