Page last updated: 2024-11-08

carbenoxolone

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

Cross-References

ID SourceID
PubMed CID636403
CHEMBL ID499915
SCHEMBL ID76013
MeSH IDM0003342

Synonyms (48)

Synonym
BRD-K12765235-304-03-8
(3beta)-3-[(3-carboxypropanoyl)oxy]-11-oxoolean-12-en-30-oic acid
3beta-hydroxy-11-oxoolean-12-en-30-saeure hydogensuccinat
olean-12-en-30-oic acid, 3-beta-hydroxy-11-oxo-, hydrogen succinate
olean-12-en-29-oic acid, 3-(3-carboxy-1-oxopropoxy)-11-oxo-, (3beta,20beta)-
carbenoxolone [inn:ban]
3-beta-(3-carboxypropionyloxy)-11-oxo-olean-12-en-30-oic acid
carbenoxolonum [inn-latin]
3beta-(3-carboxypropionyloxy)-11-oxo-olean-12-en-30-saeure
carbenoxolona [inn-spanish]
einecs 227-174-2
PRESTWICK3_000837
carbenoxolone (inn)
D07615
BSPBIO_000793
PRESTWICK2_000837
DB02329
PRESTWICK1_000837
SPBIO_002714
PRESTWICK0_000837
BPBIO1_000873
3beta-o-succinyl-18-beta-glycyrrhetinic acid
bdbm50247012
CHEMBL499915
(2s,4as,6ar,6as,6br,8ar,10s,12as,14br)-10-(4-hydroxy-4-oxobutanoyl)oxy-2,4a,6a,6b,9,9,12a-heptamethyl-13-oxo-3,4,5,6,6a,7,8,8a,10,11,12,14b-dodecahydro-1h-picene-2-carboxylic acid
AKOS015951361
AKOS016036240
carbenoxolonum
mm6384ng73 ,
unii-mm6384ng73
carbenoxolona
carbenoxolone [mi]
carbenoxolone [inn]
olean-12-en-29-oic acid, 3-(3-carboxy-1-oxopropoxy)-11-oxo, (3.beta.,20.beta.)-
carbenoxolone [who-dd]
3.beta.-hydroxy-11-oxoolean-12-en-30-oic acid hydrogen succinate
gtpl4151
olean-12-en-29-oic acid, 3-(3-carboxy-1-oxopropoxy)-11-oxo-, (3.beta.,20.beta.)-
SCHEMBL76013
3.beta.-hydroxy-11-oxoolean-12-en-30-oic acid 3-hemisuccinate
DTXSID4022733
(3beta,5beta,10alpha,14beta)-3-[(3-carboxypropanoyl)oxy]-11-oxoolean-12-en-29-oic acid
Q752861
BCP29160
biogastrone; bioral; carbenoxolona
CS-0013487
HY-B1588
olean-12-en-29-oic acid, 3-(3-carboxy-1-oxopropoxy)-11-oxo-,(3b,20b)-

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" Through modification of our initial lead 5, we have identified potent and selective 11beta-HSD1 inhibitors, such as 11n, which demonstrated improved glycemic control, decreased serum lipids, and enhanced insulin sensitivity when dosed ip in diabetic ob/ob mice."( 4-(Phenylsulfonamidomethyl)benzamides as potent and selective inhibitors of the 11beta-hydroxysteroid dehydrogenase type 1 with efficacy in diabetic ob/ob mice.
Chen, J; Du, L; Feng, Y; Leng, Y; Shen, J; Yang, H; Zhang, X; Zhou, Z, 2009
)
0.35
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (6)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Corticosteroid 11-beta-dehydrogenase isozyme 1Homo sapiens (human)IC50 (µMol)0.49910.00411.066710.0000AID1516423; AID1646812; AID1873295; AID3086; AID3089; AID461097; AID550731; AID664823
Corticosteroid 11-beta-dehydrogenase isozyme 1Homo sapiens (human)Ki0.06200.00100.10010.6200AID1516423
Sterol O-acyltransferase 1Homo sapiens (human)IC50 (µMol)0.10800.02501.79758.0000AID3088
Corticosteroid 11-beta-dehydrogenase isozyme 1Mus musculus (house mouse)IC50 (µMol)0.20030.00200.24103.7600AID1646813; AID3088; AID550732
Corticosteroid 11-beta-dehydrogenase isozyme 2Mus musculus (house mouse)IC50 (µMol)0.14400.08200.14400.2060AID433140; AID664593
Corticosteroid 11-beta-dehydrogenase isozyme 2Homo sapiens (human)IC50 (µMol)0.17000.00040.63676.4300AID1516424
Pannexin-1Mus musculus (house mouse)IC50 (µMol)10.00000.27005.135010.0000AID1772526
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Corticosteroid 11-beta-dehydrogenase isozyme 2Mus musculus (house mouse)EC50 (µMol)0.08200.08200.08200.0820AID657951
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (19)

