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Items: 35

1.

Novel benzoxaborole, nitroimidazole and aminopyrazoles with activity against experimental cutaneous leishmaniasis.

Van Bocxlaer K, Caridha D, Black C, Vesely B, Leed S, Sciotti RJ, Wijnant GJ, Yardley V, Braillard S, Mowbray CE, Ioset JR, Croft SL.

Int J Parasitol Drugs Drug Resist. 2019 Feb 26. pii: S2211-3207(18)30185-4. doi: 10.1016/j.ijpddr.2019.02.002. [Epub ahead of print]

2.

Discovery and Structural Optimization of Acridones as Broad-Spectrum Antimalarials.

Dodean RA, Kancharla P, Li Y, Melendez V, Read L, Bane CE, Vesely B, Kreishman-Deitrick M, Black C, Li Q, Sciotti RJ, Olmeda R, Luong TL, Gaona H, Potter B, Sousa J, Marcsisin S, Caridha D, Xie L, Vuong C, Zeng Q, Zhang J, Zhang P, Lin H, Butler K, Roncal N, Gaynor-Ohnstad L, Leed SE, Nolan C, Huezo SJ, Rasmussen SA, Stephens MT, Tan JC, Cooper RA, Smilkstein MJ, Pou S, Winter RW, Riscoe MK, Kelly JX.

J Med Chem. 2019 Apr 11;62(7):3475-3502. doi: 10.1021/acs.jmedchem.8b01961. Epub 2019 Mar 21.

PMID:
30852885
3.

Updating the modified Thompson test by using whole-body bioluminescence imaging to replace traditional efficacy testing in experimental models of murine malaria.

Caridha D, Hickman M, Xie L, Ngundam F, Milner E, Schenk A, Butler K, Nugent D, Lee P, Roncal N, Leed S, Hosford E, Lee J, Sciotti RJ, Reichard G, Black C, Kreishman-Deitrick M, Li Q, Vesely B.

Malar J. 2019 Feb 15;18(1):38. doi: 10.1186/s12936-019-2661-x.

4.

Repurposing Screen Identifies Unconventional Drugs With Activity Against Multidrug Resistant Acinetobacter baumannii.

Cheng YS, Sun W, Xu M, Shen M, Khraiwesh M, Sciotti RJ, Zheng W.

Front Cell Infect Microbiol. 2019 Jan 4;8:438. doi: 10.3389/fcimb.2018.00438. eCollection 2018.

5.

Improvement of Aqueous Solubility of Lapatinib-Derived Analogues: Identification of a Quinolinimine Lead for Human African Trypanosomiasis Drug Development.

Bachovchin KA, Sharma A, Bag S, Klug DM, Schneider KM, Singh B, Jalani HB, Buskes MJ, Mehta N, Tanghe S, Momper JD, Sciotti RJ, Rodriguez A, Mensa-Wilmot K, Pollastri MP, Ferrins L.

J Med Chem. 2019 Jan 24;62(2):665-687. doi: 10.1021/acs.jmedchem.8b01365. Epub 2019 Jan 10.

PMID:
30565932
6.

Anilinoquinoline based inhibitors of trypanosomatid proliferation.

Ferrins L, Sharma A, Thomas SM, Mehta N, Erath J, Tanghe S, Leed SE, Rodriguez A, Mensa-Wilmot K, Sciotti RJ, Gillingwater K, Pollastri MP.

PLoS Negl Trop Dis. 2018 Nov 26;12(11):e0006834. doi: 10.1371/journal.pntd.0006834. eCollection 2018 Nov.

7.

Series of Alkynyl-Substituted Thienopyrimidines as Inhibitors of Protozoan Parasite Proliferation.

Woodring JL, Behera R, Sharma A, Wiedeman J, Patel G, Singh B, Guyett P, Amata E, Erath J, Roncal N, Penn E, Leed SE, Rodriguez A, Sciotti RJ, Mensa-Wilmot K, Pollastri MP.

ACS Med Chem Lett. 2018 Sep 4;9(10):996-1001. doi: 10.1021/acsmedchemlett.8b00245. eCollection 2018 Oct 11.

PMID:
30344906
8.

Corrigendum to "Optimization of physicochemical properties for 4-Anilinoquinazoline inhibitors of trypanosome proliferation" [Eur. J. Med. Chem. 141 (2017) 446-459].

Woodring JL, Bachovchin KA, Brady KG, Gallerstein MF, Erath J, Tanghe S, Leed SE, Rodriguez A, Mensa-Wilmot K, Sciotti RJ, Pollastri MP.

