Recent advances in malaria drug discovery

scientific article

Recent advances in malaria drug discovery is …
instance of (P31):
scholarly articleQ13442814

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P356DOI10.1016/J.BMCL.2013.03.067
P3181OpenCitations bibliographic resource ID2677504
P932PMC publication ID3762334
P698PubMed publication ID23587422
P5875ResearchGate publication ID236184061

P2093author name stringJutta Wanner
Karine G. Le Roch
Marco A. Biamonte
P2860cites workA new world malaria map: Plasmodium falciparum endemicity in 2010Q17485680
Global malaria mortality between 1980 and 2010: a systematic analysisQ20905423
Dihydroartemisinin/Piperaquine: a review of its use in the treatment of uncomplicated Plasmodium falciparum malariaeditQ21032449
Artemisinin resistance: current status and scenarios for containmentQ21032505
Artemisinin-resistant malaria: research challenges, opportunities, and public health implicationsQ21032532
Review of the clinical pharmacokinetics of artesunate and its active metabolite dihydroartemisinin following intravenous, intramuscular, oral or rectal administrationQ21034080
A review of malaria vaccine clinical projects based on the WHO rainbow tableQ21034112
A Concise Synthesis of (+)-ArtemisininQ22061915
Continuous-Flow Synthesis of the Anti-Malaria Drug ArtemisininQ22061979
Artemether-lumefantrine (six-dose regimen) for treating uncomplicated falciparum malariaQ24245437
Thousands of chemical starting points for antimalarial lead identificationQ24289329
Spiroindolones, a potent compound class for the treatment of malariaQ24606915
Drug screen targeted at Plasmodium liver stages identifies a potent multistage antimalarial drugQ24613311
Artesunate versus quinine in the treatment of severe falciparum malaria in African children (AQUAMAT): an open-label, randomised trialQ24630683
Methylene blue and serotonin toxicity: inhibition of monoamine oxidase A (MAO A) confirms a theoretical predictionQ24678060
Potent antimalarial 4-pyridones with improved physico-chemical propertiesQ84718196
New bis-thiazolium analogues as potential antimalarial agents: design, synthesis, and biological evaluationQ85841356
Prodrugs of bisthiazolium salts are orally potent antimalarialsQ37585368
A pre-emptive strike against malaria's stealthy hepatic formsQ37624398
Targeting the hypnozoite reservoir of Plasmodium vivax: the hidden obstacle to malaria eliminationQ37687630
Road towards new antimalarials - overview of the strategies and their chemical progressQ37823625
Therapeutic potential of boron-containing compoundsQ37855884
Target identification and validation of novel antimalarialsQ37894700
A toolbox to study liver stage malariaQ37947849
Back to the future: lessons learned in modern target-based and whole-cell lead optimization of antimalarials.Q37975527
Small molecule anti-malarial patents: a review (January 2010-June 2011).Q38018392
Recent results in protein kinase inhibition for tropical diseasesQ38051892
Plasmodium cell biology should inform strategies used in the development of antimalarial transmission-blocking drugsQ38066991
G6PD deficiency: global distribution, genetic variants and primaquine therapyQ38079323
Ketotifen is an antimalarial prodrug of norketotifen with blood schizonticidal and liver-stage efficacy.Q38465613
A single, low, oral dose of a 5-carbon-linked trioxane dimer orthoester plus mefloquine cures malaria-infected miceQ38480612
Public health: Death at the doorstepQ38868062
Identification of a new chemical class of antimalarialsQ38924120
Identification and In-Vitro ADME Assessment of a Series of Novel Anti-Malarial Agents Suitable for Hit-to-Lead ChemistryQ38982327
Benzoheterocyclic amodiaquine analogues with potent antiplasmodial activity: synthesis and pharmacological evaluationQ39322349
Antimalarial activity of pyrroloiminoquinones from the Australian marine sponge Zyzzya sp.Q39333451
Enhanced gametocyte production in Fansidar-treated Plasmodium falciparum malaria patients: implications for malaria transmission control programmesQ39371852
