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Items: 16

1.

Identification and Mechanistic Understanding of Dihydroorotate Dehydrogenase Point Mutations in Plasmodium falciparum that Confer in Vitro Resistance to the Clinical Candidate DSM265.

White J, Dhingra SK, Deng X, El Mazouni F, Lee MCS, Afanador GA, Lawong A, Tomchick DR, Ng CL, Bath J, Rathod PK, Fidock DA, Phillips MA.

ACS Infect Dis. 2019 Jan 11;5(1):90-101. doi: 10.1021/acsinfecdis.8b00211. Epub 2018 Nov 13.

PMID:
30375858
2.

Isoxazolopyrimidine-Based Inhibitors of Plasmodium falciparum Dihydroorotate Dehydrogenase with Antimalarial Activity.

Kokkonda S, El Mazouni F, White KL, White J, Shackleford DM, Lafuente-Monasterio MJ, Rowland P, Manjalanagara K, Joseph JT, Garcia-Pérez A, Fernandez J, Gamo FJ, Waterson D, Burrows JN, Palmer MJ, Charman SA, Rathod PK, Phillips MA.

ACS Omega. 2018 Aug 31;3(8):9227-9240. doi: 10.1021/acsomega.8b01573. Epub 2018 Aug 15.

3.

A Triazolopyrimidine-Based Dihydroorotate Dehydrogenase Inhibitor with Improved Drug-like Properties for Treatment and Prevention of Malaria.

Phillips MA, White KL, Kokkonda S, Deng X, White J, El Mazouni F, Marsh K, Tomchick DR, Manjalanagara K, Rudra KR, Wirjanata G, Noviyanti R, Price RN, Marfurt J, Shackleford DM, Chiu FC, Campbell M, Jimenez-Diaz MB, Bazaga SF, Angulo-Barturen I, Martinez MS, Lafuente-Monasterio M, Kaminsky W, Silue K, Zeeman AM, Kocken C, Leroy D, Blasco B, Rossignol E, Rueckle T, Matthews D, Burrows JN, Waterson D, Palmer MJ, Rathod PK, Charman SA.

ACS Infect Dis. 2016 Dec 9;2(12):945-957. Epub 2016 Oct 4.

4.

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.

5.

Identification of New Human Malaria Parasite Plasmodium falciparum Dihydroorotate Dehydrogenase Inhibitors by Pharmacophore and Structure-Based Virtual Screening.

Pavadai E, El Mazouni F, Wittlin S, de Kock C, Phillips MA, Chibale K.

J Chem Inf Model. 2016 Mar 28;56(3):548-62. doi: 10.1021/acs.jcim.5b00680. Epub 2016 Mar 8.

6.

A long-duration dihydroorotate dehydrogenase inhibitor (DSM265) for prevention and treatment of malaria.

Phillips MA, Lotharius J, Marsh K, White J, Dayan A, White KL, Njoroge JW, El Mazouni F, Lao Y, Kokkonda S, Tomchick DR, Deng X, Laird T, Bhatia SN, March S, Ng CL, Fidock DA, Wittlin S, Lafuente-Monasterio M, Benito FJ, Alonso LM, Martinez MS, Jimenez-Diaz MB, Bazaga SF, Angulo-Barturen I, Haselden JN, Louttit J, Cui Y, Sridhar A, Zeeman AM, Kocken C, Sauerwein R, Dechering K, Avery VM, Duffy S, Delves M, Sinden R, Ruecker A, Wickham KS, Rochford R, Gahagen J, Iyer L, Riccio E, Mirsalis J, Bathhurst I, Rueckle T, Ding X, Campo B, Leroy D, Rogers MJ, Rathod PK, Burrows JN, Charman SA.

Sci Transl Med. 2015 Jul 15;7(296):296ra111. doi: 10.1126/scitranslmed.aaa6645.

7.

Original 2-(3-Alkoxy-1H-pyrazol-1-yl)azines Inhibitors of Human Dihydroorotate Dehydrogenase (DHODH).

Lucas-Hourani M, Munier-Lehmann H, El Mazouni F, Malmquist NA, Harpon J, Coutant EP, Guillou S, Helynck O, Noel A, Scherf A, Phillips MA, Tangy F, Vidalain PO, Janin YL.

J Med Chem. 2015 Jul 23;58(14):5579-98. doi: 10.1021/acs.jmedchem.5b00606. Epub 2015 Jun 30.

8.

Fluorine modulates species selectivity in the triazolopyrimidine class of Plasmodium falciparum dihydroorotate dehydrogenase inhibitors.

