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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.

J Med Chem. 2016 Nov 10;59(21):9890-9905. Epub 2016 Oct 26.


Discovery and optimisation studies of antimalarial phenotypic hits.

Mital A, Murugesan D, Kaiser M, Yeates C, Gilbert IH.

Eur J Med Chem. 2015 Oct 20;103:530-8. doi: 10.1016/j.ejmech.2015.08.044. Epub 2015 Sep 9.


A Novel Pyrazolopyridine with in Vivo Activity in Plasmodium berghei- and Plasmodium falciparum-Infected Mouse Models from Structure-Activity Relationship Studies around the Core of Recently Identified Antimalarial Imidazopyridazines.

Le Manach C, Paquet T, Brunschwig C, Njoroge M, Han Z, Gonzàlez Cabrera D, Bashyam S, Dhinakaran R, Taylor D, Reader J, Botha M, Churchyard A, Lauterbach S, Coetzer TL, Birkholtz LM, Meister S, Winzeler EA, Waterson D, Witty MJ, Wittlin S, Jiménez-Díaz MB, Santos Martínez M, Ferrer S, Angulo-Barturen I, Street LJ, Chibale K.

J Med Chem. 2015 Nov 12;58(21):8713-22. doi: 10.1021/acs.jmedchem.5b01605. Epub 2015 Nov 2.


Antimalarial Pyrido[1,2-a]benzimidazoles: Lead Optimization, Parasite Life Cycle Stage Profile, Mechanistic Evaluation, Killing Kinetics, and in Vivo Oral Efficacy in a Mouse Model.

Singh K, Okombo J, Brunschwig C, Ndubi F, Barnard L, Wilkinson C, Njogu PM, Njoroge M, Laing L, Machado M, Prudêncio M, Reader J, Botha M, Nondaba S, Birkholtz LM, Lauterbach S, Churchyard A, Coetzer TL, Burrows JN, Yeates C, Denti P, Wiesner L, Egan TJ, Wittlin S, Chibale K.

J Med Chem. 2017 Feb 23;60(4):1432-1448. doi: 10.1021/acs.jmedchem.6b01641. Epub 2017 Feb 7.


Structure-activity-relationship studies around the 2-amino group and pyridine core of antimalarial 3,5-diarylaminopyridines lead to a novel series of pyrazine analogues with oral in vivo activity.

Younis Y, Douelle F, González Cabrera D, Le Manach C, Nchinda AT, Paquet T, Street LJ, White KL, Zabiulla KM, Joseph JT, Bashyam S, Waterson D, Witty MJ, Wittlin S, Charman SA, Chibale K.

J Med Chem. 2013 Nov 14;56(21):8860-71. doi: 10.1021/jm401278d. Epub 2013 Oct 29.


Medicinal chemistry optimization of antiplasmodial imidazopyridazine hits from high throughput screening of a softfocus kinase library: part 2.

Le Manach C, Paquet T, Gonzàlez Cabrera D, Younis Y, Taylor D, Wiesner L, Lawrence N, Schwager S, Waterson D, Witty MJ, Wittlin S, Street LJ, Chibale K.

J Med Chem. 2014 Nov 13;57(21):8839-48. doi: 10.1021/jm500887k. Epub 2014 Oct 23.


Structure-activity relationship of new antimalarial 1-aryl-3-susbtituted propanol derivatives: Synthesis, preliminary toxicity profiling, parasite life cycle stage studies, target exploration, and targeted delivery.

Quiliano M, Pabón A, Moles E, Bonilla-Ramirez L, Fabing I, Fong KY, Nieto-Aco DA, Wright DW, Pizarro JC, Vettorazzi A, López de Cerain A, Deharo E, Fernández-Busquets X, Garavito G, Aldana I, Galiano S.

Eur J Med Chem. 2018 May 25;152:489-514. doi: 10.1016/j.ejmech.2018.04.038. Epub 2018 Apr 24.


3,5-bis(benzylidene)-4-piperidones and related N-acyl analogs: a novel cluster of antimalarials targeting the liver stage of Plasmodium falciparum.

Das U, Singh RS, Alcorn J, Hickman MR, Sciotti RJ, Leed SE, Lee PJ, Roncal N, Dimmock JR.

Bioorg Med Chem. 2013 Dec 1;21(23):7250-6. doi: 10.1016/j.bmc.2013.09.065. Epub 2013 Oct 8.


