Page last updated: 2024-11-05

proquazone

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

Description

Proquazone is a nonsteroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic properties. It was initially developed in the 1970s as a potential treatment for rheumatoid arthritis and other inflammatory conditions. Proquazone is synthesized through a multi-step process involving the condensation of a substituted pyrazolone with an aromatic aldehyde. The compound exhibits its pharmacological effects by inhibiting the enzyme cyclooxygenase (COX), which is responsible for the production of prostaglandins, inflammatory mediators. While proquazone demonstrated efficacy in treating inflammatory conditions, it was ultimately withdrawn from the market due to concerns about hepatotoxicity. Despite its withdrawal, proquazone remains an interesting molecule for research, particularly in the areas of inflammation and pain management. Its unique chemical structure and mechanism of action provide insights into the development of safer and more effective NSAIDs. Studies on proquazone have contributed to understanding the role of COX enzymes in inflammation and the potential for developing novel therapies.'

proquazone: nonsteroid anti-inflammatory agent; structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID31508
CHEMBL ID268501
CHEBI ID135151
SCHEMBL ID25341
MeSH IDM0057649

Synonyms (52)

Synonym
ru-43715
arthrex
proquazone
7-methyl-1-(1-methylethyl)-4-phenylquinazolin-2(1h)-one
proquazonum [inn-latin]
einecs 245-203-7
2(1h)-quinazolinone, 1-isopropyl-7-methyl-4-phenyl-
proquazona [inn-spanish]
sandoz 43-715
1-isopropyl-7-methyl-4-phenyl-2(1h)-quinazolinone
sah 43-715
biarison
brn 0889725
isopropyl-7-methyl-4-phenyl-2(1h)-quinazolinone
2(1h)-quinazolinone, 7-methyl-1-(1-methylethyl)-4-phenyl-
ru 43715
22760-18-5
proquazone (usan/inn)
D05638
arthrex (tn)
OPREA1_335846
CHEBI:135151
CHEMBL268501
7-methyl-4-phenyl-1-propan-2-ylquinazolin-2-one
proquazone [usan:inn:ban]
proquazona
unii-42vpj2980s
42vpj2980s ,
proquazonum
7-methyl-1-(1-methylethyl)-4-phenyl-2(1h)-quinazolinone
SCHEMBL25341
proquazone [jan]
proquazone [usan]
proquazone [who-dd]
proquazone [mart.]
proquazone [mi]
proquazone [inn]
7-methyl-1-isopropyl-4-phenyl-2(1h)-quinazolinone
7-methyl-1-isopropyl-4-phenyl-quinazolin-2(1h)-one
1-isopropyl-4-phenyl-7-methyl-2(1h)-quinazolinone
JTIGKVIOEQASGT-UHFFFAOYSA-N
1-isopropyl-4-phenyl-7-methyl-2[1h]quinazolinone
DTXSID4021210
SR-01000945079-1
sr-01000945079
AKOS030227983
7-methyl-4-phenyl-1-(propan-2-yl)-1,2-dihydroquinazolin-2-one
AS-69800
DB13649
bdbm50225112
Q7250480
anthrex; biarison;ru 43-715; san 43-715

Research Excerpts

Overview

Proquazone is a non-steroidal anti-inflammatory agent (NSAID) which, unlike most other NSAIDs, does not have a free acid group in its structure. It is orally effective as an anti- inflammatory, analgesic and anti-pyretic in animals.

ExcerptReferenceRelevance
"Proquazone is a chemically distinctive non-steroidal anti-inflammatory drug (NSAID) and is orally effective as an anti-inflammatory, analgesic and anti-pyretic in animals. "( The toxicology profile of the anti-inflammatory drug proquazone in animals.
Trapold, JH; Van Ryzin, RJ, 1980
)
1.95
"Proquazone is a non-steroidal anti-inflammatory agent (NSAID) which, unlike most other NSAIDs, does not have a free acid group in its structure. "( Proquazone. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in rheumatic diseases and pain states.
Beresford, R; Clissold, SP, 1987
)
3.16

