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Items: 1 to 50 of 57

1.

Flagellar cAMP signaling controls trypanosome progression through host tissues.

Shaw S, DeMarco SF, Rehmann R, Wenzler T, Florini F, Roditi I, Hill KL.

Nat Commun. 2019 Feb 18;10(1):803. doi: 10.1038/s41467-019-08696-y.

2.

Isothermal microcalorimetry - A quantitative method to monitor Trypanosoma congolense growth and growth inhibition by trypanocidal drugs in real time.

Gysin M, Braissant O, Gillingwater K, Brun R, Mäser P, Wenzler T.

Int J Parasitol Drugs Drug Resist. 2018 Aug;8(2):159-164. doi: 10.1016/j.ijpddr.2018.03.003. Epub 2018 Mar 16.

3.

In Vitro and In Vivo Studies of the Trypanocidal Effect of Novel Quinolines.

Nefertiti ASG, Batista MM, Da Silva PB, Batista DGJ, Da Silva CF, Peres RB, Torres-Santos EC, Cunha-Junior EF, Holt E, Boykin DW, Brun R, Wenzler T, Soeiro MNC.

Antimicrob Agents Chemother. 2018 Jan 25;62(2). pii: e01936-17. doi: 10.1128/AAC.01936-17. Print 2018 Feb.

4.

Indole and Benzimidazole Bichalcophenes: Synthesis, DNA Binding and Antiparasitic Activity.

Farahat AA, Ismail MA, Kumar A, Wenzler T, Brun R, Paul A, Wilson WD, Boykin DW.

Eur J Med Chem. 2018 Jan 1;143:1590-1596. doi: 10.1016/j.ejmech.2017.10.056. Epub 2017 Oct 22.

5.

Beyond immune escape: a variant surface glycoprotein causes suramin resistance in Trypanosoma brucei.

Wiedemar N, Graf FE, Zwyer M, Ndomba E, Kunz Renggli C, Cal M, Schmidt RS, Wenzler T, Mäser P.

Mol Microbiol. 2018 Jan;107(1):57-67. doi: 10.1111/mmi.13854. Epub 2017 Nov 20.

6.

Exploration of DAPI analogues: Synthesis, antitrypanosomal activity, DNA binding and fluorescence properties.

Farahat AA, Kumar A, Say M, Wenzler T, Brun R, Paul A, Wilson WD, Boykin DW.

Eur J Med Chem. 2017 Mar 10;128:70-78. doi: 10.1016/j.ejmech.2017.01.037. Epub 2017 Jan 24.

7.

Synthesis, DNA binding and antitrypanosomal activity of benzimidazole analogues of DAPI.

Farahat AA, Bennett-Vaughn C, Mineva EM, Kumar A, Wenzler T, Brun R, Liu Y, Wilson WD, Boykin DW.

Bioorg Med Chem Lett. 2016 Dec 15;26(24):5907-5910. doi: 10.1016/j.bmcl.2016.11.006. Epub 2016 Nov 3.

PMID:
27843114
8.

Synthesis of novel amide and urea derivatives of thiazol-2-ethylamines and their activity against Trypanosoma brucei rhodesiense.

Patrick DA, Wenzler T, Yang S, Weiser PT, Wang MZ, Brun R, Tidwell RR.

Bioorg Med Chem. 2016 Jun 1;24(11):2451-65. doi: 10.1016/j.bmc.2016.04.006. Epub 2016 Apr 2.

9.

A new approach to chemotherapy: drug-induced differentiation kills African trypanosomes.

Wenzler T, Schumann Burkard G, Schmidt RS, Mäser P, Bergner A, Roditi I, Brun R.

Sci Rep. 2016 Mar 2;6:22451. doi: 10.1038/srep22451.

10.

Synthesis and antiparasitic activity of new bis-arylimidamides: DB766 analogs modified in the terminal groups.

Liu ZY, Wenzler T, Brun R, Zhu X, Boykin DW.

Eur J Med Chem. 2014 Aug 18;83:167-73. doi: 10.1016/j.ejmech.2014.06.022. Epub 2014 Jun 12.

PMID:
24956553
11.

In vitro and in vivo evaluation of 28DAP010, a novel diamidine for treatment of second-stage African sleeping sickness.

