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antileishmanial agent

An antiprotozoal drug used to treat or prevent infections caused by protozoan parasites that belong to the genus Leishmania.

ChEBI ID: 70868

Members (17)

MemberDefinitionClass
5-o-methylembelinA member of the class of monohydroxy-1,4-benzoquinones that is embelin in which the hydroxy group at position 5 is replaced by a methoxy group. Isolated from Lysimachia punctata and Embelia ribes, it exhibits antileishmanial activity as well as inhibitory activity towards hepatitis C protease.5-O-methyl embelin
5,7-dihydroxy-2-methyl-8-(4-(3-hydroxy-1-methyl)-piperidinyl)-4h-1-benzopyran-4-oneA member of the class of chromones that is 4H-chromen-4-one in which the hydrogens at positions 2,5,7 and 8 are replaced by methyl, hydroxy, hydroxy, and (3S,4R)-3-hydroxy-1-methylpiperidin-4-yl groups, respectively. It is an alkaloid initially isolated from Amoora rohituka and is a precursor of the anti-cancer compound flavopiridol.rohitukine
acivicinAn L-alpha-amino acid that is L-alanine in which the methyl group is replaced by a (5S)-3-chloro-4,5-dihydro-1,2-oxazol-5-yl group. A glutamine analogue antimetabolite, it interferes with glutamate metabolism and several glutamate-dependent synthetic enzymes. It is obtained as a fermentation product of Streptomyces sviceus bacteria.acivicin
acteosideA glycoside that is the alpha-L-rhamnosyl-(1->3)-beta-D-glucoside of hydroxytyrosol in which the hydroxy group at position 4 of the glucopyranosyl moiety has undergone esterification by formal condensation with trans-caffeic acid.acteoside
ancistroealaine aAn isoquinoline alkaloid that is (3S)-6,8-dimethoxy-1,3-dimethyl-3,4-dihydroisoquinoline substituted by a 4,5-dimethoxy-7-methylnaphthalen-1-yl group at position 5. It is isolated from the leaves of Ancistrocladus tanzaniensis and exhibits antiplasmodial, antileishmanial and antitrypanocidal activities.ancistrotanzanine B
ascaridoleA p-menthane monoterpenoid that is p-menth-2-ene with a peroxy group across position 1 to 4.ascaridole
carbobenzoxyvalylphenylalanine aldehydeA dipeptide resulting from the formal condensation of the carboxy group of N-benzyloxycarbonyl-L-valine with the amino group of L-phenylalanine aldehyde. It is a potent cell-permeable inhibitor of calpain I and II, and is also a gamma-secretase inhibitor.Z-Val-Phe-H
ciliatamide aA lipopeptide that contains N-methylphenylalanine and lysine as the amino acid residues linked to a dec-9-enoyl moiety via an amide linkage (the R,R stereoisomer). It is isolated from the deep sea sponge Aaptos ciliata and exhibits antileishmanial activity.ciliatamide A
coronardineA monoterpenoid indole alkaloid with formula C21H26N2O2. It is isolated from the flowering plant genus, Tabernaemontana.(-)-coronaridine
dehydroemetineA pyridoisoquinoline which was developed in response to the cardiovascular toxicity associated with emetine and results from the dehydrogenation of the heterotricylic ring of emetine. It is an antiprotozoal agent and displays antimalarial, antiamoebic, and antileishmanial properties.dehydroemetine
dihydrobetulinic acidA pentacyclic triterpenoid that is lupane having a 3beta-hydroxy and 28-carboxy substituents. Isolated from the leaves of Syzygium claviflorum, it exhibits anti-HIV and antileishmanial activity.dihydrobetulinic acid
flavokawain bA member of the class of chalcones that consists of trans-chalcone substituted by hydroxy group at positions 2' and methoxy groups at positions 4' and 6'. Isolated from Piper methysticum and Piper rusbyi, it exhibits antileishmanial, anti-inflammatory and antineoplastic activities.flavokawain B
monastrolA racemate comprising equimolar amounts of R- and S-monastrol.ethyl 4-(3-hydroxyphenyl)-6-methyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate; monastrol
physalin fA physalin with antimalarial and antitumour activities isolated from Physalis angulata.physalin F
quercitrinA quercetin O-glycoside that is quercetin substituted by a alpha-L-rhamnosyl moiety at position 3 via a glycosidic linkage.quercitrin
ravuconazoleA member of the class of triazoles that is 1-butyl-1H-1,2,4-triazole in which the butyl group is substituted at positions 2, 2, and 3 by hydroxy, 2,4-difluorophenyl, and 4-(p-cyanophenyl)-1,3-thiazol-2-yl groups, respectively (the R,R stereoisomer). It exhibits antifungal activity by inhibition of 14alpha demethylase, an enzyme involved in sterol synthesis, resulting in lysis of the fungal cell wall and fungal cell death. (NCIO4)ravuconazole
rocaglamideAn organic heterotricyclic compound that is 2,3,3a,8b-tetrahydro-1H-benzo[b]cyclopenta[d]furan substituted by hydroxy groups at positions 1 and 8b, methoxy groups at positions 6 and 8, a 4-methoxyphenyl group at position 3a, a phenyl group at position 3 and a N,N-dimethylcarbamoyl group at position 1. Isolated from Aglaia odorata and Aglaia duperreana, it exhibits antineoplastic activity.rocaglamide

