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Items: 1 to 20 of 101

1.

Novel diaryl ureas with efficacy in a mouse model of malaria.

Anderson JW, Sarantakis D, Terpinski J, Kumar TR, Tsai HC, Kuo M, Ager AL, Jacobs WR Jr, Schiehser GA, Ekins S, Sacchettini JC, Jacobus DP, Fidock DA, Freundlich JS.

Bioorg Med Chem Lett. 2013 Feb 15;23(4):1022-5. doi: 10.1016/j.bmcl.2012.12.022. Epub 2012 Dec 20.

2.

Interrogating alkyl and arylalkylpolyamino (bis)urea and (bis)thiourea isosteres as potent antimalarial chemotypes against multiple lifecycle forms of Plasmodium falciparum parasites.

Verlinden BK, de Beer M, Pachaiyappan B, Besaans E, Andayi WA, Reader J, Niemand J, van Biljon R, Guy K, Egan T, Woster PM, Birkholtz LM.

Bioorg Med Chem. 2015 Aug 15;23(16):5131-43. doi: 10.1016/j.bmc.2015.01.036. Epub 2015 Jan 28.

3.

Antimalarial benzoheterocyclic 4-aminoquinolines: Structure-activity relationship, in vivo evaluation, mechanistic and bioactivation studies.

Ongarora DS, Strydom N, Wicht K, Njoroge M, Wiesner L, Egan TJ, Wittlin S, Jurva U, Masimirembwa CM, Chibale K.

Bioorg Med Chem. 2015 Sep 1;23(17):5419-32. doi: 10.1016/j.bmc.2015.07.051. Epub 2015 Jul 30.

PMID:
26264839
4.

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.

PMID:
24139941
5.

Generation of quinolone antimalarials targeting the Plasmodium falciparum mitochondrial respiratory chain for the treatment and prophylaxis of malaria.

Biagini GA, Fisher N, Shone AE, Mubaraki MA, Srivastava A, Hill A, Antoine T, Warman AJ, Davies J, Pidathala C, Amewu RK, Leung SC, Sharma R, Gibbons P, Hong DW, Pacorel B, Lawrenson AS, Charoensutthivarakul S, Taylor L, Berger O, Mbekeani A, Stocks PA, Nixon GL, Chadwick J, Hemingway J, Delves MJ, Sinden RE, Zeeman AM, Kocken CH, Berry NG, O'Neill PM, Ward SA.

Proc Natl Acad Sci U S A. 2012 May 22;109(21):8298-303. doi: 10.1073/pnas.1205651109. Epub 2012 May 7.

6.

Antimalarial activity of novel 4-aminoquinolines active against drug resistant strains.

Kondaparla S, Soni A, Manhas A, Srivastava K, Puri SK, Katti SB.

Bioorg Chem. 2017 Feb;70:74-85. doi: 10.1016/j.bioorg.2016.11.010. Epub 2016 Nov 23.

PMID:
27908538
7.

Protective activity of biflavanones from Garcinia kola against Plasmodium infection.

Konziase B.

J Ethnopharmacol. 2015 Aug 22;172:214-8. doi: 10.1016/j.jep.2015.06.038. Epub 2015 Jun 27.

PMID:
26129936
8.

New quinoline derivatives demonstrate a promising antimalarial activity against Plasmodium falciparum in vitro and Plasmodium berghei in vivo.

Soares RR, da Silva JM, Carlos BC, da Fonseca CC, de Souza LS, Lopes FV, de Paula Dias RM, Moreira PO, Abramo C, Viana GH, de Pila Varotti F, da Silva AD, Scopel KK.

Bioorg Med Chem Lett. 2015 Jun 1;25(11):2308-13. doi: 10.1016/j.bmcl.2015.04.014. Epub 2015 Apr 11.

PMID:
25920564
9.

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.

Antimicrob Agents Chemother. 2011 Dec;55(12):5740-5. doi: 10.1128/AAC.05188-11. Epub 2011 Oct 3.

10.

Antimalarial activity of compounds comprising a primary benzene sulfonamide fragment.

Andrews KT, Fisher GM, Sumanadasa SD, Skinner-Adams T, Moeker J, Lopez M, Poulsen SA.

Bioorg Med Chem Lett. 2013 Nov 15;23(22):6114-7. doi: 10.1016/j.bmcl.2013.09.015. Epub 2013 Sep 14.

PMID:
24084158
11.

