Page last updated: 2024-12-06

dazoxiben

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

Description

Dazoxiben is a synthetic, potent, and selective inhibitor of thromboxane synthase. It inhibits the biosynthesis of thromboxane A2 (TXA2), a potent vasoconstrictor and platelet aggregator, by preventing the conversion of prostaglandin H2 to TXA2. Dazoxiben is an anti-platelet agent that has been studied for the treatment of cardiovascular diseases such as thrombosis and stroke. Its selective inhibition of TXA2 is believed to contribute to its anti-thrombotic effects. It has also been investigated for its potential anti-inflammatory and anti-tumor properties. Dazoxiben is synthesized via a multi-step process that involves the reaction of 1,3-diphenyl-2-propen-1-one with ethyl acetoacetate. The resulting product is then reacted with hydrazine hydrate to yield the desired dazoxiben molecule.'

dazoxiben: RN given refers to parent cpd [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID53001
CHEMBL ID267473
SCHEMBL ID11554
MeSH IDM0093222

Synonyms (53)

Synonym
ah-p 719
4-(2-(1-imidazolyl)ethoxy)benzoic acid
ah-p-719
ah-p719
103735-00-8
4-[2-(1h-imidazol-1-yl)ethoxy]benzoic acid
CBDIVE_009681
4-(2-imidazol-1-yl-ethoxy)-benzoic acid; hydrochloride
chembl267473 ,
bdbm7962
4-(2-imidazol-1-yl-ethoxy)-benzoic acid
imidazole n-1 deriv. 13
DB03052
dazoxibene [inn-french]
uk 37248
p-(2-imidazol-1-ylethoxy)benzoic acid
dazoxiben [inn-spanish]
dazoxiben [inn:ban]
benzoic acid, 4-(2-(1h-imidazol-1-yl)ethoxy)-
4-(2-(1-imidazolyl)ethoxy)benzoesaeure
dazoxibenum [inn-latin]
dazoxiben
OPREA1_249918
NCGC00023830-02
NCGC00018938-01
4-(2-imidazol-1-ylethoxy)benzoic acid
NCGC00018938-03
4-[2-(1-imidazolyl)ethoxy]benzoic acid
A839366
78218-09-4
NCGC00018938-02
AKOS005872303
tox21_110859
dtxsid9045639 ,
dtxcid7025639
cas-78218-09-4
dazoxibene
09zfc7974q ,
unii-09zfc7974q
dazoxibenum
FT-0603126
dazoxiben [inn]
gtpl5175
MLS006010101
smr000059716
SCHEMBL11554
1-[2-(4-carboxyphenoxy)ethyl]imidazole
XQGZSYKGWHUSDH-UHFFFAOYSA-N
4-[2-(imidazol-1-yl)ethoxy]benzoic acid
4-(2-(1h-imidazol-1-yl)ethoxy)benzoic acid
Q5243688
AS-14224
dazoxiben free base

Research Excerpts

Overview

Dazoxiben is a selective and effective thromboxane synthetase inhibitor. It has a weaker effect on platelet reactivity than ASA, possibly because endoperoxide formation is not prevented.

ExcerptReferenceRelevance
"Dazoxiben is a selective inhibitor of thromboxane synthetase, with no effect on prostacyclin synthetase."( A thromboxane synthetase inhibitor in Raynaud's phenomenon.
Hawkey, CJ; Jones, EW, 1983
)
0.99
"7 Dazoxiben is an effective inhibitor of the synthesis of thromboxane but it has no effect on the subjective or objective features of stable coronary disease."( Effects of dazoxiben on exercise performance in chronic stable angina.
Cairns, J; Gyde, OH; Kuan, P; Reuben, SR, 1983
)
1.21
"Dazoxiben is a selective and effective thromboxane synthetase inhibitor, but has a weaker effect on platelet reactivity than ASA, possibly because endoperoxide formation is not prevented."( The effect of a thromboxane synthetase inhibitor, dazoxiben, and acetylsalicylic acid on platelet function and prostaglandin metabolism.
Dale, J; Myhre, E; Parry, J; Thaulow, E, 1983
)
1.24

Actions

Dazoxiben blocked the increase in thromboxane B2 level in lung but not in kidney. lowered the lung, but not the kidney albumin leak index.

ExcerptReferenceRelevance
"Dazoxiben blocked the increase in thromboxane B2 level in lung but not in kidney and lowered the lung but not the kidney albumin leak index."( Tissue eicosanoids and vascular permeability in rats with chronic biliary obstruction.
Chang, SW; Ohara, N; Voelkel, NF, 1993
)
1.01
"Dazoxiben blocked the increase in plasma TXB2, prevented pulmonary hypertension, and attenuated the increase in EVLW after E."( Indomethacin, dazoxiben and extravascular lung water after Escherichia coli infusion.
Carrico, CJ; Harlan, J; Hildebrandt, J; Price, S; Winn, R, 1986
)
1.35

Treatment

In dazoxiben-treated animals the rise in plasma concentrations of TXB2 after endotoxin was prevented. In daz Oxiben pretreatment also moderated the rise of plasma prostacyclin, but it augmented circulating prostaglandin E2 following SAO.

ExcerptReferenceRelevance
"3 In dazoxiben-treated animals the rise in plasma concentrations of TXB2 after endotoxin was prevented and, in concert, the increase in pulmonary artery and wedge pressures, the fall in cardiac output, and the initial increase in lymph flow were greatly attenuated."( Selective inhibition of thromboxane synthesis during experimental endotoxemia in the goat: effects on pulmonary haemodynamics and lung lymph flow.
Harker, L; Harlan, J; Hildebrandt, J; Winn, R, 1983
)
0.72
"In dazoxiben-treated animals, plasma concentrations of T X B2 were never significantly elevated."( Thromboxane A2 mediates lung vasoconstriction but not permeability after endotoxin.
Harker, L; Harlan, J; Hildebrandt, J; Nadir, B; Winn, R, 1983
)
0.78
"Dazoxiben pretreatment also moderated the rise of plasma prostacyclin, but it augmented circulating prostaglandin E2 following the release of SAO."( Inhibition of thromboxane biosynthesis in splanchnic ischemia shock.
Glenn, TM; Oei, HH; Robson, RD; Sakane, Y; Zoganas, HC, 1986
)
0.99

Toxicity

ExcerptReferenceRelevance
" Studies in rats and rabbits at dose levels up to 400 mg day-1 kg-1, by mouth, revealed no adverse effects on male or female fertility, embryogenesis, parturition or postnatal development."( Dazoxiben, a prototype inhibitor of thromboxane synthesis, has little toxicity in laboratory animals.
Charuel, C; Faccini, JM; Greaves, P; Irisarri, E; Kessedjian, MJ; Monro, AM; Nachbaur, J; Rabémampianina, Y, 1985
)
1.71

Bioavailability

ExcerptReferenceRelevance
" As dazoxiben is well absorbed after oral administration, the generally negative outcome to these toxicity studies suggests that selective inhibitors of thromboxane synthesis may be largely free of adverse effects which might impede their therapeutic or prophylactic use in clinical medicine."( Dazoxiben, a prototype inhibitor of thromboxane synthesis, has little toxicity in laboratory animals.
Charuel, C; Faccini, JM; Greaves, P; Irisarri, E; Kessedjian, MJ; Monro, AM; Nachbaur, J; Rabémampianina, Y, 1985
)
2.27
"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

Dosage Studied

Dazoxiben at this dosage is unlikely to be of practical clinical benefit in Raynaud's phenomenon. However, twice daily dosing with daz Oxiben was effective.