Pharmacokinetics

ExcerptReferenceRelevance
" The method described is suitable for routine clinical and pharmacokinetic studies."( Determination of proquazone and its m-hydroxy metabolite by high-performance liquid chromatography. Clinical application: pharmacokinetics of proquazone in children with juvenile rheumatoid arthritis.
Lempiäinen, M; Mäkelä, AL, 1985
)
0.61

Bioavailability

ExcerptReferenceRelevance
" The only effect of antacid, compared to fasting, was to slow the rate of absorption without appreciably altering the extent of absorption."( The effect of antacid and food on the absorption of proquazone (Biarison) in man.
Ohnhaus, EE, 1980
)
0.51

Dosage Studied

Each dosage level of proquazone and aspirin provided significant analgesia compared to placebo and was well tolerated.

ExcerptRelevanceReference
" For adequate intravenous dosing of the poorly water-soluble proquazone, advantage was taken of the high degree of protein binding of the drug."( Pharmacokinetics of the antirheumatic proquazone in healthy humans.
Hinderling, PH; Roos, A, 1984
)
0.78
" Each dosage level of proquazone and aspirin provided significant analgesia compared to placebo and was well tolerated."( An evaluation of the analgesic efficacy of proquazone and aspirin in postoperative dental pain.
Forbes, JA; Hughes, MK; White, EH; White, RW, 1980
)
0.84
" The difference between the 2 groups, however, was not statistically significant, indicating an advantage for the lower daily dosage regimen over the high daily dosage regimen."( Proquazone ('Biarison') in osteoarthritis of the knee: a double-blind, dose comparison trial.
Serry, MM, 1980
)
1.7
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
pyrimidinesAny compound having a pyrimidine as part of its structure.
[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 (4)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Prostaglandin-H2 D-isomeraseMus musculus (house mouse)IC50 (µMol)0.07000.07000.53401.1000AID160887
Prostaglandin G/H synthase 1 Bos taurus (cattle)IC50 (µMol)0.07000.00051.41288.2000AID160887
Prostaglandin G/H synthase 2 Bos taurus (cattle)IC50 (µMol)0.07000.00050.57393.4000AID160887
Epidermal growth factor receptorHomo sapiens (human)IC50 (µMol)0.00200.00000.536910.0000AID1915705
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (100)

