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Page 1
Long-Lasting and Fast-Acting in Vivo Efficacious Antiplasmodial Azepanylcarbazole Amino Alcohol.
Abla N, Bashyam S, Charman SA, Greco B, Hewitt P, Jiménez-Díaz MB, Katneni K, Kubas H, Picard D, Sambandan Y, Sanz L, Smith D, Wang T, Willis P, Wittlin S, Spangenberg T. Abla N, et al. ACS Med Chem Lett. 2017 Nov 28;8(12):1304-1308. doi: 10.1021/acsmedchemlett.7b00391. eCollection 2017 Dec 14. ACS Med Chem Lett. 2017. PMID: 29259752 Free PMC article.
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. 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.
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.
Quinolone-3-diarylethers: a new class of antimalarial drug.
Nilsen A, LaCrue AN, White KL, Forquer IP, Cross RM, Marfurt J, Mather MW, Delves MJ, Shackleford DM, Saenz FE, Morrisey JM, Steuten J, Mutka T, Li Y, Wirjanata G, Ryan E, Duffy S, Kelly JX, Sebayang BF, Zeeman AM, Noviyanti R, Sinden RE, Kocken CHM, Price RN, Avery VM, Angulo-Barturen I, Jiménez-Díaz MB, Ferrer S, Herreros E, Sanz LM, Gamo FJ, Bathurst I, Burrows JN, Siegl P, Guy RK, Winter RW, Vaidya AB, Charman SA, Kyle DE, Manetsch R, Riscoe MK. Nilsen A, et al. Sci Transl Med. 2013 Mar 20;5(177):177ra37. doi: 10.1126/scitranslmed.3005029. Sci Transl Med. 2013. PMID: 23515079 Free PMC article.
Cyclopropyl Carboxamides: A New Oral Antimalarial Series Derived from the Tres Cantos Anti-Malarial Set (TCAMS).
Rueda L, Castellote I, Castro-Pichel J, Chaparro MJ, de la Rosa JC, Garcia-Perez A, Gordo M, Jimenez-Diaz MB, Kessler A, Macdonald SJ, Martinez MS, Sanz LM, Gamo FJ, Fernandez E. Rueda L, et al. ACS Med Chem Lett. 2011 Aug 29;2(11):840-4. doi: 10.1021/ml2001517. eCollection 2011 Nov 10. ACS Med Chem Lett. 2011. PMID: 24900273 Free PMC article.
Optimization of Potent Inhibitors of P. falciparum Dihydroorotate Dehydrogenase for the Treatment of Malaria.
Skerlj RT, Bastos CM, Booker ML, Kramer ML, Barker RH Jr, Celatka CA, O'Shea TJ, Munoz B, Sidhu AB, Cortese JF, Wittlin S, Papastogiannidis P, Angulo-Barturen I, Jimenez-Diaz MB, Sybertz E. Skerlj RT, et al. ACS Med Chem Lett. 2011 Jul 11;2(9):708-13. doi: 10.1021/ml200143c. eCollection 2011 Sep 8. ACS Med Chem Lett. 2011. PMID: 24900364 Free PMC article.
Aminoazabenzimidazoles, a novel class of orally active antimalarial agents.
Hameed P S, Chinnapattu M, Shanbag G, Manjrekar P, Koushik K, Raichurkar A, Patil V, Jatheendranath S, Rudrapatna SS, Barde SP, Rautela N, Awasthy D, Morayya S, Narayan C, Kavanagh S, Saralaya R, Bharath S, Viswanath P, Mukherjee K, Bandodkar B, Srivastava A, Panduga V, Reddy J, Prabhakar KR, Sinha A, Jiménez-Díaz MB, Martínez MS, Angulo-Barturen I, Ferrer S, Sanz LM, Gamo FJ, Duffy S, Avery VM, Magistrado PA, Lukens AK, Wirth DF, Waterson D, Balasubramanian V, Iyer PS, Narayanan S, Hosagrahara V, Sambandamurthy VK, Ramachandran S. Hameed P S, et al. J Med Chem. 2014 Jul 10;57(13):5702-13. doi: 10.1021/jm500535j. Epub 2014 Jun 24. J Med Chem. 2014. PMID: 24914738
N-aryl-2-aminobenzimidazoles: novel, efficacious, antimalarial lead compounds.
Ramachandran S, Hameed P S, Srivastava A, Shanbhag G, Morayya S, Rautela N, Awasthy D, Kavanagh S, Bharath S, Reddy J, Panduga V, Prabhakar KR, Saralaya R, Nanduri R, Raichurkar A, Menasinakai S, Achar V, Jiménez-Díaz MB, Martínez MS, Angulo-Barturen I, Ferrer S, Sanz LM, Gamo FJ, Duffy S, Avery VM, Waterson D, Lee MC, Coburn-Flynn O, Fidock DA, Iyer PS, Narayanan S, Hosagrahara V, Sambandamurthy VK. Ramachandran S, et al. J Med Chem. 2014 Aug 14;57(15):6642-52. doi: 10.1021/jm500715u. Epub 2014 Jul 21. J Med Chem. 2014. PMID: 25007124
Histone methyltransferase inhibitors are orally bioavailable, fast-acting molecules with activity against different species causing malaria in humans.
Malmquist NA, Sundriyal S, Caron J, Chen P, Witkowski B, Menard D, Suwanarusk R, Renia L, Nosten F, Jiménez-Díaz MB, Angulo-Barturen I, Santos Martínez M, Ferrer S, Sanz LM, Gamo FJ, Wittlin S, Duffy S, Avery VM, Ruecker A, Delves MJ, Sinden RE, Fuchter MJ, Scherf A. Malmquist NA, et al. Antimicrob Agents Chemother. 2015 Feb;59(2):950-9. doi: 10.1128/AAC.04419-14. Epub 2014 Nov 24. Antimicrob Agents Chemother. 2015. PMID: 25421480 Free PMC article.
59 results