Compounds > oz 439
Page last updated: 2024-11-13

oz 439

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Description

artefenomel: an antimalarial ozonide; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID24999143
CHEMBL ID1828820
CHEMBL ID2322983
CHEMBL ID4061580
SCHEMBL ID12137235
SCHEMBL ID17971403
MeSH IDM0557645

Synonyms (32)

Synonym
artefenomel
oz-439
oz439
CHEMBL1828820
oz 439
artefenomel [inn]
morpholine, 4-(2-(4-cis-dispiro(cyclohexane-1,3'-(1,2,4)trioxolane-5',2''-tricyclo(3.3.1.1(sup 3,7))decan)-4-ylphenoxy)ethyl)-
unii-rik029813g
oz439 cpd
cis-adamantane-2-spiro-3'-8'-(4'-(2'-(4'-morpholinyl)ethoxy)phenyl)-1',2,'4'-trioxaspiro(4.5)decane
1029939-86-3
rik029813g ,
artefenomel [who-dd]
morpholine, 4-(2-(4-cis-dispiro(cyclohexane-1,3'-(1,2,4)trioxolane-5',2''-tricyclo(3.3.1.13,7)decan)-4-ylphenoxy)ethyl)-
4-(2-(4-(cis-dispiro(adamantane-2,3'-(1,2,4)trioxolane-5',1''-cyclohexane)-4''-yl)phenoxy)ethyl)morpholine
CHEMBL2322983
SCHEMBL12137235
SCHEMBL17971403
cis-4-[2-[4-(dispiro[cyclohexane-1,3'-[1,2,4]trioxolane-5',2''-tricyclo[3.3.1.1(3,7)]decan]-4-yl)phenoxy]ethyl]morpholine methanesulfonate;cis-4-[2-[4-(dispiro[cyclohexane-1,3'-[1,2,4]trioxolane-5',2''-tricyclo[3.3.1.1(3,7)]decan]-4-yl)phenoxy]ethyl]morph
DB11809
4-{2-{4-(cis-dispiro[adamantane-2,3'-[1,2,4]trioxolane- 5',1''-cyclohexane]-4''-yl)phenoxy]ethyl}morpholine
gtpl9971
SB19148
CHEMBL4061580
CS-0012378
HY-16762
Q27288132
MS-28689
1029939-86-3 (free base)
4-(2-(4-(dispiro[adamantane-2,3'-[1,2,4]trioxolane-5',1''-cyclohexan]-4''-yl)phenoxy)ethyl)morpholine
4-[2-(4-cis-dispiro[cyclohexane-1,3'-[1,2,4]trioxolane-5',2''-tricyclo[3.3.1.13,7]decan]-4-ylphenoxy)ethyl]-morpholine
AKOS040732470

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
"The safety and pharmacokinetic profile of OZ439 merits progression to phase 2a proof of concept studies in the target population of acute uncomplicated malaria."( First-in-man safety and pharmacokinetics of synthetic ozonide OZ439 demonstrates an improved exposure profile relative to other peroxide antimalarials.
Arbe-Barnes, S; Charman, SA; Craft, JC; Duparc, S; Gutierrez, M; Moehrle, JJ; Siethoff, C; van Giersbergen, PL; Vennerstrom, JL; Wittlin, S, 2013)		0.39

Bioavailability

ExcerptReferenceRelevance
" We have applied Flash NanoPrecipitation (FNP), a polymer-directed self-assembly process, to form stable, water-dispersible nanoparticles (NPs) of 50-400 nm in size containing OZ439, a poorly orally bioavailable but promising candidate for single-dose malaria treatment developed by Medicines for Malaria Venture (MMV)."( Encapsulation of OZ439 into Nanoparticles for Supersaturated Drug Release in Oral Malaria Therapy.
Dobrijevic, ELK; Feng, J; Lu, HD; McManus, SA; Mulhearn, WD; Patel, A; Prud'homme, RK; Ramachandruni, H; Ristroph, KD; Zhang, Y, 2018)		0.48
"Milk has been used as a vehicle for the delivery of antimalarial drugs during clinical trials to test for a food effect and artefenomel (OZ439) showed enhanced oral bioavailability with milk."( Interactions of Artefenomel (OZ439) with Milk during Digestion: Insights into Digestion-Driven Solubilization and Polymorphic Transformations.
Boyd, BJ; Clulow, AJ; Hawley, A; Khan, J; Ramachandruni, H; Ramirez, G; Salim, M, 2018)		0.48

Dosage Studied

ExcerptRelevanceReference
" Following dosing for 3 days, accumulation was less than two-fold but steady-state was not achieved."( First-in-man safety and pharmacokinetics of synthetic ozonide OZ439 demonstrates an improved exposure profile relative to other peroxide antimalarials.
Arbe-Barnes, S; Charman, SA; Craft, JC; Duparc, S; Gutierrez, M; Moehrle, JJ; Siethoff, C; van Giersbergen, PL; Vennerstrom, JL; Wittlin, S, 2013)		0.39
" While generally efficacious, ACTs and the first generation fully synthetic ozonide, arterolane (OZ277, 1), suffer from rapid clearance requiring 3-day dosing regimens."( Seeking the Elusive Long-Acting Ozonide: Discovery of Artefenomel (OZ439).
Guy, RK; Hammill, JT; Kim, HS, 2017)		0.46
"As part of its development, the new synthetic trioxolane antimalarial artefenomel (OZ439) was tested in rat whole embryo culture and in rat embryo-fetal toxicity studies with dosing throughout organogenesis or with a single dose on Gestational Day (GD) 12."( Improved safety margin for embryotoxicity in rats for the new endoperoxide artefenomel (OZ439) as compared to artesunate.
Andenmatten, N; Clark, RL; Clode, SA; Edwards, TL; Huber, AC; Kinney, J; Longo, M; Rhodes, J; Rückle, T; Walker, DK; Wells, T, 2018)		0.48
" The resistance issue is further exacerbated by a lack of patient adherence to multi-day dosing regimens."( Encapsulation of OZ439 into Nanoparticles for Supersaturated Drug Release in Oral Malaria Therapy.
Dobrijevic, ELK; Feng, J; Lu, HD; McManus, SA; Mulhearn, WD; Patel, A; Prud'homme, RK; Ramachandruni, H; Ristroph, KD; Zhang, Y, 2018)		0.48
" Mosquito feeding assays were conducted before artefenomel dosing to investigate parasite transmissibility."( Antimalarial Activity of Artefenomel Against Asexual Parasites and Transmissible Gametocytes During Experimental Blood-Stage Plasmodium vivax Infection.
