Page last updated: 2024-11-05

cycloguanil hydrochloride

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Description

cycloguanil hydrochloride : The hydrochloride salt of cycloguanil. [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]

Cross-References

ID SourceID
PubMed CID9048
CHEMBL ID544227
CHEBI ID79772
MeSH IDM0316633

Synonyms (52)

Synonym
1-(4-chlorophenyl)-6,6-dimethyl-1,6-dihydro-1,3,5-triazine-2,4-diamine hydrochloride
s-triazine, 4,6-diamino-1-(p-chlorophenyl)-1,2-dihydro-2,2-dimethyl-, monohydrochloride
1,3,5-triazine-2,4-diamine, 1-(4-chlorophenyl)-1,6-dihydro-6,6-dimethyl-, monohydrochloride
bn 2410
chloroguanide triazine hydrochloride
ai3-26080
4,2-dihydro-2,2-dimethyl-s-triazine hydrochloride
cycloguanil hydrochloride
s-triazine,6-diamino-1-(p-chlorophenyl)-1,2-dihydro-2,2-dimethyl-, monohydrochloride
nsc 3074
1,5-triazine-2,4-diamine, 1-(4-chlorophenyl)-1,6-dihydro-6,6-dimethyl-, monohydrochloride
152-53-4
wln: t6n cn en bhj ar dg & b1 b1 dz fz & gh
nsc-3074
nsc3074
1-(4-chlorophenyl)-1,6-dihydro-6,6-dimethyl-1,3,5-triazine-2,4-diamine monohydrochloride
gnf-pf-2519 ,
chebi:79772 ,
CHEMBL544227
FT-0665342
AKOS003661804
NCGC00229703-01
unii-5c8e0l7498
5c8e0l7498 ,
cycloguanil hcl
tox21_113603
dtxsid7049053 ,
dtxcid8028979
cas-152-53-4
1-(4-chlorophenyl)-1,6-dihydro-6,6-dimethyl-1,3,5-triazine-2,4-diamine hydrochloride
MLS006011693
smr002530105
s-triazine, 4,6-diamino-1-(p-chlorophenyl)-1,2-dihydro-2,2-dimethyl-, hydrochloride
40725-50-6
1,3,5-triazine-2,4-diamine, 1-(4-chlorophenyl)-1,6-dihydro-6,6-dimethyl-, hydrochloride (1:1)
bn-2410
mfcd00035308
J-008930
Q27148906
DS-14609
chloroguanide triazine
SB73714
HY-12784A
cycloguanil (hydrochloride)
CS-W012212
A883898
C72890
152-53-4 (hcl)
1-(4-chlorophenyl)-6,6-dimethyl-1,3,5-triazine-2,4-diamine;hydrochloride
EN300-818847
cycloguanil-d4hydrochloride
SY109103

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" The orally bioavailable lead imidazolopiperazine confers complete causal prophylactic protection (15 milligrams/kilogram) in rodent models of malaria and shows potent in vivo blood-stage therapeutic activity."( Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery.
Barnes, SW; Bonamy, GM; Bopp, SE; Borboa, R; Bright, AT; Chatterjee, A; Che, J; Cohen, S; Dharia, NV; Diagana, TT; Fidock, DA; Froissard, P; Gagaring, K; Gettayacamin, M; Glynne, RJ; Gordon, P; Groessl, T; Kato, N; Kuhen, KL; Lee, MC; Mazier, D; McNamara, CW; Meister, S; Nagle, A; Nam, TG; Plouffe, DM; Richmond, W; Roland, J; Rottmann, M; Sattabongkot, J; Schultz, PG; Tuntland, T; Walker, JR; Winzeler, EA; Wu, T; Zhou, B; Zhou, Y, 2011
)
0.37
"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 (2)

ClassDescription
organic molecular entityAny molecular entity that contains carbon.
hydrochlorideA salt formally resulting from the reaction of hydrochloric acid with an organic base.
[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 (5)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
TDP1 proteinHomo sapiens (human)Potency1.49800.000811.382244.6684AID686978; AID686979
estrogen nuclear receptor alphaHomo sapiens (human)Potency29.84930.000229.305416,493.5996AID743079
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency16.89680.000323.4451159.6830AID743065; AID743067
Cellular tumor antigen p53Homo sapiens (human)Potency21.13170.002319.595674.0614AID651631
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Bifunctional dihydrofolate reductase-thymidylate synthasePlasmodium falciparum K1IC50 (µMol)0.00150.00151.11635.8000AID1367779
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (124)

