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4025-64-3

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4025-64-3 Usage

Chemical Properties

white to light beige crystalline powder

General Description

3-(Chlorosulfonyl)benzoic acid is a sulfonyl halide. It participates in the synthesis of novel anthranilic acid class of PPARδ (Peroxisome proliferator-activated receptor δ) partial agonists.

Check Digit Verification of cas no

The CAS Registry Mumber 4025-64-3 includes 7 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 4 digits, 4,0,2 and 5 respectively; the second part has 2 digits, 6 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 4025-64:
(6*4)+(5*0)+(4*2)+(3*5)+(2*6)+(1*4)=63
63 % 10 = 3
So 4025-64-3 is a valid CAS Registry Number.
InChI:InChI=1/C7H5ClO4S/c8-13(11,12)6-3-1-2-5(4-6)7(9)10/h1-4H,(H,9,10)

4025-64-3 Well-known Company Product Price

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  • (Code)Product description
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  • Detail
  • Alfa Aesar

  • (B22987)  3-(Chlorosulfonyl)benzoic acid, 97%   

  • 4025-64-3

  • 5g

  • 293.0CNY

  • Detail
  • Alfa Aesar

  • (B22987)  3-(Chlorosulfonyl)benzoic acid, 97%   

  • 4025-64-3

  • 25g

  • 979.0CNY

  • Detail
  • Alfa Aesar

  • (B22987)  3-(Chlorosulfonyl)benzoic acid, 97%   

  • 4025-64-3

  • 100g

  • 3326.0CNY

  • Detail
  • Aldrich

  • (441759)  3-(Chlorosulfonyl)benzoicacid  95%

  • 4025-64-3

  • 441759-5G

  • 402.48CNY

  • Detail
  • Aldrich

  • (441759)  3-(Chlorosulfonyl)benzoicacid  95%

  • 4025-64-3

  • 441759-25G

  • 1,241.37CNY

  • Detail

4025-64-3SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 13, 2017

Revision Date: Aug 13, 2017

1.Identification

1.1 GHS Product identifier

Product name 3-(Chlorosulfonyl)benzoic acid

1.2 Other means of identification

Product number -
Other names Benzoic acid, 3-(chlorosulfonyl)-

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:4025-64-3 SDS

4025-64-3Synthetic route

benzoic acid
65-85-0

benzoic acid

3-Carboxybenzenesulfonyl chloride
4025-64-3

3-Carboxybenzenesulfonyl chloride

Conditions
ConditionsYield
With chlorosulfonic acid Reflux;97%
With chlorosulfonic acid at 100℃; for 0.75h; Temperature; Concentration;88.7%
With chlorosulfonic acid at 140℃; for 6h;88%
chlorosulfonic acid
7790-94-5

chlorosulfonic acid

benzoic acid
65-85-0

benzoic acid

3-Carboxybenzenesulfonyl chloride
4025-64-3

3-Carboxybenzenesulfonyl chloride

Conditions
ConditionsYield
at 65℃; for 4h;87%
at 150℃; for 2h; Inert atmosphere;83%
3-sulfosalicylic acid
121-53-9

3-sulfosalicylic acid

3-Carboxybenzenesulfonyl chloride
4025-64-3

3-Carboxybenzenesulfonyl chloride

Conditions
ConditionsYield
With phosphorus pentachloride
3-carboxybenzenediazonium chloride
25116-40-9

3-carboxybenzenediazonium chloride

3-Carboxybenzenesulfonyl chloride
4025-64-3

3-Carboxybenzenesulfonyl chloride

Conditions
ConditionsYield
With sulfur dioxide; copper(l) chloride; magnesium chloride
benzoyl chloride
98-88-4

benzoyl chloride

3-Carboxybenzenesulfonyl chloride
4025-64-3

3-Carboxybenzenesulfonyl chloride

Conditions
ConditionsYield
With sulfur trioxide at 130℃;
chlorosulfonic acid
7790-94-5

chlorosulfonic acid

benzoyl chloride
98-88-4

benzoyl chloride

3-Carboxybenzenesulfonyl chloride
4025-64-3

3-Carboxybenzenesulfonyl chloride

Conditions
ConditionsYield
at 130 - 140℃;
at 130 - 140℃;
sulfur trioxide
7446-11-9