ExcerptRelevanceReference
" Since none of the compounds tested produced a sustained inhibition of TXA2 synthesis, the disappointing clinical results with this class of drugs may be due to an incomplete blockade of thromboxane synthase with the dosage regimens used."( Preliminary clinical studies with thromboxane synthase inhibitors and thromboxane receptor blockers. A review.
Fiddler, GI; Lumley, P, 1990
)
0.28
" However, twice daily dosing with dazoxiben was effective."( Prolongation of platelet survival in hypercholesterolaemic rabbits by CGS 12970 (3-methyl-2-(3-pyridyl)-1 indoleoctanoic acid) and dazoxiben.
Ambler, J; Butler, KD; Butler, PA; Shand, RA; Wallis, RB, 1987
)
0.76
" Alternatively, the lack of drug efficacy may have resulted from either incomplete suppression of thromboxane biosynthesis and/or substitution for the biological effects of thromboxane A2 by prostaglandin endoperoxides during long-term dosing studies."( The biochemical pharmacology of thromboxane synthase inhibition in man.
FitzGerald, GA; Pedersen, AK; Reilly, IA, 1985
)
0.27
" In addition, because frequent repeated and synchronous dosing of aspirin was necessary, aspirin's potentiating effects appear to be produced by mechanism(s) unrelated to its potent, irreversible inhibition of platelet cyclooxygenase."( Effects of platelet-modifying drugs on arterial thromboembolism in baboons. Aspirin potentiates the antithrombotic actions of dipyridamole and sulfinpyrazone by mechanism(s) independent of platelet cyclooxygenase inhibition.
Bjornsson, TD; Hanson, SR; Harker, LA, 1985
)
0.27
" Serum thromboxane B2 and aggregation studies in whole blood and platelet-rich plasma were measured before dosing and at 1, 4, 6, 8, and 24 h after dosing."( Endogenous prostacyclin biosynthesis and platelet function during selective inhibition of thromboxane synthase in man.
Brash, AR; FitzGerald, GA; Oates, JA; Pedersen, AK, 1983
)
0.27
" We conclude that dazoxiben at this dosage is unlikely to be of practical clinical benefit in Raynaud's phenomenon."( A thromboxane synthetase inhibitor in Raynaud's phenomenon.
Hawkey, CJ; Jones, EW, 1983
)
0.6
" On oral dosing (10 mg/kg) to rats and dogs, 110 showed significant TXRA activity [concentration ratio > 64 (rat, 3 h) and > 59 +/- 11."( A novel approach to dual-acting thromboxane receptor antagonist/synthase inhibitors based on the link of 1,3-dioxane-thromboxane receptor antagonists and -thromboxane synthase inhibitors.
Ackerley, N; Brewster, AG; Brown, GR; Clarke, DS; Foubister, AJ; Griffin, SJ; Hudson, JA; Smithers, MJ; Whittamore, PR, 1995
)
0.29
" The dose-response curves to serotonin obtained in the SHR were shifted to the left compared to the WKY."( Serotonin releases a vasoconstrictor prostanoid in the kidney of the aging spontaneously hypertensive rat.
Tuncer, M; Vanhoutte, PM, 1993
)
0.29
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (10)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency35.48130.00798.23321,122.0200AID2551
[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)
Bile salt export pumpHomo sapiens (human)IC50 (µMol)1,000.00000.11007.190310.0000AID1449628
AromataseHomo sapiens (human)IC50 (µMol)1.10000.00001.290410.0000AID1796390
Cytochrome P450 11B1, mitochondrialRattus norvegicus (Norway rat)IC50 (µMol)100.00000.49503.52895.0000AID3094; AID3095
Thromboxane-A synthase Homo sapiens (human)IC50 (µMol)0.59850.00091.230410.0000AID154268; AID1796390; AID210318; AID210319; AID210502; AID212634; AID212779; AID212955; AID212966; AID212967; AID213139; AID215621; AID215771; AID215772; AID215773
Prostaglandin G/H synthase 2 Rattus norvegicus (Norway rat)IC50 (µMol)100.00000.00291.786810.0000AID161007
Thromboxane-A synthaseRattus norvegicus (Norway rat)IC50 (µMol)0.95120.00400.39231.5000AID210480; AID212800; AID213112; AID213131; AID213134
Glutaminyl-peptide cyclotransferaseHomo sapiens (human)Ki2.30000.26202.93587.0000AID1796109
Prostaglandin G/H synthase 1 Rattus norvegicus (Norway rat)IC50 (µMol)100.00000.00291.823210.0000AID161007
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (56)

