Compounds > e 5110
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e 5110

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

Description

E 5110: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID6438164
CHEMBL ID12594
SCHEMBL ID5323330
MeSH IDM0152942

Synonyms (12)

Synonym
2-pyrrolidinone, 3-((3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl)methylene)-1-methoxy-
n-methoxy-3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2-one
n-methoxy-3-(3,5-di-tert-butyl-4-hydroxybenzylidene)-2-pyrrolidone
e 5110
CHEMBL12594 ,
3-[1-(3,5-di-tert-butyl-4-hydroxy-phenyl)-meth-(e)-ylidene]-1-methoxy-pyrrolidin-2-one
3-(3,5-di-tert-butyl-4-hydroxy-benzylidene)-1-methoxy-pyrrolidin-2-one
bdbm50008954
(3e)-3-[(3,5-ditert-butyl-4-hydroxyphenyl)methylidene]-1-methoxypyrrolidin-2-one
107746-52-1
2-pyrrolidinone,3-[[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]methylene]-1-methoxy-
SCHEMBL5323330

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"Following single-dose intravenous and oral studies to determine the absolute bioavailability of E5110 in beagle dogs, repeated dose pharmacokinetic studies were conducted as toxicokinetics in a subacute toxicity test."( Auto-induction of E5110 metabolism, a novel non-steroidal anti-inflammatory drug, during toxicokinetic studies in beagle dogs.
Horie, T; Nakata, H; Sagami, F, 2000)		0.31

Dosage Studied

ExcerptRelevanceReference
" Compounds from this series also were found to inhibit the in vivo production of LTB4 when dosed orally in rats."( Styrylpyrazoles, styrylisoxazoles, and styrylisothiazoles. Novel 5-lipoxygenase and cyclooxygenase inhibitors.
Belliotti, TR; Boctor, AM; Connor, DT; Flynn, DL; Kostlan, CR; Nies, DE; Ortwine, DF; Schrier, DJ; Sircar, JC, 1991)		0.28
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Polyunsaturated fatty acid 5-lipoxygenaseRattus norvegicus (Norway rat)IC50 (µMol)4.32000.00462.018210.0000AID3635; AID6871; AID7073
Prostaglandin G/H synthase 2 Rattus norvegicus (Norway rat)IC50 (µMol)0.36000.00291.786810.0000AID161008; AID161009; AID161023
Prostaglandin G/H synthase 1 Rattus norvegicus (Norway rat)IC50 (µMol)0.36000.00291.823210.0000AID161008; AID161009; AID161023
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (28)