sulfur trioxide

benzoyl chloride
98-88-4

benzoyl chloride

3-Carboxybenzenesulfonyl chloride
4025-64-3

3-Carboxybenzenesulfonyl chloride

Conditions
ConditionsYield
at 110 - 130℃;
at 110 - 130℃;
benzoyl chloride
98-88-4

benzoyl chloride

chloro watersulfuric acid

chloro watersulfuric acid

3-Carboxybenzenesulfonyl chloride
4025-64-3

3-Carboxybenzenesulfonyl chloride

Conditions
ConditionsYield
at 130℃;
m-sulfo-benzoic acid-dichloride

m-sulfo-benzoic acid-dichloride

3-Carboxybenzenesulfonyl chloride
4025-64-3

3-Carboxybenzenesulfonyl chloride

Conditions
ConditionsYield
With water
sodium-salt of/the/ 3-sulfo-benzoic acid

sodium-salt of/the/ 3-sulfo-benzoic acid

3-Carboxybenzenesulfonyl chloride
4025-64-3

3-Carboxybenzenesulfonyl chloride

Conditions
ConditionsYield
With phosphorus pentachloride; trichlorophosphate Behandeln mit Wasser;
3-Carboxybenzenesulfonyl chloride
4025-64-3

3-Carboxybenzenesulfonyl chloride

3-carboxybenzenesulfonyl fluoride
454-95-5

3-carboxybenzenesulfonyl fluoride

Conditions
ConditionsYield
With potassium hydrogen bifluoride In 1,4-dioxane; water at 20℃; for 0.5h; Inert atmosphere;100%
With potassium hydrogen difluoride In water; acetonitrile at 20℃;97%
With potassium hydrogenfluoride In 1,4-dioxane at 20℃; for 1h; Inert atmosphere;90%
With water; sodium fluoride
3-Carboxybenzenesulfonyl chloride
4025-64-3

3-Carboxybenzenesulfonyl chloride

benzylamine
100-46-9

benzylamine

3-[(4-phenylmethyl)aminosulfonyl]benzoic acid
7326-77-4

3-[(4-phenylmethyl)aminosulfonyl]benzoic acid

Conditions
ConditionsYield
In dichloromethane100%
In dichloromethane at 0℃; for 0.5h;95%
In acetone Reflux;
In acetone Reflux;
methanol
67-56-1

methanol

3-Carboxybenzenesulfonyl chloride
4025-64-3

3-Carboxybenzenesulfonyl chloride

methyl 3-chlorosulfonylbenzoate
63555-50-0

methyl 3-chlorosulfonylbenzoate

Conditions
ConditionsYield
Stage #1: 3-Carboxybenzenesulfonyl chloride With thionyl chloride at 20℃; for 16h; Inert atmosphere;
Stage #2: methanol at 20℃; for 2h; Inert atmosphere;
100%
Stage #1: 3-Carboxybenzenesulfonyl chloride With oxalyl dichloride In dichloromethane; N,N-dimethyl-formamide at 20℃; for 1.5h; Inert atmosphere;
Stage #2: methanol In dichloromethane; N,N-dimethyl-formamide for 0.25h; Inert atmosphere;
58%
Stage #1: 3-Carboxybenzenesulfonyl chloride With thionyl chloride for 2h; Heating;
Stage #2: methanol for 0.25h;
3-Carboxybenzenesulfonyl chloride
4025-64-3

3-Carboxybenzenesulfonyl chloride

3-[(phenylamino)sulfonyl]benzenecarboxylic acid
1576-45-0

3-[(phenylamino)sulfonyl]benzenecarboxylic acid

Conditions
ConditionsYield
With aniline In dichloromethane100%
C15H14FNO4
1075749-58-4

C15H14FNO4

3-Carboxybenzenesulfonyl chloride
4025-64-3

3-Carboxybenzenesulfonyl chloride

C22H18FNO8S
1075749-63-1

C22H18FNO8S

Conditions
ConditionsYield
With pyridine100%
4-bromo-N-methylaniline
6911-87-1

4-bromo-N-methylaniline

3-Carboxybenzenesulfonyl chloride
4025-64-3

3-Carboxybenzenesulfonyl chloride

3-(N-(4-bromophenyl)-N-methylsulfamoyl)benzoic acid
1373116-31-4

3-(N-(4-bromophenyl)-N-methylsulfamoyl)benzoic acid

Conditions
ConditionsYield
With pyridine In ethyl acetate at 0 - 20℃;97%
In dichloromethane at 0 - 20℃; for 12h;
3-Carboxybenzenesulfonyl chloride
4025-64-3

