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Items: 1 to 50 of 89

1.

Synthesis and antileishmanial evaluation of thiazole orange analogs.

Abdelhameed A, Liao X, McElroy CA, Joice AC, Rakotondraibe L, Li J, Slebodnick C, Guo P, Wilson WD, Werbovetz KA.

Bioorg Med Chem Lett. 2020 Jan 1;30(1):126725. doi: 10.1016/j.bmcl.2019.126725. Epub 2019 Oct 4.

PMID:
31732409
2.

Microneedle-Based Delivery of Amphotericin B for Treatment of Cutaneous Leishmaniasis.

Nguyen AK, Yang KH, Bryant K, Li J, Joice AC, Werbovetz KA, Narayan RJ.

Biomed Microdevices. 2019 Jan 7;21(1):8. doi: 10.1007/s10544-018-0355-8.

PMID:
30617619
3.

Correction for Pandharkar et al., "Studies on the Antileishmanial Mechanism of Action of the Arylimidamide DB766: Azole Interactions and Role of CYP5122A1".

Pandharkar T, Zhu X, Mathur R, Jiang J, Schmittgen TD, Shaha C, Werbovetz KA.

Antimicrob Agents Chemother. 2017 Dec 21;62(1). pii: e01124-17. doi: 10.1128/AAC.01124-17. Print 2018 Jan. No abstract available.

4.

Antileishmanial Efficacy and Pharmacokinetics of DB766-Azole Combinations.

Joice AC, Yang S, Farahat AA, Meeds H, Feng M, Li J, Boykin DW, Wang MZ, Werbovetz KA.

Antimicrob Agents Chemother. 2017 Dec 21;62(1). pii: e01129-17. doi: 10.1128/AAC.01129-17. Print 2018 Jan.

5.

Synthesis and pharmacological evaluation of mono-arylimidamides as antileishmanial agents.

Zhu X, Farahat AA, Mattamana M, Joice A, Pandharkar T, Holt E, Banerjee M, Gragg JL, Hu L, Kumar A, Yang S, Wang MZ, Boykin DW, Werbovetz KA.

Bioorg Med Chem Lett. 2016 May 15;26(10):2551-2556. doi: 10.1016/j.bmcl.2016.03.082. Epub 2016 Mar 25.

6.

Antileishmanial and Cytotoxic Activity of Some Highly Oxidized Abietane Diterpenoids from the Bald Cypress, Taxodium distichum.

Naman CB, Gromovsky AD, Vela CM, Fletcher JN, Gupta G, Varikuti S, Zhu X, Zywot EM, Chai H, Werbovetz KA, Satoskar AR, Kinghorn AD.

J Nat Prod. 2016 Mar 25;79(3):598-606. doi: 10.1021/acs.jnatprod.5b01131. Epub 2016 Feb 23.

7.

Correction to Antileishmanial Activity of a Series of N(2),N(4)-Disubstituted Quinazoline-2,4-diamines.

Van Horn KS, Zhu X, Pandharkar T, Yang S, Vesely B, Vanaerschot M, Dujardin JC, Rijal S, Kyle DE, Wang MZ, Werbovetz KA, Manetsch R.

J Med Chem. 2016 Jan 28;59(2):775. doi: 10.1021/acs.jmedchem.5b00981. Epub 2016 Jan 12. No abstract available.

PMID:
26754204
8.

SAR refinement of antileishmanial N(2),N(4)-disubstituted quinazoline-2,4-diamines.

Zhu X, Van Horn KS, Barber MM, Yang S, Wang MZ, Manetsch R, Werbovetz KA.

Bioorg Med Chem. 2015 Aug 15;23(16):5182-9. doi: 10.1016/j.bmc.2015.02.020. Epub 2015 Feb 18.

9.

Studies on the antileishmanial mechanism of action of the arylimidamide DB766: azole interactions and role of CYP5122A1.

Pandharkar T, Zhu X, Mathur R, Jiang J, Schmittgen TD, Shaha C, Werbovetz KA.

Antimicrob Agents Chemother. 2014 Aug;58(8):4682-9. doi: 10.1128/AAC.02405-14. Epub 2014 Jun 2. Erratum in: Antimicrob Agents Chemother. 2017 Dec 21;62(1):.

10.

Antileishmanial activity of a series of N²,N⁴-disubstituted quinazoline-2,4-diamines.

Van Horn KS, Zhu X, Pandharkar T, Yang S, Vesely B, Vanaerschot M, Dujardin JC, Rijal S, Kyle DE, Wang MZ, Werbovetz KA, Manetsch R.