Assay IDTitleYearJournalArticle
AID184310Compound was evaluated for the inhibition of adjuvant-induced arthritis model in rats at a dose of 1 mg/kg1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
Synthesis and antiinflammatory activities of 3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2-ones.
AID190155Percent of rats with ulcers after the administration of compound at a dose of 10 orally.1991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Styrylpyrazoles, styrylisoxazoles, and styrylisothiazoles. Novel 5-lipoxygenase and cyclooxygenase inhibitors.
AID169217In vivo inflammatory activity measured on Gastric ulcerogenicity, expressed as percent rats with ulcers at 10 mg/kg, po (n= 10 rats per experimental group)1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Design of 5-(3,5-di-tert-butyl-4-hydroxyphenyl)-1,3,4-thiadiazoles, -1,3,4-oxadiazoles, and -1,2,4-triazoles as orally-active, nonulcerogenic antiinflammatory agents.
AID169632Compound is evaluated for gastric ulceration in rats at a dose of 10 mg/kg(1/11)1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
Synthesis and antiinflammatory activities of 3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2-ones.
AID161009Inhibition of prostaglandin G/H synthase in intact rat basophilic leukemia cells stimulated with the calcium ionophore A-231871994Journal of medicinal chemistry, Jan-21, Volume: 37, Issue:2
Synthesis and biological evaluation of 5-[[3,5-bis(1,1-dimethylethyl)- 4-hydroxyphenyl]methylene]oxazoles, -thiazoles, and -imidazoles: novel dual 5-lipoxygenase and cyclooxygenase inhibitors with antiinflammatory activity.
AID17943540% inhibition of induced edema in the rat mycobacterium foot-pad edema test1994Journal of medicinal chemistry, Jan-21, Volume: 37, Issue:2
Synthesis and biological evaluation of 5-[[3,5-bis(1,1-dimethylethyl)- 4-hydroxyphenyl]methylene]oxazoles, -thiazoles, and -imidazoles: novel dual 5-lipoxygenase and cyclooxygenase inhibitors with antiinflammatory activity.
AID183398Inhibition of rat carrageenan induced foot-pad edema at a dose of 10 mg/kg on peroral administration1994Journal of medicinal chemistry, Jan-21, Volume: 37, Issue:2
Synthesis and biological evaluation of 5-[[3,5-bis(1,1-dimethylethyl)- 4-hydroxyphenyl]methylene]oxazoles, -thiazoles, and -imidazoles: novel dual 5-lipoxygenase and cyclooxygenase inhibitors with antiinflammatory activity.
AID169637Compound is evaluated for gastric ulceration in rats at a dose of 100 mg/kg(2/12)1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
Synthesis and antiinflammatory activities of 3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2-ones.
AID161008Inhibitory activity against cyclooxygenase in rat basophilic leukemia cells using prostaglandin G/H synthase assay1991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Styrylpyrazoles, styrylisoxazoles, and styrylisothiazoles. Novel 5-lipoxygenase and cyclooxygenase inhibitors.
AID184311Compound was evaluated for the inhibition of adjuvant-induced arthritis model in rats at a dose of 3 mg/kg1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
Synthesis and antiinflammatory activities of 3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2-ones.
AID91152Compound is evaluated for inhibitory effect on the generation of Leukotriene B4 (LTB4) from human neutrophils1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
Synthesis and antiinflammatory activities of 3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2-ones.
AID161023Inhibition of prostaglandin G/H synthase by measuring the reduction of prostaglandin F2-alpha in intact basophilic rat leukemia cells1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Design of 5-(3,5-di-tert-butyl-4-hydroxyphenyl)-1,3,4-thiadiazoles, -1,3,4-oxadiazoles, and -1,2,4-triazoles as orally-active, nonulcerogenic antiinflammatory agents.
AID179441In vivo inflammatory activity measured on Carrageenan foot-pad edema (CFE) in rats, peroral administration1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Design of 5-(3,5-di-tert-butyl-4-hydroxyphenyl)-1,3,4-thiadiazoles, -1,3,4-oxadiazoles, and -1,2,4-triazoles as orally-active, nonulcerogenic antiinflammatory agents.
AID169641Compound is evaluated for gastric ulceration in rats at a dose of 3 mg/kg(0/6)1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