Abd-Rahman, AN; Ballard, E; Chalon, S; Collins, KA; Gobeau, N; Griffin, P; Marquart, L; McCarthy, JS; Möhrle, JJ, 2022)		0.72
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (83)

Assay IDTitleYearJournalArticle
AID1440476In vivo antimalarial activity against Plasmodium berghei infected in albino mouse assessed as as protection against infection at 100 mg/kg, po single dose administered 96 hrs prior to infection2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID1440473In vivo antimalarial activity against Plasmodium berghei infected in albino mouse assessed as mouse survival at 100 mg/kg, po single dose administered 72 hrs prior to infection (Rvb = 6 to 7 days)2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID1457827Antiplasmodial activity against Plasmodium berghei infected in Swiss Webster mouse assessed as cure rate at 40 mg/kg/day administered for 1 day via oral gavage starting at 1 hr post infection measured after 30 days relative to control2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Enantioselective Synthesis and in Vivo Evaluation of Regioisomeric Analogues of the Antimalarial Arterolane.
AID1849705Antimalarial activity against Plasmodium falciparum K12021European journal of medicinal chemistry, Jan-15, Volume: 210An insight into the recent development of the clinical candidates for the treatment of malaria and their target proteins.
AID1440472In vivo antimalarial activity against Plasmodium berghei infected in albino mouse assessed as as protection against infection at 100 mg/kg, po single dose administered 48 hrs prior to infection2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID728696Dissociation constant, pKa of the compound2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Comparative antimalarial activities and ADME profiles of ozonides (1,2,4-trioxolanes) OZ277, OZ439, and their 1,2-dioxolane, 1,2,4-trioxane, and 1,2,4,5-tetraoxane isosteres.
AID728699Antimalarial activity against chloroquine-sensitive Plasmodium falciparum NF54 infected mouse assessed as survival at 30 mg/kg, po2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Comparative antimalarial activities and ADME profiles of ozonides (1,2,4-trioxolanes) OZ277, OZ439, and their 1,2-dioxolane, 1,2,4-trioxane, and 1,2,4,5-tetraoxane isosteres.
AID1440478Plasma concentration in rat at 300 mg/kg, po administered every third day for 5 doses measured after 2 weeks2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID748927Half life in Sprague-Dawley rat at 3 mg/kg, iv2013Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
Recent advances in malaria drug discovery.
AID1440481Plasma concentration in rat at 100 mg/kg, po administered every third day for 5 doses measured after 2 weeks2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID1440474In vivo antimalarial activity against Plasmodium berghei infected in albino mouse assessed as as protection against infection at 100 mg/kg, po single dose administered 72 hrs prior to infection2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID1440455In vivo antimalarial activity against Plasmodium berghei infected in albino mouse assessed as protection against infection at 30 mg/kg, po single dose administered 24 hrs prior to infection2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID1777168Solubility of the compound in FaSSIF2021ACS medicinal chemistry letters, Jul-08, Volume: 12, Issue:7
Enantioselective Synthesis and Profiling of Potent, Nonlinear Analogues of Antimalarial Tetraoxanes E209 and N205.
AID728691Plasma concentration in Swiss outbred mouse at 30 mg/kg, po at 24 hrs by LC-MS analysis2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Comparative antimalarial activities and ADME profiles of ozonides (1,2,4-trioxolanes) OZ277, OZ439, and their 1,2-dioxolane, 1,2,4-trioxane, and 1,2,4,5-tetraoxane isosteres.
AID1440466Kinetic solubility of the compound in water after 30 mins by nephelometric analysis2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID620220Chemical stability of the compound assessed as iron-mediated decomposition after 24 hrs by LC/MS analysis2011Journal of medicinal chemistry, Oct-13, Volume: 54, Issue:19
Comparison of the reactivity of antimalarial 1,2,4,5-tetraoxanes with 1,2,4-trioxolanes in the presence of ferrous iron salts, heme, and ferrous iron salts/phosphatidylcholine.
AID1440463Intrinsic clearance in mouse liver microsomes at 1 uM by LC/MS analysis2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID728698Antimalarial activity against chloroquine-sensitive Plasmodium falciparum NF54 infected mouse assessed as cured animal at 30 mg/kg, po measured on day 30 postinfection2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Comparative antimalarial activities and ADME profiles of ozonides (1,2,4-trioxolanes) OZ277, OZ439, and their 1,2-dioxolane, 1,2,4-trioxane, and 1,2,4,5-tetraoxane isosteres.
AID1457810Antiplasmodial activity against Plasmodium falciparum Cam3.2 infected in human RBC assessed as time required to reduce early ring stage parasite viability by 50% by SYTO 61-staining-based flow cytometry2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Enantioselective Synthesis and in Vivo Evaluation of Regioisomeric Analogues of the Antimalarial Arterolane.
AID728694Intrinsic clearance in mouse liver microsomes at 1 uM after 60 mins by LC-MS analysis2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Comparative antimalarial activities and ADME profiles of ozonides (1,2,4-trioxolanes) OZ277, OZ439, and their 1,2-dioxolane, 1,2,4-trioxane, and 1,2,4,5-tetraoxane isosteres.
AID1777165Intrinsic clearance in rat hepatocytes measured per 10^6 cells up to 120 mins by LC-MS analysis2021ACS medicinal chemistry letters, Jul-08, Volume: 12, Issue:7
Enantioselective Synthesis and Profiling of Potent, Nonlinear Analogues of Antimalarial Tetraoxanes E209 and N205.
AID1777166Intrinsic clearance in human liver microsome up to 30 mins by LC-MS analysis2021ACS medicinal chemistry letters, Jul-08, Volume: 12, Issue:7
Enantioselective Synthesis and Profiling of Potent, Nonlinear Analogues of Antimalarial Tetraoxanes E209 and N205.
AID1625277Half life in human2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
Antimalarial Chemotherapy: Natural Product Inspired Development of Preclinical and Clinical Candidates with Diverse Mechanisms of Action.
AID1440468Cmax in FVB mouse at 30 mg/kg, administered through oral gavage as single dose by LC-MS analysis2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID728700Antimalarial activity against chloroquine-sensitive Plasmodium falciparum NF54 infected mouse assessed as reduction in parasitemia at 30 mg/kg, po measured on day 3 postinfection relative to control2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Comparative antimalarial activities and ADME profiles of ozonides (1,2,4-trioxolanes) OZ277, OZ439, and their 1,2-dioxolane, 1,2,4-trioxane, and 1,2,4,5-tetraoxane isosteres.