Processvia Protein(s)Taxonomy
response to oxidative stressProstaglandin G/H synthase 1 Bos taurus (cattle)
cellular oxidant detoxificationProstaglandin G/H synthase 1 Bos taurus (cattle)
meiotic spindle organizationProstaglandin G/H synthase 2 Bos taurus (cattle)
prostaglandin biosynthetic processProstaglandin G/H synthase 2 Bos taurus (cattle)
ovarian cumulus expansionProstaglandin G/H synthase 2 Bos taurus (cattle)
positive regulation of protein phosphorylationProstaglandin G/H synthase 2 Bos taurus (cattle)
response to oxidative stressProstaglandin G/H synthase 2 Bos taurus (cattle)
cyclooxygenase pathwayProstaglandin G/H synthase 2 Bos taurus (cattle)
positive regulation of embryonic developmentProstaglandin G/H synthase 2 Bos taurus (cattle)
cellular response to interleukin-1Prostaglandin G/H synthase 2 Bos taurus (cattle)
cellular oxidant detoxificationProstaglandin G/H synthase 2 Bos taurus (cattle)
regulation of neuroinflammatory responseProstaglandin G/H synthase 2 Bos taurus (cattle)
positive regulation of oocyte maturationProstaglandin G/H synthase 2 Bos taurus (cattle)
positive regulation of meiotic cell cycle process involved in oocyte maturationProstaglandin G/H synthase 2 Bos taurus (cattle)
cell surface receptor signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
epidermal growth factor receptor signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cell population proliferationEpidermal growth factor receptorHomo sapiens (human)
MAPK cascadeEpidermal growth factor receptorHomo sapiens (human)
ossificationEpidermal growth factor receptorHomo sapiens (human)
embryonic placenta developmentEpidermal growth factor receptorHomo sapiens (human)
positive regulation of protein phosphorylationEpidermal growth factor receptorHomo sapiens (human)
hair follicle developmentEpidermal growth factor receptorHomo sapiens (human)
translationEpidermal growth factor receptorHomo sapiens (human)
signal transductionEpidermal growth factor receptorHomo sapiens (human)
epidermal growth factor receptor signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
activation of phospholipase C activityEpidermal growth factor receptorHomo sapiens (human)
salivary gland morphogenesisEpidermal growth factor receptorHomo sapiens (human)
midgut developmentEpidermal growth factor receptorHomo sapiens (human)
learning or memoryEpidermal growth factor receptorHomo sapiens (human)
circadian rhythmEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cell population proliferationEpidermal growth factor receptorHomo sapiens (human)
diterpenoid metabolic processEpidermal growth factor receptorHomo sapiens (human)
peptidyl-tyrosine phosphorylationEpidermal growth factor receptorHomo sapiens (human)
cerebral cortex cell migrationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cell growthEpidermal growth factor receptorHomo sapiens (human)
lung developmentEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cell migrationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of superoxide anion generationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationEpidermal growth factor receptorHomo sapiens (human)
response to cobalaminEpidermal growth factor receptorHomo sapiens (human)
response to hydroxyisoflavoneEpidermal growth factor receptorHomo sapiens (human)
cellular response to reactive oxygen speciesEpidermal growth factor receptorHomo sapiens (human)
peptidyl-tyrosine autophosphorylationEpidermal growth factor receptorHomo sapiens (human)
ERBB2-EGFR signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
negative regulation of epidermal growth factor receptor signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
negative regulation of protein catabolic processEpidermal growth factor receptorHomo sapiens (human)
vasodilationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of phosphorylationEpidermal growth factor receptorHomo sapiens (human)
ovulation cycleEpidermal growth factor receptorHomo sapiens (human)
hydrogen peroxide metabolic processEpidermal growth factor receptorHomo sapiens (human)
negative regulation of apoptotic processEpidermal growth factor receptorHomo sapiens (human)
positive regulation of MAP kinase activityEpidermal growth factor receptorHomo sapiens (human)
tongue developmentEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cyclin-dependent protein serine/threonine kinase activityEpidermal growth factor receptorHomo sapiens (human)
positive regulation of DNA repairEpidermal growth factor receptorHomo sapiens (human)
positive regulation of DNA replicationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of bone resorptionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of DNA-templated transcriptionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of vasoconstrictionEpidermal growth factor receptorHomo sapiens (human)
negative regulation of mitotic cell cycleEpidermal growth factor receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIEpidermal growth factor receptorHomo sapiens (human)
regulation of JNK cascadeEpidermal growth factor receptorHomo sapiens (human)
symbiont entry into host cellEpidermal growth factor receptorHomo sapiens (human)
protein autophosphorylationEpidermal growth factor receptorHomo sapiens (human)
astrocyte activationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of fibroblast proliferationEpidermal growth factor receptorHomo sapiens (human)
digestive tract morphogenesisEpidermal growth factor receptorHomo sapiens (human)
positive regulation of smooth muscle cell proliferationEpidermal growth factor receptorHomo sapiens (human)
neuron projection morphogenesisEpidermal growth factor receptorHomo sapiens (human)
epithelial cell proliferationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of epithelial cell proliferationEpidermal growth factor receptorHomo sapiens (human)
regulation of peptidyl-tyrosine phosphorylationEpidermal growth factor receptorHomo sapiens (human)
protein insertion into membraneEpidermal growth factor receptorHomo sapiens (human)
response to calcium ionEpidermal growth factor receptorHomo sapiens (human)
regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of synaptic transmission, glutamatergicEpidermal growth factor receptorHomo sapiens (human)
positive regulation of glial cell proliferationEpidermal growth factor receptorHomo sapiens (human)
morphogenesis of an epithelial foldEpidermal growth factor receptorHomo sapiens (human)
eyelid development in camera-type eyeEpidermal growth factor receptorHomo sapiens (human)
response to UV-AEpidermal growth factor receptorHomo sapiens (human)
positive regulation of mucus secretionEpidermal growth factor receptorHomo sapiens (human)
regulation of ERK1 and ERK2 cascadeEpidermal growth factor receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeEpidermal growth factor receptorHomo sapiens (human)
cellular response to amino acid stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to mechanical stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to cadmium ionEpidermal growth factor receptorHomo sapiens (human)
cellular response to epidermal growth factor stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to estradiol stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to xenobiotic stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to dexamethasone stimulusEpidermal growth factor receptorHomo sapiens (human)
positive regulation of canonical Wnt signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
liver regenerationEpidermal growth factor receptorHomo sapiens (human)
cell-cell adhesionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of protein kinase C activityEpidermal growth factor receptorHomo sapiens (human)
positive regulation of G1/S transition of mitotic cell cycleEpidermal growth factor receptorHomo sapiens (human)
positive regulation of non-canonical NF-kappaB signal transductionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of prolactin secretionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of miRNA transcriptionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of protein localization to plasma membraneEpidermal growth factor receptorHomo sapiens (human)
negative regulation of cardiocyte differentiationEpidermal growth factor receptorHomo sapiens (human)
neurogenesisEpidermal growth factor receptorHomo sapiens (human)
multicellular organism developmentEpidermal growth factor receptorHomo sapiens (human)
positive regulation of kinase activityEpidermal growth factor receptorHomo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (28)