Antimalarial t-butylperoxyamines.

Sundar N, Jacob VT, Bhat SV, Valecha N, Biswas S.

Bioorg Med Chem Lett. 2001 Sep 3;11(17):2269-72.

PMID:
11527712
12.

In vivo and in vitro antimalarial activity of 4-nerolidylcatechol.

Rocha E Silva LF, Silva Pinto AC, Pohlit AM, Quignard EL, Vieira PP, Tadei WP, Chaves FC, Samonek JF, Lima CA, Costa MR, Alecrim Md, Andrade-Neto VF.

Phytother Res. 2011 Aug;25(8):1181-8. doi: 10.1002/ptr.3424. Epub 2011 Feb 8.

PMID:
21302338
13.

Trisubstituted Pyrimidines as Efficacious and Fast-Acting Antimalarials.

Norcross NR, Baragaña B, Wilson C, Hallyburton I, Osuna-Cabello M, Norval S, Riley J, Stojanovski L, Simeons FR, Porzelle A, Grimaldi R, Wittlin S, Duffy S, Avery VM, Meister S, Sanz L, Jiménez-Díaz B, Angulo-Barturen I, Ferrer S, Martínez MS, Gamo FJ, Frearson JA, Gray DW, Fairlamb AH, Winzeler EA, Waterson D, Campbell SF, Willis P, Read KD, Gilbert IH.

J Med Chem. 2016 Jul 14;59(13):6101-20. doi: 10.1021/acs.jmedchem.6b00028. Epub 2016 Jun 17.

14.

The cytoplasmic prolyl-tRNA synthetase of the malaria parasite is a dual-stage target of febrifugine and its analogs.

Herman JD, Pepper LR, Cortese JF, Estiu G, Galinsky K, Zuzarte-Luis V, Derbyshire ER, Ribacke U, Lukens AK, Santos SA, Patel V, Clish CB, Sullivan WJ Jr, Zhou H, Bopp SE, Schimmel P, Lindquist S, Clardy J, Mota MM, Keller TL, Whitman M, Wiest O, Wirth DF, Mazitschek R.

Sci Transl Med. 2015 May 20;7(288):288ra77. doi: 10.1126/scitranslmed.aaa3575.

15.

Imidazolopiperazines: hit to lead optimization of new antimalarial agents.

Wu T, Nagle A, Kuhen K, Gagaring K, Borboa R, Francek C, Chen Z, Plouffe D, Goh A, Lakshminarayana SB, Wu J, Ang HQ, Zeng P, Kang ML, Tan W, Tan M, Ye N, Lin X, Caldwell C, Ek J, Skolnik S, Liu F, Wang J, Chang J, Li C, Hollenbeck T, Tuntland T, Isbell J, Fischli C, Brun R, Rottmann M, Dartois V, Keller T, Diagana T, Winzeler E, Glynne R, Tully DC, Chatterjee AK.

J Med Chem. 2011 Jul 28;54(14):5116-30. doi: 10.1021/jm2003359. Epub 2011 Jun 23.

PMID:
21644570
16.

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.

Antimicrob Agents Chemother. 2015 Feb;59(2):950-9. doi: 10.1128/AAC.04419-14. Epub 2014 Nov 24.

17.

Discovery of a Quinoline-4-carboxamide Derivative with a Novel Mechanism of Action, Multistage Antimalarial Activity, and Potent in Vivo Efficacy.

Baragaña B, Norcross NR, Wilson C, Porzelle A, Hallyburton I, Grimaldi R, Osuna-Cabello M, Norval S, Riley J, Stojanovski L, Simeons FR, Wyatt PG, Delves MJ, Meister S, Duffy S, Avery VM, Winzeler EA, Sinden RE, Wittlin S, Frearson JA, Gray DW, Fairlamb AH, Waterson D, Campbell SF, Willis P, Read KD, Gilbert IH.

J Med Chem. 2016 Nov 10;59(21):9672-9685. Epub 2016 Sep 10.

18.

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.

19.

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.

PMID:
26502160
20.

Urea/oxalamide tethered β-lactam-7-chloroquinoline conjugates: synthesis and in vitro antimalarial evaluation.

Singh P, Raj R, Singh P, Gut J, Rosenthal PJ, Kumar V.

Eur J Med Chem. 2014 Jan;71:128-34. doi: 10.1016/j.ejmech.2013.10.079. Epub 2013 Nov 9.

PMID:
24287561

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