Design, synthesis, and in vitro activity of novel 2'-O-substituted 15-membered azalidesQ39387631
Antimalarial activity of 9a-N substituted 15-membered azalides with improved in vitro and in vivo activity over azithromycinQ39431851
Synthesis, antimalarial activity, and structure-activity relationship of 7-(2-phenoxyethoxy)-4(1H)-quinolonesQ39438178
Optimization of Potent Inhibitors of P. falciparum Dihydroorotate Dehydrogenase for the Treatment of MalariaQ39469622
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).Q39482802
Extracting SAR Information from a Large Collection of Anti-Malarial Screening Hits by NSG-SPT AnalysisQ39513261
Imidazolopiperazines: hit to lead optimization of new antimalarial agents.Q39530026
Antimalarial efficacy and drug interactions of the novel semi-synthetic endoperoxide artemisone in vitro and in vivo.Q39563304
Antimalarial histone deacetylase inhibitors containing cinnamate or NSAID componentsQ39588840
Synthesis and structure-activity relationships of novel benzoxaboroles as a new class of antimalarial agentsQ39613380
Spirotetrahydro beta-carbolines (spiroindolones): a new class of potent and orally efficacious compounds for the treatment of malaria.Q39616001
Identification, design and biological evaluation of heterocyclic quinolones targeting Plasmodium falciparum type II NADH:quinone oxidoreductase (PfNDH2).Q35958086
Liver-stage malaria parasites vulnerable to diverse chemical scaffoldsQ36001246
Transmission of malaria to mosquitoes blocked by bumped kinase inhibitorsQ36005409
The spiroindolone drug candidate NITD609 potently inhibits gametocytogenesis and blocks Plasmodium falciparum transmission to anopheles mosquito vectorQ36086489
Pharmacokinetics and pharmacodynamics of piperaquine in a murine malaria modelQ36422706
A combined transcriptome and proteome survey of malaria parasite liver stagesQ36423509
Perspective: artemisinin-resistant malaria and the wolfQ36450587
Counter perspective: artemisinin resistance: facts, fears, and fablesQ36450590
4(1H)-Quinolones with liver stage activity against Plasmodium berghei.Q36505423
First-in-man safety and pharmacokinetics of synthetic ozonide OZ439 demonstrates an improved exposure profile relative to other peroxide antimalarialsQ36573154
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screenQ36736936
The threat of artemisinin-resistant malariaQ37069786
Evaluation of artemisone combinations in Aotus monkeys infected with Plasmodium falciparumQ37274770
Artemisinin-naphthoquine combination (ARCO) therapy for uncomplicated falciparum malaria in adults of Papua New Guinea: a preliminary report on safety and efficacyQ37325659
Understanding the pharmacokinetics of CoartemQ37383289
Primaquine in vivax malaria: an update and review on management issuesQ27003856
Structure-Guided Lead Optimization of Triazolopyrimidine-Ring Substituents Identifies Potent Plasmodium falciparum Dihydroorotate Dehydrogenase Inhibitors with Clinical Candidate PotentialQ27670499
Malarial dihydrofolate reductase as a paradigm for drug development against a resistance-compromised targetQ27674154
Factors influencing the specificity of inhibitor binding to the human and malaria parasite dihydroorotate dehydrogenasesQ27679263
Imaging of Plasmodium Liver Stages to Drive Next-Generation Antimalarial Drug DiscoveryQ27861956
Thiostrepton and derivatives exhibit antimalarial and gametocytocidal activity by dually targeting parasite proteasome and apicoplastQ27973422
Glutathione reductase-catalyzed cascade of redox reactions to bioactivate potent antimalarial 1,4-naphthoquinones--a new strategy to combat malarial parasitesQ28241079
Targeting protein kinases in the malaria parasite: update of an antimalarial drug targetQ28257406
Glucose-6-phosphate dehydrogenase deficiencyQ28263721
Marine actinomycetes: a new source of compounds against the human malaria parasiteQ28472855
Establishment of an in vitro assay for assessing the effects of drugs on the liver stages of Plasmodium vivax malariaQ28476463
