Compounds > sc 51316
Page last updated: 2024-12-07

sc 51316

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

Description

SC 51316: structure given in first source; an angiotensin II receptor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID131654
CHEMBL ID87778
SCHEMBL ID7398914
MeSH IDM0202390

Synonyms (16)

Synonym
sc-51316 ,
CHEMBL87778 ,
bdbm50044355
2,5-dibutyl-4-[2''-(1h-tetrazol-5-yl)-biphenyl-4-ylmethyl]-2,4-dihydro-[1,2,4]triazol-3-one(sc-15316)
2,5-dibutyl-4-[2''-(2h-tetrazol-5-yl)-biphenyl-4-ylmethyl]-[1,2,4]triazolidin-3-one
2,5-dibutyl-4-[2''-(2h-tetrazol-5-yl)-biphenyl-4-ylmethyl]-2,4-dihydro-[1,2,4]triazol-3-one
133690-62-7
2,5-dibutyl-2,4-dihydro-4-((2-(1h-tetrazol-5-yl)(1,1'-biphenyl)-4'-yl)methyl)-3h-1,2,4-triazol-3-one
3h-1,2,4-triazol-3-one, 2,5-dibutyl-2,4-dihydro-4-((2'-(1h-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl)-
sc 51316
L008865
2,5-dibutyl-4-[[4-[2-(2h-tetrazol-5-yl)phenyl]phenyl]methyl]-1,2,4-triazol-3-one
2,5-dibutyl-2,4-dihydro-4-((2-(1h-tetrazol-5-yl)(1,1-biphenyl)-4-yl)methyl)-3h-1,2,4-triazol-3-one
SCHEMBL7398914
DTXSID30158321
4-((2'-(1h-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2,5-dibutyl-2,4-dihydro-3h-1,2,4-triazol-3-one
[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)
Type-1B angiotensin II receptorRattus norvegicus (Norway rat)IC50 (µMol)0.00510.00040.13343.8000AID37696
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (10)

Assay IDTitleYearJournalArticle
AID166678Antagonism of angiotensin-II mediated contraction of rabbit aortic rings expressed as pA2 (in vitro)1993Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15
Synthesis and structure-activity relationships of nonpeptide, potent triazolone-based angiotensin II receptor antagonists.
AID37696Inhibition of [125I]angiotensin-II binding to the angiotensin II receptor type 1 in rat uterine membranes1993Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15
Synthesis and structure-activity relationships of nonpeptide, potent triazolone-based angiotensin II receptor antagonists.
AID568872Antagonist activity at angiotensin AT1 receptor in rabbit aorta assessed as reduction of angiotensin 2-induced contractile response2010Bioorganic & medicinal chemistry, Dec-15, Volume: 18, Issue:24
Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists--a perspective.
AID183065Inhibition of AII pressor response expressed as peak inhibition in conscious normotensive rats at 1 mg/Kg i.v.1993Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
Triazolinones as nonpeptide angiotensin II antagonists. 1. Synthesis and evaluation of potent 2,4,5-trisubstituted triazolinones.
AID39810In vitro antagonistic activity for AT1 receptor by displacing 125I[Sar, ILe8]AII radioligand in rabbit aorta membrane using 0.2% bovine serum albumin (BSA)1993Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
Triazolinones as nonpeptide angiotensin II antagonists. 1. Synthesis and evaluation of potent 2,4,5-trisubstituted triazolinones.
AID568907Antagonist activity at angiotensin AT1 receptor in rat uterine membranes2010Bioorganic & medicinal chemistry, Dec-15, Volume: 18, Issue:24
Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists--a perspective.
AID182945In vivo inhibition of pressor response to AII in rats following intragastric administration1993Journal of medicinal chemistry, Jul-23, Volume: 36, Issue:15
Synthesis and structure-activity relationships of nonpeptide, potent triazolone-based angiotensin II receptor antagonists.
AID39811In vitro antagonistic activity for AT1 receptor by displacing 125I[Sar, ILe8]AII radioligand in rabbit aorta membrane without using bovine serum albumin (BSA)1993Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
Triazolinones as nonpeptide angiotensin II antagonists. 1. Synthesis and evaluation of potent 2,4,5-trisubstituted triazolinones.
AID39812In vitro antagonistic activity for angiotensin II receptor, type 1 by displacing 125I[Sar, ILe8 ]AII radioligand in rabbit aorta membrane without using bovine serum albumin (BSA)1993Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
Triazolinones as nonpeptide angiotensin II antagonists. 1. Synthesis and evaluation of potent 2,4,5-trisubstituted triazolinones.
AID174623Duration of inhibition of AII pressor response no longer observed in conscious normotensive rats at 1 mg/Kg i.v.1993Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
Triazolinones as nonpeptide angiotensin II antagonists. 1. Synthesis and evaluation of potent 2,4,5-trisubstituted triazolinones.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (9)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's8 (88.89)18.2507
2000's0 (0.00)29.6817
2010's1 (11.11)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.86

