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In Vitro, In Silico, and In Vivo Analyses of Novel Aromatic Amidines against Trypanosoma cruzi.

Santos CC, Lionel JR, Peres RB, Batista MM, da Silva PB, de Oliveira GM, da Silva CF, Batista DGJ, Souza SMO, Andrade CH, Neves BJ, Braga RC, Patrick DA, Bakunova SM, Tidwell RR, Soeiro MNC.

Antimicrob Agents Chemother. 2018 Jan 25;62(2). pii: e02205-17. doi: 10.1128/AAC.02205-17. Print 2018 Feb.


Role of suppression of the inward rectifier current in terminal action potential repolarization in the failing heart.

Klein MG, Shou M, Stohlman J, Solhjoo S, Haigney M, Tidwell RR, Goldstein RE, Flagg TP, Haigney MC.

Heart Rhythm. 2017 Aug;14(8):1217-1223. doi: 10.1016/j.hrthm.2017.04.001. Epub 2017 Apr 8.


In Vitro, Ex Vivo, and In Vivo Activities of Diamidines against Trypanosoma congolense and Trypanosoma vivax.

Gillingwater K, Kunz C, Braghiroli C, Boykin DW, Tidwell RR, Brun R.

Antimicrob Agents Chemother. 2017 Apr 24;61(5). pii: e02356-16. doi: 10.1128/AAC.02356-16. Print 2017 May.


Urea Derivatives of 2-Aryl-benzothiazol-5-amines: A New Class of Potential Drugs for Human African Trypanosomiasis.

Patrick DA, Gillespie JR, McQueen J, Hulverson MA, Ranade RM, Creason SA, Herbst ZM, Gelb MH, Buckner FS, Tidwell RR.

J Med Chem. 2017 Feb 9;60(3):957-971. doi: 10.1021/acs.jmedchem.6b01163. Epub 2016 Dec 19.


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.


Efficacy and Safety of Pafuramidine versus Pentamidine Maleate for Treatment of First Stage Sleeping Sickness in a Randomized, Comparator-Controlled, International Phase 3 Clinical Trial.

Pohlig G, Bernhard SC, Blum J, Burri C, Mpanya A, Lubaki JP, Mpoto AM, Munungu BF, N'tombe PM, Deo GK, Mutantu PN, Kuikumbi FM, Mintwo AF, Munungi AK, Dala A, Macharia S, Bilenge CM, Mesu VK, Franco JR, Dituvanga ND, Tidwell RR, Olson CA.

PLoS Negl Trop Dis. 2016 Feb 16;10(2):e0004363. doi: 10.1371/journal.pntd.0004363. eCollection 2016 Feb.


Efficacy, Safety, and Dose of Pafuramidine, a New Oral Drug for Treatment of First Stage Sleeping Sickness, in a Phase 2a Clinical Study and Phase 2b Randomized Clinical Studies.

Burri C, Yeramian PD, Allen JL, Merolle A, Serge KK, Mpanya A, Lutumba P, Mesu VK, Bilenge CM, Lubaki JP, Mpoto AM, Thompson M, Munungu BF, Manuel F, Josenando T, Bernhard SC, Olson CA, Blum J, Tidwell RR, Pohlig G.

PLoS Negl Trop Dis. 2016 Feb 16;10(2):e0004362. doi: 10.1371/journal.pntd.0004362. eCollection 2016 Feb.


In Vitro and In Vivo Trypanosomicidal Action of Novel Arylimidamides against Trypanosoma cruzi.

Guedes-da-Silva FH, Batista DG, Meuser MB, Demarque KC, Fulco TO, Araújo JS, Da Silva PB, Da Silva CF, Patrick DA, Bakunova SM, Bakunov SA, Tidwell RR, Oliveira GM, Britto C, Moreira OC, Soeiro MN.

Antimicrob Agents Chemother. 2016 Mar 25;60(4):2425-34. doi: 10.1128/AAC.01667-15. Print 2016 Apr.