Eur J Med Chem. 2018 May 25;152:515. doi: 10.1016/j.ejmech.2018.05.002. Epub 2018 May 10. No abstract available.

PMID:
29754075
9.

Optimization of Physicochemical Properties for 4-Anilinoquinoline Inhibitors of Plasmodium falciparum Proliferation.

Mehta N, Ferrins L, Leed SE, Sciotti RJ, Pollastri MP.

ACS Infect Dis. 2018 Apr 13;4(4):577-591. doi: 10.1021/acsinfecdis.7b00212. Epub 2018 Jan 17.

10.

Optimization of physicochemical properties for 4-anilinoquinazoline inhibitors of trypanosome proliferation.

Woodring JL, Bachovchin KA, Brady KG, Gallerstein MF, Erath J, Tanghe S, Leed SE, Rodriguez A, Mensa-Wilmot K, Sciotti RJ, Pollastri MP.

Eur J Med Chem. 2017 Dec 1;141:446-459. doi: 10.1016/j.ejmech.2017.10.007. Epub 2017 Oct 6. Erratum in: Eur J Med Chem. 2018 May 10;152:515.

11.

Alkoxycarbonate Ester Prodrugs of Preclinical Drug Candidate ELQ-300 for Prophylaxis and Treatment of Malaria.

Frueh L, Li Y, Mather MW, Li Q, Pou S, Nilsen A, Winter RW, Forquer IP, Pershing AM, Xie LH, Smilkstein MJ, Caridha D, Koop DR, Campbell RF, Sciotti RJ, Kreishman-Deitrick M, Kelly JX, Vesely B, Vaidya AB, Riscoe MK.

ACS Infect Dis. 2017 Oct 13;3(10):728-735. doi: 10.1021/acsinfecdis.7b00062. Epub 2017 Sep 27.

12.

Antiparasitic Lead Discovery: Toward Optimization of a Chemotype with Activity Against Multiple Protozoan Parasites.

Devine W, Thomas SM, Erath J, Bachovchin KA, Lee PJ, Leed SE, Rodriguez A, Sciotti RJ, Mensa-Wilmot K, Pollastri MP.

ACS Med Chem Lett. 2017 Feb 5;8(3):350-354. doi: 10.1021/acsmedchemlett.7b00011. eCollection 2017 Mar 9.

13.

Identification of "Preferred" Human Kinase Inhibitors for Sleeping Sickness Lead Discovery. Are Some Kinases Better than Others for Inhibitor Repurposing?

Amata E, Xi H, Colmenarejo G, Gonzalez-Diaz R, Cordon-Obras C, Berlanga M, Manzano P, Erath J, Roncal NE, Lee PJ, Leed SE, Rodriguez A, Sciotti RJ, Navarro M, Pollastri MP.

ACS Infect Dis. 2016 Mar 11;2(3):180-186. Epub 2016 Jan 17.

14.

Reinvestigating Old Pharmacophores: Are 4-Aminoquinolines and Tetraoxanes Potential Two-Stage Antimalarials?

Terzić N, Konstantinović J, Tot M, Burojević J, Djurković-Djaković O, Srbljanović J, Štajner T, Verbić T, Zlatović M, Machado M, Albuquerque IS, Prudêncio M, Sciotti RJ, Pecic S, D'Alessandro S, Taramelli D, Šolaja BA.

J Med Chem. 2016 Jan 14;59(1):264-81. doi: 10.1021/acs.jmedchem.5b01374. Epub 2015 Dec 18.

PMID:
26640981
15.

Protozoan Parasite Growth Inhibitors Discovered by Cross-Screening Yield Potent Scaffolds for Lead Discovery.

Devine W, Woodring JL, Swaminathan U, Amata E, Patel G, Erath J, Roncal NE, Lee PJ, Leed SE, Rodriguez A, Mensa-Wilmot K, Sciotti RJ, Pollastri MP.

J Med Chem. 2015 Jul 23;58(14):5522-37. doi: 10.1021/acs.jmedchem.5b00515. Epub 2015 Jul 8.

16.

Differential cytochrome P450 2D metabolism alters tafenoquine pharmacokinetics.

Vuong C, Xie LH, Potter BM, Zhang J, Zhang P, Duan D, Nolan CK, Sciotti RJ, Zottig VE, Nanayakkara NP, Tekwani BL, Walker LA, Smith PL, Paris RM, Read LT, Li Q, Pybus BS, Sousa JC, Reichard GA, Smith B, Marcsisin SR.