AID1440475In vivo antimalarial activity against Plasmodium berghei infected in albino mouse assessed as mouse survival at 100 mg/kg, po single dose administered 96 hrs prior to infection (Rvb = 6 to 7 days)2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID1440484Toxicity in rat assessed as induction of mortality at 100 to 100 mg/kg, po administered every third day for 5 doses measured after 2 weeks2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID1457828Antiplasmodial activity against Plasmodium berghei infected in Swiss Webster mouse assessed as cure rate at 80 mg/kg/day administered for 1 day via oral gavage starting at 1 hr post infection measured after 30 days relative to control2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Enantioselective Synthesis and in Vivo Evaluation of Regioisomeric Analogues of the Antimalarial Arterolane.
AID1777175Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D72021ACS medicinal chemistry letters, Jul-08, Volume: 12, Issue:7
Enantioselective Synthesis and Profiling of Potent, Nonlinear Analogues of Antimalarial Tetraoxanes E209 and N205.
AID728692AUC (0 to 24 hrs) in mouse at 30 mg/kg, po by LC-MS analysis2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Comparative antimalarial activities and ADME profiles of ozonides (1,2,4-trioxolanes) OZ277, OZ439, and their 1,2-dioxolane, 1,2,4-trioxane, and 1,2,4,5-tetraoxane isosteres.
AID728697Partition coefficient, log P of the compound2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Comparative antimalarial activities and ADME profiles of ozonides (1,2,4-trioxolanes) OZ277, OZ439, and their 1,2-dioxolane, 1,2,4-trioxane, and 1,2,4,5-tetraoxane isosteres.
AID1849704Antimalarial activity against Plasmodium falciparum NF542021European journal of medicinal chemistry, Jan-15, Volume: 210An insight into the recent development of the clinical candidates for the treatment of malaria and their target proteins.
AID1777177Solubility of the compound in FaSSIF assessed as equilibrium pH2021ACS medicinal chemistry letters, Jul-08, Volume: 12, Issue:7
Enantioselective Synthesis and Profiling of Potent, Nonlinear Analogues of Antimalarial Tetraoxanes E209 and N205.
AID1440460In vivo antimalarial activity against Plasmodium berghei infected in NMRI albino mouse assessed as mean survival time at 30 mg/kg, po administered as single dose 1 day post infection2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID1440461In vivo antimalarial activity against Plasmodium berghei infected in albino mouse assessed as reduction in parasitemia at 30 mg/kg, po administered as single dose 1 day post infection and measured after 3 days post infection relative to control2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID728701Antimalarial activity against chloroquine-sensitive Plasmodium falciparum NF54 infected in mouse at 30 mg/kg, po2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Comparative antimalarial activities and ADME profiles of ozonides (1,2,4-trioxolanes) OZ277, OZ439, and their 1,2-dioxolane, 1,2,4-trioxane, and 1,2,4,5-tetraoxane isosteres.
AID1440459In vivo antimalarial activity against Plasmodium berghei infected in NMRI albino mouse assessed as parasitemia cured mouse at 30 mg/kg, po administered as single dose 1 day post infection measured after 30 days post infection2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID728695Lipophilicity, log D of the compound at pH 7.42013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Comparative antimalarial activities and ADME profiles of ozonides (1,2,4-trioxolanes) OZ277, OZ439, and their 1,2-dioxolane, 1,2,4-trioxane, and 1,2,4,5-tetraoxane isosteres.
AID728702Antimalarial activity against chloroquine-resistant Plasmodium falciparum K12013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Comparative antimalarial activities and ADME profiles of ozonides (1,2,4-trioxolanes) OZ277, OZ439, and their 1,2-dioxolane, 1,2,4-trioxane, and 1,2,4,5-tetraoxane isosteres.
AID1849700Dissociation constant, pKa of compound2021European journal of medicinal chemistry, Jan-15, Volume: 210An insight into the recent development of the clinical candidates for the treatment of malaria and their target proteins.
AID1440471In vivo antimalarial activity against Plasmodium berghei infected in albino mouse assessed as mouse survival at 30 mg/kg, po single dose administered 24 hrs prior to infection (Rvb = 6 to 7 days)2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID772516Antimalarial activity against mature gametocytic stage of Plasmodium falciparum assessed as inhibition of mature gamete exflagellation at 10 uM incubated for 24 hrs prior to exflagellation induction at 21 degC measured after 20 mins by microscopic analysi2013Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
Using genetic methods to define the targets of compounds with antimalarial activity.
AID748925Toxicity in po dosed Sprague-Dawley rat2013Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
Recent advances in malaria drug discovery.
AID1440457Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 assessed as reduction in [3H]-hypoxanthine incorporation preincubated for 24 hrs followed by [3H]-hypoxanthine addition measured after 18 hrs by liquid scintillation counting2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID1457833Antiplasmodial activity against Plasmodium falciparum Cam3.2_rev infected in human RBC assessed as time required to reduce early ring stage parasite viability by 50% by SYTO 61-staining-based flow cytometry2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Enantioselective Synthesis and in Vivo Evaluation of Regioisomeric Analogues of the Antimalarial Arterolane.
AID1777164Aqueous solubility of compound in PBS at pH 7.42021ACS medicinal chemistry letters, Jul-08, Volume: 12, Issue:7
Enantioselective Synthesis and Profiling of Potent, Nonlinear Analogues of Antimalarial Tetraoxanes E209 and N205.
AID748941Terminal half life in human2013Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
Recent advances in malaria drug discovery.
AID1579649Half life of compound2019Journal of medicinal chemistry, 12-12, Volume: 62, Issue:23
The Development Process for Discovery and Clinical Advancement of Modern Antimalarials.
AID1440464Intrinsic clearance in rat liver microsomes at 1 uM by LC/MS analysis2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID1440469Plasma concentration in FVB mouse at 30 mg/kg, administered through oral gavage as single dose measured after 48 hrs post dose by LC-MS analysis2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID1440470In vivo antimalarial activity against Plasmodium berghei infected in albino mouse assessed as mouse survival at 100 mg/kg, po single dose administered 48 hrs prior to infection (Rvb = 6 to 7 days)2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID728693Half life in mouse whole blood2013Journal of medicinal chemistry, Mar-28, Volume: 56, Issue:6
Comparative antimalarial activities and ADME profiles of ozonides (1,2,4-trioxolanes) OZ277, OZ439, and their 1,2-dioxolane, 1,2,4-trioxane, and 1,2,4,5-tetraoxane isosteres.
AID1440465Intrinsic clearance in dog liver microsomes at 1 uM by LC/MS analysis2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID1625266Oral bioavailability in rat at 3 mg/kg2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
Antimalarial Chemotherapy: Natural Product Inspired Development of Preclinical and Clinical Candidates with Diverse Mechanisms of Action.
