Compounds > a-76745
Page last updated: 2024-12-06

a-76745

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

Description

fenleuton: LoFrin is tradename [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID72059
CHEMBL ID293743
SCHEMBL ID74861
MeSH IDM0284400

Synonyms (34)

Synonym
141579-54-6
lofrin [veterinary] (tn)
fenleuton (usan/inn)
D04151
fenleuton
abbott-76745
a-76745
CHEMBL293743 ,
1-[4-[3-(4-fluorophenoxy)phenyl]but-3-yn-2-yl]-1-hydroxyurea
n-{3-[3-(4-fluorophenoxy)phenyl]-1-methylprop-2-ynyl}-n-hydroxyurea
bdbm50058590
A808028
1-[4-[3-(4-fluoranylphenoxy)phenyl]but-3-yn-2-yl]-1-oxidanyl-urea
abbott 76745
fenleuton [usan:inn]
lg64454o6i ,
urea, n-(3-(3-(4-fluorophenoxy)phenyl)-1-methyl-2-propynyl)-n-hydroxy-, (+-)-
(+-)-1-(3-(m-(p-fluorophenoxy)phenyl)-1-methyl-2-propynyl)-1-hydroxyurea
unii-lg64454o6i
lofrin
fenleuton [usan]
n-hydroxy-n-(4-(3-(4-fluorophenoxy)phenyl)-3-butyn-2-yl)urea
urea, n-(3-(3-(4-fluorophenoxy)phenyl)-1-methyl-2-propynyl)-n-hydroxy-
fenleuton [inn]
urea, n-(3-(3-(4-fluorophenoxy)phenyl)-1-methyl-2-propynyl)-n-hydroxy-, (+/-)-
urea, n-(3-(3-(4-fluorophenoxy)phenyl)-1-methyl-2-propyn-1-yl)-n-hydroxy-
SCHEMBL74861
n-hydroxy-n-[4-(3-(4-fluorophenoxy)phenyl)-3-butyn-2-yl]urea
MWXPQCKCKPYBDR-UHFFFAOYSA-N
Q21834146
a76745
DTXSID40869916
urea, n-[3-[3-(4-fluorophenoxy)phenyl]-1-methyl-2-propyn-1-yl]-n-hydroxy-
AKOS040748348

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" Six horses with COPD underwent a series of four antigen challenges, one month apart, with placebo pre-treatment on three occasions and fenleuton (4 days oral dosing 5 mg/kg) pre-treatment on one occasion."( Effect of the 5-lipoxygenase inhibitor, fenleuton, on antigen-induced neutrophil accumulation and lung function changes in horses with chronic obstructive pulmonary disease.
Cunningham, FM; Lees, P; Marr, KA; Page, CP, 1998)		0.3
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Polyunsaturated fatty acid 5-lipoxygenaseRattus norvegicus (Norway rat)IC50 (µMol)0.30000.00462.018210.0000AID7101
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (10)

Assay IDTitleYearJournalArticle
AID1657000Plasma clearance in iv dosed cynomolgus monkey2020Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11
Acetylene Group, Friend or Foe in Medicinal Chemistry.
AID92880Inhibition of 5-lipoxygenase (5-LO) measured as LTB4 production in human whole blood stimulated with calcium ionophore (A23187).1997Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13
Structure-activity relationships of N-hydroxyurea 5-lipoxygenase inhibitors.
AID181942Percent inhibition of LTE4 formation in rats from peritoneal fluids at a dose of 200 micro mol/Kg1997Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13
Structure-activity relationships of N-hydroxyurea 5-lipoxygenase inhibitors.
AID24080t1/2 in monkey after IV dose (9 umol/kg)1997Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13
Structure-activity relationships of N-hydroxyurea 5-lipoxygenase inhibitors.
AID180525The compound was tested for in vivo activity for rat anaphylaxis leukotriene formation on an oral dose of 30 micro mol/Kg1997Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13
Structure-activity relationships of N-hydroxyurea 5-lipoxygenase inhibitors.
AID1656999Substrate activity at UDP-glucuronosyltransferase in cynomolgus monkey microsomes assessed as Vmax2020Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11
Acetylene Group, Friend or Foe in Medicinal Chemistry.
AID21697Measured rat plasma levels (uM) one hour post PO dose1997Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13
Structure-activity relationships of N-hydroxyurea 5-lipoxygenase inhibitors.
AID1657001Half life in cynomolgus monkey2020Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11
Acetylene Group, Friend or Foe in Medicinal Chemistry.
AID7101Inhibition of 5-lipoxygenase on rat basophil leukemia cell line lysate (RBL-1 2H3 subline) by measuring 5-HETE production1997Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13
Structure-activity relationships of N-hydroxyurea 5-lipoxygenase inhibitors.
AID18863Rate of glucuronidation (nmol/min/mg protein) in monkey microsomes1997Journal of medicinal chemistry, Jun-20, Volume: 40, Issue:13
Structure-activity relationships of N-hydroxyurea 5-lipoxygenase inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (4)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's3 (75.00)18.2507
2000's0 (0.00)29.6817
2010's0 (0.00)24.3611
2020's1 (25.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.53