Processvia Protein(s)Taxonomy
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycle G2/M phase transitionCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
ER overload responseCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
mitophagyCellular tumor antigen p53Homo sapiens (human)
in utero embryonic developmentCellular tumor antigen p53Homo sapiens (human)
somitogenesisCellular tumor antigen p53Homo sapiens (human)
release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
hematopoietic progenitor cell differentiationCellular tumor antigen p53Homo sapiens (human)
T cell proliferation involved in immune responseCellular tumor antigen p53Homo sapiens (human)
B cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
T cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
response to ischemiaCellular tumor antigen p53Homo sapiens (human)
nucleotide-excision repairCellular tumor antigen p53Homo sapiens (human)
double-strand break repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
protein import into nucleusCellular tumor antigen p53Homo sapiens (human)
autophagyCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorCellular tumor antigen p53Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
Ras protein signal transductionCellular tumor antigen p53Homo sapiens (human)
gastrulationCellular tumor antigen p53Homo sapiens (human)
neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
protein localizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA replicationCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
determination of adult lifespanCellular tumor antigen p53Homo sapiens (human)
mRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
rRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
response to salt stressCellular tumor antigen p53Homo sapiens (human)
response to inorganic substanceCellular tumor antigen p53Homo sapiens (human)
response to X-rayCellular tumor antigen p53Homo sapiens (human)
response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
positive regulation of gene expressionCellular tumor antigen p53Homo sapiens (human)
cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
viral processCellular tumor antigen p53Homo sapiens (human)
glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
cerebellum developmentCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell growthCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCellular tumor antigen p53Homo sapiens (human)
negative regulation of telomere maintenance via telomeraseCellular tumor antigen p53Homo sapiens (human)
T cell differentiation in thymusCellular tumor antigen p53Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
regulation of tissue remodelingCellular tumor antigen p53Homo sapiens (human)
cellular response to UVCellular tumor antigen p53Homo sapiens (human)
multicellular organism growthCellular tumor antigen p53Homo sapiens (human)
positive regulation of mitochondrial membrane permeabilityCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
entrainment of circadian clock by photoperiodCellular tumor antigen p53Homo sapiens (human)
mitochondrial DNA repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
transcription initiation-coupled chromatin remodelingCellular tumor antigen p53Homo sapiens (human)
negative regulation of proteolysisCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assemblyCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
response to antibioticCellular tumor antigen p53Homo sapiens (human)
fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
circadian behaviorCellular tumor antigen p53Homo sapiens (human)
bone marrow developmentCellular tumor antigen p53Homo sapiens (human)
embryonic organ developmentCellular tumor antigen p53Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationCellular tumor antigen p53Homo sapiens (human)
protein stabilizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of helicase activityCellular tumor antigen p53Homo sapiens (human)
protein tetramerizationCellular tumor antigen p53Homo sapiens (human)
chromosome organizationCellular tumor antigen p53Homo sapiens (human)
neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
hematopoietic stem cell differentiationCellular tumor antigen p53Homo sapiens (human)
negative regulation of glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
type II interferon-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
cardiac septum morphogenesisCellular tumor antigen p53Homo sapiens (human)
positive regulation of programmed necrotic cell deathCellular tumor antigen p53Homo sapiens (human)
protein-containing complex assemblyCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressCellular tumor antigen p53Homo sapiens (human)
thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
necroptotic processCellular tumor antigen p53Homo sapiens (human)
cellular response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
cellular response to xenobiotic stimulusCellular tumor antigen p53Homo sapiens (human)
cellular response to ionizing radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to UV-CCellular tumor antigen p53Homo sapiens (human)
stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
cellular response to actinomycin DCellular tumor antigen p53Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
cellular senescenceCellular tumor antigen p53Homo sapiens (human)
replicative senescenceCellular tumor antigen p53Homo sapiens (human)
oxidative stress-induced premature senescenceCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
oligodendrocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of execution phase of apoptosisCellular tumor antigen p53Homo sapiens (human)
negative regulation of mitophagyCellular tumor antigen p53Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of G1 to G0 transitionCellular tumor antigen p53Homo sapiens (human)
negative regulation of miRNA processingCellular tumor antigen p53Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
negative regulation of pentose-phosphate shuntCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
regulation of fibroblast apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
positive regulation of cellular senescenceCellular tumor antigen p53Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (34)

Processvia Protein(s)Taxonomy
transcription cis-regulatory region bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
core promoter sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
TFIID-class transcription factor complex bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
protease bindingCellular tumor antigen p53Homo sapiens (human)
p53 bindingCellular tumor antigen p53Homo sapiens (human)
DNA bindingCellular tumor antigen p53Homo sapiens (human)
chromatin bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activityCellular tumor antigen p53Homo sapiens (human)
mRNA 3'-UTR bindingCellular tumor antigen p53Homo sapiens (human)
copper ion bindingCellular tumor antigen p53Homo sapiens (human)
protein bindingCellular tumor antigen p53Homo sapiens (human)
zinc ion bindingCellular tumor antigen p53Homo sapiens (human)
enzyme bindingCellular tumor antigen p53Homo sapiens (human)
receptor tyrosine kinase bindingCellular tumor antigen p53Homo sapiens (human)
ubiquitin protein ligase bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase regulator activityCellular tumor antigen p53Homo sapiens (human)
ATP-dependent DNA/DNA annealing activityCellular tumor antigen p53Homo sapiens (human)
identical protein bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase bindingCellular tumor antigen p53Homo sapiens (human)
protein heterodimerization activityCellular tumor antigen p53Homo sapiens (human)
protein-folding chaperone bindingCellular tumor antigen p53Homo sapiens (human)
protein phosphatase 2A bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingCellular tumor antigen p53Homo sapiens (human)
14-3-3 protein bindingCellular tumor antigen p53Homo sapiens (human)
MDM2/MDM4 family protein bindingCellular tumor antigen p53Homo sapiens (human)
disordered domain specific bindingCellular tumor antigen p53Homo sapiens (human)
general transcription initiation factor bindingCellular tumor antigen p53Homo sapiens (human)
molecular function activator activityCellular tumor antigen p53Homo sapiens (human)
promoter-specific chromatin bindingCellular tumor antigen p53Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (19)

Processvia Protein(s)Taxonomy
nuclear bodyCellular tumor antigen p53Homo sapiens (human)
nucleusCellular tumor antigen p53Homo sapiens (human)
nucleoplasmCellular tumor antigen p53Homo sapiens (human)
replication forkCellular tumor antigen p53Homo sapiens (human)
nucleolusCellular tumor antigen p53Homo sapiens (human)
cytoplasmCellular tumor antigen p53Homo sapiens (human)
mitochondrionCellular tumor antigen p53Homo sapiens (human)
mitochondrial matrixCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulumCellular tumor antigen p53Homo sapiens (human)
centrosomeCellular tumor antigen p53Homo sapiens (human)
cytosolCellular tumor antigen p53Homo sapiens (human)
nuclear matrixCellular tumor antigen p53Homo sapiens (human)
PML bodyCellular tumor antigen p53Homo sapiens (human)
transcription repressor complexCellular tumor antigen p53Homo sapiens (human)
site of double-strand breakCellular tumor antigen p53Homo sapiens (human)
germ cell nucleusCellular tumor antigen p53Homo sapiens (human)
chromatinCellular tumor antigen p53Homo sapiens (human)
transcription regulator complexCellular tumor antigen p53Homo sapiens (human)
protein-containing complexCellular tumor antigen p53Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (83)