Processvia Protein(s)Taxonomy
lung developmentCorticosteroid 11-beta-dehydrogenase isozyme 1Homo sapiens (human)
steroid catabolic processCorticosteroid 11-beta-dehydrogenase isozyme 1Homo sapiens (human)
cholesterol metabolic processSterol O-acyltransferase 1Homo sapiens (human)
cholesterol metabolic processSterol O-acyltransferase 1Homo sapiens (human)
macrophage derived foam cell differentiationSterol O-acyltransferase 1Homo sapiens (human)
cholesterol storageSterol O-acyltransferase 1Homo sapiens (human)
cholesterol effluxSterol O-acyltransferase 1Homo sapiens (human)
very-low-density lipoprotein particle assemblySterol O-acyltransferase 1Homo sapiens (human)
low-density lipoprotein particle clearanceSterol O-acyltransferase 1Homo sapiens (human)
cholesterol homeostasisSterol O-acyltransferase 1Homo sapiens (human)
positive regulation of amyloid precursor protein biosynthetic processSterol O-acyltransferase 1Homo sapiens (human)
response to hypoxiaCorticosteroid 11-beta-dehydrogenase isozyme 2Homo sapiens (human)
regulation of blood volume by renal aldosteroneCorticosteroid 11-beta-dehydrogenase isozyme 2Homo sapiens (human)
female pregnancyCorticosteroid 11-beta-dehydrogenase isozyme 2Homo sapiens (human)
response to xenobiotic stimulusCorticosteroid 11-beta-dehydrogenase isozyme 2Homo sapiens (human)
response to foodCorticosteroid 11-beta-dehydrogenase isozyme 2Homo sapiens (human)
response to insulinCorticosteroid 11-beta-dehydrogenase isozyme 2Homo sapiens (human)
cortisol metabolic processCorticosteroid 11-beta-dehydrogenase isozyme 2Homo sapiens (human)
response to glucocorticoidCorticosteroid 11-beta-dehydrogenase isozyme 2Homo sapiens (human)
glucocorticoid metabolic processCorticosteroid 11-beta-dehydrogenase isozyme 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (13)

Processvia Protein(s)Taxonomy
protein homodimerization activityCorticosteroid 11-beta-dehydrogenase isozyme 1Homo sapiens (human)
7-beta-hydroxysteroid dehydrogenase (NADP+) activityCorticosteroid 11-beta-dehydrogenase isozyme 1Homo sapiens (human)
NADP bindingCorticosteroid 11-beta-dehydrogenase isozyme 1Homo sapiens (human)
11-beta-hydroxysteroid dehydrogenase (NADP+) activityCorticosteroid 11-beta-dehydrogenase isozyme 1Homo sapiens (human)
cortisol dehydrogenase activityCorticosteroid 11-beta-dehydrogenase isozyme 1Homo sapiens (human)
steroid bindingCorticosteroid 11-beta-dehydrogenase isozyme 1Homo sapiens (human)
fatty-acyl-CoA bindingSterol O-acyltransferase 1Homo sapiens (human)
sterol O-acyltransferase activitySterol O-acyltransferase 1Homo sapiens (human)
protein bindingSterol O-acyltransferase 1Homo sapiens (human)
cholesterol bindingSterol O-acyltransferase 1Homo sapiens (human)
cholesterol O-acyltransferase activitySterol O-acyltransferase 1Homo sapiens (human)
steroid bindingCorticosteroid 11-beta-dehydrogenase isozyme 2Homo sapiens (human)
NAD bindingCorticosteroid 11-beta-dehydrogenase isozyme 2Homo sapiens (human)
11-beta-hydroxysteroid dehydrogenase (NAD+) activityCorticosteroid 11-beta-dehydrogenase isozyme 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (4)