AID748922Antimalarial activity against Plasmodium infected in mouse2013Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
Recent advances in malaria drug discovery.
AID1440456Toxicity in rat assessed as induction of mortality at 100 to 300 mg/kg, po administered every third day for 5 doses measured after 2 weeks2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID748928Antiplasmodial activity against Plasmodium falciparum2013Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
Recent advances in malaria drug discovery.
AID1440462Intrinsic clearance in human liver microsomes at 1 uM by LC/MS analysis2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID1440458Antimalarial activity against chloroquine-sensitive Plasmodium falciparum NF54 assessed as reduction in [3H]-hypoxanthine incorporation preincubated for 24 hrs followed by [3H]-hypoxanthine addition measured after 18 hrs by liquid scintillation counting2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID1440467AUC (0 to infinity) in FVB mouse at 30 mg/kg, administered through oral gavage as single dose by LC-MS analysis2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).
AID1625264Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 after 24 hrs in presence of hypoxanthine2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
Antimalarial Chemotherapy: Natural Product Inspired Development of Preclinical and Clinical Candidates with Diverse Mechanisms of Action.
AID1625265Antimalarial activity against GFP-transfected Plasmodium berghei ANKA infected in mouse assessed as reduction in parasitemia at 30 mg/kg, po administered on day 1 post infection measured on day 3 post infection2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
Antimalarial Chemotherapy: Natural Product Inspired Development of Preclinical and Clinical Candidates with Diverse Mechanisms of Action.
AID1496823Antimalarial activity against Plasmodium falciparum Pf3D70087/N9 infected in po dosed humanized NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ mouse assessed as reduction in parasitemia administered as single dose measured on day 7 post infection by SYTO-16 dye-based f2018Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
Synthesis and profiling of benzylmorpholine 1,2,4,5-tetraoxane analogue N205: Towards tetraoxane scaffolds with potential for single dose cure of malaria.
AID1496727Drug degradation in mouse liver microsomes assessed as compound half life at 5 uM by UPLC-MS method2018Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
Synthesis and profiling of benzylmorpholine 1,2,4,5-tetraoxane analogue N205: Towards tetraoxane scaffolds with potential for single dose cure of malaria.
AID1496710Half life in rat blood by LC-MS method2018Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
Synthesis and profiling of benzylmorpholine 1,2,4,5-tetraoxane analogue N205: Towards tetraoxane scaffolds with potential for single dose cure of malaria.
AID1496729Intrinsic clearance in human liver microsomes assessed per mg protein at 5 uM by UPLC-MS analysis2018Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
Synthesis and profiling of benzylmorpholine 1,2,4,5-tetraoxane analogue N205: Towards tetraoxane scaffolds with potential for single dose cure of malaria.
AID1496731Intrinsic clearance in rat liver microsomes assessed per mg protein at 5 uM by UPLC-MS analysis2018Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
Synthesis and profiling of benzylmorpholine 1,2,4,5-tetraoxane analogue N205: Towards tetraoxane scaffolds with potential for single dose cure of malaria.
AID1496730Intrinsic clearance in rat liver microsomes assessed per mg protein at 1 uM by UPLC-MS analysis2018Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
Synthesis and profiling of benzylmorpholine 1,2,4,5-tetraoxane analogue N205: Towards tetraoxane scaffolds with potential for single dose cure of malaria.
AID1496851Protein binding in human liver microsomes at 1 uM by ultracentrifugation method2018Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
Synthesis and profiling of benzylmorpholine 1,2,4,5-tetraoxane analogue N205: Towards tetraoxane scaffolds with potential for single dose cure of malaria.
AID1496824Antimalarial activity against Plasmodium falciparum Pf3D70087/N9 infected in po dosed humanized NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ mouse assessed as compound concentration in whole blood require to reduce parasitemia in peripheral blood by 90% administered 2018Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
Synthesis and profiling of benzylmorpholine 1,2,4,5-tetraoxane analogue N205: Towards tetraoxane scaffolds with potential for single dose cure of malaria.
AID1496725Drug degradation in rat liver microsomes assessed as compound half life at 5 uM by UPLC-MS method2018Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
Synthesis and profiling of benzylmorpholine 1,2,4,5-tetraoxane analogue N205: Towards tetraoxane scaffolds with potential for single dose cure of malaria.
AID1873042Antimalarial activity against chloroquine resistant Plasmodium falciparum K1 assessed as inhibition of parasite growth by [3H]-hypoxanthine incorporation assay2022European journal of medicinal chemistry, Jul-05, Volume: 237Spiral molecules with antimalarial activities: A review.
AID1496724Drug degradation in rat liver microsomes assessed as compound half life at 1 uM by UPLC-MS method2018Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
Synthesis and profiling of benzylmorpholine 1,2,4,5-tetraoxane analogue N205: Towards tetraoxane scaffolds with potential for single dose cure of malaria.
AID1496733Intrinsic clearance in mouse liver microsomes assessed per mg protein at 5 uM by UPLC-MS analysis2018Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
Synthesis and profiling of benzylmorpholine 1,2,4,5-tetraoxane analogue N205: Towards tetraoxane scaffolds with potential for single dose cure of malaria.
AID1496850Protein binding in human plasma at 2000 ng/ml after 6 hrs by equilibrium dialysis method2018Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
Synthesis and profiling of benzylmorpholine 1,2,4,5-tetraoxane analogue N205: Towards tetraoxane scaffolds with potential for single dose cure of malaria.
AID1496723Drug degradation in human liver microsomes assessed as compound half life at 5 uM by UPLC-MS method2018Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
Synthesis and profiling of benzylmorpholine 1,2,4,5-tetraoxane analogue N205: Towards tetraoxane scaffolds with potential for single dose cure of malaria.
AID1496712Antimalarial activity against Plasmodium berghei infected in mouse assessed as reduction in parasitemia at 30 mg/kg, po administered as single dose measured on day 3 relative to control2018Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
Synthesis and profiling of benzylmorpholine 1,2,4,5-tetraoxane analogue N205: Towards tetraoxane scaffolds with potential for single dose cure of malaria.
AID1496709Antimalarial activity against Plasmodium falciparum 3D7 infected in human erythrocytes after 48 hrs by SYBR Green I dye-based fluorescence assay2018Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
Synthesis and profiling of benzylmorpholine 1,2,4,5-tetraoxane analogue N205: Towards tetraoxane scaffolds with potential for single dose cure of malaria.
AID1496722Drug degradation in human liver microsomes assessed as compound half life at 1 uM by UPLC-MS method2018Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
Synthesis and profiling of benzylmorpholine 1,2,4,5-tetraoxane analogue N205: Towards tetraoxane scaffolds with potential for single dose cure of malaria.