Assay IDTitleYearJournalArticle
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
AID159443Antimalarial activity as change in MST against drug-sensitive Plasmodium berghei infected mice (Mus musculus) at 160 mg/kg subcutaneous dose after 72 hr1984Journal of medicinal chemistry, Dec, Volume: 27, Issue:12
Folate antagonists. 22. Antimalarial and antibacterial effects of 2,4-diamino-6-quinazolinesulfonamides.
AID1143977Antimalarial activity against trophozoite-induced Plasmodium gallinaceum infected in white leghorn chicken assessed as disease cure from parasite infection at 60 mg/kg, sc administered 72 hrs after infection1978Journal of medicinal chemistry, Oct, Volume: 21, Issue:10
Folate antagonists. 13. 2,4-Diamino-6-](alpha,alpha,alpha-trifluoro-m-tolyl)thio]quinazoline and related 2,4-diamino-6-[(phenyl- and naphthyl)thio]quinazolines, a unique class of antimetabolites with extraordinary antimalarial and antibacterial effects.
AID124999Mean survival time against trophozoite induced Plasmodium berghei in mice minus control was evaluated at a dose 10 mg/kg.1985Journal of medicinal chemistry, Feb, Volume: 28, Issue:2
Folate antagonists. 21. Synthesis and antimalarial properties of 2,4-diamino-6-(benzylamino)pyrido[3,2-d]pyrimidines.
AID124562Antimalarial effect against trophozoite-induced Plasmodium berghei in mice (Mus musculus) after subcutaneous administration dose of 160 mg/kg; 5 survival after 60 days1983Journal of medicinal chemistry, Dec, Volume: 26, Issue:12
Folate antagonists. 20. Synthesis and antitumor and antimalarial properties of trimetrexate and related 6-[(phenylamino)methyl]-2,4-quinazolinediamines.
AID1143951Toxicity in Plasmodium berghei infected mouse assessed as mortality at 320 mg/kg, sc administered 72 hrs after infection measured after 2 to 5 days1978Journal of medicinal chemistry, Oct, Volume: 21, Issue:10
Folate antagonists. 13. 2,4-Diamino-6-](alpha,alpha,alpha-trifluoro-m-tolyl)thio]quinazoline and related 2,4-diamino-6-[(phenyl- and naphthyl)thio]quinazolines, a unique class of antimetabolites with extraordinary antimalarial and antibacterial effects.
AID1134794Antiplasmodial activity against drug-sensitive Plasmodium berghei infected in mouse assessed as change in mean survival time at 40 mg/kg, sc administered as single dose 72 hrs post infection1978Journal of medicinal chemistry, Jul, Volume: 21, Issue:7
Folate antagonists. 12. Antimalarial and antibacterial effects of 2,4-diamino-6-[(aralkyl and alicyclid)thio-, sulfinyl-, and sulfonyl]quinazolines.
AID1134972Antimalarial activity against trophozoite-induced Plasmodium gallinaceum infected in chick assessed as mean survival time at 120 mg/kg, sc single dose (Rvb = 3.6 days)1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
Folate antagonists. 15. 2,3-Diamino-6-(2-naphthylsulfonyl)quinazoline and related 2,4-diamino-6-[(phenyl and naphthyl)sulfinyl and sulfonyl]quinazolines, a potent new class of antimetabolites with phenomenal antimalarial activity.
AID125022Mean survival time against trophozoite induced Plasmodium berghei in mice minus control was evaluated at a dose 320 mg/kg; 2 toxic death and 3 survived occurred on days 2-5 after injection1985Journal of medicinal chemistry, Feb, Volume: 28, Issue:2
Folate antagonists. 21. Synthesis and antimalarial properties of 2,4-diamino-6-(benzylamino)pyrido[3,2-d]pyrimidines.
AID449706NOVARTIS: Inhibition Frequency Index (IFI) - the number of HTS assays where a compound showed > 50% inhibition/induction, expressed as a percentage of the number of assays in which the compound was tested.2008Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
AID1143939Antimalarial activity against Plasmodium berghei infected in mouse assessed as increase in mean survival days of host at 10 mg/kg, sc administered 72 hrs after infection relative to control1978Journal of medicinal chemistry, Oct, Volume: 21, Issue:10
Folate antagonists. 13. 2,4-Diamino-6-](alpha,alpha,alpha-trifluoro-m-tolyl)thio]quinazoline and related 2,4-diamino-6-[(phenyl- and naphthyl)thio]quinazolines, a unique class of antimetabolites with extraordinary antimalarial and antibacterial effects.
AID117293Parenteral antimalarial effect against Plasmodium berghei in mice (Mus musculus) at a dose of 80 mg/kg subcutaneously1981Journal of medicinal chemistry, Feb, Volume: 24, Issue:2
Folate antagonists. 18. Synthesis and antimalarial effects of N6-(arylmethyl)-N6-methyl-2,4,6-pteridinetriamines and related N6,N6-disubstituted 2,4,6-pteridinetriamines.
AID1143967Antimalarial activity against trophozoite-induced Plasmodium gallinaceum infected in white leghorn chicken assessed as disease cure from parasite infection at 160 mg/kg, sc administered 72 hrs after infection1978Journal of medicinal chemistry, Oct, Volume: 21, Issue:10
Folate antagonists. 13. 2,4-Diamino-6-](alpha,alpha,alpha-trifluoro-m-tolyl)thio]quinazoline and related 2,4-diamino-6-[(phenyl- and naphthyl)thio]quinazolines, a unique class of antimetabolites with extraordinary antimalarial and antibacterial effects.
AID1143978Antimalarial activity against trophozoite-induced Plasmodium gallinaceum infected in white leghorn chicken assessed as increase in mean survival days of host at 30 mg/kg, sc administered 72 hrs after infection relative to control1978Journal of medicinal chemistry, Oct, Volume: 21, Issue:10
Folate antagonists. 13. 2,4-Diamino-6-](alpha,alpha,alpha-trifluoro-m-tolyl)thio]quinazoline and related 2,4-diamino-6-[(phenyl- and naphthyl)thio]quinazolines, a unique class of antimetabolites with extraordinary antimalarial and antibacterial effects.