Processvia Protein(s)Taxonomy
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
negative regulation of chronic inflammatory responseAromataseHomo sapiens (human)
steroid biosynthetic processAromataseHomo sapiens (human)
estrogen biosynthetic processAromataseHomo sapiens (human)
androgen catabolic processAromataseHomo sapiens (human)
syncytium formationAromataseHomo sapiens (human)
negative regulation of macrophage chemotaxisAromataseHomo sapiens (human)
sterol metabolic processAromataseHomo sapiens (human)
female genitalia developmentAromataseHomo sapiens (human)
mammary gland developmentAromataseHomo sapiens (human)
uterus developmentAromataseHomo sapiens (human)
prostate gland growthAromataseHomo sapiens (human)
testosterone biosynthetic processAromataseHomo sapiens (human)
positive regulation of estradiol secretionAromataseHomo sapiens (human)
female gonad developmentAromataseHomo sapiens (human)
response to estradiolAromataseHomo sapiens (human)
prostaglandin biosynthetic processThromboxane-A synthase Homo sapiens (human)
icosanoid metabolic processThromboxane-A synthase Homo sapiens (human)
cyclooxygenase pathwayThromboxane-A synthase Homo sapiens (human)
intracellular chloride ion homeostasisThromboxane-A synthase Homo sapiens (human)
response to ethanolThromboxane-A synthase Homo sapiens (human)
positive regulation of vasoconstrictionThromboxane-A synthase Homo sapiens (human)
response to fatty acidThromboxane-A synthase Homo sapiens (human)
prostaglandin biosynthetic processProstacyclin synthaseHomo sapiens (human)
icosanoid metabolic processProstacyclin synthaseHomo sapiens (human)
cyclooxygenase pathwayProstacyclin synthaseHomo sapiens (human)
negative regulation of NF-kappaB transcription factor activityProstacyclin synthaseHomo sapiens (human)
NAD biosynthesis via nicotinamide riboside salvage pathwayProstacyclin synthaseHomo sapiens (human)
positive regulation of peroxisome proliferator activated receptor signaling pathwayProstacyclin synthaseHomo sapiens (human)
negative regulation of nitric oxide biosynthetic processProstacyclin synthaseHomo sapiens (human)
positive regulation of angiogenesisProstacyclin synthaseHomo sapiens (human)
negative regulation of inflammatory responseProstacyclin synthaseHomo sapiens (human)
cellular response to interleukin-1Prostacyclin synthaseHomo sapiens (human)
cellular response to interleukin-6Prostacyclin synthaseHomo sapiens (human)
cellular response to hypoxiaProstacyclin synthaseHomo sapiens (human)
apoptotic signaling pathwayProstacyclin synthaseHomo sapiens (human)
positive regulation of execution phase of apoptosisProstacyclin synthaseHomo sapiens (human)
peptidyl-pyroglutamic acid biosynthetic process, using glutaminyl-peptide cyclotransferaseGlutaminyl-peptide cyclotransferaseHomo sapiens (human)
protein modification processGlutaminyl-peptide cyclotransferaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (23)

Processvia Protein(s)Taxonomy
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
iron ion bindingAromataseHomo sapiens (human)
steroid hydroxylase activityAromataseHomo sapiens (human)
electron transfer activityAromataseHomo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenAromataseHomo sapiens (human)
oxygen bindingAromataseHomo sapiens (human)
heme bindingAromataseHomo sapiens (human)
aromatase activityAromataseHomo sapiens (human)
monooxygenase activityThromboxane-A synthase Homo sapiens (human)
thromboxane-A synthase activityThromboxane-A synthase Homo sapiens (human)
iron ion bindingThromboxane-A synthase Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygenThromboxane-A synthase Homo sapiens (human)
heme bindingThromboxane-A synthase Homo sapiens (human)
12-hydroxyheptadecatrienoic acid synthase activityThromboxane-A synthase Homo sapiens (human)
hydroperoxy icosatetraenoate dehydratase activityThromboxane-A synthase Homo sapiens (human)
monooxygenase activityProstacyclin synthaseHomo sapiens (human)
iron ion bindingProstacyclin synthaseHomo sapiens (human)
protein bindingProstacyclin synthaseHomo sapiens (human)
prostaglandin-I synthase activityProstacyclin synthaseHomo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygenProstacyclin synthaseHomo sapiens (human)
heme bindingProstacyclin synthaseHomo sapiens (human)
hydroperoxy icosatetraenoate dehydratase activityProstacyclin synthaseHomo sapiens (human)
protein bindingGlutaminyl-peptide cyclotransferaseHomo sapiens (human)
zinc ion bindingGlutaminyl-peptide cyclotransferaseHomo sapiens (human)
glutaminyl-peptide cyclotransferase activityGlutaminyl-peptide cyclotransferaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (22)

Processvia Protein(s)Taxonomy
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
endoplasmic reticulumAromataseHomo sapiens (human)
endoplasmic reticulum membraneAromataseHomo sapiens (human)
membraneAromataseHomo sapiens (human)
endoplasmic reticulumAromataseHomo sapiens (human)
endoplasmic reticulumThromboxane-A synthase Homo sapiens (human)
endoplasmic reticulum membraneThromboxane-A synthase Homo sapiens (human)
cytosolThromboxane-A synthase Homo sapiens (human)
extracellular spaceProstacyclin synthaseHomo sapiens (human)
nucleusProstacyclin synthaseHomo sapiens (human)
endoplasmic reticulumProstacyclin synthaseHomo sapiens (human)
endoplasmic reticulum membraneProstacyclin synthaseHomo sapiens (human)
caveolaProstacyclin synthaseHomo sapiens (human)
extracellular regionGlutaminyl-peptide cyclotransferaseHomo sapiens (human)
specific granule lumenGlutaminyl-peptide cyclotransferaseHomo sapiens (human)
extracellular exosomeGlutaminyl-peptide cyclotransferaseHomo sapiens (human)
tertiary granule lumenGlutaminyl-peptide cyclotransferaseHomo sapiens (human)
ficolin-1-rich granule lumenGlutaminyl-peptide cyclotransferaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (116)