3-Carboxybenzenesulfonyl chloride

di-n-propylamine
142-84-7

di-n-propylamine

3-(N,N-di-n-propylsulfamoyl)benzoic acid
53212-78-5

3-(N,N-di-n-propylsulfamoyl)benzoic acid

Conditions
ConditionsYield
In dichloromethane at 0 - 20℃;97%
3-Carboxybenzenesulfonyl chloride
4025-64-3

3-Carboxybenzenesulfonyl chloride

3-sulfamoylbenzoic acid
636-76-0

3-sulfamoylbenzoic acid

Conditions
ConditionsYield
Stage #1: 3-Carboxybenzenesulfonyl chloride With ammonia In water at 0 - 20℃; for 15h;
Stage #2: With hydrogenchloride In water
96%
With ammonium hydroxide at 0 - 20℃; for 2h;95%
With ammonium hydroxide In water at 0 - 20℃;95%
3-Carboxybenzenesulfonyl chloride
4025-64-3

3-Carboxybenzenesulfonyl chloride

3-carbonxybenzenesulfonyl azide
15980-11-7

3-carbonxybenzenesulfonyl azide

Conditions
ConditionsYield
With sodium azide In water; acetonitrile at 20℃; for 2h;96%
With sodium azide In water; acetone for 2h;80%
With sodium azide In water; acetone for 2h; Inert atmosphere;80%
With sodium azide In water; acetonitrile for 0.416667h;76%
3-Carboxybenzenesulfonyl chloride
4025-64-3

3-Carboxybenzenesulfonyl chloride

4-bromo-aniline
106-40-1

4-bromo-aniline

3-(N-(4-bromophenyl)sulfamoyl)benzoic acid
300667-30-5

3-(N-(4-bromophenyl)sulfamoyl)benzoic acid

Conditions
ConditionsYield
With pyridine In ethyl acetate at 0 - 20℃;96%
With triethylamine In dichloromethane for 120h;
In acetone Reflux;
3-Carboxybenzenesulfonyl chloride
4025-64-3

3-Carboxybenzenesulfonyl chloride

chlorosulphonyl-benzoic acid
63914-81-8

chlorosulphonyl-benzoic acid

3-sulfosalicylic acid
121-53-9

3-sulfosalicylic acid

Conditions
ConditionsYield
In 5,5-dimethyl-1,3-cyclohexadiene; water95.6%
In water; toluene95.4%
In 5,5-dimethyl-1,3-cyclohexadiene; water95.6%
3-Carboxybenzenesulfonyl chloride
4025-64-3

3-Carboxybenzenesulfonyl chloride

methylamine
74-89-5

methylamine

3-(N-methylsulfamoyl)benzoic acid
35623-11-1

3-(N-methylsulfamoyl)benzoic acid

Conditions
ConditionsYield
With triethylamine In tetrahydrofuran; dichloromethane at 0℃; for 0.5h;95%
In tetrahydrofuran at 0 - 20℃; for 1.25 - 1.33333h;86%
In water; ethyl acetate at 0℃; for 0.5h;54%
2-(p-tolylsulfonyl)ethanol
22381-54-0

2-(p-tolylsulfonyl)ethanol

3-Carboxybenzenesulfonyl chloride
4025-64-3

3-Carboxybenzenesulfonyl chloride

3-chlorosulfonylbenzoic acid 2-(toluene-4-sulfonyl)ethyl ester
651728-72-2

3-chlorosulfonylbenzoic acid 2-(toluene-4-sulfonyl)ethyl ester

Conditions
ConditionsYield
Stage #1: 3-Carboxybenzenesulfonyl chloride With thionyl chloride for 3h; Heating / reflux;
Stage #2: 2-(p-tolylsulfonyl)ethanol In acetonitrile for 20h; Heating / reflux;
95%
Stage #1: 3-Carboxybenzenesulfonyl chloride With thionyl chloride for 1h; Heating / reflux;
Stage #2: 2-(p-tolylsulfonyl)ethanol With triethylamine In dichloromethane at 20℃; for 1h;
63%
3-Carboxybenzenesulfonyl chloride
4025-64-3