AID1134787Toxicity in drug-sensitive Plasmodium berghei infected mouse at 640 mg/kg, sc administered as single dose 72 hrs post infection measured 60 days postinfection1978Journal of medicinal chemistry, Jul, Volume: 21, Issue:7
Folate antagonists. 12. Antimalarial and antibacterial effects of 2,4-diamino-6-[(aralkyl and alicyclid)thio-, sulfinyl-, and sulfonyl]quinazolines.
AID1134795Antiplasmodial activity against drug-sensitive Plasmodium berghei infected in mouse assessed as change in mean survival time at 20 mg/kg, sc administered as single dose 72 hrs post infection1978Journal of medicinal chemistry, Jul, Volume: 21, Issue:7
Folate antagonists. 12. Antimalarial and antibacterial effects of 2,4-diamino-6-[(aralkyl and alicyclid)thio-, sulfinyl-, and sulfonyl]quinazolines.
AID1143996Antimalarial activity against sporozoite-induced Plasmodium gallinaceum infected in white leghorn chicken assessed as increase in mean survival days of host at 60 mg/kg, sc administered 72 hrs after infection relative to control1978Journal of medicinal chemistry, Oct, Volume: 21, Issue:10
Folate antagonists. 13. 2,4-Diamino-6-](alpha,alpha,alpha-trifluoro-m-tolyl)thio]quinazoline and related 2,4-diamino-6-[(phenyl- and naphthyl)thio]quinazolines, a unique class of antimetabolites with extraordinary antimalarial and antibacterial effects.
AID1134956Antimalarial activity against trophozoite-induced Plasmodium berghei infected in mouse assessed as change in mean survival time at 80 mg/kg, sc single dose after 72 hrs of infection1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
Folate antagonists. 15. 2,3-Diamino-6-(2-naphthylsulfonyl)quinazoline and related 2,4-diamino-6-[(phenyl and naphthyl)sulfinyl and sulfonyl]quinazolines, a potent new class of antimetabolites with phenomenal antimalarial activity.
AID159449Antimalarial activity as change in MST against drug-sensitive Plasmodium berghei infected mice (Mus musculus) at 20 mg/kg subcutaneous dose after 72 hr1984Journal of medicinal chemistry, Dec, Volume: 27, Issue:12
Folate antagonists. 22. Antimalarial and antibacterial effects of 2,4-diamino-6-quinazolinesulfonamides.
AID1143994Toxicity in sporozoite-induced Plasmodium gallinaceum infected white leghorn chicken assessed as mortality at 120 mg/kg, sc administered 72 hrs after infection measured up to 6 days1978Journal of medicinal chemistry, Oct, Volume: 21, Issue:10
Folate antagonists. 13. 2,4-Diamino-6-](alpha,alpha,alpha-trifluoro-m-tolyl)thio]quinazoline and related 2,4-diamino-6-[(phenyl- and naphthyl)thio]quinazolines, a unique class of antimetabolites with extraordinary antimalarial and antibacterial effects.
AID1134997Antimalarial activity against sporozoite-induced Plasmodium gallinaceum infected in chick assessed as change in cured at 60 mg/kg, sc single dose1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
Folate antagonists. 15. 2,3-Diamino-6-(2-naphthylsulfonyl)quinazoline and related 2,4-diamino-6-[(phenyl and naphthyl)sulfinyl and sulfonyl]quinazolines, a potent new class of antimetabolites with phenomenal antimalarial activity.
AID1143944Antimalarial activity against Plasmodium berghei infected in mouse assessed as disease cure from parasite infection at 320 mg/kg, sc administered 72 hrs after infection1978Journal of medicinal chemistry, Oct, Volume: 21, Issue:10
Folate antagonists. 13. 2,4-Diamino-6-](alpha,alpha,alpha-trifluoro-m-tolyl)thio]quinazoline and related 2,4-diamino-6-[(phenyl- and naphthyl)thio]quinazolines, a unique class of antimetabolites with extraordinary antimalarial and antibacterial effects.
AID1144006Antimalarial activity against sporozoite-induced Plasmodium gallinaceum infected in white leghorn chicken assessed as increase in mean survival days of host at 15 mg/kg, sc administered 72 hrs after infection relative to control1978Journal of medicinal chemistry, Oct, Volume: 21, Issue:10
Folate antagonists. 13. 2,4-Diamino-6-](alpha,alpha,alpha-trifluoro-m-tolyl)thio]quinazoline and related 2,4-diamino-6-[(phenyl- and naphthyl)thio]quinazolines, a unique class of antimetabolites with extraordinary antimalarial and antibacterial effects.
AID1143974Antimalarial activity against trophozoite-induced Plasmodium gallinaceum infected in white leghorn chicken assessed as disease cure from parasite infection at 120 mg/kg, sc administered 72 hrs after infection1978Journal of medicinal chemistry, Oct, Volume: 21, Issue:10
Folate antagonists. 13. 2,4-Diamino-6-](alpha,alpha,alpha-trifluoro-m-tolyl)thio]quinazoline and related 2,4-diamino-6-[(phenyl- and naphthyl)thio]quinazolines, a unique class of antimetabolites with extraordinary antimalarial and antibacterial effects.
AID449703NOVARTIS: Inhibition of Plasmodium falciparum 3D7 (drug-susceptible) proliferation in erythrocyte-based infection assay 2008Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
AID122518Mean survival time against trophozoite induced Plasmodium berghei in mice minus control was evaluated at a dose 640 mg/kg; 5 toxic death occurred on days 2-5 after injection1985Journal of medicinal chemistry, Feb, Volume: 28, Issue:2
Folate antagonists. 21. Synthesis and antimalarial properties of 2,4-diamino-6-(benzylamino)pyrido[3,2-d]pyrimidines.
AID1134793Antiplasmodial activity against drug-sensitive Plasmodium berghei infected in mouse assessed as change in mean survival time at 80 mg/kg, sc administered as single dose 72 hrs post infection1978Journal of medicinal chemistry, Jul, Volume: 21, Issue:7
Folate antagonists. 12. Antimalarial and antibacterial effects of 2,4-diamino-6-[(aralkyl and alicyclid)thio-, sulfinyl-, and sulfonyl]quinazolines.