Synthesis and antiinflammatory activities of 3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2-ones.
AID179442In vivo inflammatory activity measured on Mycobacterium foot-pad edema (MFE) model1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Design of 5-(3,5-di-tert-butyl-4-hydroxyphenyl)-1,3,4-thiadiazoles, -1,3,4-oxadiazoles, and -1,2,4-triazoles as orally-active, nonulcerogenic antiinflammatory agents.
AID181667Compound is evaluated for inhibitory effect on the generation of Prostaglandin E2 (PGE2) from rat synovial cells1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
Synthesis and antiinflammatory activities of 3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2-ones.
AID179433Percent inhibition of carrageenan foot-pad edema in rats.1991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Styrylpyrazoles, styrylisoxazoles, and styrylisothiazoles. Novel 5-lipoxygenase and cyclooxygenase inhibitors.
AID28708Partition coefficient (logP)1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Design of 5-(3,5-di-tert-butyl-4-hydroxyphenyl)-1,3,4-thiadiazoles, -1,3,4-oxadiazoles, and -1,2,4-triazoles as orally-active, nonulcerogenic antiinflammatory agents.
AID7073Tested for inhibition of 5-LO by measuring the reduction of leukotriene B4 (LTB4) in intact basophilic rat leukemia cells1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Design of 5-(3,5-di-tert-butyl-4-hydroxyphenyl)-1,3,4-thiadiazoles, -1,3,4-oxadiazoles, and -1,2,4-triazoles as orally-active, nonulcerogenic antiinflammatory agents.
AID6871Inhibition of 5-lipoxygenase in intact rat basophilic leukemia cells stimulated with the calcium ionophore A-231871994Journal of medicinal chemistry, Jan-21, Volume: 37, Issue:2
Synthesis and biological evaluation of 5-[[3,5-bis(1,1-dimethylethyl)- 4-hydroxyphenyl]methylene]oxazoles, -thiazoles, and -imidazoles: novel dual 5-lipoxygenase and cyclooxygenase inhibitors with antiinflammatory activity.
AID169644Compound is evaluated for gastric ulceration in rats at a dose of 30 mg/kg(2/12)1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
Synthesis and antiinflammatory activities of 3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2-ones.
AID193232Compound was evaluated for edema density in adjuvant-induced arthritis model in rats at a dose of 1 mg/kg (Experiment # 1)1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
Synthesis and antiinflammatory activities of 3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2-ones.
AID3635Inhibitory activity against 5-lipoxygenase in rat basophilic leukemia cells1991Journal of medicinal chemistry, Feb, Volume: 34, Issue:2
Styrylpyrazoles, styrylisoxazoles, and styrylisothiazoles. Novel 5-lipoxygenase and cyclooxygenase inhibitors.
AID183399Inhibition of rat carrageenan induced foot-pad edema at a dose of 30 mg/kg on peroral administration1994Journal of medicinal chemistry, Jan-21, Volume: 37, Issue:2
Synthesis and biological evaluation of 5-[[3,5-bis(1,1-dimethylethyl)- 4-hydroxyphenyl]methylene]oxazoles, -thiazoles, and -imidazoles: novel dual 5-lipoxygenase and cyclooxygenase inhibitors with antiinflammatory activity.
AID177781Analgesic activity was evaluated in the rat flection pain test1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
Synthesis and antiinflammatory activities of 3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2-ones.
AID193234Compound was evaluated for edema density in adjuvant-induced arthritis model in rats at a dose of 3 mg/kg (Experiment # 1)1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
Synthesis and antiinflammatory activities of 3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2-ones.
AID192860Antiinflammatory activity expressed as minimum effective dose was screened by using adjuvant-induced local hyperthermia in rats1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
Synthesis and antiinflammatory activities of 3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2-ones.
AID177017Antiinflammatory activity was evaluated in rat carrageenan foot edema assay1987Journal of medicinal chemistry, Nov, Volume: 30, Issue:11
Synthesis and antiinflammatory activities of 3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2-ones.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (12)