Assay IDTitleYearJournalArticle
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.
AID215772In vitro inhibition of thromboxane synthase from human platelets.1986Journal of medicinal chemistry, Sep, Volume: 29, Issue:9
Selective thromboxane synthetase inhibitors. 3. 1H-imidazol-1-yl-substituted benzo[b]furan-, benzo[b]thiophene-, and indole-2- and -3-carboxylic acids.
AID187562The compound was tested for plasma levels of TXB2 in rats after 2 hr following dose 10(mg/kg) in oral administration.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Design of an antithrombotic-antihypertensive agent (Wy 27569). Synthesis and evaluation of a series of 2-heteroaryl-substituted dihydropyridines.
AID155359Inhibitory activity to inhibit Inophore-induced arachidonic acid metabolism (inhibition of PGE-2 formation) in rat1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
AID160956The compound was tested for effects of compound on 6-KPGF1alpha production at molar concentration of 10e-6 in human platelet rich plasma1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Design of an antithrombotic-antihypertensive agent (Wy 27569). Synthesis and evaluation of a series of 2-heteroaryl-substituted dihydropyridines.
AID60207Compound at an oral dose of 1 mg/Kg was tested ex vivo after 5 hr for inhibition of thromboxane synthase in dog1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
A novel approach to dual-acting thromboxane receptor antagonist/synthase inhibitors based on the link of 1,3-dioxane-thromboxane receptor antagonists and -thromboxane synthase inhibitors.
AID182499Percent inhibition of TXB2 in rat serum at 10 mg/kg dose after 2 hr2000Journal of medicinal chemistry, May-04, Volume: 43, Issue:9
1-imidazolyl(alkyl)-substituted di- and tetrahydroquinolines and analogues: syntheses and evaluation of dual inhibitors of thromboxane A(2) synthase and aromatase.
AID224487Tested for inhibition of thromboxane formation in rabbit platelets at 1.0 hr by administration of 0.3 mg/kg intravenous bolus dose1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
Thromboxane synthetase inhibitors and antihypertensive agents. 4. N-[(1H-imidazol-1-yl)alkyl] derivatives of quinazoline-2,4(1H,3H)-diones, quinazolin-4(3H)-ones, and 1,2,3-benzotriazin-4(3H)-ones.
AID161184Inhibition of ram seminal vesicle Cyclooxygenase1985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Selective thromboxane synthetase inhibitors. 1. 1-[(Aryloxy)alkyl]-1H-imidazoles.
AID224486Tested for inhibition of thromboxane formation in rabbit platelets at 0.5 hr by administration of 0.3 mg/kg intravenous bolus dose1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
Thromboxane synthetase inhibitors and antihypertensive agents. 4. N-[(1H-imidazol-1-yl)alkyl] derivatives of quinazoline-2,4(1H,3H)-diones, quinazolin-4(3H)-ones, and 1,2,3-benzotriazin-4(3H)-ones.
AID60077Compound at an oral dose of 1 mg/Kg was tested ex vivo after 1 hr for inhibition of thromboxane synthase in dog1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
A novel approach to dual-acting thromboxane receptor antagonist/synthase inhibitors based on the link of 1,3-dioxane-thromboxane receptor antagonists and -thromboxane synthase inhibitors.
AID224488Tested for inhibition of thromboxane formation in rabbit platelets at 1.0 hr by administration of 10 mg/kg intravenous bolus dose1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
Thromboxane synthetase inhibitors and antihypertensive agents. 4. N-[(1H-imidazol-1-yl)alkyl] derivatives of quinazoline-2,4(1H,3H)-diones, quinazolin-4(3H)-ones, and 1,2,3-benzotriazin-4(3H)-ones.
AID381197Inhibition of 5-lipoxygenase in Wistar rat peritoneal leukocytes at 50 ug/mL1999Journal of natural products, Sep, Volume: 62, Issue:9
Novel and known constituents from Buddleja species and their activity against leukocyte eicosanoid generation.
AID117739Activity at 25 mg/kg given intravenously against mortality in a pulmonary thromboembolism model in mice (9 animals) at -3h1989Journal of medicinal chemistry, Apr, Volume: 32, Issue:4
[(1H-imidazol-1-yl)methyl]- and [(3-pyridinyl)methyl]pyrroles as thromboxane synthetase inhibitors.
AID161608Effect on the synthesis of Thromboxane A21988Journal of medicinal chemistry, Sep, Volume: 31, Issue:9
Synthesis and in vitro activity of various derivatives of a novel thromboxane receptor antagonist, (+/-)-(5Z)-7-[3-endo-[(phenylsulfonyl)amino]bicyclo[2.2.1] hept-2-exo-yl]heptenoic acid.
AID160954The compound was tested for effects of compound on 6-KPGF1alpha production at molar concentration of 10e-4 in human platelet rich plasma1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Design of an antithrombotic-antihypertensive agent (Wy 27569). Synthesis and evaluation of a series of 2-heteroaryl-substituted dihydropyridines.
AID213139Inhibition of Thromboxane-A synthase2000Journal of medicinal chemistry, May-04, Volume: 43, Issue:9
1-imidazolyl(alkyl)-substituted di- and tetrahydroquinolines and analogues: syntheses and evaluation of dual inhibitors of thromboxane A(2) synthase and aromatase.
AID180297Inhibitory activity to inhibit Inophore-induced arachidonic acid metabolism (inhibition of LTB4 formation) in rat; Inactive = no significant inhibition at a concentration of 100 uM1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
AID212800Tested for inhibition of thromboxane synthetase from spontaneously hypertensive rats1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
Thromboxane synthetase inhibitors and antihypertensive agents. 4. N-[(1H-imidazol-1-yl)alkyl] derivatives of quinazoline-2,4(1H,3H)-diones, quinazolin-4(3H)-ones, and 1,2,3-benzotriazin-4(3H)-ones.
AID161007Inhibition of cyclooxygenase from RBL-1 cells.1986Journal of medicinal chemistry, Sep, Volume: 29, Issue:9
Selective thromboxane synthetase inhibitors. 4. 2-(1H-imidazol-1-ylmethyl) carboxylic acids of benzo[b]furan, benzo[b]thiophene, indole, and naphthalene.
AID161082The compound was tested for effects of compound on TXB2 production at molar concentration of 10e-7 in human platelet rich plasma1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Design of an antithrombotic-antihypertensive agent (Wy 27569). Synthesis and evaluation of a series of 2-heteroaryl-substituted dihydropyridines.
AID212954Compound was tested in vitro for its ability to to inhibit TXA2 biosynthesis in human microsomal platelets1986Journal of medicinal chemistry, Aug, Volume: 29, Issue:8
Thromboxane A2 synthase inhibitors. 5-(3-Pyridylmethyl)benzofuran-2-carboxylic acids.
AID222416In vivo inhibition of LTE4 (leukotriene)-induced bronchoconstrictions in guinea pig and percent inhibition was reported at 100 mg/Kg administered perorally1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
N-(heterocyclic alkyl)pyrido[2,1-b]quinazoline-8-carboxamides as orally active antiallergy agents.
AID222788Tested for inhibition of thromboxane formation in human platelets1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