Deng X, Kokkonda S, El Mazouni F, White J, Burrows JN, Kaminsky W, Charman SA, Matthews D, Rathod PK, Phillips MA.

J Med Chem. 2014 Jun 26;57(12):5381-94. doi: 10.1021/jm500481t. Epub 2014 Jun 13.

9.

Bioisosteric transformations and permutations in the triazolopyrimidine scaffold to identify the minimum pharmacophore required for inhibitory activity against Plasmodium falciparum dihydroorotate dehydrogenase.

Marwaha A, White J, El Mazouni F, Creason SA, Kokkonda S, Buckner FS, Charman SA, Phillips MA, Rathod PK.

J Med Chem. 2012 Sep 13;55(17):7425-36. doi: 10.1021/jm300351w. Epub 2012 Aug 21.

10.

Lead optimization of 3-carboxyl-4(1H)-quinolones to deliver orally bioavailable antimalarials.

Zhang Y, Clark JA, Connelly MC, Zhu F, Min J, Guiguemde WA, Pradhan A, Iyer L, Furimsky A, Gow J, Parman T, El Mazouni F, Phillips MA, Kyle DE, Mirsalis J, Guy RK.

J Med Chem. 2012 May 10;55(9):4205-19. doi: 10.1021/jm201642z. Epub 2012 Apr 18.

11.

Structure-guided lead optimization of triazolopyrimidine-ring substituents identifies potent Plasmodium falciparum dihydroorotate dehydrogenase inhibitors with clinical candidate potential.

Coteron JM, Marco M, Esquivias J, Deng X, White KL, White J, Koltun M, El Mazouni F, Kokkonda S, Katneni K, Bhamidipati R, Shackleford DM, Angulo-Barturen I, Ferrer SB, Jiménez-Díaz MB, Gamo FJ, Goldsmith EJ, Charman WN, Bathurst I, Floyd D, Matthews D, Burrows JN, Rathod PK, Charman SA, Phillips MA.

J Med Chem. 2011 Aug 11;54(15):5540-61. doi: 10.1021/jm200592f. Epub 2011 Jul 14.

12.

Lead optimization of aryl and aralkyl amine-based triazolopyrimidine inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase with antimalarial activity in mice.

Gujjar R, El Mazouni F, White KL, White J, Creason S, Shackleford DM, Deng X, Charman WN, Bathurst I, Burrows J, Floyd DM, Matthews D, Buckner FS, Charman SA, Phillips MA, Rathod PK.

J Med Chem. 2011 Jun 9;54(11):3935-49. doi: 10.1021/jm200265b. Epub 2011 May 12.

13.

Chemical genetics of Plasmodium falciparum.

Guiguemde WA, Shelat AA, Bouck D, Duffy S, Crowther GJ, Davis PH, Smithson DC, Connelly M, Clark J, Zhu F, Jiménez-Díaz MB, Martinez MS, Wilson EB, Tripathi AK, Gut J, Sharlow ER, Bathurst I, El Mazouni F, Fowble JW, Forquer I, McGinley PL, Castro S, Angulo-Barturen I, Ferrer S, Rosenthal PJ, Derisi JL, Sullivan DJ, Lazo JS, Roos DS, Riscoe MK, Phillips MA, Rathod PK, Van Voorhis WC, Avery VM, Guy RK.

Nature. 2010 May 20;465(7296):311-5. doi: 10.1038/nature09099.

14.

Structural plasticity of malaria dihydroorotate dehydrogenase allows selective binding of diverse chemical scaffolds.

Deng X, Gujjar R, El Mazouni F, Kaminsky W, Malmquist NA, Goldsmith EJ, Rathod PK, Phillips MA.

J Biol Chem. 2009 Sep 25;284(39):26999-7009. doi: 10.1074/jbc.M109.028589. Epub 2009 Jul 28.

15.

Identification of a metabolically stable triazolopyrimidine-based dihydroorotate dehydrogenase inhibitor with antimalarial activity in mice.

Gujjar R, Marwaha A, El Mazouni F, White J, White KL, Creason S, Shackleford DM, Baldwin J, Charman WN, Buckner FS, Charman S, Rathod PK, Phillips MA.

J Med Chem. 2009 Apr 9;52(7):1864-72. doi: 10.1021/jm801343r.

16.

Triazolopyrimidine-based dihydroorotate dehydrogenase inhibitors with potent and selective activity against the malaria parasite Plasmodium falciparum.

Phillips MA, Gujjar R, Malmquist NA, White J, El Mazouni F, Baldwin J, Rathod PK.

J Med Chem. 2008 Jun 26;51(12):3649-53. doi: 10.1021/jm8001026. Epub 2008 Jun 4.

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