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Results: 1 to 20 of 127

1.

Novel orally active antimalarial thiazoles.

González Cabrera D, Douelle F, Feng TS, Nchinda AT, Younis Y, White KL, Wu Q, Ryan E, Burrows JN, Waterson D, Witty MJ, Wittlin S, Charman SA, Chibale K.

J Med Chem. 2011 Nov 10;54(21):7713-9. doi: 10.1021/jm201108k. Epub 2011 Oct 11.

PMID:
21966980
[PubMed - indexed for MEDLINE]
2.

3,5-Diaryl-2-aminopyridines as a novel class of orally active antimalarials demonstrating single dose cure in mice and clinical candidate potential.

Younis Y, Douelle F, Feng TS, González Cabrera D, Le Manach C, Nchinda AT, Duffy S, White KL, Shackleford DM, Morizzi J, Mannila J, Katneni K, Bhamidipati R, Zabiulla KM, Joseph JT, Bashyam S, Waterson D, Witty MJ, Hardick D, Wittlin S, Avery V, Charman SA, Chibale K.

J Med Chem. 2012 Apr 12;55(7):3479-87. doi: 10.1021/jm3001373. Epub 2012 Mar 21.

PMID:
22390538
[PubMed - indexed for MEDLINE]
3.

2,4-Diaminothienopyrimidines as orally active antimalarial agents.

González Cabrera D, Le Manach C, Douelle F, Younis Y, Feng TS, Paquet T, Nchinda AT, Street LJ, Taylor D, de Kock C, Wiesner L, Duffy S, White KL, Zabiulla KM, Sambandan Y, Bashyam S, Waterson D, Witty MJ, Charman SA, Avery VM, Wittlin S, Chibale K.

J Med Chem. 2014 Feb 13;57(3):1014-22. doi: 10.1021/jm401760c. Epub 2014 Jan 28.

PMID:
24446664
[PubMed - indexed for MEDLINE]
4.

Medicinal chemistry optimization of antiplasmodial imidazopyridazine hits from high throughput screening of a SoftFocus kinase library: part 1.

Le Manach C, Gonzàlez Cabrera D, Douelle F, Nchinda AT, Younis Y, Taylor D, Wiesner L, White KL, Ryan E, March C, Duffy S, Avery VM, Waterson D, Witty MJ, Wittlin S, Charman SA, Street LJ, Chibale K.

J Med Chem. 2014 Mar 27;57(6):2789-98. doi: 10.1021/jm500098s. Epub 2014 Mar 13.

PMID:
24568587
[PubMed - indexed for MEDLINE]
5.

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.

PMID:
23189922
[PubMed - indexed for MEDLINE]
6.

Antimalarial pyrido[1,2-a]benzimidazoles.

Ndakala AJ, Gessner RK, Gitari PW, October N, White KL, Hudson A, Fakorede F, Shackleford DM, Kaiser M, Yeates C, Charman SA, Chibale K.

J Med Chem. 2011 Jul 14;54(13):4581-9. doi: 10.1021/jm200227r. Epub 2011 Jun 16.

PMID:
21644541
[PubMed - indexed for MEDLINE]
7.

Antimalarial activity of phenylthiazolyl-bearing hydroxamate-based histone deacetylase inhibitors.

Dow GS, Chen Y, Andrews KT, Caridha D, Gerena L, Gettayacamin M, Johnson J, Li Q, Melendez V, Obaldia N 3rd, Tran TN, Kozikowski AP.

Antimicrob Agents Chemother. 2008 Oct;52(10):3467-77. doi: 10.1128/AAC.00439-08. Epub 2008 Jul 21.

PMID:
18644969
[PubMed - indexed for MEDLINE]
Free PMC Article
8.

Quinoline antimalarials containing a dibemethin group are active against chloroquinone-resistant Plasmodium falciparum and inhibit chloroquine transport via the P. falciparum chloroquine-resistance transporter (PfCRT).

Zishiri VK, Joshi MC, Hunter R, Chibale K, Smith PJ, Summers RL, Martin RE, Egan TJ.

J Med Chem. 2011 Oct 13;54(19):6956-68. doi: 10.1021/jm2009698. Epub 2011 Sep 13.

PMID:
21875063
[PubMed - indexed for MEDLINE]
9.

Synthesis of three classes of rhodacyanine dyes and evaluation of their in vitro and in vivo antimalarial activity.

Pudhom K, Kasai K, Terauchi H, Inoue H, Kaiser M, Brun R, Ihara M, Takasu K.

Bioorg Med Chem. 2006 Dec 15;14(24):8550-63. Epub 2006 Sep 12.

PMID:
16971131
[PubMed - indexed for MEDLINE]
10.

Synthesis and antimalarial efficacy of aza-fused rhodacyanines in vitro and in the P. berghei mouse model.

Takasu K, Pudhom K, Kaiser M, Brun R, Ihara M.

J Med Chem. 2006 Jul 27;49(15):4795-8.

PMID:
16854088
[PubMed - indexed for MEDLINE]
11.