Research

Studies (1,836)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-1990214 (11.66)18.7374
1990's258 (14.05)18.2507
2000's458 (24.95)29.6817
2010's695 (37.85)24.3611
2020's211 (11.49)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials31 (1.60%)5.53%
Reviews66 (3.41%)6.00%
Case Studies10 (0.52%)4.05%
Observational0 (0.00%)0.25%
Other1,829 (94.47%)84.16%

Protein Targets (147)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency19.952611
15-lipoxygenase, partialHomo sapiens (human)Potency19.952611
67.9K proteinVaccinia virusPotency8.296226
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency11.754612
Alpha-synucleinHomo sapiens (human)Potency10.000011
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency7.459812
AR proteinHomo sapiens (human)Potency9.056033
arylsulfatase AHomo sapiens (human)Potency2.393411
ATAD5 protein, partialHomo sapiens (human)Potency20.587811
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency3.748533
Bloom syndrome protein isoform 1Homo sapiens (human)Potency0.000422
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency14.125411
Cellular tumor antigen p53Homo sapiens (human)Potency3.725522
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency31.622811
Chain A, CruzipainTrypanosoma cruziPotency0.031622
Chain A, HADH2 proteinHomo sapiens (human)Potency25.118911
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency25.863113
Chain B, HADH2 proteinHomo sapiens (human)Potency25.118911
chromobox protein homolog 1Homo sapiens (human)Potency22.387211
cytochrome P450 2C19 precursorHomo sapiens (human)Potency25.118911
cytochrome P450 2C9 precursorHomo sapiens (human)Potency29.881612
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency6.703328
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency6.682411
D(1A) dopamine receptorHomo sapiens (human)Potency2.059511
DNA polymerase eta isoform 1Homo sapiens (human)Potency20.046212
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency45.368823
DNA polymerase kappa isoform 1Homo sapiens (human)Potency30.277913
estrogen nuclear receptor alphaHomo sapiens (human)Potency19.004733
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency15.568633
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency41.456812
EWS/FLI fusion proteinHomo sapiens (human)Potency0.116344
flap endonuclease 1Homo sapiens (human)Potency64.467912
Fumarate hydrataseHomo sapiens (human)Potency0.331711
GABA theta subunitRattus norvegicus (Norway rat)Potency6.093615
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency6.093615
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency6.093615
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency6.093615
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency6.093615
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency6.093615
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency6.093615
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency6.093615
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency6.093615
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency6.093615
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency6.093615
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency6.093615
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency6.093615
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency6.093615
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency6.093615
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency6.093615
gemininHomo sapiens (human)Potency18.729136
glp-1 receptor, partialHomo sapiens (human)Potency25.118911
GLS proteinHomo sapiens (human)Potency28.934212
Glycoprotein hormones alpha chainHomo sapiens (human)Potency2.511911
GTP-binding nuclear protein Ran isoform 1Homo sapiens (human)Potency29.092911
Guanine nucleotide-binding protein GHomo sapiens (human)Potency19.952611
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency16.193612
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency29.881616
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency35.481312
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency17.782811
hypothetical protein, conservedTrypanosoma bruceiPotency30.741033
IDH1Homo sapiens (human)Potency14.549712
importin subunit beta-1 isoform 1Homo sapiens (human)Potency39.605822
lamin isoform A-delta10Homo sapiens (human)Potency18.854122
lethal(3)malignant brain tumor-like protein 1 isoform IHomo sapiens (human)Potency17.900812
LuciferasePhotinus pyralis (common eastern firefly)Potency10.691011
M-phase phosphoprotein 8Homo sapiens (human)Potency56.234111
Microtubule-associated protein tauHomo sapiens (human)Potency12.062712
mitogen-activated protein kinase 1Homo sapiens (human)Potency25.118911
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency0.014111
NFKB1 protein, partialHomo sapiens (human)Potency1.778322
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency11.220211
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency0.017622
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency24.803322
P53Homo sapiens (human)Potency22.387211
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency50.118711
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency10.691011
plasminogen precursorMus musculus (house mouse)Potency8.912511
polyproteinZika virusPotency0.331711
Rap guanine nucleotide exchange factor 3Homo sapiens (human)Potency63.095711
serine-protein kinase ATM isoform aHomo sapiens (human)Potency28.183811
Smad3Homo sapiens (human)Potency28.183811
snurportin-1Homo sapiens (human)Potency39.605822
TAR DNA-binding protein 43Homo sapiens (human)Potency31.622811
TDP1 proteinHomo sapiens (human)Potency16.7356211
thioredoxin reductaseRattus norvegicus (Norway rat)Potency22.584812
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency2.984922
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency1.584911
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency8.912511
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency8.912511
USP1 protein, partialHomo sapiens (human)Potency56.234111
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency49.338613

