Compounds > l 645151
Page last updated: 2024-11-07

l 645151

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

Description

L 645151: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID135214
CHEMBL ID312593
SCHEMBL ID2522313
MeSH IDM0129847

Synonyms (13)

Synonym
CHEMBL312593 ,
propanoic acid, 2,2-dimethyl-, 2-(aminosulfonyl)-6-benzothiazolyl ester
86394-94-7
(2-sulfamoyl-6-benzothiazolyl)-2,2-dimethylpropionate
l-645151
l 645151
(2-sulfamoyl-1,3-benzothiazol-6-yl) 2,2-dimethylpropanoate
bdbm50405865
DTXSID30235520
2-sulfamoyl-6-benzothiazolyl-2,2-dimethylpropionate
SCHEMBL2522313
2-sulfamoylbenzo[d]thiazol-6-yl pivalate
AKOS040745981
[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)
Carbonic anhydrase 2Homo sapiens (human)IC50 (µMol)0.02200.00021.10608.3000AID47735; AID47736
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (12)

Processvia Protein(s)Taxonomy
morphogenesis of an epitheliumCarbonic anhydrase 2Homo sapiens (human)
positive regulation of synaptic transmission, GABAergicCarbonic anhydrase 2Homo sapiens (human)
positive regulation of cellular pH reductionCarbonic anhydrase 2Homo sapiens (human)
angiotensin-activated signaling pathwayCarbonic anhydrase 2Homo sapiens (human)
regulation of monoatomic anion transportCarbonic anhydrase 2Homo sapiens (human)
secretionCarbonic anhydrase 2Homo sapiens (human)
regulation of intracellular pHCarbonic anhydrase 2Homo sapiens (human)
neuron cellular homeostasisCarbonic anhydrase 2Homo sapiens (human)
positive regulation of dipeptide transmembrane transportCarbonic anhydrase 2Homo sapiens (human)
regulation of chloride transportCarbonic anhydrase 2Homo sapiens (human)
carbon dioxide transportCarbonic anhydrase 2Homo sapiens (human)
one-carbon metabolic processCarbonic anhydrase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (5)

Processvia Protein(s)Taxonomy
arylesterase activityCarbonic anhydrase 2Homo sapiens (human)
carbonate dehydratase activityCarbonic anhydrase 2Homo sapiens (human)
protein bindingCarbonic anhydrase 2Homo sapiens (human)
zinc ion bindingCarbonic anhydrase 2Homo sapiens (human)
cyanamide hydratase activityCarbonic anhydrase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (6)

Processvia Protein(s)Taxonomy
cytoplasmCarbonic anhydrase 2Homo sapiens (human)
cytosolCarbonic anhydrase 2Homo sapiens (human)
plasma membraneCarbonic anhydrase 2Homo sapiens (human)
myelin sheathCarbonic anhydrase 2Homo sapiens (human)
apical part of cellCarbonic anhydrase 2Homo sapiens (human)
extracellular exosomeCarbonic anhydrase 2Homo sapiens (human)
cytoplasmCarbonic anhydrase 2Homo sapiens (human)
plasma membraneCarbonic anhydrase 2Homo sapiens (human)
apical part of cellCarbonic anhydrase 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (15)

