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Items: 1 to 20 of 60

1.

Identification of a potential anti-malarial 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, Gonzalez Cabrera D, Younis Adam 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, Jimenez-Diaz MB, Martínez-Martínez MS, Ferrer-Bazaga S, Angulo-Barturen I, Meister S, Antonova-Koch Y, Winzeler EA, Street LJ, Chibale K.

J Med Chem. 2016 Oct 17. [Epub ahead of print]

PMID:
27748596
2.

Computer-Aided Drug Discovery Approaches against the Tropical Infectious Diseases Malaria, Tuberculosis, Trypanosomiasis, and Leishmaniasis.

Njogu PM, Guantai EM, Pavadai E, Chibale K.

ACS Infect Dis. 2016 Jan 8;2(1):8-31. doi: 10.1021/acsinfecdis.5b00093.

PMID:
27622945
3.

Identification of New Human Malaria Parasite Plasmodium falciparum Dihydroorotate Dehydrogenase Inhibitors by Pharmacophore and Structure-Based Virtual Screening.

Pavadai E, El Mazouni F, Wittlin S, de Kock C, Phillips MA, Chibale K.

J Chem Inf Model. 2016 Mar 28;56(3):548-62. doi: 10.1021/acs.jcim.5b00680.

PMID:
26915022
4.

Cyclopalladated organosilane-tethered thiosemicarbazones: novel strategies for improving antiplasmodial activity.

Adams M, Barnard L, de Kock C, Smith PJ, Wiesner L, Chibale K, Smith GS.

Dalton Trans. 2016 Apr 7;45(13):5514-20. doi: 10.1039/c5dt04918k.

PMID:
26911403
5.

Antiplasmodial activity, in vivo pharmacokinetics and anti-malarial efficacy evaluation of hydroxypyridinone hybrids in a mouse model.

Dambuza NS, Smith P, Evans A, Norman J, Taylor D, Andayi A, Egan T, Chibale K, Wiesner L.

Malar J. 2015 Dec 16;14:505. doi: 10.1186/s12936-015-1032-5.

6.

Antiplasmodial drug targets: a patent review (2000 - 2013).

Okombo J, Chibale K.

Expert Opin Ther Pat. 2016;26(1):107-30. doi: 10.1517/13543776.2016.1113258. Review.

PMID:
26566576
7.

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.

PMID:
26502160
8.

Characterisation of artemisinin-chloroquinoline hybrids for potential metabolic liabilities.

Thelingwani R, Leandersson C, Bonn B, Smith P, Chibale K, Masimirembwa C.

Xenobiotica. 2016;46(3):234-40. doi: 10.3109/00498254.2015.1070975.

PMID:
26338168
9.

Structure-Activity Relationship Studies of Orally Active Antimalarial 2,4-Diamino-thienopyrimidines.

Gonzàlez Cabrera D, Douelle F, Le Manach C, Han Z, Paquet T, Taylor D, Njoroge M, Lawrence N, Wiesner L, Waterson D, Witty MJ, Wittlin S, Street LJ, Chibale K.

J Med Chem. 2015 Sep 24;58(18):7572-9. doi: 10.1021/acs.jmedchem.5b01156.

PMID:
26322748
10.

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.

PMID:
26264839
11.

Primaquine-pyrimidine hybrids: synthesis and dual-stage antiplasmodial activity.

Kaur H, Machado M, de Kock C, Smith P, Chibale K, Prudêncio M, Singh K.

Eur J Med Chem. 2015 Aug 28;101:266-73. doi: 10.1016/j.ejmech.2015.06.045.

PMID:
26142491
12.

Ferrocene-pyrimidine conjugates: Synthesis, electrochemistry, physicochemical properties and antiplasmodial activities.

Chopra R, de Kock C, Smith P, Chibale K, Singh K.

Eur J Med Chem. 2015 Jul 15;100:1-9. doi: 10.1016/j.ejmech.2015.05.043.

PMID:
26057222
13.

Chloroquine-containing compounds: a patent review (2010 - 2014).

Njaria PM, Okombo J, Njuguna NM, Chibale K.

Expert Opin Ther Pat. 2015;25(9):1003-24. doi: 10.1517/13543776.2015.1050791. Review.

PMID:
26013494
14.

A Pharmacokinetic Study of Antimalarial 3,5-Diaryl-2-aminopyridine Derivatives.

Dambuza N, Smith P, Evans A, Taylor D, Chibale K, Wiesner L.

Malar Res Treat. 2015;2015:405962. doi: 10.1155/2015/405962.

15.

Synthesis of functionalized 3-, 5-, 6- and 8-aminoquinolines via intermediate (3-pyrrolin-1-yl)- and (2-oxopyrrolidin-1-yl)quinolines and evaluation of their antiplasmodial and antifungal activity.

Vandekerckhove S, Van Herreweghe S, Willems J, Danneels B, Desmet T, de Kock C, Smith PJ, Chibale K, D'hooghe M.

Eur J Med Chem. 2015 Mar 6;92:91-102. doi: 10.1016/j.ejmech.2014.12.020.

PMID:
25544689
16.

Structure-activity relationship studies of antiplasmodial aminomethylthiazoles.

Cheuka PM, Cabrera DG, Paquet T, Chibale K.

Bioorg Med Chem Lett. 2014 Nov 15;24(22):5207-11. doi: 10.1016/j.bmcl.2014.09.071.

PMID:
25316314
17.

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.

PMID:
25313449
18.

Physicochemical and drug metabolism characterization of a series of 4-aminoquinoline-3-hydroxypyridin-4-one hybrid molecules with antimalarial activity.

Thelingwani R, Bonn B, Chibale K, Masimirembwa C.

Expert Opin Drug Metab Toxicol. 2014 Oct;10(10):1313-24. doi: 10.1517/17425255.2014.954547.

PMID:
25219629
19.

Recent approaches to chemical discovery and development against malaria and the neglected tropical diseases human African trypanosomiasis and schistosomiasis.

Njoroge M, Njuguna NM, Mutai P, Ongarora DS, Smith PW, Chibale K.

Chem Rev. 2014 Nov 26;114(22):11138-63. doi: 10.1021/cr500098f. Review. No abstract available.

PMID:
25014712
20.

Synthesis and in vitro and in vivo pharmacological evaluation of new 4-aminoquinoline-based compounds.

Tukulula M, Njoroge M, Abay ET, Mugumbate GC, Wiesner L, Taylor D, Gibhard L, Norman J, Swart KJ, Gut J, Rosenthal PJ, Barteau S, Streckfuss J, Kameni-Tcheudji J, Chibale K.

ACS Med Chem Lett. 2013 Oct 1;4(12):1198-202. doi: 10.1021/ml400311r.

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