Thromboxane synthetase inhibitors and antihypertensive agents. 4. N-[(1H-imidazol-1-yl)alkyl] derivatives of quinazoline-2,4(1H,3H)-diones, quinazolin-4(3H)-ones, and 1,2,3-benzotriazin-4(3H)-ones.
AID182500Percent inhibition of TXB2 in rat serum at 10 mg/kg dose after 3 hr2000Journal of medicinal chemistry, May-04, Volume: 43, Issue:9
1-imidazolyl(alkyl)-substituted di- and tetrahydroquinolines and analogues: syntheses and evaluation of dual inhibitors of thromboxane A(2) synthase and aromatase.
AID93431Antagonistic activity against human platelet aggregation induced by U-46,619.1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
A novel approach to dual-acting thromboxane receptor antagonist/synthase inhibitors based on the link of 1,3-dioxane-thromboxane receptor antagonists and -thromboxane synthase inhibitors.
AID77484Inhibition of Collagen-induced serum Thromboxane (TXB2) in guinea pig whole blood ex vivo after 30 mg/kg oral administration of compound.1987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
Thromboxane synthase inhibitors. Synthesis and pharmacological activity of (R)-, (S)-, and (+/-)-2,2-dimethyl-6-[2-(1H-imidazol-1-yl)-1-[[(4-methoxyphenyl)- methoxy]methyl]ethoxy]hexanoic acids.
AID210319Inhibition of platelet microsomal thromboxane A synthetase in rabbits1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Synthesis and thromboxane synthetase inhibitory activity of di- or tetrahydrobenzo[b]thiophenecarboxylic acid derivatives.
AID381196Inhibition of cyclooxygenase in Wistar rat peritoneal leukocytes at 50 ug/mL1999Journal of natural products, Sep, Volume: 62, Issue:9
Novel and known constituents from Buddleja species and their activity against leukocyte eicosanoid generation.
AID78328In vivo inhibition of LTE4 (leukotriene)-induced skin wheal formation in guinea pig and percent inhibition was reported at 10 mg/Kg administered intravenously1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
N-(heterocyclic alkyl)pyrido[2,1-b]quinazoline-8-carboxamides as orally active antiallergy agents.
AID183565Inhibition of thromboxane B2 production in whole blood of rats 1 hr following 1 mg/kg p.o.1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Thromboxane A2 synthetase inhibitors. 2. Syntheses and activities of tetrahydronaphthalene and indan derivatives.
AID155523Inhibition of PGI-2 synthetase from porcine aorta1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Selective thromboxane synthetase inhibitors. 2. 3-(1H-imidazol-1-ylmethyl)-2-methyl-1H-indole-1-propanoic acid and analogues.
AID210480Inhibition of thromboxane A2 synthetase1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Synthesis and thromboxane synthetase inhibitory activity of di- or tetrahydrobenzo[b]thiophenecarboxylic acid derivatives.
AID224490Tested for inhibition of thromboxane formation in rabbit platelets at 3 hr by administration of 0.3 mg/kg intravenous bolus dose1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
Thromboxane synthetase inhibitors and antihypertensive agents. 4. N-[(1H-imidazol-1-yl)alkyl] derivatives of quinazoline-2,4(1H,3H)-diones, quinazolin-4(3H)-ones, and 1,2,3-benzotriazin-4(3H)-ones.
AID190211Tested for antihypertensive activity in spontaneously hypertensive rats at 100 mg/kg peroral dosage for 2 days; I is inactive1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
Thromboxane synthetase inhibitors and antihypertensive agents. 4. N-[(1H-imidazol-1-yl)alkyl] derivatives of quinazoline-2,4(1H,3H)-diones, quinazolin-4(3H)-ones, and 1,2,3-benzotriazin-4(3H)-ones.
AID117596Activity at 10 mg/kg given intravenously against mortality in a pulmonary thromboembolism model in mice (10 animals) at -3h following oral administration1989Journal of medicinal chemistry, Apr, Volume: 32, Issue:4
[(1H-imidazol-1-yl)methyl]- and [(3-pyridinyl)methyl]pyrroles as thromboxane synthetase inhibitors.
AID224489Tested for inhibition of thromboxane formation in rabbit platelets at 2 hr by administration of 0.3 mg/kg intravenous bolus dose1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
Thromboxane synthetase inhibitors and antihypertensive agents. 4. N-[(1H-imidazol-1-yl)alkyl] derivatives of quinazoline-2,4(1H,3H)-diones, quinazolin-4(3H)-ones, and 1,2,3-benzotriazin-4(3H)-ones.
AID215617In vitro inhibition of Thromboxane A2 synthetase assayed on the rabbit aortic strip1993Journal of medicinal chemistry, Oct-15, Volume: 36, Issue:21
Tröger's base. An alternate synthesis and a structural analog with thromboxane A2 synthetase inhibitory activity.
AID78324In vivo inhibition of LTE4 (leukotriene)-induced bronchoconstrictions in guinea pig and percent inhibition was reported at 10 mg/Kg administered intravenously1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
N-(heterocyclic alkyl)pyrido[2,1-b]quinazoline-8-carboxamides as orally active antiallergy agents.
AID117589Activity at 10 mg/kg given intravenously against mortality in a pulmonary thromboembolism model in mice (10 animals) at -1h1989Journal of medicinal chemistry, Apr, Volume: 32, Issue:4
[(1H-imidazol-1-yl)methyl]- and [(3-pyridinyl)methyl]pyrroles as thromboxane synthetase inhibitors.
AID197381Enhancement of prostaglandin E2 levels in serum of incubated whole blood at 1 hr after an oral dose of 1 mg/kg1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Thromboxane A2 synthetase inhibitors. 2. Syntheses and activities of tetrahydronaphthalene and indan derivatives.
AID196814Compound at an oral dose of 10 mg/Kg was tested ex vivo in rat after 1 hr against platelet aggregation induced by U-46,6191995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
A novel approach to dual-acting thromboxane receptor antagonist/synthase inhibitors based on the link of 1,3-dioxane-thromboxane receptor antagonists and -thromboxane synthase inhibitors.
AID161081The compound was tested for effects of compound on TXB2 production at molar concentration of 10e-6 in human platelet rich plasma1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Design of an antithrombotic-antihypertensive agent (Wy 27569). Synthesis and evaluation of a series of 2-heteroaryl-substituted dihydropyridines.
AID215771Inhibition of thromboxane TXA2 synthetase from human platelets1986Journal of medicinal chemistry, Sep, Volume: 29, Issue:9
Selective thromboxane synthetase inhibitors. 4. 2-(1H-imidazol-1-ylmethyl) carboxylic acids of benzo[b]furan, benzo[b]thiophene, indole, and naphthalene.
AID77820Inhibition of Collagen-induced Thromboxane (TXB2) in guinea pig whole blood ex vivo by oral 30 mg/kg administration of test compound.1987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
Thromboxane synthase inhibitors. Synthesis and pharmacological activity of (R)-, (S)-, and (+/-)-2,2-dimethyl-6-[2-(1H-imidazol-1-yl)-1-[[(4-methoxyphenyl)- methoxy]methyl]ethoxy]hexanoic acids.
