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Items: 1 to 20 of 247

1.

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.

2.

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.

3.

Characterization of Novel Antimalarial Compound ACT-451840: Preclinical Assessment of Activity and Dose-Efficacy Modeling.

Le Bihan A, de Kanter R, Angulo-Barturen I, Binkert C, Boss C, Brun R, Brunner R, Buchmann S, Burrows J, Dechering KJ, Delves M, Ewerling S, Ferrer S, Fischli C, Gamo-Benito FJ, Gnädig NF, Heidmann B, Jiménez-Díaz MB, Leroy D, Martínez MS, Meyer S, Moehrle JJ, Ng CL, Noviyanti R, Ruecker A, Sanz LM, Sauerwein RW, Scheurer C, Schleiferboeck S, Sinden R, Snyder C, Straimer J, Wirjanata G, Marfurt J, Price RN, Weller T, Fischli W, Fidock DA, Clozel M, Wittlin S.

PLoS Med. 2016 Oct 4;13(10):e1002138. doi: 10.1371/journal.pmed.1002138. eCollection 2016 Oct.

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.

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.

6.

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.

7.

Lysine acetylation in sexual stage malaria parasites is a target for antimalarial small molecules.

Trenholme K, Marek L, Duffy S, Pradel G, Fisher G, Hansen FK, Skinner-Adams TS, Butterworth A, Ngwa CJ, Moecking J, Goodman CD, McFadden GI, Sumanadasa SD, Fairlie DP, Avery VM, Kurz T, Andrews KT.

Antimicrob Agents Chemother. 2014 Jul;58(7):3666-78. doi: 10.1128/AAC.02721-13. Epub 2014 Apr 14.

8.

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.

9.

JPC-2997, a new aminomethylphenol with high in vitro and in vivo antimalarial activities against blood stages of Plasmodium.

Birrell GW, Chavchich M, Ager AL, Shieh HM, Heffernan GD, Zhao W, Krasucki PE, Saionz KW, Terpinski J, Schiehser GA, Jacobus LR, Shanks GD, Jacobus DP, Edstein MD.

Antimicrob Agents Chemother. 2015 Jan;59(1):170-7. doi: 10.1128/AAC.03762-14. Epub 2014 Oct 20.

10.
11.

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
12.

Antimalarial activity of 4-amidinoquinoline and 10-amidinobenzonaphthyridine derivatives.

Korotchenko V, Sathunuru R, Gerena L, Caridha D, Li Q, Kreishman-Deitrick M, Smith PL, Lin AJ.

J Med Chem. 2015 Apr 23;58(8):3411-31. doi: 10.1021/jm501809x. Epub 2015 Apr 9.

PMID:
25654185
13.

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
14.

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
15.

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.

PMID:
25007124
16.

One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites.

Diedrich D, Stenzel K, Hesping E, Antonova-Koch Y, Gebru T, Duffy S, Fisher G, Schöler A, Meister S, Kurz T, Avery VM, Winzeler EA, Held J, Andrews KT, Hansen FK.

Eur J Med Chem. 2018 Oct 5;158:801-813. doi: 10.1016/j.ejmech.2018.09.018. Epub 2018 Sep 7.

PMID:
30245402
17.

Novel inhibitor of Plasmodium histone deacetylase that cures P. berghei-infected mice.

Agbor-Enoh S, Seudieu C, Davidson E, Dritschilo A, Jung M.

Antimicrob Agents Chemother. 2009 May;53(5):1727-34. doi: 10.1128/AAC.00729-08. Epub 2009 Feb 17.

18.

Compounds from Sorindeia juglandifolia (Anacardiaceae) exhibit potent anti-plasmodial activities in vitro and in vivo.

Kamkumo RG, Ngoutane AM, Tchokouaha LR, Fokou PV, Madiesse EA, Legac J, Kezetas JJ, Lenta BN, Boyom FF, Dimo T, Mbacham WF, Gut J, Rosenthal PJ.

Malar J. 2012 Nov 21;11:382. doi: 10.1186/1475-2875-11-382.

19.

Hexahydroquinolines are antimalarial candidates with potent blood-stage and transmission-blocking activity.

Vanaerschot M, Lucantoni L, Li T, Combrinck JM, Ruecker A, Kumar TRS, Rubiano K, Ferreira PE, Siciliano G, Gulati S, Henrich PP, Ng CL, Murithi JM, Corey VC, Duffy S, Lieberman OJ, Veiga MI, Sinden RE, Alano P, Delves MJ, Lee Sim K, Winzeler EA, Egan TJ, Hoffman SL, Avery VM, Fidock DA.

Nat Microbiol. 2017 Oct;2(10):1403-1414. doi: 10.1038/s41564-017-0007-4. Epub 2017 Aug 14.

20.

Inhibitors of plasmodial serine hydroxymethyltransferase (SHMT): cocrystal structures of pyrazolopyrans with potent blood- and liver-stage activities.

Witschel MC, Rottmann M, Schwab A, Leartsakulpanich U, Chitnumsub P, Seet M, Tonazzi S, Schwertz G, Stelzer F, Mietzner T, McNamara C, Thater F, Freymond C, Jaruwat A, Pinthong C, Riangrungroj P, Oufir M, Hamburger M, Mäser P, Sanz-Alonso LM, Charman S, Wittlin S, Yuthavong Y, Chaiyen P, Diederich F.

J Med Chem. 2015 Apr 9;58(7):3117-30. doi: 10.1021/jm501987h. Epub 2015 Mar 18.

PMID:
25785478

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