3-Carboxybenzenesulfonyl chloride

1-amino-2-propene
107-11-9

1-amino-2-propene

3-(N-allylsulfamoyl)benzoic acid
500292-31-9

3-(N-allylsulfamoyl)benzoic acid

Conditions
ConditionsYield
With sodium hydroxide In tetrahydrofuran; water at 20℃; for 17h;95%
3-Carboxybenzenesulfonyl chloride
4025-64-3

3-Carboxybenzenesulfonyl chloride

2-(1-piperazinyl)-1,3-benzoxazole
111628-39-8

2-(1-piperazinyl)-1,3-benzoxazole

3-(4-benzoxazol-2-yl-piperazin-1-sulfonyl)benzoic acid

3-(4-benzoxazol-2-yl-piperazin-1-sulfonyl)benzoic acid

Conditions
ConditionsYield
With triethylamine In tetrahydrofuran; dichloromethane at 0 - 20℃;95%
3-Carboxybenzenesulfonyl chloride
4025-64-3

3-Carboxybenzenesulfonyl chloride

chlorosulphonyl-benzoic acid
63914-81-8

chlorosulphonyl-benzoic acid

3-sulfobenzoic acid sodium salt

3-sulfobenzoic acid sodium salt

Conditions
ConditionsYield
With sodium hydroxide In 5,5-dimethyl-1,3-cyclohexadiene; water94.3%
With sodium hydroxide In water; chlorobenzene93.3%
3-Carboxybenzenesulfonyl chloride
4025-64-3

3-Carboxybenzenesulfonyl chloride

diethylamine
109-89-7

diethylamine

<(Diethylamino)sulfonyl>benzoic Acid
1576-46-1

<(Diethylamino)sulfonyl>benzoic Acid

Conditions
ConditionsYield
In dichloromethane at 0 - 20℃;94%
In water
With hydrogenchloride In dichloromethane
N-methyl(p-chloroaniline)
932-96-7

N-methyl(p-chloroaniline)

3-Carboxybenzenesulfonyl chloride
4025-64-3

3-Carboxybenzenesulfonyl chloride

3-(N-(4-chlorophenyl)-N-methylsulfamoyl)benzoic acid
361473-14-5

3-(N-(4-chlorophenyl)-N-methylsulfamoyl)benzoic acid

Conditions
ConditionsYield
With pyridine In ethyl acetate at 0 - 20℃;94%
With triethylamine In methanol at 0 - 20℃; for 5.5h;
In dichloromethane at 0 - 20℃; for 12h;
3-Carboxybenzenesulfonyl chloride
4025-64-3

3-Carboxybenzenesulfonyl chloride

4-chloro-aniline
106-47-8

4-chloro-aniline

3-(N-(4-chlorophenyl)sulfamoyl)benzoic acid
147410-78-4

3-(N-(4-chlorophenyl)sulfamoyl)benzoic acid

Conditions
ConditionsYield
With pyridine In ethyl acetate at 0 - 20℃;94%
With pyridine at 0 - 20℃;94%
In acetone for 8h; Reflux;
In acetone Reflux;
3-Carboxybenzenesulfonyl chloride
4025-64-3

3-Carboxybenzenesulfonyl chloride

3-chlorosulfonylbenzoyl dichloride
4052-92-0

3-chlorosulfonylbenzoyl dichloride

Conditions
ConditionsYield
With oxalyl dichloride; diethyl ether In N,N-dimethyl-formamide at 40℃; for 7h; Temperature;93.8%
With thionyl chloride In dichloromethane at 0 - 20℃;
With thionyl chloride In 1,2-dichloro-ethane for 1h; Reflux;
3-Carboxybenzenesulfonyl chloride
4025-64-3

3-Carboxybenzenesulfonyl chloride

cyclohexylamine
108-91-8

cyclohexylamine

3-(N-cyclohexylsulfamoyl)benzoic acid
313346-39-3

3-(N-cyclohexylsulfamoyl)benzoic acid

Conditions
ConditionsYield
With triethylamine In dichloromethane at 5 - 20℃;93%
In 4-(dicyanomethylene)-2-methyl-6-(p-dimethylaminostyryl)-4H-pyran at 0℃; for 0.5h;
With triethylamine In dichloromethane at 5 - 20℃;
With triethylamine In dichloromethane at 5 - 20℃;1.2 g
In tetrahydrofuran at 20℃;
3-Carboxybenzenesulfonyl chloride
4025-64-3