AID60078Compound at an oral dose of 1 mg/Kg was tested ex vivo after 3 hr for inhibition of thromboxane synthase in dog1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
A novel approach to dual-acting thromboxane receptor antagonist/synthase inhibitors based on the link of 1,3-dioxane-thromboxane receptor antagonists and -thromboxane synthase inhibitors.
AID210320Inhibition of rat serum thromboxane A2 synthetase after 2 hr of oral administration of compound1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Synthesis and thromboxane synthetase inhibitory activity of di- or tetrahydrobenzo[b]thiophenecarboxylic acid derivatives.
AID197384Increase in serum prostaglandin I2 levels in incubated whole blood from rats, 1 hr following 1 mg/kg p.o.1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Thromboxane A2 synthetase inhibitors. 2. Syntheses and activities of tetrahydronaphthalene and indan derivatives.
AID154269Inhibition of thromboxane synthase P450 TXA2 at 50 uM2000Journal of medicinal chemistry, Nov-02, Volume: 43, Issue:22
Synthesis and evaluation of novel steroidal oxime inhibitors of P450 17 (17 alpha-hydroxylase/C17-20-lyase) and 5 alpha-reductase types 1 and 2.
AID117594Activity at 10 mg/kg given intravenously against mortality in a pulmonary thromboembolism model in mice (10 animals) at -1h following oral administration1989Journal of medicinal chemistry, Apr, Volume: 32, Issue:4
[(1H-imidazol-1-yl)methyl]- and [(3-pyridinyl)methyl]pyrroles as thromboxane synthetase inhibitors.
AID62828Compound at an oral dose of 1 mg/Kg was tested ex vivo in dog after 3 hr against platelet aggregation induced by U-46,6191995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
A novel approach to dual-acting thromboxane receptor antagonist/synthase inhibitors based on the link of 1,3-dioxane-thromboxane receptor antagonists and -thromboxane synthase inhibitors.
AID117588Activity at 10 mg/kg given intravenously against mortality in a pulmonary thromboembolism model in mice (10 animals) at -18h following oral administration1989Journal of medicinal chemistry, Apr, Volume: 32, Issue:4
[(1H-imidazol-1-yl)methyl]- and [(3-pyridinyl)methyl]pyrroles as thromboxane synthetase inhibitors.
AID215622Inhibition of Thromboxane B2 formation in collagen-stimulated human platelets in platelet rich plasma.1987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
Thromboxane synthase inhibitors. Synthesis and pharmacological activity of (R)-, (S)-, and (+/-)-2,2-dimethyl-6-[2-(1H-imidazol-1-yl)-1-[[(4-methoxyphenyl)- methoxy]methyl]ethoxy]hexanoic acids.
AID167470Protection against sodium arachidonate induced sudden death in rabbit, 1 hr after peroral administration1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Synthesis and thromboxane synthetase inhibitory activity of di- or tetrahydrobenzo[b]thiophenecarboxylic acid derivatives.
AID197199Compound at an oral dose of 10 mg/Kg was tested ex vivo after 3 hr for inhibition of thromboxane synthase in rat1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
A novel approach to dual-acting thromboxane receptor antagonist/synthase inhibitors based on the link of 1,3-dioxane-thromboxane receptor antagonists and -thromboxane synthase inhibitors.
AID187565The compound was tested for plasma levels of TXB2 in rats after 2 hr following dose 3(mg/kg) in oral administration. (p<0.05)1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Design of an antithrombotic-antihypertensive agent (Wy 27569). Synthesis and evaluation of a series of 2-heteroaryl-substituted dihydropyridines.
AID210502Inhibitory activity to inhibit Inophore-induced arachidonic acid metabolism (inhibition of TXB2 formation) in rat1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
3,4-Dihydro-2H-1-benzopyran-2-carboxylic acids and related compounds as leukotriene antagonists.
AID224491Tested for inhibition of thromboxane formation in rabbit platelets at 3 hr by administration of 10 mg/kg intravenous bolus dose1987Journal of medicinal chemistry, Dec, Volume: 30, Issue:12
Thromboxane synthetase inhibitors and antihypertensive agents. 4. N-[(1H-imidazol-1-yl)alkyl] derivatives of quinazoline-2,4(1H,3H)-diones, quinazolin-4(3H)-ones, and 1,2,3-benzotriazin-4(3H)-ones.
AID215621Tested for inhibitory activity against intact human platelet TXA2 formation1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
Structure-activity relationships in an imidazole-based series of thromboxane synthase inhibitors.
AID161078The compound was tested for effects of compound on TXB2 production at molar concentration of 10e-3 in human platelet rich plasma1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Design of an antithrombotic-antihypertensive agent (Wy 27569). Synthesis and evaluation of a series of 2-heteroaryl-substituted dihydropyridines.
AID161610Effect on the synthesis of metabolites of arachidonic acid in human platelets1988Journal of medicinal chemistry, Sep, Volume: 31, Issue:9
Synthesis and in vitro activity of various derivatives of a novel thromboxane receptor antagonist, (+/-)-(5Z)-7-[3-endo-[(phenylsulfonyl)amino]bicyclo[2.2.1] hept-2-exo-yl]heptenoic acid.
AID179761In vitro inhibition of thromboxane A2 production in rat platelet-rich plasma.1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Thromboxane A2 synthetase inhibitors. 2. Syntheses and activities of tetrahydronaphthalene and indan derivatives.
AID213112Compound was tested for the inhibition of thromboxane formation (thromboxane synthetase) in platelets at a concentration of 10e-4 M1986Journal of medicinal chemistry, May, Volume: 29, Issue:5
Thromboxane synthetase inhibitors and antihypertensive agents. 2. N-[(1H-imidazol-1-yl)alkyl]-1H-isoindole-1,3(2H)-diones and N-[(1H-1,2,4-triazol-1-yl)alkyl]-1H-isoindole-1,3(2H)-diones as unique antihypertensive agents.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID78283Evaluated for inhibition of slow reacting substance of anaphylaxis (SRS-A) induced contractions in guinea pig ileum strips1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
N-(heterocyclic alkyl)pyrido[2,1-b]quinazoline-8-carboxamides as orally active antiallergy agents.
AID183981Compound at an oral dose of 10 mg/Kg was tested ex vivo after 1 hr for inhibition of thromboxane synthase in rat1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
A novel approach to dual-acting thromboxane receptor antagonist/synthase inhibitors based on the link of 1,3-dioxane-thromboxane receptor antagonists and -thromboxane synthase inhibitors.
AID182502Percent inhibition of TXB2 in rat serum at 10 mg/kg dose after 8 hr2000Journal of medicinal chemistry, May-04, Volume: 43, Issue:9
1-imidazolyl(alkyl)-substituted di- and tetrahydroquinolines and analogues: syntheses and evaluation of dual inhibitors of thromboxane A(2) synthase and aromatase.
AID77239Inhibition of Collagen-induced Thromboxane (TXB2) in guinea pig whole blood ex vivo after 1 hr of 30 mg/kg oral administration of compound.1987Journal of medicinal chemistry, Oct, Volume: 30, Issue:10
