Page last updated: 2024-11-05

diethylcarbamazine citrate

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Diethylcarbamazine citrate, also known as DEC, is a medication used to treat several parasitic infections, including lymphatic filariasis, onchocerciasis, and loiasis. It is synthesized by reacting diethylcarbamazine with citric acid. Diethylcarbamazine citrate works by killing the larval stages of the parasites. It also prevents the female worms from producing microfilariae, the larval form of the parasite that causes the symptoms of the disease. Diethylcarbamazine citrate is an important drug for the treatment and prevention of lymphatic filariasis, onchocerciasis, and loiasis. These diseases can cause severe disability and even death if left untreated. Diethylcarbamazine citrate is studied to find new ways to treat and prevent parasitic infections. Researchers are also studying the drug to understand its mechanism of action and to develop new drugs that are more effective and safer.'

Cross-References

ID SourceID
PubMed CID15432
CHEMBL ID937
CHEBI ID4528
SCHEMBL ID37736
MeSH IDM0006348

Synonyms (153)

Synonym
MLS002207116
os1z389k8s ,
unii-os1z389k8s
diethylcarbamazine citrate [usp:jan]
MLS001074102 ,
AKOS003390253
MLS000069762 ,
smr000058650
PRESTWICK_166
cas-1642-54-2
NCGC00017034-01
loxuran
carbam palatabs
franocide
d.e.c. sol
franozan
hetrazan
ethodryl citrate
1642-54-2
dicarocide
banocide
filazine
diro-form
dek-tabs
eosinopin
diethylcarbamazane citrate
dec chewable
caritrol
diethylcarbamazine citrate
n,n-diethyl-4-methyl-1-piperazinecarboxamide citrate
1-piperazinecarboxamide,n-diethyl-4-methyl-, citrate (1:1)
n,n-diethyl-4-methyl-1-piperazinecarboxamide dihydrogen citrate
diethylcarbamazine hydrogen citrate
diethylcarbamazine acid citrate
1-methyl-4-diethylcarbamoylpiperazine citrate
1-piperazinecarboxamide,n-diethyl-4-methyl-, 2-hydroxy-1,2,3-propanetricarboxylate (1:1)
1-diethylcarbamoyl-4-methylpiperazine dihydrogen citrate
diethylcarbamazine dihydrogen citrate
nsc-80513
wln: t6n dntj avn2&2 d1 &ov1xqvo&1vo
carricide citrate
1-piperazinecarboxamide, n,n-diethyl-4-methyl-, 2-hydroxy-1,2,3-propanetricarboxylate
dirocide
n,n-diethyl-4-methyl-1-piperazinecarboxamide citrate (1:1)
ditrazini citras
nsc 80513
hsdb 6421
einecs 216-696-6
filarabits
n,n-diethyl-4-methyl-1-piperazinecarboxamide dihydrogen citrate (1:1)
ditrazinum
n,n-diethyl-4-methyl-1-piperazine carboxamide citrate
1-piperazinecarboxamide, n,n-diethyl-4-methyl-, 2-hydroxy-1,2,3-propanetricarboxylate (1:1)
diethylcarbamazini citras
1-piperazinecarboxamide, n,n-diethyl-4-methyl-, citrate (1:1)
ditrazine
longicid
ditrazine citrate
ditrazin citrate
1-piperazinecarboxamide, n,n-diethyl-4-methyl-, citrate
nsc152050
16354-46-4
nsc-152050
diethylcarbamazine citrate (jp17/usp)
D00803
hetrazan (tn)
NCGC00094651-02
NCGC00094651-01
SPECTRUM1500242
diethylcarbamazine citrate salt
HMS2091M16
ethylaminoazine citrate
CHEMBL937
HMS501L10
D1898
HMS1568J10
HMS1920G06
citrate, diethylcarbamazine
n,n-diethyl-4-methyl-1-piperazinecarboxamide; 2-hydroxypropane-1,2,3-tricarboxylic acid
A810546
HMS2095J10
pharmakon1600-01500242
nsc-756735
nsc756735
tox21_110748
dtxcid2025555
dtxsid4045555 ,
MLS004773909
HMS2234D17
S4564
CCG-40067
NCGC00017034-02
NCGC00017034-03
FT-0624487
diethylcarbamazine citrate [mart.]
diethylcarbamazine citrate [mi]
diethylcarbamazine citrate [who-dd]
diethylcarbamazine dihydrogen citrate [who-ip]
diethylcarbamazini dihydrogenocitras [who-ip latin]
diethylcarbamazine citrate [usp impurity]
diethylcarbamazine citrate [hsdb]
diethylcarbamazine citrate [jan]
diethylcarbamazine citrate [green book]
diethylcarbamazine citrate [usp monograph]
diethylcarbamazine citrate [usp-rs]
diethylcarbamazine citrate [orange book]
HMS3370G20
SCHEMBL37736
NCGC00090954-07
tox21_110748_1
CS-3871
W-107945
diethylcarbamazine citrate, british pharmacopoeia (bp) reference standard
HY-12642
diethylcarbamazine (citrate)
OPERA_ID_558
mfcd00039124
n,n-diethyl-4-methylpiperazine-1-carboxamide;2-hydroxypropane-1,2,3-tricarboxylic acid
SR-01000759234-4
sr-01000759234
SR-01000759234-2
n,n-diethyl-4-methylpiperazine-1-carboxamide 2-hydroxypropane-1,2,3-tricarboxylate
diethylcarbamazine citrate salt, vetranal(tm), analytical standard
diethylcarbamazine citrate, united states pharmacopeia (usp) reference standard
diethylcarbamazine citrate, european pharmacopoeia (ep) reference standard
CHEBI:4528
HMS3712J10
BS-15595
Q27285812
C73172
1642-54-1(citrate); 90-89-1(free base)
n,n-diethyl-4-methylpiperazine-1-carboxamide citrate
filaribits chewable tablets
filban tablets
filban chewable wafers
diethylcarbamazine citrate (usp impurity)
nemacide chewable tablets
n,n-diethyl-4-methylpiperazine-1-carboxamide monocitrate
pet-dec
1-piperazinecarboxamide, n,n-diethyl-4-methyl-, citrate(1:1)
dirocide tablets
diethylcarbamazine citrate (usp-rs)
carbam tablets
ditrazin
dirocide syrup
1-piperazinecarboxamide, n,n-diethyl-4-methyl-, 2-hydroxy-1,2,3-propanetri-carboxylate
n,n-diethyl-4-methylpiperazine-1-carboxamide dihydrogen citrate
diethylcarbamazine citrate (mart.)
diethylcarbamazine citrate (usp:jan)
nemacide, nemacide-c
nemacide oral syrup
diethylcarbamazine citrate tab., diro-form
diethylcarbamazine citrate (usp monograph)