TimeframeStudies, This Drug (%)All Drugs %
pre-19906 (50.00)18.7374
1990's5 (41.67)18.2507
2000's1 (8.33)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

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%
Other12 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
phenytoin
[no description available]		1.9810imidazolidine-2,4-dioneanticonvulsant;
drug allergen;
sodium channel blocker;
teratogenic agent
carbamazepine
Carbamazepine: A dibenzazepine that acts as a sodium channel blocker. It is used as an anticonvulsant for the treatment of grand mal and psychomotor or focal SEIZURES. It may also be used in the management of BIPOLAR DISORDER, and has analgesic properties.. carbamazepine : A dibenzoazepine that is 5H-dibenzo[b,f]azepine carrying a carbamoyl substituent at the azepine nitrogen, used as an anticonvulsant.		1.9810dibenzoazepine;
ureas		analgesic;
anticonvulsant;
antimanic drug;
drug allergen;
EC 3.5.1.98 (histone deacetylase) inhibitor;
environmental contaminant;
glutamate transporter activator;
mitogen;
non-narcotic analgesic;
sodium channel blocker;
xenobiotic
clofibrate
angiokapsul: contains clofibrate & insoitolnicotinate		1.9810aromatic ether;
ethyl ester;
monochlorobenzenes		anticholesteremic drug;
antilipemic drug;
geroprotector;
PPARalpha agonist
clotrimazole
[no description available]		1.9810conazole antifungal drug;
imidazole antifungal drug;
imidazoles;
monochlorobenzenes		antiinfective agent;
environmental contaminant;
xenobiotic
indomethacin
Indomethacin: A non-steroidal anti-inflammatory agent (NSAID) that inhibits CYCLOOXYGENASE, which is necessary for the formation of PROSTAGLANDINS and other AUTACOIDS. It also inhibits the motility of POLYMORPHONUCLEAR LEUKOCYTES.. indometacin : A member of the class of indole-3-acetic acids that is indole-3-acetic acid in which the indole ring is substituted at positions 1, 2 and 5 by p-chlorobenzoyl, methyl, and methoxy groups, respectively. A non-steroidal anti-inflammatory drug, it is used in the treatment of musculoskeletal and joint disorders including osteoarthritis, rheumatoid arthritis, gout, bursitis and tendinitis.		2.8840aromatic ether;
indole-3-acetic acids;
monochlorobenzenes;
N-acylindole		analgesic;
drug metabolite;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
gout suppressant;
non-steroidal anti-inflammatory drug;
xenobiotic metabolite;
xenobiotic
meclofenamic acid
Meclofenamic Acid: A non-steroidal anti-inflammatory agent with antipyretic and antigranulation activities. It also inhibits prostaglandin biosynthesis.. meclofenamic acid : An aminobenzoic acid that is anthranilic acid in which one of the hydrogens attached to the nitrogen is replaced by a 2,6-dichloro-3-methylphenyl group. A non-steroidal anti-inflammatory drug, it is used as the sodium salt for the treatment of dysmenorrhoea (painful periods), osteoarthritis and rheumatoid arthritis.		1.9810aminobenzoic acid;
organochlorine compound;
secondary amino compound		analgesic;
anticonvulsant;
antineoplastic agent;
antipyretic;
antirheumatic drug;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-steroidal anti-inflammatory drug
meclofenamate sodium anhydrous
[no description available]		1.9810organic sodium salt
masoprocol
nordihydroguaretic acid: antioxidant compound found in the creosote bush (Larrea tridentata)		1.9710catechols;
lignan;
tetrol		antioxidant;
ferroptosis inhibitor;
geroprotector;
plant metabolite
omeprazole
Omeprazole: A 4-methoxy-3,5-dimethylpyridyl, 5-methoxybenzimidazole derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits an H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS.. omeprazole : A racemate comprising equimolar amounts of (R)- and (S)-omeprazole.. 5-methoxy-2-{[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl}-1H-benzimidazole : A member of the class of benzimidazoles that is 1H-benzimidazole which is substituted by a [4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl group at position 2 and a methoxy group at position 5.		1.9810aromatic ether;
benzimidazoles;
pyridines;
sulfoxide
phenobarbital
Phenobarbital: A barbituric acid derivative that acts as a nonselective central nervous system depressant. It potentiates GAMMA-AMINOBUTYRIC ACID action on GABA-A RECEPTORS, and modulates chloride currents through receptor channels. It also inhibits glutamate induced depolarizations.. phenobarbital : A member of the class of barbiturates, the structure of which is that of barbituric acid substituted at C-5 by ethyl and phenyl groups.		1.9810barbituratesanticonvulsant;
drug allergen;
excitatory amino acid antagonist;
sedative
trimethadione
Trimethadione: An anticonvulsant effective in absence seizures, but generally reserved for refractory cases because of its toxicity. (From AMA Drug Evaluations Annual, 1994, p378). trimethadione : An oxazolidinone that is 1,3-oxazolidine-2,4-dione substituted by methyl groups at positions 3, 5 and 5. It is an antiepileptic agent.		1.9810oxazolidinoneanticonvulsant;
geroprotector
dinoprostone
prostaglandin E2 : Prostaglandin F2alpha in which the hydroxy group at position 9 has been oxidised to the corresponding ketone. Prostaglandin E2 is the most common and most biologically potent of mammalian prostaglandins.		2.3720prostaglandins Ehuman metabolite;
mouse metabolite;
oxytocic
leukotriene b4
Leukotriene B4: The major metabolite in neutrophil polymorphonuclear leukocytes. It stimulates polymorphonuclear cell function (degranulation, formation of oxygen-centered free radicals, arachidonic acid release, and metabolism). (From Dictionary of Prostaglandins and Related Compounds, 1990). leukotriene B4 : A leukotriene composed of (6Z,8E,10E,14Z)-icosatetraenoic acid having (5S)- and (12R)-hydroxy substituents. It is a lipid mediator of inflammation that is generated from arachidonic acid via the 5-lipoxygenase pathway.		2.3720dihydroxy monocarboxylic acid;
hydroxy polyunsaturated fatty acid;
leukotriene;
long-chain fatty acid		human metabolite;
mouse metabolite;
plant metabolite;
vasoconstrictor agent
kme 4
KME 4: structure given in first source		2.6730
ci 987
CI 987: structure in first source		1.9810
piroxicam
[no description available]		2.8840benzothiazine;
monocarboxylic acid amide;
pyridines		analgesic;
antirheumatic drug;
cyclooxygenase 1 inhibitor;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-steroidal anti-inflammatory drug
rifampin
Rifampin: A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160)		1.9810cyclic ketal;
hydrazone;
N-iminopiperazine;
N-methylpiperazine;
rifamycins;
semisynthetic derivative;
zwitterion		angiogenesis inhibitor;
antiamoebic agent;
antineoplastic agent;
antitubercular agent;
DNA synthesis inhibitor;
EC 2.7.7.6 (RNA polymerase) inhibitor;
Escherichia coli metabolite;
geroprotector;
leprostatic drug;
neuroprotective agent;
pregnane X receptor agonist;
protein synthesis inhibitor
ConditionIndicatedRelationship StrengthStudiesTrials
Gastric Ulcer
[description not available]		02.3720
Stomach Ulcer
Ulceration of the GASTRIC MUCOSA due to contact with GASTRIC JUICE. It is often associated with HELICOBACTER PYLORI infection or consumption of nonsteroidal anti-inflammatory drugs (NSAIDS).		02.3720
Innate Inflammatory Response
[description not available]		02.3720
Inflammation
A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.		02.3720
Adjuvant Arthritis
[description not available]		01.9710
Pyrexia
[description not available]		01.9710
Ache
[description not available]		01.9710
Fever
An abnormal elevation of body temperature, usually as a result of a pathologic process.		01.9710
Pain
An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.		01.9710