AID1134999Antimalarial activity against sporozoite-induced Plasmodium gallinaceum infected in chick assessed as change in cured at 15 mg/kg, sc single dose1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
Folate antagonists. 15. 2,3-Diamino-6-(2-naphthylsulfonyl)quinazoline and related 2,4-diamino-6-[(phenyl and naphthyl)sulfinyl and sulfonyl]quinazolines, a potent new class of antimetabolites with phenomenal antimalarial activity.
AID602119NOVARTIS: Antimalarial liver stage activity measured as reduction in Plasmodium yoelii schizont area in HepG2-A16-CD81 cells by immuno-fluorescence, and median schizont size at 10uM compound concentration2011Science (New York, N.Y.), Dec-09, Volume: 334, Issue:6061
Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery.
AID1143937Antimalarial activity against Plasmodium berghei infected in mouse assessed as increase in mean survival days of host at 40 mg/kg, sc administered 72 hrs after infection relative to control1978Journal of medicinal chemistry, Oct, Volume: 21, Issue:10
Folate antagonists. 13. 2,4-Diamino-6-](alpha,alpha,alpha-trifluoro-m-tolyl)thio]quinazoline and related 2,4-diamino-6-[(phenyl- and naphthyl)thio]quinazolines, a unique class of antimetabolites with extraordinary antimalarial and antibacterial effects.
AID1367779Inhibition of Plasmodium falciparum DHFR2017Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24
Discovery of new antimalarial agents: Second-generation dual inhibitors against FP-2 and PfDHFR via fragments assembely.
AID1143982Toxicity in sporozoite-induced Plasmodium gallinaceum infected white leghorn chicken assessed as mortality at 480 mg/kg, sc administered 72 hrs after infection measured up to 6 days1978Journal of medicinal chemistry, Oct, Volume: 21, Issue:10
Folate antagonists. 13. 2,4-Diamino-6-](alpha,alpha,alpha-trifluoro-m-tolyl)thio]quinazoline and related 2,4-diamino-6-[(phenyl- and naphthyl)thio]quinazolines, a unique class of antimetabolites with extraordinary antimalarial and antibacterial effects.
AID1143954Ratio of quinine hydrochloride SD90 to compound SD90 for trophozoite-induced Plasmodium berghei infected in mouse assessed as daily dose required to suppression of 90% parasite infection administered with diet for 6 days1978Journal of medicinal chemistry, Oct, Volume: 21, Issue:10
Folate antagonists. 13. 2,4-Diamino-6-](alpha,alpha,alpha-trifluoro-m-tolyl)thio]quinazoline and related 2,4-diamino-6-[(phenyl- and naphthyl)thio]quinazolines, a unique class of antimetabolites with extraordinary antimalarial and antibacterial effects.
AID1143936Antimalarial activity against Plasmodium berghei infected in mouse assessed as increase in mean survival days of host at 80 mg/kg, sc administered 72 hrs after infection relative to control1978Journal of medicinal chemistry, Oct, Volume: 21, Issue:10
Folate antagonists. 13. 2,4-Diamino-6-](alpha,alpha,alpha-trifluoro-m-tolyl)thio]quinazoline and related 2,4-diamino-6-[(phenyl- and naphthyl)thio]quinazolines, a unique class of antimetabolites with extraordinary antimalarial and antibacterial effects.
AID1143976Antimalarial activity against trophozoite-induced Plasmodium gallinaceum infected in white leghorn chicken assessed as increase in mean survival days of host at 60 mg/kg, sc administered 72 hrs after infection relative to control1978Journal of medicinal chemistry, Oct, Volume: 21, Issue:10
Folate antagonists. 13. 2,4-Diamino-6-](alpha,alpha,alpha-trifluoro-m-tolyl)thio]quinazoline and related 2,4-diamino-6-[(phenyl- and naphthyl)thio]quinazolines, a unique class of antimetabolites with extraordinary antimalarial and antibacterial effects.
AID1143947Antimalarial activity against Plasmodium berghei infected in mouse assessed as disease cure from parasite infection at 40 mg/kg, sc administered 72 hrs after infection1978Journal of medicinal chemistry, Oct, Volume: 21, Issue:10
Folate antagonists. 13. 2,4-Diamino-6-](alpha,alpha,alpha-trifluoro-m-tolyl)thio]quinazoline and related 2,4-diamino-6-[(phenyl- and naphthyl)thio]quinazolines, a unique class of antimetabolites with extraordinary antimalarial and antibacterial effects.
AID117288Parenteral antimalarial effect against Plasmodium berghei in mice (Mus musculus) at a dose of 640 subcutaneously mg/kg1981Journal of medicinal chemistry, Feb, Volume: 24, Issue:2
Folate antagonists. 18. Synthesis and antimalarial effects of N6-(arylmethyl)-N6-methyl-2,4,6-pteridinetriamines and related N6,N6-disubstituted 2,4,6-pteridinetriamines.
AID124828Antimalarial effect against trophozoite-induced Plasmodium berghei in mice (Mus musculus) after subcutaneous administration dose of 640 mg/kg; 5 toxic deaths1983Journal of medicinal chemistry, Dec, Volume: 26, Issue:12
Folate antagonists. 20. Synthesis and antitumor and antimalarial properties of trimetrexate and related 6-[(phenylamino)methyl]-2,4-quinazolinediamines.
AID1144000Toxicity in sporozoite-induced Plasmodium gallinaceum infected white leghorn chicken assessed as mortality at 60 mg/kg, sc administered 72 hrs after infection measured up to 6 days1978Journal of medicinal chemistry, Oct, Volume: 21, Issue:10
Folate antagonists. 13. 2,4-Diamino-6-](alpha,alpha,alpha-trifluoro-m-tolyl)thio]quinazoline and related 2,4-diamino-6-[(phenyl- and naphthyl)thio]quinazolines, a unique class of antimetabolites with extraordinary antimalarial and antibacterial effects.
AID159588Antimalarial activity as change in MST for drug-sensitive Plasmodium berghei infected mice (Mus musculus) at 640 mg/kg subcutaneous dose over 72 hr1984Journal of medicinal chemistry, Dec, Volume: 27, Issue:12