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 Index11.86 (24.57)
Research Supply Index2.30 (2.92)
Research Growth Index4.17 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.86)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (22.22%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other7 (77.78%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
candesartan cilexetil
candesartan cilexetil: a prodrug which is metabolized to an active form candesartan to exert its biological effects		3.1510biphenyls
candesartan
candesartan: a nonpeptide angiotensin II receptor antagonist. candesartan : A benzimidazolecarboxylic acid that is 1H-benzimidazole-7-carboxylic acid substituted by an ethoxy group at position 2 and a ({2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl}methyl) group at position 1. It is a angiotensin receptor antagonist used for the treatment of hypertension.		3.1510benzimidazolecarboxylic acid;
biphenylyltetrazole		angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
avapro
Irbesartan: A spiro compound, biphenyl and tetrazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION, and in the treatment of kidney disease.. irbesartan : A biphenylyltetrazole that is an angiotensin II receptor antagonist used mainly for the treatment of hypertension.		3.1510azaspiro compound;
biphenylyltetrazole		angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
losartan
Losartan: An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.. losartan : A biphenylyltetrazole where a 1,1'-biphenyl group is attached at the 5-position and has an additional trisubstituted imidazol-1-ylmethyl group at the 4'-position		4.1850biphenylyltetrazole;
imidazoles		angiotensin receptor antagonist;
anti-arrhythmia drug;
antihypertensive agent;
endothelin receptor antagonist
aldosterone
[no description available]		1.981011beta-hydroxy steroid;
18-oxo steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(4) steroid;
C21-steroid hormone;
mineralocorticoid;
primary alpha-hydroxy ketone;
steroid aldehyde		human metabolite;
mouse metabolite
dup 532
DuP 532: angiotensin I receptor antagonist		3.1510
valsartan
Valsartan: A tetrazole derivative and ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKER that is used to treat HYPERTENSION.. valsartan : A monocarboxylic acid amide consisting of L-valine in which the amino hydrogens have been replaced by a pentanoyl and a [2'-(1H-tetrazol-5-yl)biphenyl]-4-yl]methyl group. It exhibits antihypertensive activity.		3.1510biphenylyltetrazole;
monocarboxylic acid amide;
monocarboxylic acid		angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
tasosartan
tasosartan: angiotensin II antagonist; structure given in first source		3.1510biphenyls
telmisartan
Telmisartan: A biphenyl compound and benzimidazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION.. telmisartan : A member of the class of benzimidazoles used widely in the treatment of hypertension.		3.1510benzimidazoles;
biphenyls;
carboxybiphenyl		angiotensin receptor antagonist;
antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
environmental contaminant;
xenobiotic
triazoles
Triazoles: Heterocyclic compounds containing a five-membered ring with two carbon atoms and three nitrogen atoms with the molecular formula C2H3N3.. triazoles : An azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms.		4.47701,2,3-triazole
gr 117289
GR 117289: angiotensin AT1 receptor antagonist; structure given in first source. zolasartan : A member of the class of 1-benzofurans that is 3-bromo-1-benzofuran which is substituted by a 2-(1H-tetrazol-5-yl)phenyl group at position 2 and by a (2-butyl-5-carboxy-4-chloro-1H-imidazol-1-yl)methyl group at position 5. It is an angiotensin II receptor type 1 (AT1) antagonist and was in clinical trials for the treatment of hypertension (now discontinued).		3.15101-benzofurans;
biaryl;
imidazolyl carboxylic acid;
monocarboxylic acid;
organobromine compound;
organochlorine compound;
tetrazoles		angiotensin receptor antagonist;
antihypertensive agent
exp3174
losartan carboxylic acid: structure given in first source. losartan carboxylic acid : A biphenylyltetrazole that is losartan with the hydroxymethyl group at position 5 on the imidazole ring replaced with a carboxylic acid.		3.5120biphenylyltetrazole;
imidazoles;
organochlorine compound		metabolite
3-((2'-carboxybiphenyl-4-yl)methyl)-2-cyclopropyl-7-methyl-3h-imidazo(4,5-b)pyridine
3-((2'-carboxybiphenyl-4-yl)methyl)-2-cyclopropyl-7-methyl-3H-imidazo(4,5-b)pyridine: a non-peptide angiotensin II-receptor antagonist; structure given in first source		3.1510
a 81988
A 81988: angiotensin II antagonist selective for type 1 receptors		3.1510
ici d8731
ICI D8731: structure given in first source; an angiotensin II receptor antagonist		3.1510
forasartan
forasartan: structure given in first source; an angiotensin AT(1) receptor antagonist; angiotensin II receptor antagonist; used in treatment of congestive heart failure. forasartan : A member of the class of pyridines that is pyridine which is substituted at positions 2 and 5 by o-(tetrazol-5-yl)phenyl and (3,5-dibutyl-1,2,4-triazol-1-yl)methyl groups, respectively. It is a nonpeptide antagonist of angiotensin II, type 1 (AT1) receptors, used for the treatment of hypertension.		3.1510benzenes;
