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Items: 26

1.

Antimalarial efficacy of MMV390048, an inhibitor of Plasmodium phosphatidylinositol 4-kinase.

Paquet T, Le Manach C, Cabrera DG, Younis Y, Henrich PP, Abraham TS, Lee MCS, Basak R, Ghidelli-Disse S, Lafuente-Monasterio MJ, Bantscheff M, Ruecker A, Blagborough AM, Zakutansky SE, Zeeman AM, White KL, Shackleford DM, Mannila J, Morizzi J, Scheurer C, Angulo-Barturen I, Martínez MS, Ferrer S, Sanz LM, Gamo FJ, Reader J, Botha M, Dechering KJ, Sauerwein RW, Tungtaeng A, Vanachayangkul P, Lim CS, Burrows J, Witty MJ, Marsh KC, Bodenreider C, Rochford R, Solapure SM, Jiménez-Díaz MB, Wittlin S, Charman SA, Donini C, Campo B, Birkholtz LM, Hanson KK, Drewes G, Kocken CHM, Delves MJ, Leroy D, Fidock DA, Waterson D, Street LJ, Chibale K.

Sci Transl Med. 2017 Apr 26;9(387). pii: eaad9735. doi: 10.1126/scitranslmed.aad9735.

2.

Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).

Dong Y, Wang X, Kamaraj S, Bulbule VJ, Chiu FC, Chollet J, Dhanasekaran M, Hein CD, Papastogiannidis P, Morizzi J, Shackleford DM, Barker H, Ryan E, Scheurer C, Tang Y, Zhao Q, Zhou L, White KL, Urwyler H, Charman WN, Matile H, Wittlin S, Charman SA, Vennerstrom JL.

J Med Chem. 2017 Apr 13;60(7):2654-2668. doi: 10.1021/acs.jmedchem.6b01586. Epub 2017 Jan 18.

PMID:
28052200
3.

Tetrahydro-2-naphthyl and 2-Indanyl Triazolopyrimidines Targeting Plasmodium falciparum Dihydroorotate Dehydrogenase Display Potent and Selective Antimalarial Activity.

Kokkonda S, Deng X, White KL, Coteron JM, Marco M, de Las Heras L, White J, El Mazouni F, Tomchick DR, Manjalanagara K, Rudra KR, Chen G, Morizzi J, Ryan E, Kaminsky W, Leroy D, Martínez-Martínez MS, Jimenez-Diaz MB, Bazaga SF, Angulo-Barturen I, Waterson D, Burrows JN, Matthews D, Charman SA, Phillips MA, Rathod PK.

J Med Chem. 2016 Jun 9;59(11):5416-31. doi: 10.1021/acs.jmedchem.6b00275. Epub 2016 May 21.

4.

Two analogues of fenarimol show curative activity in an experimental model of Chagas disease.

Keenan M, Chaplin JH, Alexander PW, Abbott MJ, Best WM, Khong A, Botero A, Perez C, Cornwall S, Thompson RA, White KL, Shackleford DM, Koltun M, Chiu FC, Morizzi J, Ryan E, Campbell M, von Geldern TW, Scandale I, Chatelain E, Charman SA.

J Med Chem. 2013 Dec 27;56(24):10158-70. doi: 10.1021/jm401610c. Epub 2013 Dec 4.

5.

In vitro and in vivo characterization of the antimalarial lead compound SSJ-183 in Plasmodium models.

Schleiferböck S, Scheurer C, Ihara M, Itoh I, Bathurst I, Burrows JN, Fantauzzi P, Lotharius J, Charman SA, Morizzi J, Shackleford DM, White KL, Brun R, Wittlin S.

Drug Des Devel Ther. 2013 Nov 15;7:1377-84. doi: 10.2147/DDDT.S51298. eCollection 2013.

6.

A prodrug approach toward cancer-related carbonic anhydrase inhibition.

Carroux CJ, Rankin GM, Moeker J, Bornaghi LF, Katneni K, Morizzi J, Charman SA, Vullo D, Supuran CT, Poulsen SA.

J Med Chem. 2013 Dec 12;56(23):9623-34. doi: 10.1021/jm401163e. Epub 2013 Nov 20.

PMID:
24200125
7.

3',4'-Bis-difluoromethoxycinnamoylanthranilate (FT061): an orally-active antifibrotic agent that reduces albuminuria in a rat model of progressive diabetic nephropathy.

Williams SJ, Zammit SC, Cox AJ, Shackleford DM, Morizzi J, Zhang Y, Powell AK, Gilbert RE, Krum H, Kelly DJ.

Bioorg Med Chem Lett. 2013 Dec 15;23(24):6868-73. doi: 10.1016/j.bmcl.2013.09.100. Epub 2013 Oct 8.

PMID:
24169234
8.

Discovery and structure-activity relationships of pyrrolone antimalarials.

Murugesan D, Mital A, Kaiser M, Shackleford DM, Morizzi J, Katneni K, Campbell M, Hudson A, Charman SA, Yeates C, Gilbert IH.