Folate antagonists. 22. Antimalarial and antibacterial effects of 2,4-diamino-6-quinazolinesulfonamides.
AID1143952Toxicity in Plasmodium berghei infected mouse assessed as mortality at 640 mg/kg, sc administered 72 hrs after infection measured after 2 to 5 days1978Journal of medicinal chemistry, Oct, Volume: 21, Issue:10
Folate antagonists. 13. 2,4-Diamino-6-](alpha,alpha,alpha-trifluoro-m-tolyl)thio]quinazoline and related 2,4-diamino-6-[(phenyl- and naphthyl)thio]quinazolines, a unique class of antimetabolites with extraordinary antimalarial and antibacterial effects.
AID1143988Toxicity in sporozoite-induced Plasmodium gallinaceum infected white leghorn chicken assessed as mortality at 240 mg/kg, sc administered 72 hrs after infection measured up to 6 days1978Journal of medicinal chemistry, Oct, Volume: 21, Issue:10
Folate antagonists. 13. 2,4-Diamino-6-](alpha,alpha,alpha-trifluoro-m-tolyl)thio]quinazoline and related 2,4-diamino-6-[(phenyl- and naphthyl)thio]quinazolines, a unique class of antimetabolites with extraordinary antimalarial and antibacterial effects.
AID449704NOVARTIS: Inhibition of Plasmodium falciparum W2 (drug-resistant) proliferation in erythrocyte-based infection assay2008Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
AID602118NOVARTIS: Antimalarial liver stage activity measured as a greater than 50% reduction in Plasmodium yoelii schizont area in HepG2-A16-CD81 cells at 10uM compound concentration, determined by immuno-fluorescence.2011Science (New York, N.Y.), Dec-09, Volume: 334, Issue:6061
Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery.
AID1144001Antimalarial activity against sporozoite-induced Plasmodium gallinaceum infected in white leghorn chicken assessed as increase in mean survival days of host at 30 mg/kg, sc administered 72 hrs after infection relative to control1978Journal of medicinal chemistry, Oct, Volume: 21, Issue:10
Folate antagonists. 13. 2,4-Diamino-6-](alpha,alpha,alpha-trifluoro-m-tolyl)thio]quinazoline and related 2,4-diamino-6-[(phenyl- and naphthyl)thio]quinazolines, a unique class of antimetabolites with extraordinary antimalarial and antibacterial effects.
AID1134790Toxicity in drug-sensitive Plasmodium berghei infected mouse at 320 mg/kg, sc administered as single dose 72 hrs post infection measured 2 to 5 days postinfection1978Journal of medicinal chemistry, Jul, Volume: 21, Issue:7
Folate antagonists. 12. Antimalarial and antibacterial effects of 2,4-diamino-6-[(aralkyl and alicyclid)thio-, sulfinyl-, and sulfonyl]quinazolines.
AID122520Mean survival time against trophozoite induced Plasmodium berghei in mice minus control was evaluated at a dose 80 mg/kg; 2 survived occurred on days 2-5 after injection1985Journal of medicinal chemistry, Feb, Volume: 28, Issue:2
Folate antagonists. 21. Synthesis and antimalarial properties of 2,4-diamino-6-(benzylamino)pyrido[3,2-d]pyrimidines.
AID1144016Antimalarial activity against DDS-resistant Plasmodium berghei assessed as drug resistance relative to control1978Journal of medicinal chemistry, Oct, Volume: 21, Issue:10
Folate antagonists. 13. 2,4-Diamino-6-](alpha,alpha,alpha-trifluoro-m-tolyl)thio]quinazoline and related 2,4-diamino-6-[(phenyl- and naphthyl)thio]quinazolines, a unique class of antimetabolites with extraordinary antimalarial and antibacterial effects.
AID124556Antimalarial effect against trophozoite-induced Plasmodium berghei in mice (Mus musculus) after subcutaneous dose of 10 mg/kg1983Journal of medicinal chemistry, Dec, Volume: 26, Issue:12
Folate antagonists. 20. Synthesis and antitumor and antimalarial properties of trimetrexate and related 6-[(phenylamino)methyl]-2,4-quinazolinediamines.
AID117133Parenteral antimalarial effect against Plasmodium berghei in mice (Mus musculus) at a dose of 160 subcutaneously mg/kg1981Journal of medicinal chemistry, Feb, Volume: 24, Issue:2
Folate antagonists. 18. Synthesis and antimalarial effects of N6-(arylmethyl)-N6-methyl-2,4,6-pteridinetriamines and related N6,N6-disubstituted 2,4,6-pteridinetriamines.
AID1134994Toxicity in trophozoite-induced Plasmodium gallinaceum infected in chick assessed as death at 30 mg/kg, sc single dose measured within 48 hrs1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
Folate antagonists. 15. 2,3-Diamino-6-(2-naphthylsulfonyl)quinazoline and related 2,4-diamino-6-[(phenyl and naphthyl)sulfinyl and sulfonyl]quinazolines, a potent new class of antimetabolites with phenomenal antimalarial activity.
AID124679Antimalarial effect against trophozoite-induced Plasmodium berghei in mice (Mus musculus) at 20 mg/kg subcutaneous dose1983Journal of medicinal chemistry, Dec, Volume: 26, Issue:12
Folate antagonists. 20. Synthesis and antitumor and antimalarial properties of trimetrexate and related 6-[(phenylamino)methyl]-2,4-quinazolinediamines.
AID1134959Antimalarial activity against trophozoite-induced Plasmodium berghei infected in mouse assessed as change in mean survival time at 10 mg/kg, sc single dose after 72 hrs of infection1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
Folate antagonists. 15. 2,3-Diamino-6-(2-naphthylsulfonyl)quinazoline and related 2,4-diamino-6-[(phenyl and naphthyl)sulfinyl and sulfonyl]quinazolines, a potent new class of antimetabolites with phenomenal antimalarial activity.
AID159574Antimalarial activity as change in MST for drug-sensitive Plasmodium berghei infected mice (Mus musculus) after 72 hrs at 320 mg/kg subcutaneous dose1984Journal of medicinal chemistry, Dec, Volume: 27, Issue:12