Thromboxane synthase inhibitors. Synthesis and pharmacological activity of (R)-, (S)-, and (+/-)-2,2-dimethyl-6-[2-(1H-imidazol-1-yl)-1-[[(4-methoxyphenyl)- methoxy]methyl]ethoxy]hexanoic acids.
AID212634Inhibition of Thromboxane A2 synthase after oral administration of 0.03 mmol/kg1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Design of an antithrombotic-antihypertensive agent (Wy 27569). Synthesis and evaluation of a series of 2-heteroaryl-substituted dihydropyridines.
AID3095Inhibition of rat adrenal 11-beta-hydroxylase1985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Selective thromboxane synthetase inhibitors. 1. 1-[(Aryloxy)alkyl]-1H-imidazoles.
AID62829Compound at an oral dose of 1 mg/Kg was tested ex vivo in dog after 5 hr against platelet aggregation induced by U-46,6191995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
A novel approach to dual-acting thromboxane receptor antagonist/synthase inhibitors based on the link of 1,3-dioxane-thromboxane receptor antagonists and -thromboxane synthase inhibitors.
AID187564The compound was tested for plasma levels of TXB2 in rats after 2 hr following dose 3(mg/kg) in oral administration.1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Design of an antithrombotic-antihypertensive agent (Wy 27569). Synthesis and evaluation of a series of 2-heteroaryl-substituted dihydropyridines.
AID212951Compound was tested for thromboxane synthase activity in microsomal preparations from guinea pig lung(GPLM)1986Journal of medicinal chemistry, Aug, Volume: 29, Issue:8
Thromboxane A2 synthase inhibitors. 5-(3-Pyridylmethyl)benzofuran-2-carboxylic acids.
AID160957The compound was tested for effects of compound on 6-KPGF1alpha production at molar concentration of 10e-7 in human platelet rich plasma1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Design of an antithrombotic-antihypertensive agent (Wy 27569). Synthesis and evaluation of a series of 2-heteroaryl-substituted dihydropyridines.
AID212779Inhibitory activity against thromboxane A2 synthetase1985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Selective thromboxane synthetase inhibitors. 1. 1-[(Aryloxy)alkyl]-1H-imidazoles.
AID183551Inhibition of thromboxane B2 production in whole blood of rat 15 min after intravenous injection of compound at 0.1 mg/kg1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Thromboxane A2 synthetase inhibitors. 2. Syntheses and activities of tetrahydronaphthalene and indan derivatives.
AID212952Compound was tested for thromboxane synthase activity in microsomal preparations from human platelets(HPM)1986Journal of medicinal chemistry, Aug, Volume: 29, Issue:8
Thromboxane A2 synthase inhibitors. 5-(3-Pyridylmethyl)benzofuran-2-carboxylic acids.
AID213134Inhibition of thromboxane formation at a concentration of 10e -6 M.1987Journal of medicinal chemistry, Jun, Volume: 30, Issue:6
Thromboxane synthetase inhibitors and antihypertensive agents. 3. N-[(1H-imidazol-1-yl)alkyl]heteroaryl amides as potent enzyme inhibitors.
AID210318Inhibition of platelet microsomal thromboxane A synthetase in humans1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Synthesis and thromboxane synthetase inhibitory activity of di- or tetrahydrobenzo[b]thiophenecarboxylic acid derivatives.
AID215770In vitro inhibition of thromboxane B2 production in rat whole blood.1993Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
Imidazol-1-yl and pyridin-3-yl derivatives of 4-phenyl-1,4-dihydropyridines combining Ca2+ antagonism and thromboxane A2 synthase inhibition.
AID3093Inhibition of 11 beta-hydroxylase from rat adrenal gland1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Selective thromboxane synthetase inhibitors. 2. 3-(1H-imidazol-1-ylmethyl)-2-methyl-1H-indole-1-propanoic acid and analogues.
AID155525Inhibition of porcine aorta prostacyclin PGI-2 synthase1985Journal of medicinal chemistry, Oct, Volume: 28, Issue:10
Selective thromboxane synthetase inhibitors. 1. 1-[(Aryloxy)alkyl]-1H-imidazoles.
AID215773Inhibition of TXA2 synthetase from human platelets1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Selective thromboxane synthetase inhibitors. 2. 3-(1H-imidazol-1-ylmethyl)-2-methyl-1H-indole-1-propanoic acid and analogues.
AID212950Compound was tested for thromboxane synthase activity in microsomal preparations from dog lung(DLM)1986Journal of medicinal chemistry, Aug, Volume: 29, Issue:8
Thromboxane A2 synthase inhibitors. 5-(3-Pyridylmethyl)benzofuran-2-carboxylic acids.
AID160953The compound was tested for effects of compound on 6-KPGF1alpha production at molar concentration of 10e-3 in human platelet rich plasma1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Design of an antithrombotic-antihypertensive agent (Wy 27569). Synthesis and evaluation of a series of 2-heteroaryl-substituted dihydropyridines.
AID183570Inhibition of thromboxane B2 production in whole blood of rats, 6 hr after a peroral dose of 1.0 mg/kg1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Thromboxane A2 synthetase inhibitors. 2. Syntheses and activities of tetrahydronaphthalene and indan derivatives.
AID212967Inhibition of human platelet thromboxane synthase (TXA2) was determined in human platelets1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
N-(heterocyclic alkyl)pyrido[2,1-b]quinazoline-8-carboxamides as orally active antiallergy agents.
AID161739The synthesis of cyclooxygenase or lipoxygenase derived products (HHT and HETE) in human washed platelets1988Journal of medicinal chemistry, Sep, Volume: 31, Issue:9
Synthesis and in vitro activity of various derivatives of a novel thromboxane receptor antagonist, (+/-)-(5Z)-7-[3-endo-[(phenylsulfonyl)amino]bicyclo[2.2.1] hept-2-exo-yl]heptenoic acid.
AID117592Activity at 10 mg/kg given intravenously against mortality in a pulmonary thromboembolism model in mice (10 animals) at -7h following oral administration1989Journal of medicinal chemistry, Apr, Volume: 32, Issue:4
[(1H-imidazol-1-yl)methyl]- and [(3-pyridinyl)methyl]pyrroles as thromboxane synthetase inhibitors.
AID62827Compound at an oral dose of 1 mg/Kg was tested ex vivo in dog after 1 hr against platelet aggregation induced by U-46,6191995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
A novel approach to dual-acting thromboxane receptor antagonist/synthase inhibitors based on the link of 1,3-dioxane-thromboxane receptor antagonists and -thromboxane synthase inhibitors.
AID213137Inhibitory activity for thromboxane synthetase determined by TXB2 levels in platelets from spontaneously hypertensive rats.1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
Thromboxane synthetase inhibitors and antihypertensive agents. 1. N-[(1H-imidazol-1-yl)alkyl]aryl amides and N-[(1H-1,2,4-triazol-1-yl)alkyl]aryl amides.
AID117597Activity at 10 mg/kg given intravenously against mortality in a pulmonary thromboembolism model in mice (10 animals) at -5h following oral administration1989Journal of medicinal chemistry, Apr, Volume: 32, Issue:4