Chemotherapy of second stage human African trypanosomiasis: comparison between the parenteral diamidine DB829 and its oral prodrug DB868 in vervet monkeys.

Thuita JK, Wolf KK, Murilla GA, Bridges AS, Boykin DW, Mutuku JN, Liu Q, Jones SK, Gem CO, Ching S, Tidwell RR, Wang MZ, Paine MF, Brun R.

PLoS Negl Trop Dis. 2015 Feb 5;9(2):e0003409. doi: 10.1371/journal.pntd.0003409. eCollection 2015 Feb.


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.


In vitro and in vivo biological effects of novel arylimidamide derivatives against Trypanosoma cruzi.

Timm BL, da Silva PB, Batista MM, da Silva FH, da Silva CF, Tidwell RR, Patrick DA, Jones SK, Bakunov SA, Bakunova SM, Soeiro Mde N.

Antimicrob Agents Chemother. 2014 Jul;58(7):3720-6. doi: 10.1128/AAC.02353-14. Epub 2014 Apr 21.


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.


CYP1A1 and CYP1B1-mediated biotransformation of the antitrypanosomal methamidoxime prodrug DB844 forms novel metabolites through intramolecular rearrangement.

Ju W, Yang S, Ansede JH, Stephens CE, Bridges AS, Voyksner RD, Ismail MA, Boykin DW, Tidwell RR, Hall JE, Wang MZ.

J Pharm Sci. 2014 Jan;103(1):337-49. doi: 10.1002/jps.23765. Epub 2013 Nov 1.


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.


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.


Safety, pharmacokinetic, and efficacy studies of oral DB868 in a first stage vervet monkey model of human African trypanosomiasis.

Thuita JK, Wolf KK, Murilla GA, Liu Q, Mutuku JN, Chen Y, Bridges AS, Mdachi RE, Ismail MA, Ching S, Boykin DW, Hall JE, Tidwell RR, Paine MF, Brun R, Wang MZ.

PLoS Negl Trop Dis. 2013 Jun 6;7(6):e2230. doi: 10.1371/journal.pntd.0002230. Print 2013.


Efficient and specific cardiac IK₁ inhibition by a new pentamidine analogue.

Takanari H, Nalos L, Stary-Weinzinger A, de Git KC, Varkevisser R, Linder T, Houtman MJ, Peschar M, de Boer TP, Tidwell RR, Rook MB, Vos MA, van der Heyden MA.

Cardiovasc Res. 2013 Jul 1;99(1):203-14. doi: 10.1093/cvr/cvt103. Epub 2013 Apr 25.


Structure-activity relationships of pentamidine-affected ion channel trafficking and dofetilide mediated rescue.

Varkevisser R, Houtman MJ, Linder T, de Git KC, Beekman HD, Tidwell RR, Ijzerman AP, Stary-Weinzinger A, Vos MA, van der Heyden MA.

Br J Pharmacol. 2013 Jul;169(6):1322-34. doi: 10.1111/bph.12208.


Compartmental and enzyme kinetic modeling to elucidate the biotransformation pathway of a centrally acting antitrypanosomal prodrug.

Generaux CN, Ainslie GR, Bridges AS, Ismail MA, Boykin DW, Tidwell RR, Thakker DR, Paine MF.

Drug Metab Dispos. 2013 Feb;41(2):518-28. doi: 10.1124/dmd.112.048231. Epub 2012 Dec 6.


A mouse diversity panel approach reveals the potential for clinical kidney injury due to DB289 not predicted by classical rodent models.

Harrill AH, Desmet KD, Wolf KK, Bridges AS, Eaddy JS, Kurtz CL, Hall JE, Paine MF, Tidwell RR, Watkins PB.

Toxicol Sci. 2012 Dec;130(2):416-26. doi: 10.1093/toxsci/kfs238. Epub 2012 Aug 31.


Pharmacology of DB844, an orally active aza analogue of pafuramidine, in a monkey model of second stage human African trypanosomiasis.

