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Items: 1 to 50 of 123

1.

Pharmacokinetics and Ex vivo Antimalarial Activity of Artesunate-Amodiaquine plus Methylene Blue in Healthy Volunteers.

Anh CX, Chavchich M, Birrell GW, Van Breda K, Travers T, Rowcliffe K, Lord AR, Shanks GD, Edstein MD.

Antimicrob Agents Chemother. 2020 Jan 6. pii: AAC.01441-19. doi: 10.1128/AAC.01441-19. [Epub ahead of print]

PMID:
31907186
2.

In Vivo Efficacy and Pharmacokinetics of the 2-Aminomethylphenol Antimalarial, JPC-3210, in the Aotus Monkey-Human Malaria Model.

McCallum F, Birrell GW, Chavchich M, Harris I, Obaldia N 3rd, Van Breda K, Heffernan GD, Jacobus DP, Shanks D, Edstein MD.

Antimicrob Agents Chemother. 2019 Dec 16. pii: AAC.01538-19. doi: 10.1128/AAC.01538-19. [Epub ahead of print]

PMID:
31843994
3.

Multi-omic Characterization of the Mode of Action of a Potent New Antimalarial Compound, JPC-3210, Against Plasmodium falciparum.

Birrell GW, Challis MP, De Paoli A, Anderson D, Devine SM, Heffernan GD, Jacobus DP, Edstein MD, Siddiqui G, Creek DJ.

Mol Cell Proteomics. 2020 Feb;19(2):308-325. doi: 10.1074/mcp.RA119.001797. Epub 2019 Dec 13.

PMID:
31836637
4.

Sulfide, sulfoxide and sulfone bridged acyclic nucleoside phosphonates as inhibitors of the Plasmodium falciparum and human 6-oxopurine phosphoribosyltransferases: Synthesis and evaluation.

Klejch T, Keough DT, Chavchich M, Travis J, Skácel J, Pohl R, Janeba Z, Edstein MD, Avery VM, Guddat LW, Hocková D.

Eur J Med Chem. 2019 Dec 1;183:111667. doi: 10.1016/j.ejmech.2019.111667. Epub 2019 Sep 4.

PMID:
31536893
5.

Development of pyridyl thiosemicarbazones as highly potent agents for the treatment of malaria after oral administration.

Parkinson CJ, Birrell GW, Chavchich M, Mackenzie D, Haynes RK, de Kock C, Richardson DR, Edstein MD.

J Antimicrob Chemother. 2019 Oct 1;74(10):2965-2973. doi: 10.1093/jac/dkz290.

PMID:
31325302
6.
7.

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
8.

Susceptibility of Plasmodium falciparum to artemisinins and Plasmodium vivax to chloroquine in Phuoc Chien Commune, Ninh Thuan Province, south-central Vietnam.

Phong NC, Chavchich M, Quang HH, San NN, Birrell GW, Chuang I, Martin NJ, Manh ND, Edstein MD.

Malar J. 2019 Jan 17;18(1):10. doi: 10.1186/s12936-019-2640-2.

9.

Comparison of the Pharmacokinetics and Ex Vivo Antimalarial Activities of Artesunate-Amodiaquine and Artemisinin-Piperaquine in Healthy Volunteers for Preselection Malaria Therapy.

Quang NN, Chavchich M, Anh CX, Birrell GW, van Breda K, Travers T, Rowcliffe K, Edstein MD.

Am J Trop Med Hyg. 2018 Jul;99(1):65-72. doi: 10.4269/ajtmh.17-0434. Epub 2018 May 3.

10.

Characterization of the Preclinical Pharmacology of the New 2-Aminomethylphenol, JPC-3210, for Malaria Treatment and Prevention.

Birrell GW, Heffernan GD, Schiehser GA, Anderson J, Ager AL, Morales P, MacKenzie D, van Breda K, Chavchich M, Jacobus LR, Shanks GD, Jacobus DP, Edstein MD.

Antimicrob Agents Chemother. 2018 Mar 27;62(4). pii: e01335-17. doi: 10.1128/AAC.01335-17. Print 2018 Apr.

11.

Design of Plasmodium vivax Hypoxanthine-Guanine Phosphoribosyltransferase Inhibitors as Potential Antimalarial Therapeutics.

Keough DT, Rejman D, Pohl R, Zborníková E, Hocková D, Croll T, Edstein MD, Birrell GW, Chavchich M, Naesens LMJ, Pierens GK, Brereton IM, Guddat LW.