The next opportunity in anti-malaria drug discovery: the liver stageQ28477177
Towards an in vitro model of Plasmodium hypnozoites suitable for drug discoveryQ28477602
Integrated dataset of screening hits against multiple neglected disease pathogensQ28478485
The activities of current antimalarial drugs on the life cycle stages of Plasmodium: a comparative study with human and rodent parasitesQ28480979
Activity of clinically relevant antimalarial drugs on Plasmodium falciparum mature gametocytes in an ATP bioluminescence "transmission blocking" assayQ28482292
Discovery of gene function by expression profiling of the malaria parasite life cycleQ29547840
Chemical genetics of Plasmodium falciparumQ29617272
Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferaseQ33272939
A systematic approach to understand the mechanism of action of the bisthiazolium compound T4 on the human malaria parasite, Plasmodium falciparumQ33381401
Structure-activity relationships amongst 4-position quinoline methanol antimalarials that inhibit the growth of drug sensitive and resistant strains of Plasmodium falciparumQ33526131
A repurposing strategy identifies novel synergistic inhibitors of Plasmodium falciparum heat shock protein 90.Q33547134
Discovery of Novel Benzo[a]phenoxazine SSJ-183 as a Drug Candidate for MalariaQ33557946
An Invitation to Open Innovation in Malaria Drug Discovery: 47 Quality Starting Points from the TCAMSQ33598760
A Divergent SAR Study Allows Optimization of a Potent 5-HT2c Inhibitor to a Promising Antimalarial ScaffoldQ33630572
In vitro sensitivities of Plasmodium falciparum to different antimalarial drugs in UgandaQ33676088
Identification of inhibitors for putative malaria drug targets among novel antimalarial compoundsQ33682916
A research agenda for malaria eradication: cross-cutting issues for eradicationQ33808738
A Research Agenda to Underpin Malaria EradicationQ33818020
Aminoindoles, a novel scaffold with potent activity against Plasmodium falciparumQ33851108
Malaria gametocytogenesisQ33894262
Revisiting the circulation time of Plasmodium falciparum gametocytes: molecular detection methods to estimate the duration of gametocyte carriage and the effect of gametocytocidal drugsQ33898575
Pharmacological properties of a new antimalarial bisthiazolium salt, T3, and a corresponding prodrug, TE3.Q33935408
Structure-activity relationships of 4-position diamine quinoline methanols as intermittent preventative treatment (IPT) against Plasmodium falciparumQ33997571
Design and synthesis of small molecular dual inhibitor of falcipain-2 and dihydrofolate reductase as antimalarial agentQ39672806
Deciphering the Resistance-Counteracting Functions of Ferroquine in Plasmodium falciparum-Infected ErythrocytesQ39734520
New anti-malarial phenylpropanoid conjugated iridoids from Morinda morindoides.Q39740789
Synthesis and evaluation of phenylequine for antimalarial activity in vitro and in vivoQ39759075
Pharmacokinetics of piperaquine after repeated oral administration of the antimalarial combination CV8 in 12 healthy male subjectsQ40338733
Malaria-infected mice are completely cured by one 6 mg/kg oral dose of a new monomeric trioxane sulfide combined with mefloquineQ40369518
Efficacy of oral single dose therapy with artemisinin-naphthoquine phosphate in uncomplicated falciparum malariaQ40388919
A class of potent antimalarials and their specific accumulation in infected erythrocytesQ40750735
Plasmodium falciparum gametocytes: their longevity and infectivityQ40752602
The action of metabolic inhibitors on microgametogenesis in Plasmodium yoelii nigeriensisQ41776885
Chloroquine increases Plasmodium falciparum gametocytogenesis in vitro.Q41924042
Vaccines: The take-home lessonQ41929699
A new class of phenazines with activity against a chloroquine resistant Plasmodium falciparum strain and antimicrobial activityQ41932739
New imidazolidinedione derivatives as antimalarial agentsQ41933757
Bis-alkylamine quindolone derivatives as new antimalarial leadsQ41935132