J Med Chem. 2014 Jun 26;57(12):5141-56. doi: 10.1021/jm5000408. Epub 2014 Jun 17.

11.

Evaluation of Antitrypanosomal Dihydroquinolines for Hepatotoxicity, Mutagenicity, and Methemoglobin Formation In Vitro.

Werbovetz KA, Riccio ES, Furimsky A, Richard JV, He S, Iyer L, Mirsalis J.

Int J Toxicol. 2014 Jul;33(4):282-287. Epub 2014 May 12.

12.

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
13.

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
14.

Discovery of benzamide analogs as negative allosteric modulators of human neuronal nicotinic receptors: pharmacophore modeling and structure-activity relationship studies.

Yi B, Long S, González-Cestari TF, Henderson BJ, Pavlovicz RE, Werbovetz K, Li C, McKay DB.

Bioorg Med Chem. 2013 Aug 1;21(15):4730-43. doi: 10.1016/j.bmc.2013.03.082. Epub 2013 Apr 6.

15.

Novel amidines and analogues as promising agents against intracellular parasites: a systematic review.

Soeiro MN, Werbovetz K, Boykin DW, Wilson WD, Wang MZ, Hemphill A.

Parasitology. 2013 Jul;140(8):929-51. doi: 10.1017/S0031182013000292. Epub 2013 Apr 8. Review.

16.

8,8-dialkyldihydroberberines with potent antiprotozoal activity.

Endeshaw M, Zhu X, He S, Pandharkar T, Cason E, Mahasenan KV, Agarwal H, Li C, Munde M, Wilson WD, Bahar M, Doskotch RW, Kinghorn AD, Kaiser M, Brun R, Drew ME, Werbovetz KA.

J Nat Prod. 2013 Mar 22;76(3):311-5. doi: 10.1021/np300638f. Epub 2012 Nov 20.

PMID:
23167812
17.

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.

18.

Antileishmanial bis-arylimidamides: DB766 analogs modified in the linker region and bis-arylimidamide structure-activity relationships.

Reid CS, Farahat AA, Zhu X, Pandharkar T, Boykin DW, Werbovetz KA.

Bioorg Med Chem Lett. 2012 Nov 15;22(22):6806-10. doi: 10.1016/j.bmcl.2012.06.037. Epub 2012 Jun 16.

PMID:
22765899
19.

Evaluation of arylimidamides DB1955 and DB1960 as candidates against visceral leishmaniasis and Chagas' disease: in vivo efficacy, acute toxicity, pharmacokinetics, and toxicology studies.

Zhu X, Liu Q, Yang S, Parman T, Green CE, Mirsalis JC, de Nazaré Correia Soeiro M, Mello de Souza E, da Silva CF, da Gama Jaen Batista D, Stephens CE, Banerjee M, Farahat AA, Munde M, Wilson WD, Boykin DW, Wang MZ, Werbovetz KA.

Antimicrob Agents Chemother. 2012 Jul;56(7):3690-9. doi: 10.1128/AAC.06404-11. Epub 2012 Apr 16.

20.

Induction of oxidative stress in Trypanosoma brucei by the antitrypanosomal dihydroquinoline OSU-40.

He S, Dayton A, Kuppusamy P, Werbovetz KA, Drew ME.

Antimicrob Agents Chemother. 2012 May;56(5):2428-34. doi: 10.1128/AAC.06386-11. Epub 2012 Feb 6.

21.

Identification of new antileishmanial leads from hits obtained by high-throughput screening.

Zhu X, Pandharkar T, Werbovetz K.

Antimicrob Agents Chemother. 2012 Mar;56(3):1182-9. doi: 10.1128/AAC.05412-11. Epub 2011 Dec 5.

22.

Antiparasitic activity of C-geranyl flavonoids from Mimulus bigelovii.

Salem MM, Capers J, Rito S, Werbovetz KA.

Phytother Res. 2011 Aug;25(8):1246-9. doi: 10.1002/ptr.3404. Epub 2011 Feb 1.

PMID:
21796699
23.

Molecular factors governing inhibition of arylimidamides against Leishmania: conservative computational modeling to improve chemotherapies.

Collar CJ, Zhu X, Werbovetz K, Boykin DW, Wilson WD.

Bioorg Med Chem. 2011 Aug 1;19(15):4552-61. doi: 10.1016/j.bmc.2011.06.026. Epub 2011 Jun 16.

24.
25.

Potent antiprotozoal activity of a novel semi-synthetic berberine derivative.