Folate antagonists. 22. Antimalarial and antibacterial effects of 2,4-diamino-6-quinazolinesulfonamides.
AID1134973Antimalarial activity against trophozoite-induced Plasmodium gallinaceum infected in chick assessed as mean survival time at 60 mg/kg, sc single dose (Rvb = 3.6 days)1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
Folate antagonists. 15. 2,3-Diamino-6-(2-naphthylsulfonyl)quinazoline and related 2,4-diamino-6-[(phenyl and naphthyl)sulfinyl and sulfonyl]quinazolines, a potent new class of antimetabolites with phenomenal antimalarial activity.
AID449705NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)2008Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
AID1143953Antimalarial activity against trophozoite-induced Plasmodium berghei infected in mouse assessed as daily dose required to suppression of 90% parasite infection administered with diet for 6 days1978Journal of medicinal chemistry, Oct, Volume: 21, Issue:10
Folate antagonists. 13. 2,4-Diamino-6-](alpha,alpha,alpha-trifluoro-m-tolyl)thio]quinazoline and related 2,4-diamino-6-[(phenyl- and naphthyl)thio]quinazolines, a unique class of antimetabolites with extraordinary antimalarial and antibacterial effects.
AID122504Mean survival time against trophozoite induced Plasmodium berghei in mice minus control was evaluated at a dose 40 mg/kg; 1 survived occurred on days 2-5 after injection1985Journal of medicinal chemistry, Feb, Volume: 28, Issue:2
Folate antagonists. 21. Synthesis and antimalarial properties of 2,4-diamino-6-(benzylamino)pyrido[3,2-d]pyrimidines.
AID125020Mean survival time against trophozoite induced Plasmodium berghei in mice minus control was evaluated at a dose 20 mg/kg.1985Journal of medicinal chemistry, Feb, Volume: 28, Issue:2
Folate antagonists. 21. Synthesis and antimalarial properties of 2,4-diamino-6-(benzylamino)pyrido[3,2-d]pyrimidines.
AID1143938Antimalarial activity against Plasmodium berghei infected in mouse assessed as increase in mean survival days of host at 20 mg/kg, sc administered 72 hrs after infection relative to control1978Journal of medicinal chemistry, Oct, Volume: 21, Issue:10
Folate antagonists. 13. 2,4-Diamino-6-](alpha,alpha,alpha-trifluoro-m-tolyl)thio]quinazoline and related 2,4-diamino-6-[(phenyl- and naphthyl)thio]quinazolines, a unique class of antimetabolites with extraordinary antimalarial and antibacterial effects.
AID117272Parenteral antimalarial effect against Plasmodium berghei in mice (Mus musculus) at a dose of 320 subcutaneous mg/kg1981Journal of medicinal chemistry, Feb, Volume: 24, Issue:2
Folate antagonists. 18. Synthesis and antimalarial effects of N6-(arylmethyl)-N6-methyl-2,4,6-pteridinetriamines and related N6,N6-disubstituted 2,4,6-pteridinetriamines.
AID1134958Antimalarial activity against trophozoite-induced Plasmodium berghei infected in mouse assessed as change in mean survival time at 20 mg/kg, sc single dose after 72 hrs of infection1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
Folate antagonists. 15. 2,3-Diamino-6-(2-naphthylsulfonyl)quinazoline and related 2,4-diamino-6-[(phenyl and naphthyl)sulfinyl and sulfonyl]quinazolines, a potent new class of antimetabolites with phenomenal antimalarial activity.
AID1143975Toxicity in trophozoite-induced Plasmodium gallinaceum infected white leghorn chicken assessed as mortality at 120 mg/kg, sc administered 72 hrs after infection measured after 48 hrs1978Journal of medicinal chemistry, Oct, Volume: 21, Issue:10
Folate antagonists. 13. 2,4-Diamino-6-](alpha,alpha,alpha-trifluoro-m-tolyl)thio]quinazoline and related 2,4-diamino-6-[(phenyl- and naphthyl)thio]quinazolines, a unique class of antimetabolites with extraordinary antimalarial and antibacterial effects.
AID117268Parenteral antimalarial effect against Plasmodium berghei in mice (Mus musculus) at a dose of 20sc mg/kg1981Journal of medicinal chemistry, Feb, Volume: 24, Issue:2
Folate antagonists. 18. Synthesis and antimalarial effects of N6-(arylmethyl)-N6-methyl-2,4,6-pteridinetriamines and related N6,N6-disubstituted 2,4,6-pteridinetriamines.
AID1143946Antimalarial activity against Plasmodium berghei infected in mouse assessed as disease cure from parasite infection at 80 mg/kg, sc administered 72 hrs after infection1978Journal of medicinal chemistry, Oct, Volume: 21, Issue:10
Folate antagonists. 13. 2,4-Diamino-6-](alpha,alpha,alpha-trifluoro-m-tolyl)thio]quinazoline and related 2,4-diamino-6-[(phenyl- and naphthyl)thio]quinazolines, a unique class of antimetabolites with extraordinary antimalarial and antibacterial effects.
AID159582Antimalarial activity as change in MST for drug-sensitive Plasmodium berghei infected mice (Mus musculus) at 40 mg/kg subcutaneous dose over 72 hr1984Journal of medicinal chemistry, Dec, Volume: 27, Issue:12
Folate antagonists. 22. Antimalarial and antibacterial effects of 2,4-diamino-6-quinazolinesulfonamides.
AID1134974Antimalarial activity against trophozoite-induced Plasmodium gallinaceum infected in chick assessed as mean survival time at 30 mg/kg, sc single dose (Rvb = 3.6 days)1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
Folate antagonists. 15. 2,3-Diamino-6-(2-naphthylsulfonyl)quinazoline and related 2,4-diamino-6-[(phenyl and naphthyl)sulfinyl and sulfonyl]quinazolines, a potent new class of antimetabolites with phenomenal antimalarial activity.
AID122521Mean survival time against trophozoite induced Plasmodium berghei in mice minus control was evaluated at a dose 80 mg/kg; 2 survived occurred on days 2-5 after injection. 1985Journal of medicinal chemistry, Feb, Volume: 28, Issue:2
