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Page 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. Coteron JM, et al. Among authors: ferrer sb. J Med Chem. 2011 Aug 11;54(15):5540-61. doi: 10.1021/jm200592f. Epub 2011 Jul 14. J Med Chem. 2011. PMID: 21696174 Free PMC article.
Falcipain inhibitors: optimization studies of the 2-pyrimidinecarbonitrile lead series.
Coterón JM, Catterick D, Castro J, Chaparro MJ, Díaz B, Fernández E, Ferrer S, Gamo FJ, Gordo M, Gut J, de las Heras L, Legac J, Marco M, Miguel J, Muñoz V, Porras E, de la Rosa JC, Ruiz JR, Sandoval E, Ventosa P, Rosenthal PJ, Fiandor JM. Coterón JM, et al. J Med Chem. 2010 Aug 26;53(16):6129-52. doi: 10.1021/jm100556b. J Med Chem. 2010. PMID: 20672841
Identification of a Potential Antimalarial Drug Candidate from a Series of 2-Aminopyrazines by Optimization of Aqueous Solubility and Potency across the Parasite Life Cycle.
Le Manach C, Nchinda AT, Paquet T, Gonzàlez Cabrera D, Younis Y, Han Z, Bashyam S, Zabiulla M, Taylor D, Lawrence N, White KL, Charman SA, Waterson D, Witty MJ, Wittlin S, Botha ME, Nondaba SH, Reader J, Birkholtz LM, Jiménez-Díaz MB, Martínez MS, Ferrer S, Angulo-Barturen I, Meister S, Antonova-Koch Y, Winzeler EA, Street LJ, Chibale K. Le Manach C, et al. J Med Chem. 2016 Nov 10;59(21):9890-9905. doi: 10.1021/acs.jmedchem.6b01265. Epub 2016 Oct 26. J Med Chem. 2016. PMID: 27748596
Synthesis and Structure-Activity Relationships of the Novel Antimalarials 5-Pyridinyl-4(1 H)-Pyridones.
Bueno JM, Calderon F, Chicharro J, De la Rosa JC, Díaz B, Fernández J, Fiandor JM, Fraile MT, García M, Herreros E, García-Pérez A, Lorenzo M, Mallo A, Puente M, Saadeddin A, Ferrer S, Angulo-Barturen I, Burrows JN, León ML. Bueno JM, et al. J Med Chem. 2018 Apr 26;61(8):3422-3435. doi: 10.1021/acs.jmedchem.7b01256. Epub 2018 Apr 5. J Med Chem. 2018. PMID: 29589932
Identification of Fast-Acting 2,6-Disubstituted Imidazopyridines That Are Efficacious in the in Vivo Humanized Plasmodium falciparum NODscidIL2Rγ null Mouse Model of Malaria.
Nchinda AT, Le Manach C, Paquet T, Gonzàlez Cabrera D, Wicht KJ, Brunschwig C, Njoroge M, Abay E, Taylor D, Lawrence N, Wittlin S, Jiménez-Díaz MB, Santos Martínez M, Ferrer S, Angulo-Barturen I, Lafuente-Monasterio MJ, Duffy J, Burrows J, Street LJ, Chibale K. Nchinda AT, et al. J Med Chem. 2018 May 10;61(9):4213-4227. doi: 10.1021/acs.jmedchem.8b00382. Epub 2018 Apr 27. J Med Chem. 2018. PMID: 29665687
Lead Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series for the Treatment of Malaria.
Kokkonda S, Deng X, White KL, El Mazouni F, White J, Shackleford DM, Katneni K, Chiu FCK, Barker H, McLaren J, Crighton E, Chen G, Angulo-Barturen I, Jimenez-Diaz MB, Ferrer S, Huertas-Valentin L, Martinez-Martinez MS, Lafuente-Monasterio MJ, Chittimalla R, Shahi SP, Wittlin S, Waterson D, Burrows JN, Matthews D, Tomchick D, Rathod PK, Palmer MJ, Charman SA, Phillips MA. Kokkonda S, et al. J Med Chem. 2020 May 14;63(9):4929-4956. doi: 10.1021/acs.jmedchem.0c00311. Epub 2020 Apr 16. J Med Chem. 2020. PMID: 32248693 Free PMC article.
A potent series targeting the malarial cGMP-dependent protein kinase clears infection and blocks transmission.
Baker DA, Stewart LB, Large JM, Bowyer PW, Ansell KH, Jiménez-Díaz MB, El Bakkouri M, Birchall K, Dechering KJ, Bouloc NS, Coombs PJ, Whalley D, Harding DJ, Smiljanic-Hurley E, Wheldon MC, Walker EM, Dessens JT, Lafuente MJ, Sanz LM, Gamo FJ, Ferrer SB, Hui R, Bousema T, Angulo-Barturén I, Merritt AT, Croft SL, Gutteridge WE, Kettleborough CA, Osborne SA. Baker DA, et al. Among authors: ferrer sb. Nat Commun. 2017 Sep 5;8(1):430. doi: 10.1038/s41467-017-00572-x. Nat Commun. 2017. PMID: 28874661 Free PMC article.
A murine model of falciparum-malaria by in vivo selection of competent strains in non-myelodepleted mice engrafted with human erythrocytes.
Angulo-Barturen I, Jiménez-Díaz MB, Mulet T, Rullas J, Herreros E, Ferrer S, Jiménez E, Mendoza A, Regadera J, Rosenthal PJ, Bathurst I, Pompliano DL, Gómez de las Heras F, Gargallo-Viola D. Angulo-Barturen I, et al. PLoS One. 2008 May 21;3(5):e2252. doi: 10.1371/journal.pone.0002252. PLoS One. 2008. PMID: 18493601 Free PMC article.
Cyclopropyl carboxamides, a chemically novel class of antimalarial agents identified in a phenotypic screen.
Sanz LM, Jiménez-Díaz MB, Crespo B, De-Cozar C, Almela MJ, Angulo-Barturen I, Castañeda P, Ibañez J, Fernández EP, Ferrer S, Herreros E, Lozano S, Martínez MS, Rueda L, Burrows JN, García-Bustos JF, Gamo FJ. Sanz LM, et al. Antimicrob Agents Chemother. 2011 Dec;55(12):5740-5. doi: 10.1128/AAC.05188-11. Epub 2011 Oct 3. Antimicrob Agents Chemother. 2011. PMID: 21968362 Free PMC article.
35 results