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
piperazinecarboxamide
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (23)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Beta-lactamaseEscherichia coli K-12Potency15.71430.044717.8581100.0000AID485294; AID485341
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency56.23410.631035.7641100.0000AID504339
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency32.46480.177814.390939.8107AID2147
15-lipoxygenase, partialHomo sapiens (human)Potency6.30960.012610.691788.5700AID887
TDP1 proteinHomo sapiens (human)Potency5.10680.000811.382244.6684AID686978; AID686979
Microtubule-associated protein tauHomo sapiens (human)Potency7.94330.180013.557439.8107AID1468
AR proteinHomo sapiens (human)Potency3.73810.000221.22318,912.5098AID743040; AID743042; AID743054
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency7.07950.011212.4002100.0000AID1030
thyroid stimulating hormone receptorHomo sapiens (human)Potency10.00000.001318.074339.8107AID926
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency8.71870.000214.376460.0339AID720691; AID720719
estrogen nuclear receptor alphaHomo sapiens (human)Potency9.02260.000229.305416,493.5996AID743080
67.9K proteinVaccinia virusPotency3.98110.00018.4406100.0000AID720580
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency56.23410.707936.904389.1251AID504333
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency14.12540.035520.977089.1251AID504332
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency3.20130.001723.839378.1014AID743083
activating transcription factor 6Homo sapiens (human)Potency2.13140.143427.612159.8106AID1159516
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency12.99530.00419.984825.9290AID504444
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency89.12513.548119.542744.6684AID743266
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency89.12510.050127.073689.1251AID588590
gemininHomo sapiens (human)Potency0.14580.004611.374133.4983AID624296
lamin isoform A-delta10Homo sapiens (human)Potency11.22020.891312.067628.1838AID1487
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency10.00000.316212.765731.6228AID881
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency10.00000.00638.235039.8107AID881
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (21)