AID1496728Intrinsic clearance in human liver microsomes assessed per mg protein at 1 uM by UPLC-MS analysis2018Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
Synthesis and profiling of benzylmorpholine 1,2,4,5-tetraoxane analogue N205: Towards tetraoxane scaffolds with potential for single dose cure of malaria.
AID1873043Antimalarial activity against chloroquine sensitive Plasmodium falciparum NF54 assessed as inhibition of parasite growth by [3H]-hypoxanthine incorporation assay2022European journal of medicinal chemistry, Jul-05, Volume: 237Spiral molecules with antimalarial activities: A review.
AID1496713Antimalarial activity against Plasmodium berghei infected in mouse assessed as mouse mean survival days at 30 mg/kg, po administered as single dose2018Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
Synthesis and profiling of benzylmorpholine 1,2,4,5-tetraoxane analogue N205: Towards tetraoxane scaffolds with potential for single dose cure of malaria.
AID1810306Invivo antimalarial activity against Plasmodium berghei at 20 mg/kg, po administered as single dose in presence of ferroquine2021Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10
Aminoalkoxycarbonyloxymethyl Ether Prodrugs with a pH-Triggered Release Mechanism: A Case Study Improving the Solubility, Bioavailability, and Efficacy of Antimalarial 4(1
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (46)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's33 (71.74)24.3611
2020's13 (28.26)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 10.57

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index10.57 (24.57)
Research Supply Index4.03 (2.92)
Research Growth Index4.60 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.57)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials9 (19.57%)5.53%
Reviews7 (15.22%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other30 (65.22%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
fosmidomycin
fosmidomycin: from Streptomyces lavendulae; RN given refers to parent cpd; structure in second source. fosmidomycin : Propylphosphonic acid in which one of the hydrogens at position 3 is substituted by a formyl(hydroxy)amino group. An antibiotic obtained from Streptomyces lavendulae, it specifically inhibits DXP reductoisomerase (EC 1.1.1.267), a key enzyme in the non-mevalonate pathway of isoprenoid biosynthesis.		3.2310hydroxamic acid;
phosphonic acids		antimicrobial agent;
bacterial metabolite;
EC 1.1.1.267 (1-deoxy-D-xylulose-5-phosphate reductoisomerase) inhibitor
formaldehyde
paraform: polymerized formaldehyde; RN given refers to parent cpd; used in root canal therapy		2.3110aldehyde;
one-carbon compound		allergen;
carcinogenic agent;
disinfectant;
EC 3.5.1.4 (amidase) inhibitor;
environmental contaminant;
Escherichia coli metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
albendazole
[no description available]		2.3110aryl sulfide;
benzimidazoles;
benzimidazolylcarbamate fungicide;
carbamate ester		anthelminthic drug;
microtubule-destabilising agent;
tubulin modulator
amiodarone
Amiodarone: An antianginal and class III antiarrhythmic drug. It increases the duration of ventricular and atrial muscle action by inhibiting POTASSIUM CHANNELS and VOLTAGE-GATED SODIUM CHANNELS. There is a resulting decrease in heart rate and in vascular resistance.. amiodarone : A member of the class of 1-benzofurans that is 1-benzofuran substituted by a butyl group at position 2 and a 4-[2-(diethylamino)ethoxy]-3,5-diiodobenzoyl group at position 3. It is a cardiovascular drug used for the treatment of cardiac dysrhythmias.		2.15101-benzofurans;
aromatic ketone;
organoiodine compound;
tertiary amino compound		cardiovascular drug
amodiaquine
Amodiaquine: A 4-aminoquinoline compound with anti-inflammatory properties.. amodiaquine : A quinoline having a chloro group at the 7-position and an aryl amino group at the 4-position.		5.1831aminoquinoline;
organochlorine compound;
phenols;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antimalarial;
drug allergen;
EC 2.1.1.8 (histamine N-methyltransferase) inhibitor;
non-steroidal anti-inflammatory drug;
prodrug
carbamazepine
Carbamazepine: A dibenzazepine that acts as a sodium channel blocker. It is used as an anticonvulsant for the treatment of grand mal and psychomotor or focal SEIZURES. It may also be used in the management of BIPOLAR DISORDER, and has analgesic properties.. carbamazepine : A dibenzoazepine that is 5H-dibenzo[b,f]azepine carrying a carbamoyl substituent at the azepine nitrogen, used as an anticonvulsant.		2.3110dibenzoazepine;
ureas		analgesic;
anticonvulsant;
antimanic drug;
drug allergen;
EC 3.5.1.98 (histone deacetylase) inhibitor;
environmental contaminant;
glutamate transporter activator;
mitogen;
non-narcotic analgesic;
sodium channel blocker;
xenobiotic
chloroquine
Chloroquine: The prototypical antimalarial agent with a mechanism that is not well understood. It has also been used to treat rheumatoid arthritis, systemic lupus erythematosus, and in the systemic therapy of amebic liver abscesses.. chloroquine : An aminoquinoline that is quinoline which is substituted at position 4 by a [5-(diethylamino)pentan-2-yl]amino group at at position 7 by chlorine. It is used for the treatment of malaria, hepatic amoebiasis, lupus erythematosus, light-sensitive skin eruptions, and rheumatoid arthritis.		5.2880aminoquinoline;
organochlorine compound;
secondary amino compound;
tertiary amino compound		anticoronaviral agent;
antimalarial;
antirheumatic drug;
autophagy inhibitor;
dermatologic drug
diclofenac
Diclofenac: A non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt.. diclofenac : A monocarboxylic acid consisting of phenylacetic acid having a (2,6-dichlorophenyl)amino group at the 2-position.		2.1510amino acid;
aromatic amine;
dichlorobenzene;
monocarboxylic acid;
secondary amino compound		antipyretic;
drug allergen;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic
furafylline
[no description available]		2.1710oxopurine
ketoconazole
1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine : A dioxolane that is 1,3-dioxolane which is substituted at positions 2, 2, and 4 by imidazol-1-ylmethyl, 2,4-dichlorophenyl, and [para-(4-acetylpiperazin-1-yl)phenoxy]methyl groups, respectively.		2.1710dichlorobenzene;