Processvia Protein(s)Taxonomy
peroxidase activityProstaglandin G/H synthase 1 Bos taurus (cattle)
heme bindingProstaglandin G/H synthase 1 Bos taurus (cattle)
metal ion bindingProstaglandin G/H synthase 1 Bos taurus (cattle)
peroxidase activityProstaglandin G/H synthase 2 Bos taurus (cattle)
prostaglandin-endoperoxide synthase activityProstaglandin G/H synthase 2 Bos taurus (cattle)
heme bindingProstaglandin G/H synthase 2 Bos taurus (cattle)
metal ion bindingProstaglandin G/H synthase 2 Bos taurus (cattle)
epidermal growth factor receptor activityEpidermal growth factor receptorHomo sapiens (human)
virus receptor activityEpidermal growth factor receptorHomo sapiens (human)
chromatin bindingEpidermal growth factor receptorHomo sapiens (human)
double-stranded DNA bindingEpidermal growth factor receptorHomo sapiens (human)
MAP kinase kinase kinase activityEpidermal growth factor receptorHomo sapiens (human)
protein tyrosine kinase activityEpidermal growth factor receptorHomo sapiens (human)
transmembrane receptor protein tyrosine kinase activityEpidermal growth factor receptorHomo sapiens (human)
transmembrane signaling receptor activityEpidermal growth factor receptorHomo sapiens (human)
epidermal growth factor receptor activityEpidermal growth factor receptorHomo sapiens (human)
integrin bindingEpidermal growth factor receptorHomo sapiens (human)
protein bindingEpidermal growth factor receptorHomo sapiens (human)
calmodulin bindingEpidermal growth factor receptorHomo sapiens (human)
ATP bindingEpidermal growth factor receptorHomo sapiens (human)
enzyme bindingEpidermal growth factor receptorHomo sapiens (human)
kinase bindingEpidermal growth factor receptorHomo sapiens (human)
protein kinase bindingEpidermal growth factor receptorHomo sapiens (human)
protein phosphatase bindingEpidermal growth factor receptorHomo sapiens (human)
protein tyrosine kinase activator activityEpidermal growth factor receptorHomo sapiens (human)
transmembrane receptor protein tyrosine kinase activator activityEpidermal growth factor receptorHomo sapiens (human)
ubiquitin protein ligase bindingEpidermal growth factor receptorHomo sapiens (human)
identical protein bindingEpidermal growth factor receptorHomo sapiens (human)
cadherin bindingEpidermal growth factor receptorHomo sapiens (human)
actin filament bindingEpidermal growth factor receptorHomo sapiens (human)
ATPase bindingEpidermal growth factor receptorHomo sapiens (human)
epidermal growth factor bindingEpidermal growth factor receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (29)