Assay IDTitleYearJournalArticle
AID167689Maximum decrease in intraocular pressure in Albino rabbit during 5 hours observation period after topical instillation of 5% suspension in alpha-Chymotrypsin assay1989Journal of medicinal chemistry, Nov, Volume: 32, Issue:11
Topically active carbonic anhydrase inhibitors. 1. O-acyl derivatives of 6-hydroxybenzothiazole-2-sulfonamide.
AID167685Maximum decrease in intraocular pressure in Albino rabbit during 5 hours observation period after topical instillation of 0.5% suspension in alpha-Chymotrypsin assay1989Journal of medicinal chemistry, Nov, Volume: 32, Issue:11
Topically active carbonic anhydrase inhibitors. 1. O-acyl derivatives of 6-hydroxybenzothiazole-2-sulfonamide.
AID20165In vitro susceptibility to nucleophilic attack by reduced glutathione at 37 degree C and at pH 7.41989Journal of medicinal chemistry, Nov, Volume: 32, Issue:11
Topically active carbonic anhydrase inhibitors. 1. O-acyl derivatives of 6-hydroxybenzothiazole-2-sulfonamide.
AID165649Change in intraocular pressure in Albino rabbit when 2% suspension of compound bilaterally instilled in a single dose of 50 microL determined by recovery rate assay1989Journal of medicinal chemistry, Nov, Volume: 32, Issue:11
Topically active carbonic anhydrase inhibitors. 1. O-acyl derivatives of 6-hydroxybenzothiazole-2-sulfonamide.
AID165487Reduction in maximum Intra ocular pressure in the rabbit model of ocular hypertension, when treated with a minimum effective oral dose of 0.251989Journal of medicinal chemistry, Dec, Volume: 32, Issue:12
Topically active carbonic anhydrase inhibitors. 2. Benzo[b]thiophenesulfonamide derivatives with ocular hypotensive activity.
AID167687Maximum decrease in intraocular pressure in Albino rabbit during 5 hours observation period after topical instillation of 1% suspension in alpha-Chymotrypsin assay1989Journal of medicinal chemistry, Nov, Volume: 32, Issue:11
Topically active carbonic anhydrase inhibitors. 1. O-acyl derivatives of 6-hydroxybenzothiazole-2-sulfonamide.
AID24473Cleavage by corneal esterase at 37 degree C and at pH 7.41989Journal of medicinal chemistry, Nov, Volume: 32, Issue:11
Topically active carbonic anhydrase inhibitors. 1. O-acyl derivatives of 6-hydroxybenzothiazole-2-sulfonamide.
AID21987Solubility (pH 7.4 buffer ar 25 degree C)1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Thienothiopyran-2-sulfonamides: a novel class of water-soluble carbonic anhydrase inhibitors.
AID47736In vitro inhibition of human Carbonic Anhydrase II1989Journal of medicinal chemistry, Nov, Volume: 32, Issue:11
Topically active carbonic anhydrase inhibitors. 1. O-acyl derivatives of 6-hydroxybenzothiazole-2-sulfonamide.
AID166788Corneal penetration rate constant (k) for excised denuded cornea of albino rabbit1989Journal of medicinal chemistry, Nov, Volume: 32, Issue:11
Topically active carbonic anhydrase inhibitors. 1. O-acyl derivatives of 6-hydroxybenzothiazole-2-sulfonamide.
AID165647Change in intraocular pressure in Albino rabbit when 10% of compound suspension bilaterally instilled in 3 doses of 20, 15 and 15 microL at 5 minute intervals determined by recovery rate assay1989Journal of medicinal chemistry, Nov, Volume: 32, Issue:11
Topically active carbonic anhydrase inhibitors. 1. O-acyl derivatives of 6-hydroxybenzothiazole-2-sulfonamide.
AID165650Change in intraocular pressure in Albino rabbit when 5% of compound suspension bilaterally instilled in 3 doses of 20, 15 and 15 microL at 5 minute intervals determined by recovery rate assay1989Journal of medicinal chemistry, Nov, Volume: 32, Issue:11
Topically active carbonic anhydrase inhibitors. 1. O-acyl derivatives of 6-hydroxybenzothiazole-2-sulfonamide.
AID166790Corneal penetration rate constant (k) for excised intact cornea of albino rabbit1989Journal of medicinal chemistry, Nov, Volume: 32, Issue:11
Topically active carbonic anhydrase inhibitors. 1. O-acyl derivatives of 6-hydroxybenzothiazole-2-sulfonamide.
AID47735In vitro inhibition against purified human erythrocyte carbonic anhydrase II was determined (acetozolamide used as control.)1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Thienothiopyran-2-sulfonamides: a novel class of water-soluble carbonic anhydrase inhibitors.
AID165646Change in intraocular pressure in Albino rabbit when 1% suspension of compound bilaterally instilled in a single dose of 50 microL determined by recovery rate assay1989Journal of medicinal chemistry, Nov, Volume: 32, Issue:11
Topically active carbonic anhydrase inhibitors. 1. O-acyl derivatives of 6-hydroxybenzothiazole-2-sulfonamide.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (7)

TimeframeStudies, This Drug (%)All Drugs %
pre-19905 (71.43)18.7374
1990's0 (0.00)18.2507
2000's2 (28.57)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]

Market Indicators

Research Demand Index: 12.06

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 Index12.06 (24.57)
Research Supply Index2.08 (2.92)
Research Growth Index4.14 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.06)