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.Q41938916
Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st centuryQ41939096
Novel inhibitor of Plasmodium histone deacetylase that cures P. berghei-infected miceQ42098631
New approach for high-throughput screening of drug activity on Plasmodium liver stagesQ42121275
Transport and pharmacodynamics of albitiazolium, an antimalarial drug candidateQ42324155
Comparison and Optimization of Different Methods for the In Vitro Production of Plasmodium falciparum GametocytesQ42560487
Disulfide prodrugs of albitiazolium (T3/SAR97276): synthesis and biological activities.Q42718072
Evaluation of bis-alkylamidoxime O-alkylsulfonates as orally available antimalarials.Q42718584
Synthesis and in vitro antiprotozoal activities of 5-phenyliminobenzo[a]phenoxazine derivativesQ42727313
Synthesis, structure-activity relationship, and antimalarial activity of ureas and thioureas of 15-membered azalidesQ42743441
Potent antiprotozoal activity of a novel semi-synthetic berberine derivative.Q42743627
Synthesis and antimalarial assessment of a new series of orally active amino-functionalized spiro 1,2,4-trioxanesQ42862617
Endochin optimization: structure-activity and structure-property relationship studies of 3-substituted 2-methyl-4(1H)-quinolones with antimalarial activityQ42912336
Falcipain Inhibitors: Optimization Studies of the 2-Pyrimidinecarbonitrile Lead SeriesQ42951472
Exploration of potential prodrug approach of the bis-thiazolium salts T3 and T4 for orally delivered antimalarials.Q42982619
6-(4'-Aryloxy-phenyl)vinyl-1,2,4-trioxanes: a new series of orally active peroxides effective against multidrug-resistant Plasmodium yoelii in Swiss miceQ42991396
Editorial commentary: single-dose primaquine as gametocytocidal treatment in patients with uncomplicated falciparum malariaQ43149117
The comparative antimalarial properties of weak base and neutral synthetic ozonidesQ43229262
Synthesis and evaluation of hybrid bis-cationic salts as antimalarial drugs.Q43234703
Antiplasmodial activity of piperazine sulfonamidesQ43242186
Effects of antimalarial molecules on the gametocyte stage of Plasmodium falciparum: the debateQ43543088
Control of malariaQ44008732
Perspectives: The missing piecesQ44163652
A high-throughput assay for the identification of malarial transmission-blocking drugs and vaccinesQ44166008
Pyrimethamine-sulfadoxine resistance in Plasmodium falciparum must be delayed in AfricaQ44179422
In vivo efficacy of mefloquine for the treatment of Falciparum malaria in BrazilQ44597437
Antiplasmodial agents from the Bhutanese medicinal plant Corydalis calliantha.Q45983206
Novel bis- and tris-1,2,4-trioxanes: synthesis and antimalarial activity against multidrug-resistant Plasmodium yoelii in Swiss miceQ46249132
Discovery of novel 1H-imidazol-2-yl-pyrimidine-4,6-diamines as potential antimalarialsQ47946828
Determining the absolute configuration of (+)-mefloquine HCl, the side-effect-reducing enantiomer of the antimalaria drug LariamQ47996976
Linker-based hemisuccinate derivatives of artemisinin: synthesis and antimalarial assessment against multidrug-resistant Plasmodium yoelii nigeriensis in miceQ47998943
The numbers gameQ48007998
Drug development: Holding out for reinforcementsQ48008007
A pharmacokinetic approach to assess artemisinin-naphthoquine combination therapy for uncomplicated pediatric malariaQ48024466
Intersex effect of lamotrigine on the pharmacokinetic parameters of CDRI-97/78, a novel trioxane antimalarial compound, in rats.Q51346130
MalariaQ56767483
Broadly applicable synthesis of 1,2,4,5-tetraoxanesQ83100273
Benzoxaborole antimalarial agents. Part 2: Discovery of fluoro-substituted 7-(2-carboxyethyl)-1,3-dihydro-1-hydroxy-2,1-benzoxaborolesQ83239769
CoMSIA and POM analyses of anti-malarial activity of synthetic prodigininesQ84457169
Artemisone effective against murine cerebral malariaQ34084173
Heat shock protein 90: inhibitors in clinical trials.Q34091401
Assessment of azithromycin in combination with other antimalarial drugs against Plasmodium falciparum in vitroQ34111879