Processvia Protein(s)Taxonomy
nucleoplasmProstaglandin-H2 D-isomeraseMus musculus (house mouse)
endoplasmic reticulum membraneProstaglandin G/H synthase 1 Bos taurus (cattle)
nuclear inner membraneProstaglandin G/H synthase 2 Bos taurus (cattle)
nuclear outer membraneProstaglandin G/H synthase 2 Bos taurus (cattle)
endoplasmic reticulum membraneProstaglandin G/H synthase 2 Bos taurus (cattle)
endosomeEpidermal growth factor receptorHomo sapiens (human)
plasma membraneEpidermal growth factor receptorHomo sapiens (human)
ruffle membraneEpidermal growth factor receptorHomo sapiens (human)
Golgi membraneEpidermal growth factor receptorHomo sapiens (human)
extracellular spaceEpidermal growth factor receptorHomo sapiens (human)
nucleusEpidermal growth factor receptorHomo sapiens (human)
cytoplasmEpidermal growth factor receptorHomo sapiens (human)
endosomeEpidermal growth factor receptorHomo sapiens (human)
endoplasmic reticulum membraneEpidermal growth factor receptorHomo sapiens (human)
plasma membraneEpidermal growth factor receptorHomo sapiens (human)
focal adhesionEpidermal growth factor receptorHomo sapiens (human)
cell surfaceEpidermal growth factor receptorHomo sapiens (human)
endosome membraneEpidermal growth factor receptorHomo sapiens (human)
membraneEpidermal growth factor receptorHomo sapiens (human)
basolateral plasma membraneEpidermal growth factor receptorHomo sapiens (human)
apical plasma membraneEpidermal growth factor receptorHomo sapiens (human)
cell junctionEpidermal growth factor receptorHomo sapiens (human)
clathrin-coated endocytic vesicle membraneEpidermal growth factor receptorHomo sapiens (human)
early endosome membraneEpidermal growth factor receptorHomo sapiens (human)
nuclear membraneEpidermal growth factor receptorHomo sapiens (human)
membrane raftEpidermal growth factor receptorHomo sapiens (human)
perinuclear region of cytoplasmEpidermal growth factor receptorHomo sapiens (human)
multivesicular body, internal vesicle lumenEpidermal growth factor receptorHomo sapiens (human)
intracellular vesicleEpidermal growth factor receptorHomo sapiens (human)
protein-containing complexEpidermal growth factor receptorHomo sapiens (human)
receptor complexEpidermal growth factor receptorHomo sapiens (human)
Shc-EGFR complexEpidermal growth factor receptorHomo sapiens (human)
basal plasma membraneEpidermal growth factor receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (36)