Processvia Protein(s)Taxonomy
endoplasmic reticulum membraneCorticosteroid 11-beta-dehydrogenase isozyme 1Homo sapiens (human)
membraneCorticosteroid 11-beta-dehydrogenase isozyme 1Homo sapiens (human)
endoplasmic reticulum membraneCorticosteroid 11-beta-dehydrogenase isozyme 1Homo sapiens (human)
intracellular membrane-bounded organelleCorticosteroid 11-beta-dehydrogenase isozyme 1Homo sapiens (human)
endoplasmic reticulumSterol O-acyltransferase 1Homo sapiens (human)
endoplasmic reticulum membraneSterol O-acyltransferase 1Homo sapiens (human)
membraneSterol O-acyltransferase 1Homo sapiens (human)
endoplasmic reticulum membraneSterol O-acyltransferase 1Homo sapiens (human)
endoplasmic reticulum membraneCorticosteroid 11-beta-dehydrogenase isozyme 2Homo sapiens (human)
intracellular membrane-bounded organelleCorticosteroid 11-beta-dehydrogenase isozyme 2Homo sapiens (human)
intracellular membrane-bounded organelleCorticosteroid 11-beta-dehydrogenase isozyme 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (76)

Assay IDTitleYearJournalArticle
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID75524Evaluation of bronchodilator activity at dose 60 mg/kg perorally 1 hr prior to histamine aerosol exposure1980Journal of medicinal chemistry, Sep, Volume: 23, Issue:9
Bronchodilator and antiulcer phenoxypyrimidinones.
AID1328531Gastroprotective activity in Swiss albino mouse assessed as reduction in HCl/EtOH-induced gastric lesions by measuring lesion index at 100 mg/kg, po pretreated for 50 mins followed by HCl/EtOH challenge measured after 1 hr (Rvb = 38.8 +/- 1.6 millimeter)2016Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23
Gastroprotective activity of synthetic coumarins: Role of endogenous prostaglandins, nitric oxide, non-protein sulfhydryls and vanilloid receptors.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID664823Inhibition of human 11beta-HSD1 expressed in CHO-K1 cells using cortisone as substrate after 3 hrs by HTRF assay2012ACS medicinal chemistry letters, Feb-09, Volume: 3, Issue:2
Synthesis and biological evaluation of cyclic sulfamide derivatives as 11β-hydroxysteroid dehydrogenase 1 inhibitors.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID496830Antimicrobial activity against Leishmania major2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID550732Inhibition of mouse 11beta-HSD1 expressed in CHO cells after 3 hrs by HTRF cortisol assay2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
Synthesis and 11β hydroxysteroid dehydrogenase 1 inhibition of thiazolidine derivatives with an adamantyl group.
AID1516425Cytotoxicity against mouse 3T3L1 cells measured after 72 hrs by celltiter-glo luminescent cell viability assay2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Mechanistic Insight on the Mode of Action of Colletoic Acid.
AID664593Inhibition of mouse 11beta-HSD2 expressed in HEK293 cells assessed as conversion of [3H]cortisone into [3H]cortisol by scintillation proximity assay2012Journal of natural products, Apr-27, Volume: 75, Issue:4
Cycloartane and friedelane triterpenoids from the leaves of Caloncoba glauca and their evaluation for inhibition of 11β-hydroxysteroid dehydrogenases.
AID749046Inhibition of full-length human 11beta-HSD1 expressed in HEK293 cells at 10 uM after 2 hrs by scintillation proximity assay relative to control2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Discovery, synthesis and in combo studies of a tetrazole analogue of clofibric acid as a potent hypoglycemic agent.
AID496818Antimicrobial activity against Trypanosoma brucei brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1772526Inhibition of mouse Panx-1 expressed in Xenopus laevis oocytes assessed as inhibition of membrane current cells held at -60 mV and voltage steps to +60 mV in presence of CBX measured by Whole cell voltage clamp assay relative to control2021European journal of medicinal chemistry, Nov-05, Volume: 223Design and synthesis of the first indole-based blockers of Panx-1 channel.