[(1H-imidazol-1-yl)methyl]- and [(3-pyridinyl)methyl]pyrroles as thromboxane synthetase inhibitors.
AID78329In vivo inhibition of LTE4 (leukotriene)-induced skin wheal formation in guinea pig and percent inhibition was reported at 100 mg/Kg administered perorally1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
N-(heterocyclic alkyl)pyrido[2,1-b]quinazoline-8-carboxamides as orally active antiallergy agents.
AID161164Inhibition of Prostaglandin G/H synthase from ram seminal vesicle microsomes1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Selective thromboxane synthetase inhibitors. 2. 3-(1H-imidazol-1-ylmethyl)-2-methyl-1H-indole-1-propanoic acid and analogues.
AID212955In vitro inhibition of Thromboxane synthase using [14C]arachidonic acid as radioligand1991Journal of medicinal chemistry, Jun, Volume: 34, Issue:6
Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 1. (+/-)-(3-pyridinylbicycloheptyl)alkanoic acids.
AID212966In vitro inhibitory activity against human microsomal thromboxane synthase.1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
A novel approach to dual-acting thromboxane receptor antagonist/synthase inhibitors based on the link of 1,3-dioxane-thromboxane receptor antagonists and -thromboxane synthase inhibitors.
AID196815Compound at an oral dose of 10 mg/Kg was tested ex vivo in rat after 3 hr against platelet aggregation induced by U-46,6191995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
A novel approach to dual-acting thromboxane receptor antagonist/synthase inhibitors based on the link of 1,3-dioxane-thromboxane receptor antagonists and -thromboxane synthase inhibitors.
AID3094Inhibition of rat adrenal 11-beta-hydroxylase1986Journal of medicinal chemistry, Sep, Volume: 29, Issue:9
Selective thromboxane synthetase inhibitors. 4. 2-(1H-imidazol-1-ylmethyl) carboxylic acids of benzo[b]furan, benzo[b]thiophene, indole, and naphthalene.
AID182501Percent inhibition of TXB2 in rat serum at 10 mg/kg dose after 5 hr2000Journal of medicinal chemistry, May-04, Volume: 43, Issue:9
1-imidazolyl(alkyl)-substituted di- and tetrahydroquinolines and analogues: syntheses and evaluation of dual inhibitors of thromboxane A(2) synthase and aromatase.
AID183566Inhibition of thromboxane B2 production in whole blood of rats, 3h after a peroral dose of 1.0 mg/kg1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Thromboxane A2 synthetase inhibitors. 2. Syntheses and activities of tetrahydronaphthalene and indan derivatives.
AID183555Inhibition of thromboxane B2 production in whole blood of rat 45 min after intravenous injection of compound at 0.1 mg/kg1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Thromboxane A2 synthetase inhibitors. 2. Syntheses and activities of tetrahydronaphthalene and indan derivatives.
AID212975Compound was tested in vitro for its ability to to inhibit TXA2 biosynthesis in human microsomal platelets1986Journal of medicinal chemistry, Aug, Volume: 29, Issue:8
Thromboxane A2 synthase inhibitors. 5-(3-Pyridylmethyl)benzofuran-2-carboxylic acids.
AID154268Inhibition of thromboxane synthase P450 TXA22000Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23
Synthesis and evaluation of 17-aliphatic heterocycle-substituted steroidal inhibitors of 17alpha-hydroxylase/C17-20-lyase (P450 17).
AID161080The compound was tested for effects of compound on TXB2 production at molar concentration of 10e-5 in human platelet rich plasma1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Design of an antithrombotic-antihypertensive agent (Wy 27569). Synthesis and evaluation of a series of 2-heteroaryl-substituted dihydropyridines.
AID160955The compound was tested for effects of compound on 6-KPGF1alpha production at molar concentration of 10e-5 in human platelet rich plasma1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Design of an antithrombotic-antihypertensive agent (Wy 27569). Synthesis and evaluation of a series of 2-heteroaryl-substituted dihydropyridines.
AID161079The compound was tested for effects of compound on TXB2 production at molar concentration of 10e-4 in human platelet rich plasma1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Design of an antithrombotic-antihypertensive agent (Wy 27569). Synthesis and evaluation of a series of 2-heteroaryl-substituted dihydropyridines.
AID155524Inhibition of porcine aorta prostacyclin PGI-2 synthetase1986Journal of medicinal chemistry, Sep, Volume: 29, Issue:9
Selective thromboxane synthetase inhibitors. 4. 2-(1H-imidazol-1-ylmethyl) carboxylic acids of benzo[b]furan, benzo[b]thiophene, indole, and naphthalene.
AID213131Compound was tested for inhibitory activity against thromboxane synthetase1986Journal of medicinal chemistry, Apr, Volume: 29, Issue:4
Thromboxane synthetase inhibitors and antihypertensive agents. 1. N-[(1H-imidazol-1-yl)alkyl]aryl amides and N-[(1H-1,2,4-triazol-1-yl)alkyl]aryl amides.
AID89450In vitro inhibition of ADP-induced aggregation of human platelet rich plasma in the presence of pig aortal microsomes.1989Journal of medicinal chemistry, Apr, Volume: 32, Issue:4
[(1H-imidazol-1-yl)methyl]- and [(3-pyridinyl)methyl]pyrroles as thromboxane synthetase inhibitors.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
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.
AID1796390Aromatase Assay from Article 10.1021/jm991180u: \\1-imidazolyl(alkyl)-substituted di- and tetrahydroquinolines and analogues: syntheses and evaluation of dual inhibitors of thromboxane A(2) synthase and aromatase.\\2000Journal of medicinal chemistry, May-04, Volume: 43, Issue:9
1-imidazolyl(alkyl)-substituted di- and tetrahydroquinolines and analogues: syntheses and evaluation of dual inhibitors of thromboxane A(2) synthase and aromatase.
AID1796109QC Inhibition Testing from Article 10.1074/jbc.M309077200: \\Identification of human glutaminyl cyclase as a metalloenzyme. Potent inhibition by imidazole derivatives and heterocyclic chelators.\\2003The Journal of biological chemistry, Dec-12, Volume: 278, Issue:50
Identification of human glutaminyl cyclase as a metalloenzyme. Potent inhibition by imidazole derivatives and heterocyclic chelators.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (288)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990207 (71.88)18.7374
1990's53 (18.40)18.2507
2000's17 (5.90)29.6817
2010's9 (3.13)24.3611
2020's2 (0.69)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 25.59

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 Index25.59 (24.57)
Research Supply Index5.77 (2.92)
Research Growth Index4.18 (4.65)
Search Engine Demand Index34.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (25.59)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials27 (9.25%)5.53%
Reviews10 (3.42%)6.00%
Case Studies2 (0.68%)4.05%
Observational0 (0.00%)0.25%
Other253 (86.64%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]