Processvia Protein(s)Taxonomy
lipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
phospholipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
apoptotic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell population proliferationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of macrophage derived foam cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell migrationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
prostate gland developmentPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
regulation of epithelial cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of chemokine productionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of peroxisome proliferator activated receptor signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of keratinocyte differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell cyclePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of growthPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
hepoxilin biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
endocannabinoid signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cannabinoid biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxin A4 biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid oxidationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxygenase pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (8)

Processvia Protein(s)Taxonomy
iron ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
calcium ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
protein bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 13S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 8(S)-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 15-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 9S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (8)

Processvia Protein(s)Taxonomy
nucleusPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytosolPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytoskeletonPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
plasma membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
adherens junctionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
focal adhesionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
extracellular exosomePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (100)

Assay IDTitleYearJournalArticle
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID394898Antifilarial activity against Brugia malayi sub-periodic strain at 200 uM by MTT reduction assay2008European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
Synthesis of 2-sulfanyl-6-methyl-1,4-dihydropyrimidines as a new class of antifilarial agents.
AID394894Antifilarial activity against Brugia malayi sub-periodic strain at 100 uM by MTT reduction assay2008European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
Synthesis of 2-sulfanyl-6-methyl-1,4-dihydropyrimidines as a new class of antifilarial agents.
AID646614Antifilarial activity against 5 to 7 months old Brugia malayi infected in Mastomys coucha assessed as reduction in worm burden at 50 mg/kg, sc administered 7 to 8 days post-adult worm transplantation for 5 days measured on day 91 relative to control2012Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4
In vitro and in vivo antifilarial activity evaluation of 3,6-epoxy [1,5]dioxocines: a new class of antifilarial agents.
AID108571The compound was evaluated for sterilization effect on female Acanthocheilonema viteae in Mastomys natalensis2000Bioorganic & medicinal chemistry letters, Jul-03, Volume: 10, Issue:13
Syntheses and antifilarial profile of 7-chloro-4-(substituted amino) quinolines: a new class of antifilarial agents.
AID745024Antifilarial activity against female adult Brugia malayi assessed as inhibition of motility after 24 hrs by microscopic analysis2013Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9
Glycyrrhetinic acid and its analogs: a new class of antifilarial agents.
AID394911Embryostatic activity against transplanted adult worms of Brugia malayi sub-periodic strain in Meriones unguiculatus assessed as sterilized female worms at 12.5 mg/kg, ip for 5 days2008European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
Synthesis of 2-sulfanyl-6-methyl-1,4-dihydropyrimidines as a new class of antifilarial agents.
AID394886Antifilarial activity against Brugia malayi sub-periodic strain assessed as motility at 50 uM2008European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
Synthesis of 2-sulfanyl-6-methyl-1,4-dihydropyrimidines as a new class of antifilarial agents.
AID9234Tested in vivo for Acanthocheilonema viteae at 200 mg/kg X 5 days(perorally)2000Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11
Quinolones: novel probes in antifilarial chemotheraphy.
AID108569In vivo microfilariacidal activity against Acanthocheilonema viteae infection in Mastomys natalensis at 200 mg/kg for 5 days after peroral administration2000Bioorganic & medicinal chemistry letters, Jul-03, Volume: 10, Issue:13