Thuita JK, Wang MZ, Kagira JM, Denton CL, Paine MF, Mdachi RE, Murilla GA, Ching S, Boykin DW, Tidwell RR, Hall JE, Brun R.

PLoS Negl Trop Dis. 2012;6(7):e1734. doi: 10.1371/journal.pntd.0001734. Epub 2012 Jul 24.


Designed compounds for recognition of 10 base pairs of DNA with two at binding sites.

Liu Y, Chai Y, Kumar A, Tidwell RR, Boykin DW, Wilson WD.

J Am Chem Soc. 2012 Mar 21;134(11):5290-9. doi: 10.1021/ja211628j. Epub 2012 Mar 9.


A semiphysiologically based pharmacokinetic modeling approach to predict the dose-exposure relationship of an antiparasitic prodrug/active metabolite pair.

Yan GZ, Generaux CN, Yoon M, Goldsmith RB, Tidwell RR, Hall JE, Olson CA, Clewell HJ, Brouwer KL, Paine MF.

Drug Metab Dispos. 2012 Jan;40(1):6-17. doi: 10.1124/dmd.111.040063. Epub 2011 Sep 27.


Novel diamidines with activity against Babesia divergens in vitro and Babesia microti in vivo.

Nehrbass-Stuedli A, Boykin D, Tidwell RR, Brun R.

Antimicrob Agents Chemother. 2011 Jul;55(7):3439-45. doi: 10.1128/AAC.01482-10. Epub 2011 May 2.


Mechanisms underlying differences in systemic exposure of structurally similar active metabolites: comparison of two preclinical hepatic models.

Yan GZ, Brouwer KL, Pollack GM, Wang MZ, Tidwell RR, Hall JE, Paine MF.

J Pharmacol Exp Ther. 2011 May;337(2):503-12. doi: 10.1124/jpet.110.177220. Epub 2011 Feb 14.


A novel tropically stable oral amphotericin B formulation (iCo-010) exhibits efficacy against visceral Leishmaniasis in a murine model.

Wasan EK, Gershkovich P, Zhao J, Zhu X, Werbovetz K, Tidwell RR, Clement JG, Thornton SJ, Wasan KM.

PLoS Negl Trop Dis. 2010 Dec 7;4(12):e913. doi: 10.1371/journal.pntd.0000913.


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.


Diamidines for human African trypanosomiasis.

Paine MF, Wang MZ, Generaux CN, Boykin DW, Wilson WD, De Koning HP, Olson CA, Pohlig G, Burri C, Brun R, Murilla GA, Thuita JK, Barrett MP, Tidwell RR.

Curr Opin Investig Drugs. 2010 Aug;11(8):876-83. Review.


The biological in vitro effect and selectivity of aromatic dicationic compounds on Trypanosoma cruzi.

da Silva CF, da Silva PB, Batista MM, Daliry A, Tidwell RR, Soeiro Mde N.

Mem Inst Oswaldo Cruz. 2010 May;105(3):239-45.


Application of monoclonal antibodies to measure metabolism of an anti-trypanosomal compound in vitro and in vivo.

Goldsmith RB, Gray DR, Yan Z, Generaux CN, Tidwell RR, Reisner HM.

J Clin Lab Anal. 2010;24(3):187-94. doi: 10.1002/jcla.20380. Erratum in: J Clin Lab Anal. 2011;25(4):309.


Novel arylimidamides for treatment of visceral leishmaniasis.

Wang MZ, Zhu X, Srivastava A, Liu Q, Sweat JM, Pandharkar T, Stephens CE, Riccio E, Parman T, Munde M, Mandal S, Madhubala R, Tidwell RR, Wilson WD, Boykin DW, Hall JE, Kyle DE, Werbovetz KA.

Antimicrob Agents Chemother. 2010 Jun;54(6):2507-16. doi: 10.1128/AAC.00250-10. Epub 2010 Apr 5.


In vitro activity and preliminary toxicity of various diamidine compounds against Trypanosoma evansi.

Gillingwater K, Kumar A, Ismail MA, Arafa RK, Stephens CE, Boykin DW, Tidwell RR, Brun R.