dioxolane;
ether;
imidazoles;
N-acylpiperazine;
N-arylpiperazine
midazolam
Midazolam: A short-acting hypnotic-sedative drug with anxiolytic and amnestic properties. It is used in dentistry, cardiac surgery, endoscopic procedures, as preanesthetic medication, and as an adjunct to local anesthesia. The short duration and cardiorespiratory stability makes it useful in poor-risk, elderly, and cardiac patients. It is water-soluble at pH less than 4 and lipid-soluble at physiological pH.. midazolam : An imidazobenzodiazepine that is 4H-imidazo[1,5-a][1,4]benzodiazepine which is substituted by a methyl, 2-fluorophenyl and chloro groups at positions 1, 6 and 8, respectively.		2.1510imidazobenzodiazepine;
monofluorobenzenes;
organochlorine compound		anticonvulsant;
antineoplastic agent;
anxiolytic drug;
apoptosis inducer;
central nervous system depressant;
GABAA receptor agonist;
general anaesthetic;
muscle relaxant;
sedative
primaquine
Primaquine: An aminoquinoline that is given by mouth to produce a radical cure and prevent relapse of vivax and ovale malarias following treatment with a blood schizontocide. It has also been used to prevent transmission of falciparum malaria by those returning to areas where there is a potential for re-introduction of malaria. Adverse effects include anemias and GI disturbances. (From Martindale, The Extra Pharmacopeia, 30th ed, p404). primaquine : An N-substituted diamine that is pentane-1,4-diamine substituted by a 6-methoxyquinolin-8-yl group at the N(4) position. It is a drug used in the treatment of malaria and Pneumocystis pneumonia.		8.5172aminoquinoline;
aromatic ether;
N-substituted diamine		antimalarial
pyrimethamine
Maloprim: contains above 2 cpds		4.4430aminopyrimidine;
monochlorobenzenes		antimalarial;
antiprotozoal drug;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor
sulfaphenazole
Sulfaphenazole: A sulfonilamide anti-infective agent.. sulfaphenazole : A sulfonamide that is sulfanilamide in which the sulfonamide nitrogen is substituted by a 1-phenyl-1H-pyrazol-5-yl group. It is a selective inhibitor of cytochrome P450 (CYP) 2C9 isozyme, and antibacterial agent.		2.1710primary amino compound;
pyrazoles;
substituted aniline;
sulfonamide antibiotic;
sulfonamide		antibacterial drug;
EC 1.14.13.181 (13-deoxydaunorubicin hydroxylase) inhibitor;
EC 1.14.13.67 (quinine 3-monooxygenase) inhibitor;
P450 inhibitor
methylene blue
Methylene Blue: A compound consisting of dark green crystals or crystalline powder, having a bronze-like luster. Solutions in water or alcohol have a deep blue color. Methylene blue is used as a bacteriologic stain and as an indicator. It inhibits GUANYLATE CYCLASE, and has been used to treat cyanide poisoning and to lower levels of METHEMOGLOBIN.. methylene blue : An organic chloride salt having 3,7-bis(dimethylamino)phenothiazin-5-ium as the counterion. A commonly used dye that also exhibits antioxidant, antimalarial, antidepressant and cardioprotective properties.		3.1810organic chloride saltacid-base indicator;
antidepressant;
antimalarial;
antimicrobial agent;
antioxidant;
cardioprotective agent;
EC 1.4.3.4 (monoamine oxidase) inhibitor;
EC 3.1.1.8 (cholinesterase) inhibitor;
EC 4.6.1.2 (guanylate cyclase) inhibitor;
fluorochrome;
histological dye;
neuroprotective agent;
physical tracer
cycloguanil
cycloguanil: the active metabolite of proguanil; antifolate drug; structure in first source. cycloguanil : A triazine in which a 1,6-dihydro-1,3,5-triazine ring is substituted at N-1 by a 4-chlorophenyl group, at C-2 and -4 by amino groups and at C-6 by gem-dimethyl groups. A dihydrofolate reductase inhibitor, it is a metabolite of the antimalarial drug proguanil.		3.1810triazinesantifolate;
antiinfective agent;
antimalarial;
antiparasitic agent;
antiprotozoal drug;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor
adamantane
Adamantane: A tricyclo bridged hydrocarbon.		11.84328adamantanes;
polycyclic alkane
pamaquine
pamaquine: structure; RN given refers to parent cpd		3.4110aminoquinoline
alpha-aminopyridine
alpha-aminopyridine: RN given refers to parent cpd; structure in Merck Index, 9th ed, #485. aminopyridine : Compounds containing a pyridine skeleton substituted by one or more amine groups.		2.2510
erythromycin
Erythromycin: A bacteriostatic antibiotic macrolide produced by Streptomyces erythreus. Erythromycin A is considered its major active component. In sensitive organisms, it inhibits protein synthesis by binding to 50S ribosomal subunits. This binding process inhibits peptidyl transferase activity and interferes with translocation of amino acids during translation and assembly of proteins.. erythromycin : Any of several wide-spectrum macrolide antibiotics obtained from actinomycete Saccharopolyspora erythraea (formerly known as Streptomyces erythraeus).. erythromycin A : An erythromycin that consists of erythronolide A having 2,6-dideoxy-3-C-methyl-3-O-methyl-alpha-L-ribo-hexopyranosyl and 3,4,6-trideoxy-3-(dimethylamino)-beta-D-xylo-hexopyranosyl residues attahced at positions 4 and 6 respectively.		3.2310cyclic ketone;
erythromycin
formal glycol
[no description available]		2.0810cyclic acetal;
dioxolane
sulfadoxine
Sulfadoxine: A long acting sulfonamide that is used, usually in combination with other drugs, for respiratory, urinary tract, and malarial infections.. sulfadoxine : A sulfonamide consisting of pyrimidine having methoxy substituents at the 5- and 6-positions and a 4-aminobenzenesulfonamido group at the 4-position. In combination with the antiprotozoal pyrimethamine (CHEBI:8673) it is used as an antimalarial.		3.1810pyrimidines;
sulfonamide		antibacterial drug;
antimalarial
pentaquine
pentaquine: RN given refers to parent cpd		3.4110
decoquinate
Decoquinate: A coccidiostat for poultry.		3.1810
mefloquine
(-)-(11S,2'R)-erythro-mefloquine : An optically active form of [2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol having (-)-(11S,2'R)-erythro-configuration. An antimalarial agent, used in racemic form, which acts as a blood schizonticide; its mechanism of action is unknown.		5.1550[2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanolantimalarial
triazoles