Wenzler T, Yang S, Patrick DA, Braissant O, Ismail MA, Tidwell RR, Boykin DW, Wang MZ, Brun R.

Antimicrob Agents Chemother. 2014 Aug;58(8):4452-63. doi: 10.1128/AAC.02309-13. Epub 2014 May 27.

12.

Pharmacokinetic comparison to determine the mechanisms underlying the differential efficacies of cationic diamidines against first- and second-stage human African trypanosomiasis.

Yang S, Wenzler T, Miller PN, Wu H, Boykin DW, Brun R, Wang MZ.

Antimicrob Agents Chemother. 2014 Jul;58(7):4064-74. doi: 10.1128/AAC.02605-14. Epub 2014 May 5.

13.

Substituted 2-phenylimidazopyridines: a new class of drug leads for human African trypanosomiasis.

Tatipaka HB, Gillespie JR, Chatterjee AK, Norcross NR, Hulverson MA, Ranade RM, Nagendar P, Creason SA, McQueen J, Duster NA, Nagle A, Supek F, Molteni V, Wenzler T, Brun R, Glynne R, Buckner FS, Gelb MH.

J Med Chem. 2014 Feb 13;57(3):828-35. doi: 10.1021/jm401178t. Epub 2014 Jan 15.

14.

Antiprotozoal activity of dicationic 3,5-diphenylisoxazoles, their prodrugs and aza-analogues.

Patrick DA, Bakunov SA, Bakunova SM, Wenzler T, Brun R, Tidwell RR.

Bioorg Med Chem. 2014 Jan 1;22(1):559-76. doi: 10.1016/j.bmc.2013.10.050. Epub 2013 Nov 9.

PMID:
24268543
15.

Aquaporin 2 mutations in Trypanosoma brucei gambiense field isolates correlate with decreased susceptibility to pentamidine and melarsoprol.

Graf FE, Ludin P, Wenzler T, Kaiser M, Brun R, Pyana PP, Büscher P, de Koning HP, Horn D, Mäser P.

PLoS Negl Trop Dis. 2013 Oct 10;7(10):e2475. doi: 10.1371/journal.pntd.0002475. eCollection 2013.

16.

Synthesis and antiprotozoal activity of dicationic 2,6-diphenylpyrazines and aza-analogues.

Hu L, Patel A, Bondada L, Yang S, Wang MZ, Munde M, Wilson WD, Wenzler T, Brun R, Boykin DW.

Bioorg Med Chem. 2013 Nov 1;21(21):6732-41. doi: 10.1016/j.bmc.2013.08.006. Epub 2013 Aug 13.

17.

Pharmacokinetics, Trypanosoma brucei gambiense efficacy, and time of drug action of DB829, a preclinical candidate for treatment of second-stage human African trypanosomiasis.

Wenzler T, Yang S, Braissant O, Boykin DW, Brun R, Wang MZ.

Antimicrob Agents Chemother. 2013 Nov;57(11):5330-43. doi: 10.1128/AAC.00398-13. Epub 2013 Aug 19.

18.

Synthesis and antiprotozoal activities of benzyl phenyl ether diamidine derivatives.

Patrick DA, Bakunov SA, Bakunova SM, Jones SK, Wenzler T, Barszcz T, Kumar A, Boykin DW, Werbovetz KA, Brun R, Tidwell RR.

Eur J Med Chem. 2013 Sep;67:310-24. doi: 10.1016/j.ejmech.2013.06.033. Epub 2013 Jun 25.

PMID:
23871911
19.

Synthesis and antiprotozoal activity of dicationic m-terphenyl and 1,3-dipyridylbenzene derivatives.

Patrick DA, Ismail MA, Arafa RK, Wenzler T, Zhu X, Pandharkar T, Jones SK, Werbovetz KA, Brun R, Boykin DW, Tidwell RR.

J Med Chem. 2013 Jul 11;56(13):5473-94. doi: 10.1021/jm400508e. Epub 2013 Jun 24.

PMID:
23795673
20.

Anti-protozoal activity of aporphine and protoberberine alkaloids from Annickia kummeriae (Engl. & Diels) Setten & Maas (Annonaceae).