AID496832Antimicrobial activity against Trypanosoma brucei rhodesiense2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID3088In vitro inhibitory activity against mouse 11 beta hydroxysteroid dehydrogenase type 1 using scintillation proximity assay (SPA).2002Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18
Arylsulfonamidothiazoles as a new class of potential antidiabetic drugs. Discovery of potent and selective inhibitors of the 11beta-hydroxysteroid dehydrogenase type 1.
AID1516424Inhibition of 11beta-HSD2 (unknown origin) expressed in HEK293 cells using cortisone as substrate measured after 2 hrs in presence of NAD+ by HTRF assay2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Mechanistic Insight on the Mode of Action of Colletoic Acid.
AID587114Inhibition of human 11beta-HSD2 expressed in HEK293 cells assessed as residual conversion of [1,2,6,7-[3H]cortisol to cortisone at 1000 nM after 10 mins by scintillation counting2011Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
Synthesis of new glycyrrhetinic acid derived ring A azepanone, 29-urea and 29-hydroxamic acid derivatives as selective 11β-hydroxysteroid dehydrogenase 2 inhibitors.
AID496827Antimicrobial activity against Leishmania amazonensis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID3089Ability to convert [3H]cortisol to the tritium labeled cortisone in the presence of human 11 beta hydroxysteroid dehydrogenase type 22002Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18
Arylsulfonamidothiazoles as a new class of potential antidiabetic drugs. Discovery of potent and selective inhibitors of the 11beta-hydroxysteroid dehydrogenase type 1.
AID461097Inhibition of 11beta-HSD1 in human microsomes by HTRF cortisol assay2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Discovery of cyclicsulfonamide derivatives as 11 beta-hydroxysteroid dehydrogenase 1 inhibitors.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID456097Inhibition of human recombinant 11beta-HSD2 expressed in HEK293 cells assessed as oxidation of [1,2,6,7-3H]cortisol to cortisone at 1 uM after 10 mins by scintillation counting2010Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1
Synthesis of glycyrrhetinic acid derivatives for the treatment of metabolic diseases.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID496831Antimicrobial activity against Cryptosporidium parvum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID587123Inhibition of human recombinant 11beta-HSD2 expressed in HEK293 cells assessed as conversion of [1,2-[3H]cortisone to cortisol at 1 uM after 10 mins by scintillation counting2011Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
Synthesis of new glycyrrhetinic acid derived ring A azepanone, 29-urea and 29-hydroxamic acid derivatives as selective 11β-hydroxysteroid dehydrogenase 2 inhibitors.
AID496817Antimicrobial activity against Trypanosoma cruzi2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1516423Inhibition of N-terminal MKHQHQHQHQHQHQQPL-tagged 11beta-HSD1 C272S mutant (unknown origin) expressed in Escherichia coli BL21 (DE3) using cortisol as substrate measured for 1 hr in presence of NADPH by fluorescence assay2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Mechanistic Insight on the Mode of Action of Colletoic Acid.
AID526978Inhibition of human recombinant 11beta-HSD2 expressed in HEK293 cells assessed as residual conversion of [1,2,6,7-3H]-cortisol to cortisone at 1 uM by scintillation counting2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
Synthesis of novel 3-amino and 29-hydroxamic acid derivatives of glycyrrhetinic acid as selective 11β-hydroxysteroid dehydrogenase 2 inhibitors.
AID496820Antimicrobial activity against Trypanosoma brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID433140Inhibition of mouse microsomal 11beta-HSD2 expressed in HEK293 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