ACS Chem Biol. 2018 Jan 19;13(1):82-90. doi: 10.1021/acschembio.7b00916. Epub 2017 Dec 5.

PMID:
29161011
12.

Synthesis and Evaluation of Asymmetric Acyclic Nucleoside Bisphosphonates as Inhibitors of Plasmodium falciparum and Human Hypoxanthine-Guanine-(Xanthine) Phosphoribosyltransferase.

Špaček P, Keough DT, Chavchich M, Dračínský M, Janeba Z, Naesens L, Edstein MD, Guddat LW, Hocková D.

J Med Chem. 2017 Sep 14;60(17):7539-7554. doi: 10.1021/acs.jmedchem.7b00926. Epub 2017 Aug 30.

PMID:
28813147
13.

Synthesis and evaluation of symmetric acyclic nucleoside bisphosphonates as inhibitors of the Plasmodium falciparum, Plasmodium vivax and human 6-oxopurine phosphoribosyltransferases and the antimalarial activity of their prodrugs.

Špaček P, Keough DT, Chavchich M, Dračínský M, Janeba Z, Naesens L, Edstein MD, Guddat LW, Hocková D.

Bioorg Med Chem. 2017 Aug 1;25(15):4008-4030. doi: 10.1016/j.bmc.2017.05.048. Epub 2017 May 24.

PMID:
28601510
14.

The Plasmodium PI(4)K inhibitor KDU691 selectively inhibits dihydroartemisinin-pretreated Plasmodium falciparum ring-stage parasites.

Dembele L, Ang X, Chavchich M, Bonamy GMC, Selva JJ, Lim MY, Bodenreider C, Yeung BKS, Nosten F, Russell BM, Edstein MD, Straimer J, Fidock DA, Diagana TT, Bifani P.

Sci Rep. 2017 May 24;7(1):2325. doi: 10.1038/s41598-017-02440-6.

15.

Population Pharmacokinetic Properties of Piperaquine in Falciparum Malaria: An Individual Participant Data Meta-Analysis.

Hoglund RM, Workman L, Edstein MD, Thanh NX, Quang NN, Zongo I, Ouedraogo JB, Borrmann S, Mwai L, Nsanzabana C, Price RN, Dahal P, Sambol NC, Parikh S, Nosten F, Ashley EA, Phyo AP, Lwin KM, McGready R, Day NP, Guerin PJ, White NJ, Barnes KI, Tarning J.

PLoS Med. 2017 Jan 10;14(1):e1002212. doi: 10.1371/journal.pmed.1002212. eCollection 2017 Jan.

16.
17.

The Spiroindolone KAE609 Does Not Induce Dormant Ring Stages in Plasmodium falciparum Parasites.

Chavchich M, Van Breda K, Rowcliffe K, Diagana TT, Edstein MD.

Antimicrob Agents Chemother. 2016 Aug 22;60(9):5167-74. doi: 10.1128/AAC.02838-15. Print 2016 Sep.

18.

Persistence and immunogenicity of chemically attenuated blood stage Plasmodium falciparum in Aotus monkeys.

De SL, Stanisic DI, van Breda K, Bellete B, Harris I, McCallum F, Edstein MD, Good MF.

Int J Parasitol. 2016 Aug;46(9):581-91. doi: 10.1016/j.ijpara.2016.05.002. Epub 2016 May 26.

PMID:
27238088
19.

In Vivo Efficacy and Tolerability of Artesunate-Azithromycin for the Treatment of Falciparum Malaria in Vietnam.

Phong NC, Quang HH, Thanh NX, Trung TN, Dai B, Shanks GD, Chavchich M, Edstein MD.

Am J Trop Med Hyg. 2016 Jul 6;95(1):164-7. doi: 10.4269/ajtmh.16-0144. Epub 2016 May 23.

20.

Efficacy of Artesunate-mefloquine for Chloroquine-resistant Plasmodium vivax Malaria in Malaysia: An Open-label, Randomized, Controlled Trial.

Grigg MJ, William T, Menon J, Barber BE, Wilkes CS, Rajahram GS, Edstein MD, Auburn S, Price RN, Yeo TW, Anstey NM.

Clin Infect Dis. 2016 Jun 1;62(11):1403-1411. doi: 10.1093/cid/ciw121. Epub 2016 Apr 22.

21.

Lead Selection of a New Aminomethylphenol, JPC-3210, for Malaria Treatment and Prevention.