J Med Chem. 2013 Apr 11;56(7):2975-90. doi: 10.1021/jm400009c. Epub 2013 Mar 21.

9.

Comparative antimalarial activities and ADME profiles of ozonides (1,2,4-trioxolanes) OZ277, OZ439, and their 1,2-dioxolane, 1,2,4-trioxane, and 1,2,4,5-tetraoxane isosteres.

Wang X, Dong Y, Wittlin S, Charman SA, Chiu FC, Chollet J, Katneni K, Mannila J, Morizzi J, Ryan E, Scheurer C, Steuten J, Santo Tomas J, Snyder C, Vennerstrom JL.

J Med Chem. 2013 Mar 28;56(6):2547-55. doi: 10.1021/jm400004u. Epub 2013 Mar 15.

PMID:
23489135
10.

Synthesis of acylated glycoconjugates as templates to investigate in vitro biopharmaceutical properties.

Carroux CJ, Moeker J, Motte J, Lopez M, Bornaghi LF, Katneni K, Ryan E, Morizzi J, Shackleford DM, Charman SA, Poulsen SA.

Bioorg Med Chem Lett. 2013 Jan 15;23(2):455-9. doi: 10.1016/j.bmcl.2012.11.056. Epub 2012 Nov 29.

PMID:
23245512
11.

Probing a potential in vivo drug-excipient interaction: temporal effects of a modified β-cyclodextrin on the intravenous pharmacokinetics of a model high-affinity drug ligand.

Mannila A, Morizzi J, Nguyen TT, Charman SA, McIntosh MP, Shackleford DM.

J Pharm Sci. 2012 Sep;101(9):3381-9. doi: 10.1002/jps.23177. Epub 2012 May 1.

PMID:
22549698
12.

Metallocene-based inhibitors of cancer-associated carbonic anhydrase enzymes IX and XII.

Salmon AJ, Williams ML, Wu QK, Morizzi J, Gregg D, Charman SA, Vullo D, Supuran CT, Poulsen SA.

J Med Chem. 2012 Jun 14;55(11):5506-17. doi: 10.1021/jm300427m. Epub 2012 May 22.

PMID:
22540953
13.

Analogues of fenarimol are potent inhibitors of Trypanosoma cruzi and are efficacious in a murine model of Chagas disease.

Keenan M, Abbott MJ, Alexander PW, Armstrong T, Best WM, Berven B, Botero A, Chaplin JH, Charman SA, Chatelain E, von Geldern TW, Kerfoot M, Khong A, Nguyen T, McManus JD, Morizzi J, Ryan E, Scandale I, Thompson RA, Wang SZ, White KL.

J Med Chem. 2012 May 10;55(9):4189-204. doi: 10.1021/jm2015809. Epub 2012 Apr 27.

PMID:
22536986
14.

3,5-Diaryl-2-aminopyridines as a novel class of orally active antimalarials demonstrating single dose cure in mice and clinical candidate potential.

Younis Y, Douelle F, Feng TS, González Cabrera D, Le Manach C, Nchinda AT, Duffy S, White KL, Shackleford DM, Morizzi J, Mannila J, Katneni K, Bhamidipati R, Zabiulla KM, Joseph JT, Bashyam S, Waterson D, Witty MJ, Hardick D, Wittlin S, Avery V, Charman SA, Chibale K.

J Med Chem. 2012 Apr 12;55(7):3479-87. doi: 10.1021/jm3001373. Epub 2012 Mar 21.

PMID:
22390538
15.

The involvement of a Na⁺- and Cl⁻-dependent transporter in the brain uptake of amantadine and rimantadine.

Kooijmans SA, Senyschyn D, Mezhiselvam MM, Morizzi J, Charman SA, Weksler B, Romero IA, Couraud PO, Nicolazzo JA.

Mol Pharm. 2012 Apr 2;9(4):883-93. doi: 10.1021/mp2004127. Epub 2012 Mar 1.

PMID:
22352408
16.

Diacetylbis(N(4)-methylthiosemicarbazonato) copper(II) (CuII(atsm)) protects against peroxynitrite-induced nitrosative damage and prolongs survival in amyotrophic lateral sclerosis mouse model.

Soon CP, Donnelly PS, Turner BJ, Hung LW, Crouch PJ, Sherratt NA, Tan JL, Lim NK, Lam L, Bica L, Lim S, Hickey JL, Morizzi J, Powell A, Finkelstein DI, Culvenor JG, Masters CL, Duce J, White AR, Barnham KJ, Li QX.

J Biol Chem. 2011 Dec 23;286(51):44035-44. doi: 10.1074/jbc.M111.274407. Epub 2011 Oct 27.

17.

Discovery of 7-hydroxy-6-methoxy-2-methyl-3-(3,4,5-trimethoxybenzoyl)benzo[b]furan (BNC105), a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties.