Malebo HM, Wenzler T, Cal M, Swaleh SM, Omolo MO, Hassanali A, Séquin U, Häussinger D, Dalsgaard P, Hamburger M, Brun R, Ndiege IO.

BMC Complement Altern Med. 2013 Feb 27;13:48. doi: 10.1186/1472-6882-13-48.

21.

Synthesis, DNA binding and antileishmanial activity of low molecular weight bis-arylimidamides.

Banerjee M, Farahat AA, Kumar A, Wenzler T, Brun R, Munde MM, Wilson WD, Zhu X, Werbovetz KA, Boykin DW.

Eur J Med Chem. 2012 Sep;55:449-54. doi: 10.1016/j.ejmech.2012.06.058. Epub 2012 Jul 14.

22.

Isothermal microcalorimetry, a new tool to monitor drug action against Trypanosoma brucei and Plasmodium falciparum.

Wenzler T, Steinhuber A, Wittlin S, Scheurer C, Brun R, Trampuz A.

PLoS Negl Trop Dis. 2012;6(6):e1668. doi: 10.1371/journal.pntd.0001668. Epub 2012 Jun 5.

23.

Antiparasitic agents: new drugs on the horizon.

Mäser P, Wittlin S, Rottmann M, Wenzler T, Kaiser M, Brun R.

Curr Opin Pharmacol. 2012 Oct;12(5):562-6. doi: 10.1016/j.coph.2012.05.001. Epub 2012 May 29. Review.

PMID:
22652215
24.

Molecular modeling study and synthesis of novel dicationic flexible triaryl guanidines and imidamides as antiprotozoal agents.

Arafa RK, Wenzler T, Brun R, Chai Y, Wilson WD.

Eur J Med Chem. 2011 Dec;46(12):5852-60. doi: 10.1016/j.ejmech.2011.09.047. Epub 2011 Oct 2.

PMID:
22005186
25.

Exploration of larger central ring linkers in furamidine analogues: synthesis and evaluation of their DNA binding, antiparasitic and fluorescence properties.

Farahat AA, Paliakov E, Kumar A, Barghash AE, Goda FE, Eisa HM, Wenzler T, Brun R, Liu Y, Wilson WD, Boykin DW.

Bioorg Med Chem. 2011 Apr 1;19(7):2156-67. doi: 10.1016/j.bmc.2011.02.045. Epub 2011 Mar 1.

PMID:
21421317
26.

Dicationic phenyl-2,2'-bichalcophenes and analogues as antiprotozoal agents.

Ismail MA, Bialy SA, Brun R, Wenzler T, Nanjunda R, Wilson WD, Boykin DW.

Bioorg Med Chem. 2011 Jan 15;19(2):978-84. doi: 10.1016/j.bmc.2010.11.047. Epub 2010 Dec 5.

27.

Synthesis and antitrypanosomal evaluation of derivatives of N-benzyl-1,2-dihydroquinolin-6-ols: Effect of core substitutions and salt formation.

Reid CS, Patrick DA, He S, Fotie J, Premalatha K, Tidwell RR, Wang MZ, Liu Q, Gershkovich P, Wasan KM, Wenzler T, Brun R, Werbovetz KA.

Bioorg Med Chem. 2011 Jan 1;19(1):513-23. doi: 10.1016/j.bmc.2010.11.003. Epub 2010 Nov 5.

PMID:
21112788
28.

Pharmacophore model for pentamidine analogs active against Plasmodium falciparum.

Athri P, Wenzler T, Tidwell R, Bakunova SM, Wilson WD.

Eur J Med Chem. 2010 Dec;45(12):6147-51. doi: 10.1016/j.ejmech.2010.09.012. Epub 2010 Sep 18.

PMID:
20884090
29.

Synthesis and antiprotozoal activity of 2,5-bis[amidinoaryl]thiazoles.

Branowska D, Farahat AA, Kumar A, Wenzler T, Brun R, Liu Y, Wilson WD, Boykin DW.

Bioorg Med Chem. 2010 May 15;18(10):3551-8. doi: 10.1016/j.bmc.2010.03.058. Epub 2010 Mar 27.

30.

A Trk/HKT-type K+ transporter from Trypanosoma brucei.

Mosimann M, Goshima S, Wenzler T, Lüscher A, Uozumi N, Mäser P.