Assay IDTitleYearJournalArticle
AID187314Relative Oral Anti inflammatory activity in the 5-h Evans Blue-Carrageenan pleural assay using indomethacin as reference compound1984Journal of medicinal chemistry, Oct, Volume: 27, Issue:10
Antiinflammatory activity of N-(2-benzoylphenyl)alanine derivatives.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID177006Anti-inflammatory activity following oral administration1985Journal of medicinal chemistry, May, Volume: 28, Issue:5
Studies on 4(1H)-quinazolinones. 5. Synthesis and antiinflammatory activity of 4(1H)-quinazolinone derivatives.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID185400Percent inhibition against carrageenan-induced rat paw edema at 50 mg/kg dose administered perorally; 41-50%1985Journal of medicinal chemistry, May, Volume: 28, Issue:5
Studies on 4(1H)-quinazolinones. 5. Synthesis and antiinflammatory activity of 4(1H)-quinazolinone derivatives.
AID160887Inhibition of PG synthetase activity obtained from bovine seminal vesicles1984Journal of medicinal chemistry, Oct, Volume: 27, Issue:10
Antiinflammatory activity of N-(2-benzoylphenyl)alanine derivatives.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID177004Analgesic activity by oral administration route1985Journal of medicinal chemistry, May, Volume: 28, Issue:5
Studies on 4(1H)-quinazolinones. 5. Synthesis and antiinflammatory activity of 4(1H)-quinazolinone derivatives.
AID185055Nonnarcotic analgesic effect was determined after peroral administration in rats.1982Journal of medicinal chemistry, Sep, Volume: 25, Issue:9
Antiinflammatory properties of 8-aryl-5-isopropyl-2H-1,3-dioxolo[4,5-g]quinazolin-6(5H)-ones and -thiones.
AID123255Toxicity by number of mice dead at dose 500 mg/kg out of 5 mice tested by oral administration route; Value represented as 0/51985Journal of medicinal chemistry, May, Volume: 28, Issue:5
Studies on 4(1H)-quinazolinones. 5. Synthesis and antiinflammatory activity of 4(1H)-quinazolinone derivatives.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID177891Inhibition of carrageenan edema in rats was determined after peroral administration of 100 mg/kg1982Journal of medicinal chemistry, Sep, Volume: 25, Issue:9
Antiinflammatory properties of 8-aryl-5-isopropyl-2H-1,3-dioxolo[4,5-g]quinazolin-6(5H)-ones and -thiones.
AID118116Number of mice bearing ulcer at dose 30 mg/kg out of 5 mices tested1985Journal of medicinal chemistry, May, Volume: 28, Issue:5
Studies on 4(1H)-quinazolinones. 5. Synthesis and antiinflammatory activity of 4(1H)-quinazolinone derivatives.
AID177890Inhibition of carrageenan edema in normal rats was determined after peroral administration1982Journal of medicinal chemistry, Sep, Volume: 25, Issue:9
Antiinflammatory properties of 8-aryl-5-isopropyl-2H-1,3-dioxolo[4,5-g]quinazolin-6(5H)-ones and -thiones.
AID1915705Inhibition of EGFR (unknown origin)2021European journal of medicinal chemistry, Feb-05, Volume: 211Therapeutic progression of quinazolines as targeted chemotherapeutic agents.
AID178986Inhibition of the development of adjuvant-induced polyarthritis in rats was determined1982Journal of medicinal chemistry, Sep, Volume: 25, Issue:9
Antiinflammatory properties of 8-aryl-5-isopropyl-2H-1,3-dioxolo[4,5-g]quinazolin-6(5H)-ones and -thiones.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID123868Ulcer index by number of mice bearing ulcer at dose 30 mg/kg out of 5 mice tested1985Journal of medicinal chemistry, May, Volume: 28, Issue:5
Studies on 4(1H)-quinazolinones. 5. Synthesis and antiinflammatory activity of 4(1H)-quinazolinone derivatives.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1712996Selectivity for COX-2 (unknown origin) over COX-1 (unknown origin)2016European journal of medicinal chemistry, Oct-04, Volume: 121Synthesis, anti-inflammatory, analgesic, COX-1/2 inhibitory activities and molecular docking studies of substituted 2-mercapto-4(3H)-quinazolinones.
AID1132863Antiinflammatory activity in po dosed rat assessed as inhibition of carrageenan-induced foot edema compound administered 1 hr before carrageenan challenge measured after 3 to 3.5 hrs relative to untreated control1978Journal of medicinal chemistry, Jul, Volume: 21, Issue:7
Synthesis and antiinflammatory activity of trisubstituted pyrimidines and triazines.
AID177889Inhibition of carrageenan edema in adrenalectomized rats was determined after peroral administration1982Journal of medicinal chemistry, Sep, Volume: 25, Issue:9
Antiinflammatory properties of 8-aryl-5-isopropyl-2H-1,3-dioxolo[4,5-g]quinazolin-6(5H)-ones and -thiones.
AID588220Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset2008Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (43)

TimeframeStudies, This Drug (%)All Drugs %
pre-199036 (83.72)18.7374
1990's1 (2.33)18.2507
2000's4 (9.30)29.6817
2010's1 (2.33)24.3611
2020's1 (2.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 22.39

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index22.39 (24.57)
Research Supply Index4.16 (2.92)
Research Growth Index4.91 (4.65)
Search Engine Demand Index23.28 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (22.39)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials15 (31.25%)5.53%
Reviews4 (8.33%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other29 (60.42%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]