Syntheses and antifilarial profile of 7-chloro-4-(substituted amino) quinolines: a new class of antifilarial agents.
AID745011Antifilarial activity adult against Brugia malayi infected in jirds assessed as sterile female worms recovered from host at 25 mg/kg, sc qd for 5 days measured after 56 days relative to control2013Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9
Glycyrrhetinic acid and its analogs: a new class of antifilarial agents.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID394897Antifilarial activity against Brugia malayi sub-periodic strain at 400 uM by MTT reduction assay2008European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
Synthesis of 2-sulfanyl-6-methyl-1,4-dihydropyrimidines as a new class of antifilarial agents.
AID108281In vivo anti-filarial (microfilaricidal) activity at an ip dose of 50 mg/kg (for 5 days) against A. viteae in Mastomys coucha.1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Potent 1,3-disubstituted-9H-pyrido[3,4-b]indoles as new lead compounds in antifilarial chemotherapy.
AID394907Embryostatic activity against Brugia malayi sub-periodic strain in Mastomys coucha assessed as sterilized female worms at 25 mg/kg, ip for 5 days2008European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
Synthesis of 2-sulfanyl-6-methyl-1,4-dihydropyrimidines as a new class of antifilarial agents.
AID168777Antifilarial activity evaluated as percent of surviving Litomosoides carinii in cotton rats that were sterlized after an ip dose of 30 mg/kg (for 5 days)1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Potent 1,3-disubstituted-9H-pyrido[3,4-b]indoles as new lead compounds in antifilarial chemotherapy.
AID108279In vivo anti-filarial (mif-microfilaricidal) activity at an ip dose of 100 mg/kg (for 5 days) against Brugia malayi1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Potent 1,3-disubstituted-9H-pyrido[3,4-b]indoles as new lead compounds in antifilarial chemotherapy.
AID646612Antifilarial activity against 5 to 7 months old Brugia malayi infected in Mastomys coucha assessed as sterilized female worm at 50 mg/kg, sc administered 7 to 8 days post-adult worm transplantation for 5 days measured on day 91 (Rvb = 19.62%)2012Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4
In vitro and in vivo antifilarial activity evaluation of 3,6-epoxy [1,5]dioxocines: a new class of antifilarial agents.
AID745022Cytotoxicity against african green monkey Vero cells2013Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9
Glycyrrhetinic acid and its analogs: a new class of antifilarial agents.
AID745021Selectivity index, ratio of CC50 for african green monkey Vero cells to IC50 for female adult Brugia malayi2013Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9
Glycyrrhetinic acid and its analogs: a new class of antifilarial agents.
AID394889Antifilarial activity against Brugia malayi sub-periodic strain assessed as sluggish motility at 400 uM2008European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
Synthesis of 2-sulfanyl-6-methyl-1,4-dihydropyrimidines as a new class of antifilarial agents.
AID9235Tested in vivo for Acanthocheilonema viteae at 200 mg/kg X 5 days(perorally)2000Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11
Quinolones: novel probes in antifilarial chemotheraphy.
AID646615Antifilarial activity against Brugia malayi infected in Meriones unguiculatus assessed as sterilized female worm at 25 mg/kg, sc administered 7 to 8 days post-adult worm transplantation for 5 days measured after 42 days2012Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4
In vitro and in vivo antifilarial activity evaluation of 3,6-epoxy [1,5]dioxocines: a new class of antifilarial agents.
AID108269Antifilarial activity as percent of surviving A. viteae in Mastomys coucha sterlized after an intraperitoneal dose of 50 mg/kg (for 5 days).1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Potent 1,3-disubstituted-9H-pyrido[3,4-b]indoles as new lead compounds in antifilarial chemotherapy.
AID394885Antifilarial activity against Brugia malayi sub-periodic strain assessed as motility at 100 uM2008European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
Synthesis of 2-sulfanyl-6-methyl-1,4-dihydropyrimidines as a new class of antifilarial agents.
AID745025Antifilarial activity against female adult Brugia malayi assessed as inhibition of MTT reduction at LC100 concentration after 24 hrs2013Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9
Glycyrrhetinic acid and its analogs: a new class of antifilarial agents.
AID745020Selectivity index, ratio of CC50 for african green monkey Vero cells to IC50 for microfilariae Brugia malayi2013Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9
Glycyrrhetinic acid and its analogs: a new class of antifilarial agents.
AID108567In vivo macrofilaricidal activity against Acanthocheilonema viteae infection in Mastomys natalensis at 200 mg/kg for 5 days after peroral administration2000Bioorganic & medicinal chemistry letters, Jul-03, Volume: 10, Issue:13