Bahar M, Deng Y, Zhu X, He S, Pandharkar T, Drew ME, Navarro-Vázquez A, Anklin C, Gil RR, Doskotch RW, Werbovetz KA, Kinghorn AD.

Bioorg Med Chem Lett. 2011 May 1;21(9):2606-10. doi: 10.1016/j.bmcl.2011.01.101. Epub 2011 Jan 27.

PMID:
21474310
26.

Structure-activity relationship investigations of leishmanicidal N-benzylcytisine derivatives.

Turabekova MA, Vinogradova VI, Werbovetz KA, Capers J, Rasulev BF, Levkovich MG, Rakhimov SB, Abdullaev ND.

Chem Biol Drug Des. 2011 Jul;78(1):183-9. doi: 10.1111/j.1747-0285.2011.01092.x. Epub 2011 May 25.

PMID:
21457471
27.

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.

28.

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
29.

α-Tubulin mutations alter oryzalin affinity and microtubule assembly properties to confer dinitroaniline resistance.

Lyons-Abbott S, Sackett DL, Wloga D, Gaertig J, Morgan RE, Werbovetz KA, Morrissette NS.

Eukaryot Cell. 2010 Dec;9(12):1825-34. doi: 10.1128/EC.00140-10. Epub 2010 Sep 24.

30.

Synthesis and evaluation of oryzalin analogs against Toxoplasma gondii.

Endeshaw MM, Li C, de Leon J, Yao N, Latibeaudiere K, Premalatha K, Morrissette N, Werbovetz KA.

Bioorg Med Chem Lett. 2010 Sep 1;20(17):5179-83. doi: 10.1016/j.bmcl.2010.07.003. Epub 2010 Jul 8.

31.

Isolating tubulin from nonneural sources.

Sackett DL, Werbovetz KA, Morrissette NS.

Methods Cell Biol. 2010;95:17-32. doi: 10.1016/S0091-679X(10)95002-4. Review.

PMID:
20466127
32.

New antileishmanial candidates and lead compounds.

Richard JV, Werbovetz KA.

Curr Opin Chem Biol. 2010 Aug;14(4):447-55. doi: 10.1016/j.cbpa.2010.03.023. Epub 2010 Apr 17. Review.

PMID:
20400358
33.

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.

34.

Dinitroaniline activity in Toxoplasma gondii expressing wild-type or mutant alpha-tubulin.

Ma C, Tran J, Gu F, Ochoa R, Li C, Sept D, Werbovetz K, Morrissette N.

Antimicrob Agents Chemother. 2010 Apr;54(4):1453-60. doi: 10.1128/AAC.01150-09. Epub 2010 Feb 9.

35.

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
36.

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.

PMID:
20026611
37.

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.

38.

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
39.

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
40.

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.

PMID:
19545212
41.

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
42.

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
43.

Inhibitors of tubulin assembly identified through screening a compound library.

Morgan RE, Ahn S, Nzimiro S, Fotie J, Phelps MA, Cotrill J, Yakovich AJ, Sackett DL, Dalton JT, Werbovetz KA.

Chem Biol Drug Des. 2008 Dec;72(6):513-24. doi: 10.1111/j.1747-0285.2008.00729.x.

44.

Redox-active dinitrodiphenylthioethers against Leishmania: synthesis, structure-activity relationships and mechanism of action studies.

Delfín DA, Morgan RE, Zhu X, Werbovetz KA.

Bioorg Med Chem. 2009 Jan 15;17(2):820-9. doi: 10.1016/j.bmc.2008.11.031. Epub 2008 Nov 19.

PMID:
19058972
45.

Pharmacological and biological screening of ascorbigen: protection against glucose-induced endothelial cell toxicity.

Joshi MS, Bauer JA, Werbovetz KA, Barszcz T, Patil PN.

Phytother Res. 2008 Dec;22(12):1581-6. doi: 10.1002/ptr.2494.

PMID:
18844288
46.

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
47.

Inhibition by Dications of in vitro growth of Leishmania major and Leishmania tropica: causative agents of old world cutaneous leishmaniasis.

Rosypal AC, Werbovetz KA, Salem M, Stephens CE, Kumar A, Boykin DW, Hall JE, Tidwell RR.

J Parasitol. 2008 Jun;94(3):743-9. doi: 10.1645/GE-1387.1.

PMID:
18605790
48.

Selective lead compounds against kinetoplastid tubulin.

Morgan RE, Werbovetz KA.

Adv Exp Med Biol. 2008;625:33-47. doi: 10.1007/978-0-387-77570-8_4. Review.

PMID:
18365657
49.

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
50.

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

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