Flynn BL, Gill GS, Grobelny DW, Chaplin JH, Paul D, Leske AF, Lavranos TC, Chalmers DK, Charman SA, Kostewicz E, Shackleford DM, Morizzi J, Hamel E, Jung MK, Kremmidiotis G.

J Med Chem. 2011 Sep 8;54(17):6014-27. doi: 10.1021/jm200454y. Epub 2011 Aug 5.

18.

Synthetic ozonide drug candidate OZ439 offers new hope for a single-dose cure of uncomplicated malaria.

Charman SA, Arbe-Barnes S, Bathurst IC, Brun R, Campbell M, Charman WN, Chiu FC, Chollet J, Craft JC, Creek DJ, Dong Y, Matile H, Maurer M, Morizzi J, Nguyen T, Papastogiannidis P, Scheurer C, Shackleford DM, Sriraghavan K, Stingelin L, Tang Y, Urwyler H, Wang X, White KL, Wittlin S, Zhou L, Vennerstrom JL.

Proc Natl Acad Sci U S A. 2011 Mar 15;108(11):4400-5. doi: 10.1073/pnas.1015762108. Epub 2011 Feb 7.

19.

Discovery of Novel Benzo[a]phenoxazine SSJ-183 as a Drug Candidate for Malaria.

Ge JF, Arai C, Yang M, Bakar Md A, Lu J, Ismail NS, Wittlin S, Kaiser M, Brun R, Charman SA, Nguyen T, Morizzi J, Itoh I, Ihara M.

ACS Med Chem Lett. 2010 Jul 12;1(7):360-4. doi: 10.1021/ml100120a. eCollection 2010 Oct 14.

20.

Preclinical comparison of intravenous melphalan pharmacokinetics administered in formulations containing either (SBE)7 m-β-cyclodextrin or a co-solvent system.

Koltun M, Morizzi J, Katneni K, Charman SA, Shackleford DM, McIntosh MP.

Biopharm Drug Dispos. 2010 Nov;31(8-9):450-4. doi: 10.1002/bdd.725.

PMID:
20865695
21.

Impact of chlorpromazine self-association on its apparent binding constants with cyclodextrins: Effect of SBE(7)-beta-CD on the disposition of chlorpromazine in the rat.

McIntosh MP, Leong N, Katneni K, Morizzi J, Shackleford DM, Prankerd RJ.

J Pharm Sci. 2010 Jul;99(7):2999-3008. doi: 10.1002/jps.22064.

PMID:
20091817
22.

The comparative antimalarial properties of weak base and neutral synthetic ozonides.

Tang Y, Wittlin S, Charman SA, Chollet J, Chiu FC, Morizzi J, Johnson LM, Tomas JS, Scheurer C, Snyder C, Zhou L, Dong Y, Charman WN, Matile H, Urwyler H, Dorn A, Vennerstrom JL.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):563-6. doi: 10.1016/j.bmcl.2009.11.088. Epub 2009 Nov 22.

PMID:
19962893
23.

The structure-activity relationship of the antimalarial ozonide arterolane (OZ277).

Dong Y, Wittlin S, Sriraghavan K, Chollet J, Charman SA, Charman WN, Scheurer C, Urwyler H, Santo Tomas J, Snyder C, Creek DJ, Morizzi J, Koltun M, Matile H, Wang X, Padmanilayam M, Tang Y, Dorn A, Brun R, Vennerstrom JL.

J Med Chem. 2010 Jan 14;53(1):481-91. doi: 10.1021/jm901473s.

PMID:
19924861
24.

S-glycosyl primary sulfonamides--a new structural class for selective inhibition of cancer-associated carbonic anhydrases.

Lopez M, Paul B, Hofmann A, Morizzi J, Wu QK, Charman SA, Innocenti A, Vullo D, Supuran CT, Poulsen SA.

J Med Chem. 2009 Oct 22;52(20):6421-32. doi: 10.1021/jm900914e.

PMID:
19827837
25.

Simultaneous determination of OZ277, a synthetic 1,2,4-trioxolane antimalarial, and its polar metabolites in rat plasma using hydrophilic interaction chromatography.

Bhamidipati RK, Morizzi J, Chiu FC, Shackleford DM, Charman SA.

J Chromatogr B Analyt Technol Biomed Life Sci. 2009 Oct 1;877(27):2989-95. doi: 10.1016/j.jchromb.2009.07.015. Epub 2009 Jul 17.

PMID:
19646936
26.

Characterization of the two major CYP450 metabolites of ozonide (1,2,4-trioxolane) OZ277.

Zhou L, Alker A, Ruf A, Wang X, Chiu FC, Morizzi J, Charman SA, Charman WN, Scheurer C, Wittlin S, Dong Y, Hunziker D, Vennerstrom JL.

Bioorg Med Chem Lett. 2008 Mar 1;18(5):1555-8. doi: 10.1016/j.bmcl.2008.01.087. Epub 2008 Jan 30.

PMID:
18262417

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