4-(Phenylsulfonamidomethyl)benzamides as potent and selective inhibitors of the 11beta-hydroxysteroid dehydrogenase type 1 with efficacy in diabetic ob/ob mice.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1877784Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production2022Bioorganic & medicinal chemistry letters, 02-15, Volume: 58Microbial transformation and inhibitory effect assessment of uvaol derivates against LPS and HMGB1 induced NO production in RAW264.7 macrophages.
AID496825Antimicrobial activity against Leishmania mexicana2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID3086In vitro inhibitory activity against human 11 beta hydroxysteroid dehydrogenase type 1 using scintillation proximity assay (SPA)2002Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18
Arylsulfonamidothiazoles as a new class of potential antidiabetic drugs. Discovery of potent and selective inhibitors of the 11beta-hydroxysteroid dehydrogenase type 1.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID343737Inhibition of chymotrypsin-like activity of human 20S proteasome2008Bioorganic & medicinal chemistry, Jul-15, Volume: 16, Issue:14
Synthesis and proteasome inhibition of glycyrrhetinic acid derivatives.
AID496829Antimicrobial activity against Leishmania infantum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1877786Cytotoxicity against mouse RAW264.7 cells assessed as cell viability at 50 uM2022Bioorganic & medicinal chemistry letters, 02-15, Volume: 58Microbial transformation and inhibitory effect assessment of uvaol derivates against LPS and HMGB1 induced NO production in RAW264.7 macrophages.
AID496823Antimicrobial activity against Trichomonas vaginalis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID657951Inhibition of mouse 11beta-HSD2 expressed in HEK293 cells assessed as [3H]cortisol production after 60 mins by SPA2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Synthesis and evaluation of piperidine urea derivatives as efficacious 11β-hydroxysteroid dehydrogenase type 1 inhibitors in diabetic ob/ob mice.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID526979Inhibition of human recombinant 11beta-HSD1 expressed in HEK293 cells assessed as residual conversion of [1,2-3H]-cortisone to cortisol at 1 uM by scintillation counting2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
Synthesis of novel 3-amino and 29-hydroxamic acid derivatives of glycyrrhetinic acid as selective 11β-hydroxysteroid dehydrogenase 2 inhibitors.
AID1646812Inhibition of human 11beta-HSD1 expressed in CHOK1 cells using XL665-labeled cortisol as substrate measured after 24 hrs by HTRF assay2020Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2
Optimization of cyclic sulfamide derivatives as 11β-hydroxysteroid dehydrogenase 1 inhibitors for the potential treatment of ischemic brain injury.
AID496826Antimicrobial activity against Entamoeba histolytica2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID496821Antimicrobial activity against Leishmania2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496819Antimicrobial activity against Plasmodium falciparum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1831041Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of HMGB1-induced NO production pretreated with compounds for 15 mins followed by HMGB1 stimulation measured after 24 hrs by Griess reagent based assay2021Bioorganic & medicinal chemistry, 12-15, Volume: 52Microbial transformation of pentacyclic triterpenes for anti-inflammatory agents on the HMGB1 stimulated RAW 264.7 cells by Streptomyces olivaceus CICC 23628.
AID1873295Inhibition of human 11beta-HSD12022Bioorganic & medicinal chemistry letters, 08-01, Volume: 69Discovery of 1'-(1-phenylcyclopropane-carbonyl)-3H-spiro[isobenzofuran-1,3'-pyrrolidin]-3-one as a novel steroid mimetic scaffold for the potent and tissue-specific inhibition of 11β-HSD1 using a scaffold-hopping approach.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1877785Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of HMGB1-induced NO production2022Bioorganic & medicinal chemistry letters, 02-15, Volume: 58Microbial transformation and inhibitory effect assessment of uvaol derivates against LPS and HMGB1 induced NO production in RAW264.7 macrophages.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID409954Inhibition of mouse brain MAOA2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID497005Antimicrobial activity against Pneumocystis carinii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496824Antimicrobial activity against Toxoplasma gondii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID550731Inhibition of human 11beta-HSD1 expressed in CHO cells after 3 hrs by HTRF cortisol assay2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