3-Carboxybenzenesulfonyl chloride

1-methyl-2-(1-piperazinyl)-1H-benzimidazole
137898-68-1

1-methyl-2-(1-piperazinyl)-1H-benzimidazole

3-[4-(1-methylbenzimidazol-2-yl)piperazin-1-yl]sulfonylbenzoic acid
1454676-40-4

3-[4-(1-methylbenzimidazol-2-yl)piperazin-1-yl]sulfonylbenzoic acid

Conditions
ConditionsYield
With triethylamine In dichloromethane at 0 - 20℃; for 23h;93%
With triethylamine In tetrahydrofuran; dichloromethane at 0 - 20℃;93%
3-Carboxybenzenesulfonyl chloride
4025-64-3

3-Carboxybenzenesulfonyl chloride

2-piperazinobenzothiazole
55745-83-0

2-piperazinobenzothiazole

3-(4-benzothiazol-2-yl-piperazin-1-sulfonyl)benzoic acid

3-(4-benzothiazol-2-yl-piperazin-1-sulfonyl)benzoic acid

Conditions
ConditionsYield
With triethylamine In tetrahydrofuran; dichloromethane at 0 - 20℃;93%
3-Carboxybenzenesulfonyl chloride
4025-64-3

3-Carboxybenzenesulfonyl chloride

3-mercapto benzoic acid
4869-59-4

3-mercapto benzoic acid

Conditions
ConditionsYield
Stage #1: 3-Carboxybenzenesulfonyl chloride With phosphorus; iodine In acetic acid at 100 - 110℃; for 0.5h;
Stage #2: With water for 1.66667h; Heating / reflux;
92%
With phosphorus; water; iodine In acetic acid91.7%
With triphenylphosphine In toluene for 0.166667h; Inert atmosphere; chemoselective reaction;73%
3-Carboxybenzenesulfonyl chloride
4025-64-3

3-Carboxybenzenesulfonyl chloride

dimethyl amine
124-40-3

dimethyl amine

3-<(Dimethylamino)sulfonyl>benzoic Acid
7326-73-0

3-<(Dimethylamino)sulfonyl>benzoic Acid

Conditions
ConditionsYield
With ammonia In water; ethyl acetate at 0℃; for 0.5h;91%
Stage #1: 3-Carboxybenzenesulfonyl chloride; dimethyl amine In tetrahydrofuran; dichloromethane for 0.5h;
Stage #2: With hydrogenchloride In tetrahydrofuran; dichloromethane; water
65%
Stage #1: 3-Carboxybenzenesulfonyl chloride; dimethyl amine In tetrahydrofuran; dichloromethane for 0.5h;
Stage #2: With hydrogenchloride In tetrahydrofuran; dichloromethane; water
65%
3-Carboxybenzenesulfonyl chloride
4025-64-3

3-Carboxybenzenesulfonyl chloride

5-chloro-4-methyl-2-nitroaniline
7149-80-6

5-chloro-4-methyl-2-nitroaniline

sodium 3-(N-(5-chloro-4-methyl-2-nitrophenyl)sulfamoyl)benzoate

sodium 3-(N-(5-chloro-4-methyl-2-nitrophenyl)sulfamoyl)benzoate

Conditions
ConditionsYield
With pyridine at 20℃; for 19h; Inert atmosphere;91%
3-Carboxybenzenesulfonyl chloride
4025-64-3

3-Carboxybenzenesulfonyl chloride

5-bromo-4-methyl-2-nitroaniline
40371-63-9

5-bromo-4-methyl-2-nitroaniline

C14H11BrN2O6S

C14H11BrN2O6S

Conditions
ConditionsYield
With pyridine for 19h; Inert atmosphere; Cooling with ice;91%
piperidine
110-89-4

piperidine

3-Carboxybenzenesulfonyl chloride
4025-64-3

3-Carboxybenzenesulfonyl chloride

3-(piperidin-1-ylsulfonyl)benzoic acid
7311-93-5

3-(piperidin-1-ylsulfonyl)benzoic acid

Conditions
ConditionsYield
In dichloromethane at 0℃; for 0.5h;90%
In dichloromethane at 0℃; for 2h;90%
In dichloromethane at 0℃; for 0.5h;90%
In dichloromethane at 0 - 20℃;85%
In dichloromethane at 20℃;
hexamethylene imine
111-49-9

hexamethylene imine

3-Carboxybenzenesulfonyl chloride
4025-64-3

3-Carboxybenzenesulfonyl chloride

3-(azepan-1-ylsulfonyl)benzoic acid
326182-57-4

3-(azepan-1-ylsulfonyl)benzoic acid

Conditions
ConditionsYield
In dichloromethane at 0 - 20℃;90%
With pyridine In ethyl acetate at 0 - 20℃;55%
With pyridine In dichloromethane at 0 - 20℃; for 5h;