Chavchich M, Birrell GW, Ager AL, MacKenzie DO, Heffernan GD, Schiehser GA, Jacobus LR, Shanks GD, Jacobus DP, Edstein MD.

Antimicrob Agents Chemother. 2016 Apr 22;60(5):3115-8. doi: 10.1128/AAC.03066-15. Print 2016 May.

22.

Evaluation of the 2-Aminomethylphenol JPC-2997 in Aotus Monkeys Infected with Plasmodium falciparum.

McCallum F, Harris I, van Breda K, De SL, Stanisic DI, Good MF, Jacobus DP, Edstein MD.

Antimicrob Agents Chemother. 2015 Dec 14;60(3):1948-9. doi: 10.1128/AAC.02799-15. No abstract available.

23.

Baseline data of parasite clearance in patients with falciparum malaria treated with an artemisinin derivative: an individual patient data meta-analysis.

WWARN Parasite Clearance Study Group, Abdulla S, Ashley EA, Bassat Q, Bethell D, Björkman A, Borrmann S, D'Alessandro U, Dahal P, Day NP, Diakite M, Djimde AA, Dondorp AM, Duong S, Edstein MD, Fairhurst RM, Faiz MA, Falade C, Flegg JA, Fogg C, Gonzalez R, Greenwood B, Guérin PJ, Guthmann JP, Hamed K, Hien TT, Htut Y, Juma E, Lim P, Mårtensson A, Mayxay M, Mokuolu OA, Moreira C, Newton P, Noedl H, Nosten F, Ogutu BR, Onyamboko MA, Owusu-Agyei S, Phyo AP, Premji Z, Price RN, Pukrittayakamee S, Ramharter M, Sagara I, Se Y, Suon S, Stepniewska K, Ward SA, White NJ, Winstanley PA.

Malar J. 2015 Sep 22;14:359. doi: 10.1186/s12936-015-0874-1.

24.

Synthesis and Evaluation of Novel Acyclic Nucleoside Phosphonates as Inhibitors of Plasmodium falciparum and Human 6-Oxopurine Phosphoribosyltransferases.

Kaiser MM, Hocková D, Wang TH, Dračínský M, Poštová-Slavětínská L, Procházková E, Edstein MD, Chavchich M, Keough DT, Guddat LW, Janeba Z.

ChemMedChem. 2015 Oct;10(10):1707-23. doi: 10.1002/cmdc.201500322. Epub 2015 Aug 25.

PMID:
26368337
25.

Antimalarial activity of prodrugs of N-branched acyclic nucleoside phosphonate inhibitors of 6-oxopurine phosphoribosyltransferases.

Hocková D, Janeba Z, Naesens L, Edstein MD, Chavchich M, Keough DT, Guddat LW.

Bioorg Med Chem. 2015 Sep 1;23(17):5502-10. doi: 10.1016/j.bmc.2015.07.038. Epub 2015 Jul 27.

PMID:
26275679
26.

Evolution from double to triple-antimalarial drug combinations.

Shanks GD, Edstein MD, Jacobus D.

Trans R Soc Trop Med Hyg. 2015 Mar;109(3):182-8. doi: 10.1093/trstmh/tru199. Epub 2014 Dec 30. Review.

PMID:
25549631
27.

Aza-acyclic nucleoside phosphonates containing a second phosphonate group as inhibitors of the human, Plasmodium falciparum and vivax 6-oxopurine phosphoribosyltransferases and their prodrugs as antimalarial agents.

Keough DT, Hocková D, Janeba Z, Wang TH, Naesens L, Edstein MD, Chavchich M, Guddat LW.

J Med Chem. 2015 Jan 22;58(2):827-46. doi: 10.1021/jm501416t. Epub 2014 Dec 24.

PMID:
25494538
28.

Synthesis and antimalarial evaluation of amide and urea derivatives based on the thiaplakortone A natural product scaffold.

Schwartz BD, Skinner-Adams TS, Andrews KT, Coster MJ, Edstein MD, MacKenzie D, Charman SA, Koltun M, Blundell S, Campbell A, Pouwer RH, Quinn RJ, Beattie KD, Healy PC, Davis RA.

Org Biomol Chem. 2015 Feb 7;13(5):1558-70. doi: 10.1039/c4ob01849d.

PMID:
25490858
29.

JPC-2997, a new aminomethylphenol with high in vitro and in vivo antimalarial activities against blood stages of Plasmodium.