pyridines;
tetrazoles;
triazoles		angiotensin receptor antagonist;
antihypertensive agent
up 269-6
UP 269-6: structure given in first source; angiotensin receptor antagonist		3.1510
mk 996
MK 996: an AT1-selective angiotensin II receptor antagonist; structure given in first source		3.1510
olmesartan
olmesartan: an active metabolite of CS 866		3.1510biphenylyltetrazoleangiotensin receptor antagonist;
antihypertensive agent
angiotensin ii
Giapreza: injectable form of angiotensin II used to increase blood pressure in adult patients with septic or other distributive shock. Ile(5)-angiotensin II : An angiotensin II that acts on the central nervous system (PDB entry: 1N9V).		3.7730amino acid zwitterion;
angiotensin II		human metabolite
me 3221
ME 3221: an angiotensin II receptor antagonist; structure given in first source		3.1510
l 158809
L 158809: RN & structure given in first source; angiotensin receptor antagonist		3.1510
cv 11194
CV 11194: structure given in first source; an angiotensin II receptor antagonist		3.1510
milfasartan
milfasartan: angiotensin I receptor antagonist; structure in first source		3.1510
dmp 811
DMP 811: angiotensin II receptor antagonist; structure given in first source		3.1510
eprosartan
eprosartan: angiotensin II receptor antagonist. eprosartan : A member of the class of imidazoles and thiophenes that is an angiotensin II receptor antagonist used for the treatment of high blood pressure.		3.1510dicarboxylic acid;
imidazoles;
thiophenes		angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
enalapril
Enalapril: An angiotensin-converting enzyme inhibitor that is used to treat HYPERTENSION and HEART FAILURE.. enalapril : A dicarboxylic acid monoester that is ethyl 4-phenylbutanoate in which a hydrogen alpha to the carboxy group is substituted by the amino group of L-alanyl-L-proline (S-configuration).		4.1850dicarboxylic acid monoester;
dipeptide		antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
geroprotector;
prodrug
pratosartan
pratosartan: angiotensin II type 1 receptor blocker		3.1510biphenylyltetrazoleantihypertensive agent
transforming growth factor beta
Transforming Growth Factor beta: A factor synthesized in a wide variety of tissues. It acts synergistically with TGF-alpha in inducing phenotypic transformation and can also act as a negative autocrine growth factor. TGF-beta has a potential role in embryonal development, cellular differentiation, hormone secretion, and immune function. TGF-beta is found mostly as homodimer forms of separate gene products TGF-beta1, TGF-beta2 or TGF-beta3. Heterodimers composed of TGF-beta1 and 2 (TGF-beta1.2) or of TGF-beta2 and 3 (TGF-beta2.3) have been isolated. The TGF-beta proteins are synthesized as precursor proteins.		3.4920
azilsartan
azilsartan: an angiotensin type 1 receptor blocker; receptor blocker. azilsartan : A benzimidazolecarboxylic acid that is benzimidazole-7-carboxylic acid substituted at position 2 by a methoxy group and at position 1 by a 2'-[(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl group. Used (as the prodrug, azilsartan medoxomil) for treatment of hypertension.		3.15101,2,4-oxadiazole;
aromatic ether;
benzimidazolecarboxylic acid		angiotensin receptor antagonist;
antihypertensive agent
ConditionIndicatedRelationship StrengthStudiesTrials
Cirrhosis
[description not available]		02.910
Ureteral Obstruction
Blockage in any part of the URETER causing obstruction of urine flow from the kidney to the URINARY BLADDER. The obstruction may be congenital, acquired, unilateral, bilateral, complete, partial, acute, or chronic. Depending on the degree and duration of the obstruction, clinical features vary greatly such as HYDRONEPHROSIS and obstructive nephropathy.		03.630
Fibrosis
Any pathological condition where fibrous connective tissue invades any organ, usually as a consequence of inflammation or other injury.		02.910
Kidney Diseases
Pathological processes of the KIDNEY or its component tissues.		02.910
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.3920
Interstitial Nephritis
[description not available]		01.9810
Nephritis, Interstitial
Inflammation of the interstitial tissue of the kidney. This term is generally used for primary inflammation of KIDNEY TUBULES and/or surrounding interstitium. For primary inflammation of glomerular interstitium, see GLOMERULONEPHRITIS. Infiltration of the inflammatory cells into the interstitial compartment results in EDEMA, increased spaces between the tubules, and tubular renal dysfunction.		01.9810
Blood Pressure, High
[description not available]		01.9810
Hypertension
Persistently high systemic arterial BLOOD PRESSURE. Based on multiple readings (BLOOD PRESSURE DETERMINATION), hypertension is currently defined as when SYSTOLIC PRESSURE is consistently greater than 140 mm Hg or when DIASTOLIC PRESSURE is consistently 90 mm Hg or more.		01.9810
Arteriosclerosis
Thickening and loss of elasticity of the walls of ARTERIES of all sizes. There are many forms classified by the types of lesions and arteries involved, such as ATHEROSCLEROSIS with fatty lesions in the ARTERIAL INTIMA of medium and large muscular arteries.		01.9810