Triazoles: Heterocyclic compounds containing a five-membered ring with two carbon atoms and three nitrogen atoms with the molecular formula C2H3N3.. triazoles : An azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms.		5.18311,2,3-triazole
artemisinin
(+)-artemisinin : A sesquiterpene lactone obtained from sweet wormwood, Artemisia annua, which is used as an antimalarial for the treatment of multi-drug resistant strains of falciparum malaria.		3.0340organic peroxide;
sesquiterpene lactone		antimalarial;
plant metabolite
artemether
Artemether: An artemisinin derivative that is used in the treatment of MALARIA.. artemether : An artemisinin derivative that is artemisinin in which the lactone has been converted to the corresponding lactol methyl ether. It is used in combination with lumefantrine as an antimalarial for the treatment of multi-drug resistant strains of falciparum malaria.		7.1351artemisinin derivative;
cyclic acetal;
organic peroxide;
semisynthetic derivative;
sesquiterpenoid		antimalarial
quinocide
quinocide: Russian drug; RN given refers to parent cpd; structure		3.4110
coptisine
coptisine: RN given refers to parent cpd		3.4110alkaloidmetabolite
atovaquone
Atovaquone: A hydroxynaphthoquinone that has antimicrobial activity and is being used in antimalarial protocols.. atovaquone : A naphthoquinone compound having a 4-(4-chlorophenyl)cyclohexyl group at the 2-position and a hydroxy substituent at the 3-position.		4.4430hydroxy-1,2-naphthoquinone
s 53482
flumioxazin : A benzoxazine that is N-(prop-2-yn-1-yl)-2H-1,4-benzoxazin-3(4H)-one which is substituted at position 6 by a 1,3-dioxo-1,3,4,5,6,7-hexahydro-2H-isoindol-2-yl group and at position 7 by a fluorine. A protoporphyrinogen oxidase inhibitor, it is used for the control of weeds in soya, peanuts, and a variety of vegetable and fruit crops.		2.1710benzoxazine;
dicarboximide;
organofluorine compound;
terminal acetylenic compound		agrochemical;
EC 1.3.3.4 (protoporphyrinogen oxidase) inhibitor;
herbicide;
teratogenic agent
artesunic acid
[no description available]		5.1531
pyronaridine
[no description available]		3.1810aminoquinoline
tafenoquine
tafenoquine : A racemate comprising equimolar amounts of (R)- and (S)-tafenoquine.. N(4)-{2,6-dimethoxy-4-methyl-5-[3-(trifluoromethyl)phenoxy]quinolin-8-yl}pentane-1,4-diamine : An aminoquinoline that is 8-aminoquinoline which is substituted by methoxy groups at positions 2 and 6, a methyl group at position 4, and a m-(trifluoromethyl)phenoxy group at position 5, and in which the amino substituent at position 8 is itself substituted by a 5-aminopentan-2-yl group.		3.1810(trifluoromethyl)benzenes;
aminoquinoline;
aromatic ether;
primary amino compound;
secondary amino compound
piperaquine
piperaquine : An aminoquinoline that is 1,3-di(piperazin-1-yl)propane in which the nitrogen at position 4 of each of the piperazine moieties is replaced by a 7-chloroquinolin-4-yl group.		9.9694aminoquinoline;
N-arylpiperazine;
organochlorine compound		antimalarial
3-(n-acetyl-n-hydroxy)aminopropylphosphonic acid
3-(N-acetyl-N-hydroxy)aminopropylphosphonic acid: from Streptomyces rubellomurinus sp. nov.; interferes with bacterial cell wall synthesis; structure in first source		3.2310phosphonoacetic acid
speciophylline
speciophylline: RN refers to (3beta,7alpha,19alpha,20alpha)-isomer; from leaves of Mitragyna inermis (Rubiaceae); structure given in first source		3.5110indolizines
erysodine
erysodine: structure given in first source. erysodine : An erythrina alkaloid with formula C18H21NO3 isolated from several erythrina plant species. It is a competitive antagonist of nicotinic acetylcholine receptors and exhibits antiparasitic and insecticidal activities.		3.5110aromatic ether;
diether;
Erythrina alkaloid;
organic heterotetracyclic compound;
phenols		antiparasitic agent;
nicotinic antagonist;
phytogenic insecticide
quinidine
Quinidine: An optical isomer of quinine, extracted from the bark of the CHINCHONA tree and similar plant species. This alkaloid dampens the excitability of cardiac and skeletal muscles by blocking sodium and potassium currents across cellular membranes. It prolongs cellular ACTION POTENTIALS, and decreases automaticity. Quinidine also blocks muscarinic and alpha-adrenergic neurotransmission.. quinidine : A cinchona alkaloid consisting of cinchonine with the hydrogen at the 6-position of the quinoline ring substituted by methoxy.		2.1710cinchona alkaloidalpha-adrenergic antagonist;
anti-arrhythmia drug;
antimalarial;
drug allergen;
EC 1.14.13.181 (13-deoxydaunorubicin hydroxylase) inhibitor;
EC 3.6.3.44 (xenobiotic-transporting ATPase) inhibitor;
muscarinic antagonist;
P450 inhibitor;
potassium channel blocker;
sodium channel blocker
clindamycin
Clindamycin: An antibacterial agent that is a semisynthetic analog of LINCOMYCIN.. clindamycin : A carbohydrate-containing antibiotic that is the semisynthetic derivative of lincomycin, a natural antibiotic.		3.2310
zithromax
Azithromycin: A semi-synthetic macrolide antibiotic structurally related to ERYTHROMYCIN. It has been used in the treatment of Mycobacterium avium intracellulare infections, toxoplasmosis, and cryptosporidiosis.. azithromycin : A macrolide antibiotic useful for the treatment of bacterial infections.		3.2310macrolide antibioticantibacterial drug;
environmental contaminant;
xenobiotic
artenimol
[no description available]		4.2840
quinine
[no description available]		3.1810cinchona alkaloidantimalarial;
muscle relaxant;
non-narcotic analgesic
erysovine
erysovine: antifeedant from Chinese medicinal herb, Erythrina variegata var. orientalis, against maize weevil Sitophilus zeamais; structure in first source		3.5110
erythraline
erythraline: isolated from Erythrina crista-galli; structure in first source		3.5110alkaloid
proguanil
Proguanil: A biguanide compound which metabolizes in the body to form cycloguanil, an anti-malaria agent.. proguanil : A biguanide compound which has isopropyl and p-chlorophenyl substituents on the terminal N atoms. A prophylactic antimalarial drug, it works by inhibiting the enzyme dihydrofolate reductase, which is involved in the reproduction of the malaria parasites Plasmodium falciparum and P. vivax within the red blood cells.		3.1810biguanides;
monochlorobenzenes		antimalarial;
antiprotozoal drug;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor
lumefantrine
Lumefantrine: A fluorene derivative that is used in combination with ARTEMETHER for the treatment of MALARIA (see ARTEMETHER-LUMEFANTRINE DRUG COMBINATION).. lumefantrine : A member of the class of fluorenes that is 9-(p-chlorobenzylidene)-9H-fluorene which is substitutec by chlorine at positions 2 and 7, and by a 2-(dibutylamino)-1-hydroxyethyl group at position 4. An antimalarial drug used in combination with artemether for the treatment of multi-drug resistant strains of falciparum malaria.		3.620fluorenes;
monochlorobenzenes;
secondary alcohol;
tertiary amine		antimalarial
cgp-56697
Artemether, Lumefantrine Drug Combination: Drug combination of artemether and lumefantrine that is used to treat PLASMODIUM FALCIPARUM MALARIA.		4.7211
artesunate
artesunic acid: RN given for (3R-(3alpha,5abeta,6beta,8abeta,9alpha,10alpha,12beta,(2aR*))-isomer; succinic ester of artemether		4.6240artemisinin derivative;
cyclic acetal;
dicarboxylic acid monoester;
hemisuccinate;
semisynthetic derivative;
sesquiterpenoid		antimalarial;
antineoplastic agent;
ferroptosis inducer
mer nf5003f
stachybotrydial: a pancreatic cholesterol esterase inhibitor; also inhibits fucosyltransferase and sialyltransferase; structure in first source		3.5110
1,2,6,7-tetraoxaspiro(7.11)nonadecane
1,2,6,7-tetraoxaspiro(7.11)nonadecane: structure in first source		3.5110
artenimol
artenimol: derivative of antimalarial drug artemisinin (quinghaosu)		4.6140
aculeatin a
aculeatin A: antineoplastic from Amomum aculeatum; structure in first source		3.5110
arterolane
arterolane: a trioxolane with antimalarial activity; structure in first source. arterolane : An oxaspiro compound that is dispiro[cyclohexane-1,3'-[1,2,4]trioxolane-5',2''-tricyclo[3.3.1.1(3,7)]decane] substituted by a 2-[(2-amino-2-methylpropyl)amino]-2-oxoethyl group at position 4s. Its maleic acid salt is used as an antimalarial drug in combination with piperaquine.		6.41150
marizomib
marizomib: a proteasome inhibitor from a marine bacterium Salinospora; structure in first source		3.1810beta-lactone;
gamma-lactam;
organic heterobicyclic compound;
organochlorine compound;
salinosporamide		antineoplastic agent;
proteasome inhibitor
artemisone
artemisone: second-generation semi-synthetic artemisinin derivative for antimalarial therapy devoid of neurotoxicity		3.5820
cladosporin
cladosporin: antifungal metabolite from Cladosporium cladosporioides; toxic, minor metabolite of Aspersillus flavus; inhibits tRNA synthetase in Plasmodium falciparum		3.1810
amodiaquine hydrochloride
[no description available]		4.120
1,2,4-trioxane
1,2,4-trioxane: structure in first source		3.0340
bix 01294
[no description available]		3.1810piperidines
nitd 609
NITD 609: an antimalarial and coccidiostat; structure in first source		5.5960
rka 182
RKA 182: structure in first source		4.4730
kaf156
ganaplacide: antimalarial		4.2720
heme
Heme: The color-furnishing portion of hemoglobin. It is found free in tissues and as the prosthetic group in many hemeproteins.. ferroheme : Any iron(II)--porphyrin coordination complex.. ferroheme b : Heme b in which the iron has oxidation state +2.. heme : A heme is any tetrapyrrolic chelate of iron.		2.1710
6-chloro-7-methoxy-2-methyl-3-(4-(4-(trifluoromethoxy)phenoxy)phenyl)quinolin-4(1h)-one
6-Chloro-7-methoxy-2-methyl-3-(4-(4-(trifluoromethoxy)phenoxy)phenyl)quinolin-4(1H)-one: structure in first source		4.220
sj733
SJ733: antimalarial; structure in first source		2.2510
ferroquine
ferroquine: an antimalarial agent; structure in first source		7.2463
ConditionIndicatedRelationship StrengthStudiesTrials
Infections, Plasmodium
[description not available]		09.02181
Malaria
A protozoan disease caused in humans by four species of the PLASMODIUM genus: PLASMODIUM FALCIPARUM; PLASMODIUM VIVAX; PLASMODIUM OVALE; and PLASMODIUM MALARIAE; and transmitted by the bite of an infected female mosquito of the genus ANOPHELES. Malaria is endemic in parts of Asia, Africa, Central and South America, Oceania, and certain Caribbean islands. It is characterized by extreme exhaustion associated with paroxysms of high FEVER; SWEATING; shaking CHILLS; and ANEMIA. Malaria in ANIMALS is caused by other species of plasmodia.		09.02181
Plasmodium falciparum Malaria
[description not available]		011.521710
Malaria, Falciparum
Malaria caused by PLASMODIUM FALCIPARUM. This is the severest form of malaria and is associated with the highest levels of parasites in the blood. This disease is characterized by irregularly recurring febrile paroxysms that in extreme cases occur with acute cerebral, renal, or gastrointestinal manifestations.		011.521710
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.6320
Schistosoma haematobia Infection
[description not available]		04.7211
Schistosomiasis haematobia
A human disease caused by the infection of parasitic worms SCHISTOSOMA HAEMATOBIUM. It is endemic in AFRICA and parts of the MIDDLE EAST. Tissue damages most often occur in the URINARY TRACT, specifically the URINARY BLADDER.		04.7211
Babesia Infection
[description not available]		02.610
Bovine Diseases
[description not available]		02.610
Parasitemia
The presence of parasites (especially malarial parasites) in the blood. (Dorland, 27th ed)		05.1831
Acute Liver Injury, Drug-Induced
[description not available]		02.2510
Chemical and Drug Induced Liver Injury
A spectrum of clinical liver diseases ranging from mild biochemical abnormalities to ACUTE LIVER FAILURE, caused by drugs, drug metabolites, herbal and dietary supplements and chemicals from the environment.		02.2510
Plasmodium vivax Malaria
[description not available]		05.3921
Malaria, Vivax
Malaria caused by PLASMODIUM VIVAX. This form of malaria is less severe than MALARIA, FALCIPARUM, but there is a higher probability for relapses to occur. Febrile paroxysms often occur every other day.		05.3921
Electrocardiogram QT Prolonged
[description not available]		03.511
Long QT Syndrome
A condition that is characterized by episodes of fainting (SYNCOPE) and varying degree of ventricular arrhythmia as indicated by the prolonged QT interval. The inherited forms are caused by mutation of genes encoding cardiac ion channel proteins. The two major forms are ROMANO-WARD SYNDROME and JERVELL-LANGE NIELSEN SYNDROME.		03.511