4025-64-3Relevant articles and documents

-

Limpricht,v.Uslar

, p. 30 (1858)

-

Molecular hybrid design, synthesis and biological evaluation of N-phenyl sulfonamide linked N-acyl hydrazone derivatives functioning as COX-2 inhibitors: New anti-inflammatory, anti-oxidant and anti-bacterial agents

Gorantla, Vasubabu,Gundla, Rambabu,Jadav, Surender Singh,Anugu, Sreenivasa Reddy,Chimakurthy, Jithendra,Nidasanametla, Satya Kameswararao,Korupolu, Raghubabu

, p. 13516 - 13532 (2017)

Herein, we report the design, synthesis and biological evaluation of the anti-inflammatory activities of N-phenyl sulfonamide linked N-acylhydrazones (NPS-NAH), using the molecular hybridization approach. Hybrid compounds were further validated by theoretical studies. Compound 1f from series-1 and compound 2a from series-2 exhibited strong selective COX-2 enzyme inhibition at IC50 = 8.9 μM and 8.4 μM respectively. Effective in vivo anti-inflammatory profiling of potent and selective COX-2 inhibitors, including compound 1f and 2a was carried out and compared with known COX-2 inhibitors. Subsequently, these compounds were tested for antioxidant activity, and 1h (IC50 = 28.62 μM) from series-1 and compound 2d (IC50 = 25.34 μM) from series-2 were found to be potent anti-oxidants. Additionally, these compounds were screened for antibacterial activity, and compound 1l and 2b exhibited better Gram +ve and -ve anti-bacterial activity than the reference standards, Ciprofloxacin and Norfloxacin. These results validated the idea of exploiting the hybridization strategy for the identification of new N-phenyl sulfonamide-NAH derivatives for optimizing anti-inflammatory, antioxidant and anti-bacterial activities.

Catalyst-controlled site-selective N-H and C3-arylation of carbazoleviacarbene transfer reactions

Bahukhandi, Srishti Ballabh,Bera, Sourav Sekhar,Empel, Claire,Koenigs, Rene M.

supporting information, p. 6193 - 6196 (2021/06/30)

A site-selective direct arylation reaction of carbazole and other N-heterocycles with diazo-naphthalen-2(1H)-ones has been developed. While Au(i)-NHC catalysts lead to selective C3-arylation, palladium acetate allows for selective N-H arylation, displaying complete site-selectivity each. To show the applicability of these arylation reactions, one-pot, two-fold diarylation reactions of carbazole were demonstrated.

3-Functionalised benzenesulphonamide based 1,3,4-oxadiazoles as selective carbonic anhydrase XIII inhibitors: Design, synthesis and biological evaluation

Swain, Baijayantimala,Abhay,Singh, Priti,Angeli, Andrea,Aashritha, Kamtam,Nagesh, Narayana,Supuran, Claudiu T.,Arifuddin, Mohammed

, (2021/02/27)

A new series of benzenesulphonamide linked-1,3,4-oxadiazole hybrids (6a–s) has been synthesized and tested for their carbonic anhydrase inhibition against human (h) carbonic anhydrase (CA) isoforms hCA I, II, IX, and XIII. Fluorescence properties of some of the synthesized molecules were studied. Most of the molecules exhibited significant inhibitory power, comparable or better than the standard drug acetazolamide (AAZ) on hCA XIII. Out of 19 tested molecules, compound 6e (75.8 nM) was 3 times more potent than AAZ (250.0 nM) against hCA I, whereas compound 6e (15.4 nM), 6g (16.2 nM), 6h (16.4 nM) and 6i (17.0 nM) were found to be more potent than AAZ (17.0 nM) against isoform hCA XIII. It is anticipated that these compounds could be taken as the potential leads for the development of selective hCA XIII isoform inhibitors with improved potency.

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