Vet Parasitol. 2010 May 11;169(3-4):264-72. doi: 10.1016/j.vetpar.2010.01.019. Epub 2010 Jan 25.


Visceral leishmaniasis affects liver and spleen concentrations of amphotericin B following administration to mice.

Gershkovich P, Wasan EK, Sivak O, Li R, Zhu X, Werbovetz KA, Tidwell RR, Clement JG, Thornton SJ, Wasan KM.

J Antimicrob Chemother. 2010 Mar;65(3):535-7. doi: 10.1093/jac/dkp465. Epub 2009 Dec 21.


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.


Surveillance for antibodies to Leishmania spp. in dogs from Sri Lanka.

Rosypal AC, Tripp S, Kinlaw C, Hailemariam S, Tidwell RR, Lindsay DS, Rajapakse RP, Sreekumar C, Dubey JP.

J Parasitol. 2010 Feb;96(1):230-1. doi: 10.1645/GE-2288.


In vivo investigations of selected diamidine compounds against Trypanosoma evansi using a mouse model.

Gillingwater K, Kumar A, Anbazhagan M, Boykin DW, Tidwell RR, Brun R.

Antimicrob Agents Chemother. 2009 Dec;53(12):5074-9. doi: 10.1128/AAC.00422-09. Epub 2009 Sep 28.


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.


In vitro analyses of the effect of aromatic diamidines upon Trypanosoma cruzi.

Daliry A, Da Silva PB, Da Silva CF, Batista MM, De Castro SL, Tidwell RR, Soeiro Mde N.

J Antimicrob Chemother. 2009 Oct;64(4):747-50. doi: 10.1093/jac/dkp290. Epub 2009 Aug 11.


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.


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.


Highly effective oral amphotericin B formulation against murine visceral leishmaniasis.

Wasan KM, Wasan EK, Gershkovich P, Zhu X, Tidwell RR, Werbovetz KA, Clement JG, Thornton SJ.

J Infect Dis. 2009 Aug 1;200(3):357-60. doi: 10.1086/600105.


The diamidine DB75 targets the nucleus of Plasmodium falciparum.

Purfield AE, Tidwell RR, Meshnick SR.

Malar J. 2009 May 14;8:104. doi: 10.1186/1475-2875-8-104.


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.


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.


Minor groove binding compounds that jump a gc base pair and bind to adjacent AT base pair sites.

Rahimian M, Kumar A, Say M, Bakunov SA, Boykin DW, Tidwell RR, Wilson WD.

Biochemistry. 2009 Feb 24;48(7):1573-83. doi: 10.1021/bi801944g.


Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration.

Mdachi RE, Thuita JK, Kagira JM, Ngotho JM, Murilla GA, Ndung'u JM, Tidwell RR, Hall JE, Brun R.

Antimicrob Agents Chemother. 2009 Mar;53(3):953-7. doi: 10.1128/AAC.00831-08. Epub 2008 Dec 8.


Transport of dicationic drugs pentamidine and furamidine by human organic cation transporters.

Ming X, Ju W, Wu H, Tidwell RR, Hall JE, Thakker DR.

Drug Metab Dispos. 2009 Feb;37(2):424-30. doi: 10.1124/dmd.108.024083. Epub 2008 Oct 29.


Survey of dogs from Vietnam for antibodies to visceralizing Leishmania spp.

Rosypal AC, Hailemariam S, Wekheye V, Huong LT, Dubey JP, Lindsay DS, Tidwell RR.

J Parasitol. 2009 Jun;95(3):767. doi: 10.1645/GE-1828.1.


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.


A gel-free MS-based quantitative proteomic approach accurately measures cytochrome P450 protein concentrations in human liver microsomes.

Wang MZ, Wu JQ, Dennison JB, Bridges AS, Hall SD, Kornbluth S, Tidwell RR, Smith PC, Voyksner RD, Paine MF, Hall JE.

Proteomics. 2008 Oct;8(20):4186-96. doi: 10.1002/pmic.200800144.


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