Birrell GW, Chavchich M, Ager AL, Shieh HM, Heffernan GD, Zhao W, Krasucki PE, Saionz KW, Terpinski J, Schiehser GA, Jacobus LR, Shanks GD, Jacobus DP, Edstein MD.

Antimicrob Agents Chemother. 2015 Jan;59(1):170-7. doi: 10.1128/AAC.03762-14. Epub 2014 Oct 20.

30.

Assessment of the induction of dormant ring stages in Plasmodium falciparum parasites by artemisone and artemisone entrapped in Pheroid vesicles in vitro.

Grobler L, Chavchich M, Haynes RK, Edstein MD, Grobler AF.

Antimicrob Agents Chemother. 2014 Dec;58(12):7579-82. doi: 10.1128/AAC.02707-14. Epub 2014 Oct 6.

31.

Total synthesis of thiaplakortone a: derivatives as metabolically stable leads for the treatment of malaria.

Pouwer RH, Deydier SM, Le PV, Schwartz BD, Franken NC, Davis RA, Coster MJ, Charman SA, Edstein MD, Skinner-Adams TS, Andrews KT, Jenkins ID, Quinn RJ.

ACS Med Chem Lett. 2013 Dec 27;5(2):178-82. doi: 10.1021/ml400447v. eCollection 2014 Feb 13.

32.

Acyclic nucleoside phosphonates containing a second phosphonate group are potent inhibitors of 6-oxopurine phosphoribosyltransferases and have antimalarial activity.

Keough DT, Špaček P, Hocková D, Tichý T, Vrbková S, Slavětínská L, Janeba Z, Naesens L, Edstein MD, Chavchich M, Wang TH, de Jersey J, Guddat LW.

J Med Chem. 2013 Mar 28;56(6):2513-26. doi: 10.1021/jm301893b. Epub 2013 Mar 19.

PMID:
23448281
33.

Population pharmacokinetics of halofantrine in healthy volunteers and patients with symptomatic falciparum malaria.

Klein K, Aarons L, Ter Kuile FO, Nosten F, White NJ, Edstein MD, Teja-Isavadharm P.

J Pharm Pharmacol. 2012 Nov;64(11):1603-13. doi: 10.1111/j.2042-7158.2012.01554.x. Epub 2012 Jul 9.

PMID:
23058047
34.
35.

Antimalarial activity of pyrroloiminoquinones from the Australian marine sponge Zyzzya sp.

Davis RA, Buchanan MS, Duffy S, Avery VM, Charman SA, Charman WN, White KL, Shackleford DM, Edstein MD, Andrews KT, Camp D, Quinn RJ.

J Med Chem. 2012 Jun 28;55(12):5851-8. doi: 10.1021/jm3002795. Epub 2012 Jun 20.

PMID:
22686608
36.

Acute dapsone overdose: the effects of continuous veno-venous haemofiltration on the elimination of dapsone.

Masurkar VA, Edstein MD, Gorton CJ, Anstey CM.

Anaesth Intensive Care. 2011 Nov;39(6):1131-5.

37.

Evaluation of the safety and tolerability of a short higher-dose primaquine regimen for presumptive anti-relapse therapy in healthy subjects.

Ebringer A, Heathcote G, Baker J, Waller M, Shanks GD, Edstein MD.

Trans R Soc Trop Med Hyg. 2011 Oct;105(10):568-73. doi: 10.1016/j.trstmh.2011.07.001. Epub 2011 Sep 3.

PMID:
21890160
38.

Pharmacokinetics and ex vivo antimalarial activity of artesunate-azithromycin in healthy volunteers.

Chinh NT, Quang NN, Anh CX, Thanh NX, Dai B, Birrell GW, Chavchich M, Edstein MD.

Antimicrob Agents Chemother. 2011 Sep;55(9):4412-5. doi: 10.1128/AAC.00365-11. Epub 2011 Jul 5.

39.

Phenolic glycosides with antimalarial activity from Grevillea "Poorinda Queen".

Ovenden SP, Cobbe M, Kissell R, Birrell GW, Chavchich M, Edstein MD.

J Nat Prod. 2011 Jan 28;74(1):74-8. doi: 10.1021/np100737q. Epub 2010 Dec 14.

PMID:
21155593
40.

Malaria vectors of Timor-Leste.

Cooper RD, Edstein MD, Frances SP, Beebe NW.

Malar J. 2010 Feb 2;9:40. doi: 10.1186/1475-2875-9-40.