Antimicrob Agents Chemother. 2015 Jul;59(7):3864-9. doi: 10.1128/AAC.00343-15. Epub 2015 Apr 13.

17.

Investigation into novel thiophene- and furan-based 4-amino-7-chloroquinolines afforded antimalarials that cure mice.

Opsenica IM, Verbić TŽ, Tot M, Sciotti RJ, Pybus BS, Djurković-Djaković O, Slavić K, Šolaja BA.

Bioorg Med Chem. 2015 May 1;23(9):2176-86. doi: 10.1016/j.bmc.2015.02.061. Epub 2015 Mar 7.

PMID:
25801154
18.

EVALUATION OF AROMATIC 6-SUBSTITUTED THIENOPYRIMIDINES AS SCAFFOLDS AGAINST PARASITES THAT CAUSE TRYPANOSOMIASIS, LEISHMANIASIS, AND MALARIA.

Woodring JL, Patel G, Erath J, Behera R, Lee PJ, Leed SE, Rodriguez A, Sciotti RJ, Mensa-Wilmot K, Pollastri MP.

Medchemcomm. 2015 Feb;6(2):339-346.

19.

Differential CYP 2D6 metabolism alters primaquine pharmacokinetics.

Potter BM, Xie LH, Vuong C, Zhang J, Zhang P, Duan D, Luong TL, Bandara Herath HM, Dhammika Nanayakkara NP, Tekwani BL, Walker LA, Nolan CK, Sciotti RJ, Zottig VE, Smith PL, Paris RM, Read LT, Li Q, Pybus BS, Sousa JC, Reichard GA, Marcsisin SR.

Antimicrob Agents Chemother. 2015 Apr;59(4):2380-7. doi: 10.1128/AAC.00015-15. Epub 2015 Feb 2.

20.

The synthesis, antimalarial activity and CoMFA analysis of novel aminoalkylated quercetin analogs.

Helgren TR, Sciotti RJ, Lee P, Duffy S, Avery VM, Igbinoba O, Akoto M, Hagen TJ.

Bioorg Med Chem Lett. 2015 Jan 15;25(2):327-32. doi: 10.1016/j.bmcl.2014.11.039. Epub 2014 Nov 21.

PMID:
25488841
21.

Repurposing human Aurora kinase inhibitors as leads for anti-protozoan drug discovery.

Patel G, Roncal NE, Lee PJ, Leed SE, Erath J, Rodriguez A, Sciotti RJ, Pollastri MP.

Medchemcomm. 2014 May 1;5(5):655-658.

22.

Second generation steroidal 4-aminoquinolines are potent, dual-target inhibitors of the botulinum neurotoxin serotype A metalloprotease and P. falciparum malaria.

Videnović M, Opsenica DM, Burnett JC, Gomba L, Nuss JE, Selaković Z, Konstantinović J, Krstić M, Segan S, Zlatović M, Sciotti RJ, Bavari S, Solaja BA.

J Med Chem. 2014 May 22;57(10):4134-53. doi: 10.1021/jm500033r. Epub 2014 May 1.

23.

Tafenoquine and NPC-1161B require CYP 2D metabolism for anti-malarial activity: implications for the 8-aminoquinoline class of anti-malarial compounds.

Marcsisin SR, Sousa JC, Reichard GA, Caridha D, Zeng Q, Roncal N, McNulty R, Careagabarja J, Sciotti RJ, Bennett JW, Zottig VE, Deye G, Li Q, Read L, Hickman M, Dhammika Nanayakkara NP, Walker LA, Smith B, Melendez V, Pybus BS.

Malar J. 2014 Jan 3;13:2. doi: 10.1186/1475-2875-13-2.

24.

Auranofin is an apoptosis-simulating agent with in vitro and in vivo anti-leishmanial activity.

Sharlow ER, Leimgruber S, Murray S, Lira A, Sciotti RJ, Hickman M, Hudson T, Leed S, Caridha D, Barrios AM, Close D, Grögl M, Lazo JS.

ACS Chem Biol. 2014 Mar 21;9(3):663-72. doi: 10.1021/cb400800q. Epub 2013 Dec 23.

PMID:
24328400
25.

3,5-bis(benzylidene)-4-piperidones and related N-acyl analogs: a novel cluster of antimalarials targeting the liver stage of Plasmodium falciparum.

Das U, Singh RS, Alcorn J, Hickman MR, Sciotti RJ, Leed SE, Lee PJ, Roncal N, Dimmock JR.