Diversity-Oriented Synthesis Yields a Novel Lead for the Treatment of MalariaQ34157359
Efficacy and safety of artemisinin-naphthoquine versus dihydroartemisinin-piperaquine in adult patients with uncomplicated malaria: a multi-centre study in IndonesiaQ34254961
Imidazolopiperazines: lead optimization of the second-generation antimalarial agentsQ34270117
Selective and specific inhibition of the plasmodium falciparum lysyl-tRNA synthetase by the fungal secondary metabolite cladosporinQ34306714
The global public health significance of Plasmodium vivax.Q34314657
Small-molecule histone methyltransferase inhibitors display rapid antimalarial activity against all blood stage forms in Plasmodium falciparumQ34421556
A class of tricyclic compounds blocking malaria parasite oocyst development and transmissionQ34467923
Pyrimethamine-sulfadoxine resistance in Plasmodium falciparum: what next?Q34470236
Whole-cell in vitro screening for gametocytocidal compoundsQ34509609
Targeting the ERAD pathway via inhibition of signal peptide peptidase for antiparasitic therapeutic designQ34510075
Vector control: The last biteQ34637816
A chemotype that inhibits three unrelated pathogenic targets: the botulinum neurotoxin serotype A light chain, P. falciparum malaria, and the Ebola filovirus.Q34665879
Synthetic ozonide drug candidate OZ439 offers new hope for a single-dose cure of uncomplicated malariaQ34693880
The structure-activity relationship of the antimalarial ozonide arterolane (OZ277).Q35013670
In vivo and in vitro antimalarial properties of azithromycin-chloroquine combinations that include the resistance reversal agent amlodipineQ35065754
Lead optimization of aryl and aralkyl amine-based triazolopyrimidine inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase with antimalarial activity in miceQ35071496
Antimalarial activity of the bisquinoline trans-N1,N2-bis (7-chloroquinolin-4-yl)cyclohexane-1,2-diamine: comparison of two stereoisomers and detailed evaluation of the S,S enantiomer, Ro 47-7737Q35134156
Radical curative efficacy of tafenoquine combination regimens in Plasmodium cynomolgi-infected Rhesus monkeys (Macaca mulatta)Q35181605
Discovery of novel alkylated (bis)urea and (bis)thiourea polyamine analogues with potent antimalarial activitiesQ35318393
Lead optimization of antimalarial propafenone analogues.Q35535315
A chemical genomic analysis of decoquinate, a Plasmodium falciparum cytochrome b inhibitorQ35563452
Quantitative assessment of Plasmodium falciparum sexual development reveals potent transmission-blocking activity by methylene blueQ35571456
Cyclopropyl carboxamides, a chemically novel class of antimalarial agents identified in a phenotypic screenQ35598598
Cytotoxic effect of curcumin on malaria parasite Plasmodium falciparum: inhibition of histone acetylation and generation of reactive oxygen speciesQ35635984
Adherence to a six-dose regimen of artemether-lumefantrine among uncomplicated Plasmodium falciparum patients in the Tigray Region, EthiopiaQ35642797
Febrifugine analogue compounds: synthesis and antimalarial evaluationQ35675211
Identification, design and biological evaluation of bisaryl quinolones targeting Plasmodium falciparum type II NADH:quinone oxidoreductase (PfNDH2).Q35814421
Artemisinin-naphthoquine combination therapy for uncomplicated pediatric malaria: a pharmacokinetic studyQ35941440
Artemisinin-naphthoquine combination therapy for uncomplicated pediatric malaria: a tolerability, safety, and preliminary efficacy studyQ35941455
Lead optimization of 3-carboxyl-4(1H)-quinolones to deliver orally bioavailable antimalarialsQ35951799
P433issue10
P407language of work or nameEnglishQ1860
P921main subjectdrug discoveryQ1418791
malariaQ12156
P304page(s)2829-43
P577publication date2013-05-15
P1433published inBioorganic & Medicinal Chemistry LettersQ2709483
P1476titleRecent advances in malaria drug discovery
P478volume23

Reverse relations

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