41.

Randomized, double-blind study of the safety, tolerability, and efficacy of tafenoquine versus mefloquine for malaria prophylaxis in nonimmune subjects.

Nasveld PE, Edstein MD, Reid M, Brennan L, Harris IE, Kitchener SJ, Leggat PA, Pickford P, Kerr C, Ohrt C, Prescott W; Tafenoquine Study Team.

Antimicrob Agents Chemother. 2010 Feb;54(2):792-8. doi: 10.1128/AAC.00354-09. Epub 2009 Dec 7.

42.

Sex affects the steady-state pharmacokinetics of primaquine but not doxycycline in healthy subjects.

Binh VQ, Chinh NT, Thanh NX, Cuong BT, Quang NN, Dai B, Travers T, Edstein MD.

Am J Trop Med Hyg. 2009 Nov;81(5):747-53. doi: 10.4269/ajtmh.2009.09-0214.

PMID:
19861604
43.

Pharmacokinetics and ex vivo pharmacodynamic antimalarial activity of dihydroartemisinin-piperaquine in patients with uncomplicated falciparum malaria in Vietnam.

Nguyen DV, Nguyen QP, Nguyen ND, Le TT, Nguyen TD, Dinh DN, Nguyen TX, Bui D, Chavchich M, Edstein MD.

Antimicrob Agents Chemother. 2009 Aug;53(8):3534-7. doi: 10.1128/AAC.01717-08. Epub 2009 Jun 15.

44.

Evaluation of artemisone combinations in Aotus monkeys infected with Plasmodium falciparum.

Obaldia N 3rd, Kotecka BM, Edstein MD, Haynes RK, Fugmann B, Kyle DE, Rieckmann KH.

Antimicrob Agents Chemother. 2009 Aug;53(8):3592-4. doi: 10.1128/AAC.00471-09. Epub 2009 Jun 8.

45.

Open label randomized comparison of dihydroartemisinin-piperaquine and artesunate-amodiaquine for the treatment of uncomplicated Plasmodium falciparum malaria in central Vietnam.

Thanh NX, Trung TN, Phong NC, Thien NX, Dai B, Shanks GD, Chavchich M, Edstein MD.

Trop Med Int Health. 2009 May;14(5):504-11. doi: 10.1111/j.1365-3156.2009.02269.x. Epub 2009 Mar 19.

46.

Pharmacokinetics and bioequivalence evaluation of two fixed-dose tablet formulations of dihydroartemisinin and piperaquine in Vietnamese subjects.

Chinh NT, Quang NN, Thanh NX, Dai B, Geue JP, Addison RS, Travers T, Edstein MD.

Antimicrob Agents Chemother. 2009 Feb;53(2):828-31. doi: 10.1128/AAC.00927-08. Epub 2008 Dec 1.

47.

Pharmacokinetics of the antimalarial drug piperaquine in healthy Vietnamese subjects.

Nguyen TC, Nguyen NQ, Nguyen XT, Bui D, Travers T, Edstein MD.

Am J Trop Med Hyg. 2008 Oct;79(4):620-3.

PMID:
18840754
48.

First assessment in humans of the safety, tolerability, pharmacokinetics, and ex vivo pharmacodynamic antimalarial activity of the new artemisinin derivative artemisone.

Nagelschmitz J, Voith B, Wensing G, Roemer A, Fugmann B, Haynes RK, Kotecka BM, Rieckmann KH, Edstein MD.

Antimicrob Agents Chemother. 2008 Sep;52(9):3085-91. doi: 10.1128/AAC.01585-07. Epub 2008 Jun 16.

49.

The efficacy and tolerability of three different regimens of tafenoquine versus primaquine for post-exposure prophylaxis of Plasmodium vivax malaria in the Southwest Pacific.

Elmes NJ, Nasveld PE, Kitchener SJ, Kocisko DA, Edstein MD.

Trans R Soc Trop Med Hyg. 2008 Nov;102(11):1095-101. doi: 10.1016/j.trstmh.2008.04.024. Epub 2008 Jun 9.

PMID:
18541280
50.

Plasmodium vivax trophozoites insensitive to chloroquine.

Sharrock WW, Suwanarusk R, Lek-Uthai U, Edstein MD, Kosaisavee V, Travers T, Jaidee A, Sriprawat K, Price RN, Nosten F, Russell B.

Malar J. 2008 May 27;7:94. doi: 10.1186/1475-2875-7-94.

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