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CYP5122A1 encodes an essential sterol C4-methyl oxidase in Leishmania donovani and determines the antileishmanial activity of antifungal azoles.
Jin Y, Basu S, Feng M, Ning Y, Munasinghe I, Joachim AM, Li J, Qin L, Madden R, Burks H, Gao P, Wu JQ, Sheikh SW, Joice AC, Perera C, Werbovetz KA, Zhang K, Wang MZ
Nat Commun, 15(1):9409, 31 Oct 2024
Cited by: 0 articles | PMID: 39482311 | PMCID: PMC11528044
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N-substituted-4-(pyridin-4-ylalkyl)piperazine-1-carboxamides and related compounds as Leishmania CYP51 and CYP5122A1 inhibitors.
La Rosa C, Sharma P, Junaid Dar M, Jin Y, Qin L, Roy A, Kendall A, Wu M, Lin Z, Uchenik D, Li J, Basu S, Moitra S, Zhang K, Zhuo Wang M, Werbovetz KA
Bioorg Med Chem, 113:117907, 06 Sep 2024
Cited by: 2 articles | PMID: 39288704
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Sterol profiling of Leishmania parasites using a new HPLC-tandem mass spectrometry-based method and antifungal azoles as chemical probes reveals a key intermediate sterol that supports a branched ergosterol biosynthetic pathway.
Feng M, Jin Y, Yang S, Joachim AM, Ning Y, Mori-Quiroz LM, Fromm J, Perera C, Zhang K, Werbovetz KA, Wang MZ
Int J Parasitol Drugs Drug Resist, 20:27-42, 15 Aug 2022
Cited by: 6 articles | PMID: 35994895 | PMCID: PMC9418051
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Imidazoles as Potential Anticancer Agents: An Update on Recent Studies.
Sharma P, LaRosa C, Antwi J, Govindarajan R, Werbovetz KA
Molecules, 26(14):4213, 11 Jul 2021
Cited by: 28 articles | PMID: 34299488 | PMCID: PMC8307698
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Synthesis and Antileishmanial Evaluation of Arylimidamide-Azole Hybrids Containing a Phenoxyalkyl Linker.
Abdelhameed A, Feng M, Joice AC, Zywot EM, Jin Y, La Rosa C, Liao X, Meeds HL, Kim Y, Li J, McElroy CA, Wang MZ, Werbovetz KA
ACS Infect Dis, 7(7):1901-1922, 04 Feb 2021
Cited by: 3 articles | PMID: 33538576 | PMCID: PMC8553517
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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, 30(1):126725, 04 Oct 2019
Cited by: 5 articles | PMID: 31732409
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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, 21(1):8, 07 Jan 2019
Cited by: 7 articles | PMID: 30617619 | PMCID: PMC10357955
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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, 62(1):e01129-17, 21 Dec 2017
Cited by: 7 articles | PMID: 29061761 | PMCID: PMC5740383
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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, 62(1):e01124-17, 21 Dec 2017
Cited by: 2 articles | PMID: 29269427 | PMCID: PMC5740369
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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, 26(10):2551-2556, 25 Mar 2016
Cited by: 9 articles | PMID: 27048943 | PMCID: PMC4841789
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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, 59(2):775, 12 Jan 2016
Cited by: 0 articles | PMID: 26754204
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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, 79(3):598-606, 23 Feb 2016
Cited by: 8 articles | PMID: 26905523 | PMCID: PMC4831050
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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, 23(16):5182-5189, 18 Feb 2015
Cited by: 9 articles | PMID: 25749014 | PMCID: PMC4536136
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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, 57(12):5141-5156, 17 Jun 2014
Cited by: 17 articles | PMID: 24874647 | PMCID: PMC4216219
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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, 33(4):282-287, 12 May 2014
Cited by: 2 articles | PMID: 24819520 | PMCID: PMC4229492
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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, 58(8):4682-4689, 02 Jun 2014
Cited by: 11 articles | PMID: 24890590 | PMCID: PMC4135980
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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, 67:310-324, 25 Jun 2013
Cited by: 9 articles | PMID: 23871911
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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, 56(13):5473-5494, 24 Jun 2013
Cited by: 14 articles | PMID: 23795673
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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, 55:449-454, 14 Jul 2012
Cited by: 8 articles | PMID: 22840696 | PMCID: PMC3560421
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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, 76(3):311-315, 20 Nov 2012
Cited by: 4 articles | PMID: 23167812
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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, 22(22):6806-6810, 16 Jun 2012
Cited by: 12 articles | PMID: 22765899
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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, 56(7):3690-3699, 16 Apr 2012
Cited by: 16 articles | PMID: 22508306 | PMCID: PMC3393454
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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, 56(5):2428-2434, 06 Feb 2012
Cited by: 10 articles | PMID: 22314522 | PMCID: PMC3346584
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Simultaneous determination of a novel antitrypanosomal compound (OSU-36) and its ester derivative (OSU-40) in plasma by HPLC: application to first pharmacokinetic study in rats.
Gershkovich P, Wasan KM, Sivak O, Lysakowski S, Reid C, Premalatha K, Werbovetz KA
J Pharm Pharm Sci, 14(1):36-45, 01 Jan 2011
Cited by: 3 articles | PMID: 21501551
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Antiparasitic activity of C-geranyl flavonoids from Mimulus bigelovii.
Salem MM, Capers J, Rito S, Werbovetz KA
Phytother Res, 25(8):1246-1249, 01 Feb 2011
Cited by: 13 articles | PMID: 21796699
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