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%
Other7 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
hydrogen carbonate
Bicarbonates: Inorganic salts that contain the -HCO3 radical. They are an important factor in determining the pH of the blood and the concentration of bicarbonate ions is regulated by the kidney. Levels in the blood are an index of the alkali reserve or buffering capacity.. hydrogencarbonate : The carbon oxoanion resulting from the removal of a proton from carbonic acid.		2.0110carbon oxoanioncofactor;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
acetazolamide
Acetazolamide: One of the CARBONIC ANHYDRASE INHIBITORS that is sometimes effective against absence seizures. It is sometimes useful also as an adjunct in the treatment of tonic-clonic, myoclonic, and atonic seizures, particularly in women whose seizures occur or are exacerbated at specific times in the menstrual cycle. However, its usefulness is transient often because of rapid development of tolerance. Its antiepileptic effect may be due to its inhibitory effect on brain carbonic anhydrase, which leads to an increased transneuronal chloride gradient, increased chloride current, and increased inhibition. (From Smith and Reynard, Textbook of Pharmacology, 1991, p337)		2.940monocarboxylic acid amide;
sulfonamide;
thiadiazoles		anticonvulsant;
diuretic;
EC 4.2.1.1 (carbonic anhydrase) inhibitor
dichlorphenamide
Dichlorphenamide: A carbonic anhydrase inhibitor that is used in the treatment of glaucoma.. diclofenamide : A sulfonamide that is benzene-1,3-disulfonamide in which the hydrogens at positions 4 and 5 are substituted by chlorine. An oral carbonic anhydrase inhibitor, it partially suppresses the secretion (inflow) of aqueous humor in the eye and so reduces intraocular pressure. It is used for the treatment of glaucoma.		2.3820dichlorobenzene;
sulfonamide		antiglaucoma drug;
EC 4.2.1.1 (carbonic anhydrase) inhibitor;
ophthalmology drug
ethoxzolamide
Ethoxzolamide: A carbonic anhydrase inhibitor used as diuretic and in glaucoma. It may cause hypokalemia.. ethoxzolamide : A sulfonamide that is 1,3-benzothiazole-2-sulfonamide which is substituted by an ethoxy group at position 6. A carbonic anhydrase inhibitor, it has been used in the treatment of glaucoma, and as a diuretic.		3.0850aromatic ether;
benzothiazoles;
sulfonamide		antiglaucoma drug;
diuretic;
EC 4.2.1.1 (carbonic anhydrase) inhibitor
methazolamide
Methazolamide: A carbonic anhydrase inhibitor that is used as a diuretic and in the treatment of glaucoma.		2.3820sulfonamide;
thiadiazoles
thiazoles
[no description available]		3.08501,3-thiazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
benzolamide
Benzolamide: Selective renal carbonic anhydrase inhibitor. It may also be of use in certain cases of respiratory failure.		2.0110
hepes
[no description available]		2.0110HEPES;
organosulfonic acid
fura-2
Fura-2: A fluorescent calcium chelating agent which is used to study intracellular calcium in tissues.		2.0110
l 650719
[no description available]		1.9710
chlorzolamide
chlorzolamide: structure		2.4120
alpha-chymotrypsin
Chymotrypsin: A serine endopeptidase secreted by the pancreas as its zymogen, CHYMOTRYPSINOGEN and carried in the pancreatic juice to the duodenum where it is activated by TRYPSIN. It selectively cleaves aromatic amino acids on the carboxyl side.		1.9610
6-hydroxybenzothiazide-2-sulfonamide
6-hydroxybenzothiazide-2-sulfonamide: structure given in first source		1.9710
ConditionIndicatedRelationship StrengthStudiesTrials
Glaucoma, Suspect
[description not available]		01.9710
Glaucoma
An ocular disease, occurring in many forms, having as its primary characteristics an unstable or a sustained increase in the intraocular pressure which the eye cannot withstand without damage to its structure or impairment of its function. The consequences of the increased pressure may be manifested in a variety of symptoms, depending upon type and severity, such as excavation of the optic disk, hardness of the eyeball, corneal anesthesia, reduced visual acuity, seeing of colored halos around lights, disturbed dark adaptation, visual field defects, and headaches. (Dictionary of Visual Science, 4th ed)		02.3720
Intraocular Pressure
The pressure of the fluids in the eye.		02.8840
Ocular Hypertension
A condition in which the intraocular pressure is elevated above normal and which may lead to glaucoma.		01.9710
Muscle Contraction
A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.		02.4120
Muscle Relaxation
That phase of a muscle twitch during which a muscle returns to a resting position.		02.0110