Eukaryot Cell. 2010 Apr;9(4):539-46. doi: 10.1128/EC.00314-09. Epub 2010 Feb 26.

31.

Antitrypanosomal activity of 1,2-dihydroquinolin-6-ols and their ester derivatives.

Fotie J, Kaiser M, Delfín DA, Manley J, Reid CS, Paris JM, Wenzler T, Maes L, Mahasenan KV, Li C, Werbovetz KA.

J Med Chem. 2010 Feb 11;53(3):966-82. doi: 10.1021/jm900723w.

PMID:
20047276
32.

Synthesis, DNA binding, fluorescence measurements and antiparasitic activity of DAPI related diamidines.

Farahat AA, Kumar A, Say M, Barghash Ael-D, Goda FE, Eisa HM, Wenzler T, Brun R, Liu Y, Mickelson L, Wilson WD, Boykin DW.

Bioorg Med Chem. 2010 Jan 15;18(2):557-66. doi: 10.1016/j.bmc.2009.12.011. Epub 2009 Dec 11.

PMID:
20031421
33.

Synthesis and antiprotozoal activity of cationic 1,4-diphenyl-1H-1,2,3-triazoles.

Bakunov SA, Bakunova SM, Wenzler T, Ghebru M, Werbovetz KA, Brun R, Tidwell RR.

J Med Chem. 2010 Jan 14;53(1):254-72. doi: 10.1021/jm901178d. Erratum in: J Med Chem. 2011 Jun 23;54(12):4281.

34.

Synthesis and antiprotozoal properties of pentamidine congeners bearing the benzofuran motif.

Bakunov SA, Bakunova SM, Bridges AS, Wenzler T, Barszcz T, Werbovetz KA, Brun R, Tidwell RR.

J Med Chem. 2009 Sep 24;52(18):5763-7. doi: 10.1021/jm9006406.

PMID:
19757840
35.

Synthesis and activity of azaterphenyl diamidines against Trypanosoma brucei rhodesiense and Plasmodium falciparum.

Hu L, Arafa RK, Ismail MA, Patel A, Munde M, Wilson WD, Wenzler T, Brun R, Boykin DW.

Bioorg Med Chem. 2009 Sep 15;17(18):6651-8. doi: 10.1016/j.bmc.2009.07.080. Epub 2009 Aug 7.

36.

New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289.

Wenzler T, Boykin DW, Ismail MA, Hall JE, Tidwell RR, Brun R.

Antimicrob Agents Chemother. 2009 Oct;53(10):4185-92. doi: 10.1128/AAC.00225-09. Epub 2009 Jul 20.

37.

Synthesis and antiprotozoal activity of pyridyl analogues of pentamidine.

Bakunova SM, Bakunov SA, Wenzler T, Barszcz T, Werbovetz KA, Brun R, Tidwell RR.

J Med Chem. 2009 Aug 13;52(15):4657-67. doi: 10.1021/jm900805v.

PMID:
19606902
38.

Synthesis and antiprotozoal activities of dicationic bis(phenoxymethyl)benzenes, bis(phenoxymethyl)naphthalenes, and bis(benzyloxy)naphthalenes.

Patrick DA, Bakunov SA, Bakunova SM, Kumar EV, Chen H, Jones SK, Wenzler T, Barzcz T, Werbovetz KA, Brun R, Tidwell RR.

Eur J Med Chem. 2009 Sep;44(9):3543-51. doi: 10.1016/j.ejmech.2009.03.014. Epub 2009 Mar 24.

PMID:
19409677
39.

Structure-activity study of pentamidine analogues as antiprotozoal agents.

Bakunova SM, Bakunov SA, Patrick DA, Kumar EV, Ohemeng KA, Bridges AS, Wenzler T, Barszcz T, Jones SK, Werbovetz KA, Brun R, Tidwell RR.

J Med Chem. 2009 Apr 9;52(7):2016-35. doi: 10.1021/jm801547t.

PMID:
19267462
40.

Synthesis and antiprotozoal activity of cationic 2-phenylbenzofurans.

Bakunov SA, Bakunova SM, Wenzler T, Barszcz T, Werbovetz KA, Brun R, Tidwell RR.