Synthesis and 11β hydroxysteroid dehydrogenase 1 inhibition of thiazolidine derivatives with an adamantyl group.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID587122Inhibition of human recombinant 11beta-HSD1 expressed in HEK293 cells assessed as conversion of [1,2-[3H]cortisone to cortisol at 1 uM after 10 mins by scintillation counting2011Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
Synthesis of new glycyrrhetinic acid derived ring A azepanone, 29-urea and 29-hydroxamic acid derivatives as selective 11β-hydroxysteroid dehydrogenase 2 inhibitors.
AID456095Inhibition of human recombinant 11beta-HSD1 expressed in HEK293 cells assessed as conversion of [1,2-3H]cortisone to cortisol at 1 uM after 10 mins by scintillation counting2010Bioorganic & medicinal chemistry, Jan-01, Volume: 18, Issue:1
Synthesis of glycyrrhetinic acid derivatives for the treatment of metabolic diseases.
AID1646813Inhibition of mouse 11beta-HSD1 expressed in CHOK1 cells using XL665-labeled cortisol as substrate measured after 24 hrs by HTRF assay2020Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2
Optimization of cyclic sulfamide derivatives as 11β-hydroxysteroid dehydrogenase 1 inhibitors for the potential treatment of ischemic brain injury.
AID496828Antimicrobial activity against Leishmania donovani2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1678918Inhibition of Cx43 in hypoxic-acidic ion-shifted ringers solution-induced human cerebral microvascular endothelial cell model of ischaemic injury assessed as ATP release at 10 uM measured after 2 hrs by luciferin-luciferase based luminescence assay relati2020RSC medicinal chemistry, Sep-01, Volume: 11, Issue:9
Synthesis and biological evaluation of
AID587111Inhibition of human recombinant 11beta-HSD1 expressed in HEK293 cells assessed as residual conversion of [1,2-[3H]cortisone to cortisol at 1000 nM after 10 mins by scintillation counting2011Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
Synthesis of new glycyrrhetinic acid derived ring A azepanone, 29-urea and 29-hydroxamic acid derivatives as selective 11β-hydroxysteroid dehydrogenase 2 inhibitors.
AID1599286Cytotoxicity against human A549 cells assessed as cell survival at 200 uM after 24 hrs by MTT assay relative to control2019European journal of medicinal chemistry, Aug-15, Volume: 176Recent update on anti-dengue drug discovery.
AID1233392Gastroprotective activity in Swiss albino mouse model of HCl/EtOH-induced lesion assessed as gastric lesion index at 100 mg/kg, po dosed 50 mins before HCl/EtOH challenge and measured 1 hr post HCl/EtOH challenge (Rvb = 42 +/- 1.9 mm)2015Bioorganic & medicinal chemistry letters, Jul-15, Volume: 25, Issue:14
Gastroprotective activity of ent-beyerene derivatives in mice: Effects on gastric secretion, endogenous prostaglandins and non-protein sulfhydryls.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (27)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901 (3.70)18.7374
1990's0 (0.00)18.2507
2000's4 (14.81)29.6817
2010's16 (59.26)24.3611
2020's6 (22.22)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 52.99

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 very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index52.99 (24.57)
Research Supply Index3.37 (2.92)
Research Growth Index4.55 (4.65)
Search Engine Demand Index87.40 (26.88)
Search Engine Supply Index2.15 (0.95)

This Compound (52.99)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (3.57%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other27 (96.43%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]