Syntheses and antifilarial profile of 7-chloro-4-(substituted amino) quinolines: a new class of antifilarial agents.
AID394895Antifilarial activity against Brugia malayi sub-periodic strain at 50 uM by MTT reduction assay2008European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
Synthesis of 2-sulfanyl-6-methyl-1,4-dihydropyrimidines as a new class of antifilarial agents.
AID169070In vivo anti-filarial (maf-macrofilaricidal) activity at an ip dose of 30 mg/kg (for 5 days) against Litomosoides carinii in cotton rats1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Potent 1,3-disubstituted-9H-pyrido[3,4-b]indoles as new lead compounds in antifilarial chemotherapy.
AID108273In vivo anti-filarial (maf-macrofilaricidal) activity at an ip dose of 100 mg/kg (for 5 days) against Brugia malayi1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Potent 1,3-disubstituted-9H-pyrido[3,4-b]indoles as new lead compounds in antifilarial chemotherapy.
AID169074In vivo anti-filarial (mif-microfilaricidal) activity at an ip dose of 75 mg/kg (for 5 days) against Litomosoides carinii in cotton rats1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Potent 1,3-disubstituted-9H-pyrido[3,4-b]indoles as new lead compounds in antifilarial chemotherapy.
AID108274In vivo anti-filarial (macrofilaricidal) activity at an ip dose of 50 mg/kg (for 5 days) against A. viteae in Mastomys coucha.1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Potent 1,3-disubstituted-9H-pyrido[3,4-b]indoles as new lead compounds in antifilarial chemotherapy.
AID108271Antifilarial activity evaluated as percent of surviving Brugia malayi that were sterlized after an ip dose of 100 mg/kg (for 5 days)1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Potent 1,3-disubstituted-9H-pyrido[3,4-b]indoles as new lead compounds in antifilarial chemotherapy.
AID394888Antifilarial activity against Brugia malayi sub-periodic strain assessed as motility at 200 uM2008European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
Synthesis of 2-sulfanyl-6-methyl-1,4-dihydropyrimidines as a new class of antifilarial agents.
AID745013Antifilarial activity against adult Brugia malayi infected in jirds assessed as reduction in worms recovered from host at 25 mg/kg, sc qd for 5 days measured after 56 days relative to control2013Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9
Glycyrrhetinic acid and its analogs: a new class of antifilarial agents.
AID745023Antifilarial activity against microfilariae Brugia malayi assessed as inhibition of motility after 24 hrs by microscopic analysis2013Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9
Glycyrrhetinic acid and its analogs: a new class of antifilarial agents.
AID394909Antifilarial activity against transplanted adult worms of Brugia malayi sub-periodic strain in Meriones unguiculatus assessed as reduction in worm burden 12.5 mg/kg, ip for 5 days relative to control2008European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
Synthesis of 2-sulfanyl-6-methyl-1,4-dihydropyrimidines as a new class of antifilarial agents.
AID71907Tested in vivo for sterilization of female worms2000Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11
Quinolones: novel probes in antifilarial chemotheraphy.
AID394901Antifilarial activity against Brugia malayi sub-periodic strain in Mastomys coucha assessed as microfilarial count at 25 mg/kg, ip for 5 days measured after 8 days2008European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
Synthesis of 2-sulfanyl-6-methyl-1,4-dihydropyrimidines as a new class of antifilarial agents.
AID745015Antifilarial activity against adult Brugia malayi infected in jirds assessed as decrease in microfilarial activity isolated from host peritoneal cavity at 25 mg/kg, sc qd for 5 days measured after 7 to 8 days2013Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9
Glycyrrhetinic acid and its analogs: a new class of antifilarial agents.
AID394904Antifilarial activity against Brugia malayi sub-periodic strain in Mastomys coucha assessed as reduction in worm burden at 25 mg/kg, ip for 5 days relative to control2008European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
Synthesis of 2-sulfanyl-6-methyl-1,4-dihydropyrimidines as a new class of antifilarial agents.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (25)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's1 (4.00)18.2507
2000's4 (16.00)29.6817
2010's14 (56.00)24.3611
2020's6 (24.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 79.20

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 very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index79.20 (24.57)
Research Supply Index3.26 (2.92)
Research Growth Index4.94 (4.65)
Search Engine Demand Index133.23 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (79.20)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (4.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other24 (96.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]