J Med Chem. 2008 Nov 13;51(21):6927-44. doi: 10.1021/jm800918v. Epub 2008 Oct 9.

PMID:
18841956
41.

Efficacy of the diamidine DB75 and its prodrug DB289, against murine models of human African trypanosomiasis.

Thuita JK, Karanja SM, Wenzler T, Mdachi RE, Ngotho JM, Kagira JM, Tidwell R, Brun R.

Acta Trop. 2008 Oct;108(1):6-10. doi: 10.1016/j.actatropica.2008.07.006. Epub 2008 Aug 5.

PMID:
18722336
42.

Novel linear triaryl guanidines, N-substituted guanidines and potential prodrugs as antiprotozoal agents.

Arafa RK, Ismail MA, Munde M, Wilson WD, Wenzler T, Brun R, Boykin DW.

Eur J Med Chem. 2008 Dec;43(12):2901-8. doi: 10.1016/j.ejmech.2008.02.008. Epub 2008 Feb 29.

43.

Azaterphenyl diamidines as antileishmanial agents.

Hu L, Arafa RK, Ismail MA, Wenzler T, Brun R, Munde M, Wilson WD, Nzimiro S, Samyesudhas S, Werbovetz KA, Boykin DW.

Bioorg Med Chem Lett. 2008 Jan 1;18(1):247-51. Epub 2007 Oct 30.

PMID:
18006310
44.

Synthesis and antiprotozoal activity of novel bis-benzamidino imidazo[1,2-a]pyridines and 5,6,7,8-tetrahydro-imidazo[1,2-a]pyridines.

Ismail MA, Arafa RK, Wenzler T, Brun R, Tanious FA, Wilson WD, Boykin DW.

Bioorg Med Chem. 2008 Jan 15;16(2):683-91. Epub 2007 Oct 18.

PMID:
17976993
45.

Synthesis and in vitro antiprotozoal activity of bisbenzofuran cations.

Bakunova SM, Bakunov SA, Wenzler T, Barszcz T, Werbovetz KA, Brun R, Hall JE, Tidwell RR.

J Med Chem. 2007 Nov 15;50(23):5807-23. Epub 2007 Oct 19.

PMID:
17948982
46.

Diphenyl furans and aza analogs: effects of structural modification on in vitro activity, DNA binding, and accumulation and distribution in trypanosomes.

Mathis AM, Bridges AS, Ismail MA, Kumar A, Francesconi I, Anbazhagan M, Hu Q, Tanious FA, Wenzler T, Saulter J, Wilson WD, Brun R, Boykin DW, Tidwell RR, Hall JE.

Antimicrob Agents Chemother. 2007 Aug;51(8):2801-10. Epub 2007 May 21.

47.

Synthesis and in vitro antiprotozoal activities of dicationic 3,5-diphenylisoxazoles.

Patrick DA, Bakunov SA, Bakunova SM, Kumar EV, Lombardy RJ, Jones SK, Bridges AS, Zhirnov O, Hall JE, Wenzler T, Brun R, Tidwell RR.

J Med Chem. 2007 May 17;50(10):2468-85. Epub 2007 Apr 18.

PMID:
17439202
48.

Synthesis and antiparasitic evaluation of bis-2,5-[4-guanidinophenyl]thiophenes.

Gonzalez JL, Stephens CE, Wenzler T, Brun R, Tanious FA, Wilson WD, Barszcz T, Werbovetz KA, Boykin DW.

Eur J Med Chem. 2007 Apr;42(4):552-7. Epub 2006 Nov 22.

PMID:
17178177
49.

Synthesis, DNA affinity, and antiprotozoal activity of linear dications: Terphenyl diamidines and analogues.

Ismail MA, Arafa RK, Brun R, Wenzler T, Miao Y, Wilson WD, Generaux C, Bridges A, Hall JE, Boykin DW.

J Med Chem. 2006 Aug 24;49(17):5324-32.

PMID:
16913722
50.

Dicationic DNA-targeted antiprotozoal agents: naphthalene replacement of benzimidazole.

Chackal-Catoen S, Miao Y, Wilson WD, Wenzler T, Brun R, Boykin DW.

Bioorg Med Chem. 2006 Nov 15;14(22):7434-45. Epub 2006 Aug 2.

PMID:
16889966

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