Bioorg Med Chem. 2013 Dec 1;21(23):7250-6. doi: 10.1016/j.bmc.2013.09.065. Epub 2013 Oct 8.

PMID:
24139941
26.

4-Amino-7-chloroquinolines: probing ligand efficiency provides botulinum neurotoxin serotype A light chain inhibitors with significant antiprotozoal activity.

Opsenica IM, Tot M, Gomba L, Nuss JE, Sciotti RJ, Bavari S, Burnett JC, Solaja BA.

J Med Chem. 2013 Jul 25;56(14):5860-71. doi: 10.1021/jm4006077. Epub 2013 Jul 12.

27.

CYP450 phenotyping and metabolite identification of quinine by accurate mass UPLC-MS analysis: a possible metabolic link to blackwater fever.

Marcsisin SR, Jin X, Bettger T, McCulley N, Sousa JC, Shanks GD, Tekwani BL, Sahu R, Reichard GA, Sciotti RJ, Melendez V, Pybus BS.

Malar J. 2013 Jun 21;12:214. doi: 10.1186/1475-2875-12-214.

28.

Drug discovery algorithm for cutaneous leishmaniasis.

Grogl M, Hickman M, Ellis W, Hudson T, Lazo JS, Sharlow ER, Johnson J, Berman J, Sciotti RJ.

Am J Trop Med Hyg. 2013 Feb;88(2):216-21. doi: 10.4269/ajtmh.11-0812. Review.

29.

CYP450 phenotyping and accurate mass identification of metabolites of the 8-aminoquinoline, anti-malarial drug primaquine.

Pybus BS, Sousa JC, Jin X, Ferguson JA, Christian RE, Barnhart R, Vuong C, Sciotti RJ, Reichard GA, Kozar MP, Walker LA, Ohrt C, Melendez V.

Malar J. 2012 Aug 2;11:259. doi: 10.1186/1475-2875-11-259.

30.

A chemotype that inhibits three unrelated pathogenic targets: the botulinum neurotoxin serotype A light chain, P. falciparum malaria, and the Ebola filovirus.

Opsenica I, Burnett JC, Gussio R, Opsenica D, Todorović N, Lanteri CA, Sciotti RJ, Gettayacamin M, Basilico N, Taramelli D, Nuss JE, Wanner L, Panchal RG, Solaja BA, Bavari S.

J Med Chem. 2011 Mar 10;54(5):1157-69. doi: 10.1021/jm100938u. Epub 2011 Jan 25.

31.

5-(2-Pyrimidinyl)-imidazo[1,2-a]pyridines are antibacterial agents targeting the ATPase domains of DNA gyrase and topoisomerase IV.

Starr JT, Sciotti RJ, Hanna DL, Huband MD, Mullins LM, Cai H, Gage JW, Lockard M, Rauckhorst MR, Owen RM, Lall MS, Tomilo M, Chen H, McCurdy SP, Barbachyn MR.

Bioorg Med Chem Lett. 2009 Sep 15;19(18):5302-6. doi: 10.1016/j.bmcl.2009.07.141. Epub 2009 Aug 3.

PMID:
19683922
32.
33.

The synthesis and biological evaluation of a novel series of antimicrobials of the oxazolidinone class.

Sciotti RJ, Pliushchev M, Wiedeman PE, Balli D, Flamm R, Nilius AM, Marsh K, Stolarik D, Jolly R, Ulrich R, Djuric SW.

Bioorg Med Chem Lett. 2002 Aug 19;12(16):2121-3.

PMID:
12127518
34.

3,5-Bis(trifluoromethyl)pyrazoles: a novel class of NFAT transcription factor regulator.

Djuric SW, BaMaung NY, Basha A, Liu H, Luly JR, Madar DJ, Sciotti RJ, Tu NP, Wagenaar FL, Wiedeman PE, Zhou X, Ballaron S, Bauch J, Chen YW, Chiou XG, Fey T, Gauvin D, Gubbins E, Hsieh GC, Marsh KC, Mollison KW, Pong M, Shaughnessy TK, Sheets MP, Smith M, Trevillyan JM, Warrior U, Wegner CD, Carter GW.

J Med Chem. 2000 Aug 10;43(16):2975-81.

PMID:
10956206
35.

Development of a p38 Kinase Binding Assay for High Throughput Screening.

Warrior U, Chiou XG, Sheets MP, Sciotti RJ, Parry JM, Simmer RL, Surber BW, Burns DJ, Beutel BA, Mollison KW, Djuric SW, Trevillyan JM.

J Biomol Screen. 1999;4(3):129-135.

PMID:
10838421

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