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.53 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.32 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.53)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other5 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
hydroxyurea
[no description available]		2.420one-carbon compound;
ureas		antimetabolite;
antimitotic;
antineoplastic agent;
DNA synthesis inhibitor;
EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor;
genotoxin;
immunomodulator;
radical scavenger;
teratogenic agent
bromouracil
Bromouracil: 5-Bromo-2,4(1H,3H)-pyrimidinedione. Brominated derivative of uracil that acts as an antimetabolite, substituting for thymine in DNA. It is used mainly as an experimental mutagen, but its deoxyriboside (BROMODEOXYURIDINE) is used to treat neoplasms.. 5-bromouracil : A pyrimidine having keto groups at the 2- and 4-positions and a bromo group at the 5-position. Used mainly as an experimental mutagen.		2.2510nucleobase analogue;
pyrimidines		mutagen
trifluoromethyluracil
[no description available]		2.2510
stavudine
Stavudine: A dideoxynucleoside analog that inhibits reverse transcriptase and has in vitro activity against HIV.. stavudine : A nucleoside analogue obtained by formal dehydration across positions 2 and 3 of thymidine. An inhibitor of HIV-1 reverse transcriptase		2.2510dihydrofuran;
nucleoside analogue;
organic molecular entity		antimetabolite;
antiviral agent;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor
selegiline
Selegiline: A selective, irreversible inhibitor of Type B monoamine oxidase that is used for the treatment of newly diagnosed patients with PARKINSON DISEASE, and for the treatment of depressive disorders. The compound without isomeric designation is Deprenyl.		2.2510selegiline;
terminal acetylenic compound		geroprotector
eniluracil
eniluracil: structure in first source; inactivates dihydropyrimidine dehydrogenase		2.2510pyrimidone
mifepristone
Mifepristone: A progestational and glucocorticoid hormone antagonist. Its inhibition of progesterone induces bleeding during the luteal phase and in early pregnancy by releasing endogenous prostaglandins from the endometrium or decidua. As a glucocorticoid receptor antagonist, the drug has been used to treat hypercortisolism in patients with nonpituitary CUSHING SYNDROME.		2.25103-oxo-Delta(4) steroid;
acetylenic compound;
tertiary amino compound		abortifacient;
contraceptive drug;
hormone antagonist;
synthetic oral contraceptive
zileuton
[no description available]		2.45201-benzothiophenes;
ureas		anti-asthmatic drug;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
ferroptosis inhibitor;
leukotriene antagonist;
non-steroidal anti-inflammatory drug
a 78773
A 78773: a 5-lipoxygenase inhibitor		1.9910
5-diazouracil
5-diazouracil: RN given refers to parent cpd; structure		2.2510
5-cyanouracil
[no description available]		2.2510
gefitinib
[no description available]		2.2510aromatic ether;
monochlorobenzenes;
monofluorobenzenes;
morpholines;
quinazolines;
secondary amino compound;
tertiary amino compound		antineoplastic agent;
epidermal growth factor receptor antagonist
erlotinib
[no description available]		2.2510aromatic ether;
quinazolines;
secondary amino compound;
terminal acetylenic compound		antineoplastic agent;
epidermal growth factor receptor antagonist;
protein kinase inhibitor
tv3326
[no description available]		2.2510indanes
5-(2-bromovinyl)uracil
5-(2-bromovinyl)uracil: RN given refers to (E)-isomer		2.2510
2',3'-didehydro-3'-deoxy-4'-ethynylthymidine
2',3'-didehydro-3'-deoxy-4'-ethynylthymidine: a highly active anti-HIV agent; structure in first source		2.2510
via 2291
atreleuton: structure given in first source		1.9910
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.		1.9910dihydroxy monocarboxylic acid;
hydroxy polyunsaturated fatty acid;
leukotriene;
long-chain fatty acid		human metabolite;
mouse metabolite;
plant metabolite;
vasoconstrictor agent
bw b70c
BW B70C: arachidonic acid antagonist. BW B70C : A hydroxamic acid that is urea in which both the hydrogens attached to one of the nitrogens are replaced by a hydroxy and a (1E)-1-[3-(4-fluorophenoxy)phenyl]but-1-en-3-yl group. A selective inhibitor of arachidonate 5-lipoxygenase, it can be used for the treatment of asthma.		2.2510aromatic ether;
hydroxamic acid;
organofluorine compound;
ureas		EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor
enviradene
[no description available]		2.2510
epoxyfarnesyl diazoacetate
2'-deoxy-4'-C-ethynyl-2-fluoroadenosine: has anti-HIV activity; structure in first source		2.2510
pf9601n
[no description available]		2.2510
abbott 66193
N-dehydroxyzileuton: structure given in first source		1.99101-benzothiophenes
ConditionIndicatedRelationship StrengthStudiesTrials
Body Weight
The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.		01.9910
Besnoitiasis
[description not available]		01.9910
Poultry Diseases
Diseases of birds which are raised as a source of meat or eggs for human consumption and are usually found in barnyards, hatcheries, etc. The concept is differentiated from BIRD DISEASES which is for diseases of birds not considered poultry and usually found in zoos, parks, and the wild.		01.9910
Aging
The gradual irreversible changes in structure and function of an organism that occur as a result of the passage of time.		01.9910
Equine Diseases
[description not available]		01.9910
Obstructive Lung Diseases
[description not available]		01.9910
Lung Diseases, Obstructive
Any disorder marked by obstruction of conducting airways of the lung. AIRWAY OBSTRUCTION may be acute, chronic, intermittent, or persistent.		01.9910