Optimization of 4-aminoquinoline/clotrimazole-based hybrid antimalarials: further structure-activity relationships, in vivo studies, and preliminary toxicity profiling.

Gemma S, Camodeca C, Sanna Coccone S, Joshi BP, Bernetti M, Moretti V, Brogi S, Bonache de Marcos MC, Savini L, Taramelli D, Basilico N, Parapini S, Rottmann M, Brun R, Lamponi S, Caccia S, Guiso G, Summers RL, Martin RE, Saponara S, Gorelli B, Novellino E, Campiani G, Butini S.

J Med Chem. 2012 Aug 9;55(15):6948-67. doi: 10.1021/jm300802s. Epub 2012 Jul 27.

PMID:
22783984
[PubMed - indexed for MEDLINE]
12.

Pharmacological properties of a new antimalarial bisthiazolium salt, T3, and a corresponding prodrug, TE3.

Nicolas O, Margout D, Taudon N, Wein S, Calas M, Vial HJ, Bressolle FM.

Antimicrob Agents Chemother. 2005 Sep;49(9):3631-9.

PMID:
16127032
[PubMed - indexed for MEDLINE]
Free PMC Article
13.

Antimalarial activity of 9a-N substituted 15-membered azalides with improved in vitro and in vivo activity over azithromycin.

Perić M, Fajdetić A, Rupčić R, Alihodžić S, Ziher D, Bukvić Krajačić M, Smith KS, Ivezić-Schönfeld Z, Padovan J, Landek G, Jelić D, Hutinec A, Mesić M, Ager A, Ellis WY, Milhous WK, Ohrt C, Spaventi R.

J Med Chem. 2012 Feb 9;55(3):1389-401. doi: 10.1021/jm201615t. Epub 2012 Jan 25.

PMID:
22148880
[PubMed - indexed for MEDLINE]
14.

Structure-activity relationships of the antimalarial agent artemisinin. 7. Direct modification of (+)-artemisinin and in vivo antimalarial screening of new, potential preclinical antimalarial candidates.

Avery MA, Alvim-Gaston M, Vroman JA, Wu B, Ager A, Peters W, Robinson BL, Charman W.

J Med Chem. 2002 Sep 12;45(19):4321-35.

PMID:
12213073
[PubMed - indexed for MEDLINE]
15.

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.

PMID:
24099149
[PubMed - indexed for MEDLINE]
16.

Identification of a metabolically stable triazolopyrimidine-based dihydroorotate dehydrogenase inhibitor with antimalarial activity in mice.

Gujjar R, Marwaha A, El Mazouni F, White J, White KL, Creason S, Shackleford DM, Baldwin J, Charman WN, Buckner FS, Charman S, Rathod PK, Phillips MA.

J Med Chem. 2009 Apr 9;52(7):1864-72. doi: 10.1021/jm801343r.

PMID:
19296651
[PubMed - indexed for MEDLINE]
Free PMC Article
17.

Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.

O'Neill PM, Shone AE, Stanford D, Nixon G, Asadollahy E, Park BK, Maggs JL, Roberts P, Stocks PA, Biagini G, Bray PG, Davies J, Berry N, Hall C, Rimmer K, Winstanley PA, Hindley S, Bambal RB, Davis CB, Bates M, Gresham SL, Brigandi RA, Gomez-de-Las-Heras FM, Gargallo DV, Parapini S, Vivas L, Lander H, Taramelli D, Ward SA.

J Med Chem. 2009 Apr 9;52(7):1828-44. doi: 10.1021/jm8012757.

PMID:
19284751
[PubMed - indexed for MEDLINE]
18.

Synthesis and antimalarial property of orally active phenoxazinium salts.

Takasu K, Shimogama T, Satoh C, Kaiser M, Brun R, Ihara M.

J Med Chem. 2007 May 17;50(10):2281-4. Epub 2007 Apr 19.

PMID:
17441706
[PubMed - indexed for MEDLINE]
19.

Synthesis and evaluation of sulfonylurea derivatives as novel antimalarials.

León C, Rodrigues J, Gamboa de Domínguez N, Charris J, Gut J, Rosenthal PJ, Domínguez JN.

Eur J Med Chem. 2007 Jun;42(6):735-42. Epub 2007 Jan 14.

PMID:
17321641
[PubMed - indexed for MEDLINE]
20.

Identification, design and biological evaluation of bisaryl quinolones targeting Plasmodium falciparum type II NADH:quinone oxidoreductase (PfNDH2).

Pidathala C, Amewu R, Pacorel B, Nixon GL, Gibbons P, Hong WD, Leung SC, Berry NG, Sharma R, Stocks PA, Srivastava A, Shone AE, Charoensutthivarakul S, Taylor L, Berger O, Mbekeani A, Hill A, Fisher NE, Warman AJ, Biagini GA, Ward SA, O'Neill PM.

J Med Chem. 2012 Mar 8;55(5):1831-43. doi: 10.1021/jm201179h. Epub 2012 Feb 24.

PMID:
22364416
[PubMed - indexed for MEDLINE]
Free PMC Article

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