Small-molecule histone methyltransferase inhibitors display rapid antimalarial activity against all blood stage forms in Plasmodium falciparum.

Malmquist NA, Moss TA, Mecheri S, Scherf A, Fuchter MJ.

Proc Natl Acad Sci U S A. 2012 Oct 9;109(41):16708-13. doi: 10.1073/pnas.1205414109. Epub 2012 Sep 24.


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.


Structure-activity relationship studies of orally active antimalarial 3,5-substituted 2-aminopyridines.

González Cabrera D, Douelle F, Younis Y, Feng TS, Le Manach C, Nchinda AT, Street LJ, Scheurer C, Kamber J, White KL, Montagnat OD, Ryan E, Katneni K, Zabiulla KM, Joseph JT, Bashyam S, Waterson D, Witty MJ, Charman SA, Wittlin S, Chibale K.

J Med Chem. 2012 Dec 27;55(24):11022-30. doi: 10.1021/jm301476b. Epub 2012 Dec 14.


Synergistic blending of high-valued heterocycles inhibits growth of Plasmodium falciparum in culture and P. berghei infection in mouse model.

Kumar P, Achieng AO, Rajendran V, Ghosh PC, Singh BK, Rawat M, Perkins DJ, Kempaiah P, Rathi B.

Sci Rep. 2017 Jul 27;7(1):6724. doi: 10.1038/s41598-017-06097-z.


4-(1H)-Quinolones and 1,2,3,4-Tetrahydroacridin-9(10H)-ones prevent the transmission of Plasmodium falciparum to Anopheles freeborni.

Sáenz FE, Lacrue AN, Cross RM, Maignan JR, Udenze KO, Manetsch R, Kyle DE.

Antimicrob Agents Chemother. 2013 Dec;57(12):6187-95. doi: 10.1128/AAC.00492-13. Epub 2013 Sep 30.


The activities of current antimalarial drugs on the life cycle stages of Plasmodium: a comparative study with human and rodent parasites.

Delves M, Plouffe D, Scheurer C, Meister S, Wittlin S, Winzeler EA, Sinden RE, Leroy D.

PLoS Med. 2012 Feb;9(2):e1001169. doi: 10.1371/journal.pmed.1001169. Epub 2012 Feb 21.


Novel 4-aminoquinoline analogs highly active against the blood and sexual stages of Plasmodium in vivo and in vitro.

Sáenz FE, Mutka T, Udenze K, Oduola AM, Kyle DE.

Antimicrob Agents Chemother. 2012 Sep;56(9):4685-92. doi: 10.1128/AAC.01061-12. Epub 2012 Jun 18.


N-Cinnamoylation of Antimalarial Classics: Effects of Using Acyl Groups Other than Cinnamoyl toward Dual-Stage Antimalarials.

Gomes A, Machado M, Lobo L, Nogueira F, Prudêncio M, Teixeira C, Gomes P.

ChemMedChem. 2015 Aug;10(8):1344-9. doi: 10.1002/cmdc.201500164. Epub 2015 Jun 2.


Benzoxaborole antimalarial agents. Part 4. Discovery of potent 6-(2-(alkoxycarbonyl)pyrazinyl-5-oxy)-1,3-dihydro-1-hydroxy-2,1-benzoxaboroles.

Zhang YK, Plattner JJ, Easom EE, Jacobs RT, Guo D, Sanders V, Freund YR, Campo B, Rosenthal PJ, Bu W, Gamo FJ, Sanz LM, Ge M, Li L, Ding J, Yang Y.

J Med Chem. 2015 Jul 9;58(13):5344-54. doi: 10.1021/acs.jmedchem.5b00678. Epub 2015 Jun 23.


Discovery of new antimalarial agents: Second-generation dual inhibitors against FP-2 and PfDHFR via fragments assembely.

Chen W, Huang Z, Wang W, Mao F, Guan L, Tang Y, Jiang H, Li J, Huang J, Jiang L, Zhu J.

Bioorg Med Chem. 2017 Dec 15;25(24):6467-6478. doi: 10.1016/j.bmc.2017.10.017. Epub 2017 Oct 16.


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.

J Med Chem. 2014 Aug 14;57(15):6642-52. doi: 10.1021/jm500715u. Epub 2014 Jul 21.


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