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Items: 1 to 20 of 117

1.

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.

2.

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.

3.

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.

4.

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.

5.

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.

6.

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.

7.

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.

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.

Novel inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase with anti-malarial activity in the mouse model.

Booker ML, Bastos CM, Kramer ML, Barker RH Jr, Skerlj R, Sidhu AB, Deng X, Celatka C, Cortese JF, Guerrero Bravo JE, Crespo Llado KN, Serrano AE, Angulo-Barturen I, Jiménez-Díaz MB, Viera S, Garuti H, Wittlin S, Papastogiannidis P, Lin JW, Janse CJ, Khan SM, Duraisingh M, Coleman B, Goldsmith EJ, Phillips MA, Munoz B, Wirth DF, Klinger JD, Wiegand R, Sybertz E.

J Biol Chem. 2010 Oct 22;285(43):33054-64. doi: 10.1074/jbc.M110.162081. Epub 2010 Aug 11.

10.

Chemometric modeling, docking and in silico design of triazolopyrimidine-based dihydroorotate dehydrogenase inhibitors as antimalarials.

Ojha PK, Roy K.

Eur J Med Chem. 2010 Oct;45(10):4645-56. doi: 10.1016/j.ejmech.2010.07.034. Epub 2010 Jul 24.

PMID:
20708304
12.

Plasmodium dihydroorotate dehydrogenase: a promising target for novel anti-malarial chemotherapy.

Phillips MA, Rathod PK.

Infect Disord Drug Targets. 2010 Jun;10(3):226-39. Review.

13.

In vitro resistance selections for Plasmodium falciparum dihydroorotate dehydrogenase inhibitors give mutants with multiple point mutations in the drug-binding site and altered growth.

Ross LS, Gamo FJ, Lafuente-Monasterio MJ, Singh OM, Rowland P, Wiegand RC, Wirth DF.

J Biol Chem. 2014 Jun 27;289(26):17980-95. doi: 10.1074/jbc.M114.558353. Epub 2014 Apr 29.

14.

Novel selective and potent inhibitors of malaria parasite dihydroorotate dehydrogenase: discovery and optimization of dihydrothiophenone derivatives.

Xu M, Zhu J, Diao Y, Zhou H, Ren X, Sun D, Huang J, Han D, Zhao Z, Zhu L, Xu Y, Li H.

J Med Chem. 2013 Oct 24;56(20):7911-24. doi: 10.1021/jm400938g. Epub 2013 Oct 11.

PMID:
24073986
15.
16.

Structure of Plasmodium falciparum dihydroorotate dehydrogenase with a bound inhibitor.

Hurt DE, Widom J, Clardy J.

Acta Crystallogr D Biol Crystallogr. 2006 Mar;62(Pt 3):312-23. Epub 2006 Feb 22.

PMID:
16510978
17.

Harnessing evolutionary fitness in Plasmodium falciparum for drug discovery and suppressing resistance.

Lukens AK, Ross LS, Heidebrecht R, Javier Gamo F, Lafuente-Monasterio MJ, Booker ML, Hartl DL, Wiegand RC, Wirth DF.

Proc Natl Acad Sci U S A. 2014 Jan 14;111(2):799-804. doi: 10.1073/pnas.1320886110. Epub 2013 Dec 31.

18.

In silico identification of novel inhibitors against Plasmodium falciparum dihydroorate dehydrogenase.

Wadood A, Ulhaq ZU.

J Mol Graph Model. 2013 Mar;40:40-7. doi: 10.1016/j.jmgm.2012.11.010. Epub 2012 Dec 20.

PMID:
23353582
19.

Identification and characterization of small molecule inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase.

Patel V, Booker M, Kramer M, Ross L, Celatka CA, Kennedy LM, Dvorin JD, Duraisingh MT, Sliz P, Wirth DF, Clardy J.

J Biol Chem. 2008 Dec 12;283(50):35078-85. doi: 10.1074/jbc.M804990200. Epub 2008 Oct 8.

20.

Design and synthesis of potent inhibitors of the malaria parasite dihydroorotate dehydrogenase.

Heikkilä T, Ramsey C, Davies M, Galtier C, Stead AM, Johnson AP, Fishwick CW, Boa AN, McConkey GA.

J Med Chem. 2007 Jan 25;50(2):186-91.

PMID:
17228860
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