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)IC500.300011
Adenosine receptor A1Rattus norvegicus (Norway rat)IC502,000.000011
Adenosine receptor A2aRattus norvegicus (Norway rat)IC502,000.000011
Aldo-keto reductase family 1 member B1Bos taurus (cattle)IC5010.000011
Aldo-keto reductase family 1 member B1Homo sapiens (human)IC501.075022
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC500.120023
Aldo-keto reductase family 1 member C21Mus musculus (house mouse)IC5033.300011
Arginase Leishmania amazonensisIC5012.200011
Arginase Leishmania amazonensisKi4.300022
Aurora kinase AHomo sapiens (human)IC5050.000011
Bifunctional epoxide hydrolase 2Homo sapiens (human)IC5011.800011
Bifunctional epoxide hydrolase 2Homo sapiens (human)Ki39.600011
Calpain-1 catalytic subunitHomo sapiens (human)IC500.300011
Calpain-1 catalytic subunitHomo sapiens (human)Ki0.008011
Calpain-1 catalytic subunitSus scrofa (pig)Ki0.010011
Cathepsin BHomo sapiens (human)Ki0.024011
Chymotrypsinogen ABos taurus (cattle)Ki54.000011
Cyclin-A2Homo sapiens (human)IC507.300033
Cyclin-dependent kinase 2Homo sapiens (human)IC507.300033
Cyclin-dependent kinase 9Homo sapiens (human)IC500.300033
Cyclin-T1Homo sapiens (human)IC500.300033
Cytochrome P450 3A4Homo sapiens (human)IC501.010011
Eukaryotic initiation factor 4A-IHomo sapiens (human)IC500.104444
Integrase Human immunodeficiency virus 1IC507.800011
integrase, partialHuman immunodeficiency virus 1IC5012.419824
Kinesin-like protein KIF11Homo sapiens (human)IC5012.824799
Kinesin-like protein KIFC1Homo sapiens (human)IC50100.000011
lens epithelium-derived growth factor p75Homo sapiens (human)IC5012.419824
Macrophage-expressed gene 1 proteinHomo sapiens (human)IC509.100011
Mitogen-activated protein kinase 10Homo sapiens (human)IC5024.150012
Mitogen-activated protein kinase 14Homo sapiens (human)IC5024.150012
NeuraminidaseInfluenza A virus (A/USSR/90/1977(H1N1))IC50115.100022
NF-kappa-B inhibitor alphaHomo sapiens (human)IC5027.100011
Non-structural protein 1 Dengue virusIC501.700011
Nuclear factor NF-kappa-B p105 subunitHomo sapiens (human)IC501.037522
Polyphenol oxidase 2Agaricus bisporusIC50125.000022
Polyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)IC501.926733
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC5010.370011