Folate antagonists. 21. Synthesis and antimalarial properties of 2,4-diamino-6-(benzylamino)pyrido[3,2-d]pyrimidines.
AID124699Antimalarial effect against trophozoite-induced Plasmodium berghei in mice (Mus musculus) after subcutaneous administration dose of 40 mg/kg; 1 survival after 60 days1983Journal of medicinal chemistry, Dec, Volume: 26, Issue:12
Folate antagonists. 20. Synthesis and antitumor and antimalarial properties of trimetrexate and related 6-[(phenylamino)methyl]-2,4-quinazolinediamines.
AID1134957Antimalarial activity against trophozoite-induced Plasmodium berghei infected in mouse assessed as change in mean survival time at 40 mg/kg, sc single dose after 72 hrs of infection1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
Folate antagonists. 15. 2,3-Diamino-6-(2-naphthylsulfonyl)quinazoline and related 2,4-diamino-6-[(phenyl and naphthyl)sulfinyl and sulfonyl]quinazolines, a potent new class of antimetabolites with phenomenal antimalarial activity.
AID159709Antimalarial activity as change in MST for drug-sensitive Plasmodium berghei infected mice (Mus musculus) at 80 mg/kg subcutaneous dose over 72 hr1984Journal of medicinal chemistry, Dec, Volume: 27, Issue:12
Folate antagonists. 22. Antimalarial and antibacterial effects of 2,4-diamino-6-quinazolinesulfonamides.
AID1143979Antimalarial activity against trophozoite-induced Plasmodium gallinaceum infected in white leghorn chicken assessed as disease cure from parasite infection at 30 mg/kg, sc administered 72 hrs after infection1978Journal of medicinal chemistry, Oct, Volume: 21, Issue:10
Folate antagonists. 13. 2,4-Diamino-6-](alpha,alpha,alpha-trifluoro-m-tolyl)thio]quinazoline and related 2,4-diamino-6-[(phenyl- and naphthyl)thio]quinazolines, a unique class of antimetabolites with extraordinary antimalarial and antibacterial effects.
AID1143945Antimalarial activity against Plasmodium berghei infected in mouse assessed as disease cure from parasite infection at 160 mg/kg, sc administered 72 hrs after infection1978Journal of medicinal chemistry, Oct, Volume: 21, Issue:10
Folate antagonists. 13. 2,4-Diamino-6-](alpha,alpha,alpha-trifluoro-m-tolyl)thio]quinazoline and related 2,4-diamino-6-[(phenyl- and naphthyl)thio]quinazolines, a unique class of antimetabolites with extraordinary antimalarial and antibacterial effects.
AID124833Antimalarial effect against trophozoite-induced Plasmodium berghei in mice (Mus musculus) after subcutaneous after 60 days1983Journal of medicinal chemistry, Dec, Volume: 26, Issue:12
Folate antagonists. 20. Synthesis and antitumor and antimalarial properties of trimetrexate and related 6-[(phenylamino)methyl]-2,4-quinazolinediamines.
AID124690Antimalarial effect against trophozoite-induced Plasmodium berghei in mice (Mus musculus) after subcutaneous administration dose of 320 mg/kg; 3 survived after 2-5 days of injection1983Journal of medicinal chemistry, Dec, Volume: 26, Issue:12
Folate antagonists. 20. Synthesis and antitumor and antimalarial properties of trimetrexate and related 6-[(phenylamino)methyl]-2,4-quinazolinediamines.
AID1134791Antiplasmodial activity against drug-sensitive Plasmodium berghei infected in mouse assessed as cure from infection at 160 mg/kg, sc administered as single dose 72 hrs post infection measured 60 days postinfection1978Journal of medicinal chemistry, Jul, Volume: 21, Issue:7
Folate antagonists. 12. Antimalarial and antibacterial effects of 2,4-diamino-6-[(aralkyl and alicyclid)thio-, sulfinyl-, and sulfonyl]quinazolines.
AID117280Parenteral antimalarial effect against Plasmodium berghei in mice (Mus musculus) at a dose of 40 mg/kg subcutaneously1981Journal of medicinal chemistry, Feb, Volume: 24, Issue:2
Folate antagonists. 18. Synthesis and antimalarial effects of N6-(arylmethyl)-N6-methyl-2,4,6-pteridinetriamines and related N6,N6-disubstituted 2,4,6-pteridinetriamines.
AID124689Antimalarial effect against trophozoite-induced Plasmodium berghei in mice (Mus musculus) after subcutaneous administration dose of 320 mg/kg; 2 toxic deaths after 2-5 days of injection1983Journal of medicinal chemistry, Dec, Volume: 26, Issue:12
Folate antagonists. 20. Synthesis and antitumor and antimalarial properties of trimetrexate and related 6-[(phenylamino)methyl]-2,4-quinazolinediamines.
AID1134998Antimalarial activity against sporozoite-induced Plasmodium gallinaceum infected in chick assessed as change in cured at 30 mg/kg, sc single dose1979Journal of medicinal chemistry, Oct, Volume: 22, Issue:10
Folate antagonists. 15. 2,3-Diamino-6-(2-naphthylsulfonyl)quinazoline and related 2,4-diamino-6-[(phenyl and naphthyl)sulfinyl and sulfonyl]quinazolines, a potent new class of antimetabolites with phenomenal antimalarial activity.
AID125002Mean survival time against trophozoite induced Plasmodium berghei in mice minus control was evaluated at a dose 160 mg/kg; 5 survived occurred on days 2-5 after injection1985Journal of medicinal chemistry, Feb, Volume: 28, Issue:2
Folate antagonists. 21. Synthesis and antimalarial properties of 2,4-diamino-6-(benzylamino)pyrido[3,2-d]pyrimidines.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (13)

TimeframeStudies, This Drug (%)All Drugs %
pre-19907 (53.85)18.7374
1990's0 (0.00)18.2507
2000's1 (7.69)29.6817
2010's3 (23.08)24.3611
2020's2 (15.38)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.33

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 Index12.33 (24.57)
Research Supply Index2.64 (2.92)
Research Growth Index4.97 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.33)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other13 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]