Prostaglandin G/H synthase 1 Bos taurus (cattle)IC502,000.000033
Prostaglandin G/H synthase 2Ovis aries (sheep)IC501,337.100033
Protein kinase C alpha typeHomo sapiens (human)IC509.300011
Protein kinase C alpha typeRattus norvegicus (Norway rat)IC5015.356033
Protein kinase C alpha typeRattus norvegicus (Norway rat)Ki25.000022
Protein kinase C beta typeRattus norvegicus (Norway rat)IC5015.356033
Protein kinase C beta typeRattus norvegicus (Norway rat)Ki25.000022
Protein kinase C delta typeRattus norvegicus (Norway rat)IC5015.356033
Protein kinase C delta typeRattus norvegicus (Norway rat)Ki25.000022
Protein kinase C epsilon typeRattus norvegicus (Norway rat)IC5015.356033
Protein kinase C epsilon typeRattus norvegicus (Norway rat)Ki25.000022
Protein kinase C eta typeRattus norvegicus (Norway rat)IC5015.356033
Protein kinase C eta typeRattus norvegicus (Norway rat)Ki25.000022
Protein kinase C gamma typeRattus norvegicus (Norway rat)IC5015.356033
Protein kinase C gamma typeRattus norvegicus (Norway rat)Ki25.000022
Protein kinase C theta typeRattus norvegicus (Norway rat)IC5015.356033
Protein kinase C theta typeRattus norvegicus (Norway rat)Ki25.000022
Protein kinase C zeta typeRattus norvegicus (Norway rat)IC5015.356033
Protein kinase C zeta typeRattus norvegicus (Norway rat)Ki25.000022
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2IC5012.270022
Serine/threonine-protein kinase pim-2Homo sapiens (human)IC5025.000011
Transcription factor p65Homo sapiens (human)IC500.736766
UreaseCanavalia ensiformis (jack bean)Ki25.660011
Urease subunit alphaHelicobacter pylori 26695IC501,220.000011
Urease subunit betaHelicobacter pylori 26695IC501,220.000011
Xanthine dehydrogenase/oxidaseHomo sapiens (human)IC5057.370022
Zinc finger protein GLI1Homo sapiens (human)IC500.660011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Eukaryotic initiation factor 4A-IHomo sapiens (human)Kd0.156011

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Arginase Leishmania amazonensisKis7.200011
glycogen synthase kinase-3 alphaHomo sapiens (human)AC5029.770011
Nuclear factor NF-kappa-B p105 subunitHomo sapiens (human)ED502.000011
Prolyl 4-hydroxylase, beta polypeptideHomo sapiens (human)AC502.480022
Transcription factor p65Homo sapiens (human)ED500.080011