60000-87-5

Usage

Uses

Used in Pharmaceutical Industry:
4-ACETYL-N,N-DIMETHYL-BENZENESULFONAMIDE is used as a diuretic for its ability to increase the rate of urine production and reduce the amount of sodium and water reabsorption in the kidneys, which is beneficial in treating edema and certain types of glaucoma.
4-ACETYL-N,N-DIMETHYL-BENZENESULFONAMIDE is used as a treatment for glaucoma because it helps to reduce the production of aqueous humor, thereby decreasing intraocular pressure and alleviating the symptoms associated with this eye condition.
In the Neurological Treatment Industry:
4-ACETYL-N,N-DIMETHYL-BENZENESULFONAMIDE is used as an anticonvulsant in the treatment of epilepsy, particularly for certain types of seizures, due to its ability to alter the pH of cerebrospinal fluid and affect the excitability of neurons.
For Altitude Sickness Treatment:
4-ACETYL-N,N-DIMETHYL-BENZENESULFONAMIDE is used as a prophylactic medication to prevent and treat altitude sickness, as it helps to counteract the effects of high altitude on the body by promoting acclimatization and reducing the symptoms of acute mountain sickness.
Overall, 4-ACETYL-N,N-DIMETHYL-BENZENESULFONAMIDE, or acetazolamide, is an essential medication in the medical field due to its versatile applications in treating a range of conditions, from glaucoma to epilepsy and altitude sickness, leveraging its unique ability to inhibit carbonic anhydrase.

InChI:InChI=1/C10H13NO3S/c1-8(12)9-4-6-10(7-5-9)15(13,14)11(2)3/h4-7H,1-3H3

Upstream product

• 25837-65-4 4-ethyl-N,N-dimethylbenzenesulfonamide 
• 1788-10-9 4-Acetylbenzenesulfonyl chloride 
• 124-40-3 dimethyl amine 
• 16712-69-9 p-ethylbenzenesulfonyl chloride 

Downstream Products

• 161804-80-4 N'-[1-(4-Dimethylsulfamoyl-phenyl)-eth-(Z)-ylidene]-hydrazinecarbodithioic acid methyl ester 
• 1042947-74-9 C₁₃H₁₈N₂O₃S 
• 104622-34-6 4-(N-dichloroacetyl-glycyl)-benzenesulfonic acid dimethylamide 
• 89102-54-5 4-(2-bromoacetyl)-N,N-dimethylbenzenesulfonamide 

Relevant academic research and scientific papers

Optimization of Hydantoins as Potent Antimycobacterial Decaprenylphosphoryl-β-d-Ribose Oxidase (DprE1) Inhibitors

In search of novel drugs against tuberculosis, we previously discovered and profiled a novel hydantoin-based family that demonstrated highly promising in vitro potency against Mycobacterium. tuberculosis. The compounds were found to be noncovalent inhibitors of DprE1, a subunit of decaprenylphosphoryl-β-d-ribose-2′-epimerase. This protein, localized in the periplasmic space of the mycobacterial cell wall, was shown to be an essential and vulnerable antimycobacterial drug target. Here, we report the further SAR exploration of this chemical family through more than 80 new analogues. Among these, the most active representatives combined submicromolar cellular potency and nanomolar target affinity with balanced physicochemical properties and low human cytotoxicity. Moreover, we demonstrate in vivo activity in an acute Mtb infection model and provide further proof of DprE1 being the target of the hydantoins. Overall, the hydantoin family of DprE1 inhibitors represents a promising noncovalent lead series for the discovery of novel antituberculosis agents.

Design, Synthesis, and Biological Evaluation of Novel Allosteric Protein Disulfide Isomerase Inhibitors

Protein disulfide isomerase (PDI) is responsible for nascent protein folding in the endoplasmic reticulum (ER) and is critical for glioblastoma survival. To improve the potency of lead PDI inhibitor BAP2 ((E)-3-(3-(4-hydroxyphenyl)-3-oxoprop-1-en-1-yl)benzonitrile), we designed and synthesized 67 analogues. We determined that PDI inhibition relied on the A ring hydroxyl group of the chalcone scaffold and cLogP increase in the sulfonamide chain improved potency. Docking studies revealed that BAP2 and analogues bind to His256 in the b′ domain of PDI, and mutation of His256 to Ala abolishes BAP2 analogue activity. BAP2 and optimized analogue 59 have modest thiol reactivity; however, we propose that PDI inhibition by BAP2 analogues depends on the b′ domain. Importantly, analogues inhibit glioblastoma cell growth, induce ER stress, increase expression of G2M checkpoint proteins, and reduce expression of DNA repair proteins. Cumulatively, our results support inhibition of PDI as a novel strategy to treat glioblastoma.

PYRAZOLONE DERIVATIVES AS NITROXYL DONORS

The disclosed subject matter provides pyrazolone derivative compounds, pharmaceutical compositions comprising such compounds, kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the disclosed subject matter provides methods of using such compounds or pharmaceutical compositions for treating heart failure.

Synthesis and structure-activity relationship of aminopyrimidine IKK2 inhibitors

The synthesis and structure-activity relationship of a novel series of aminopyrimidines are exemplified. Results of key compounds from within this series in the E-selectin reporter cell assay are also reported.

Remarkably Mild and Simple Preparations of Sulfinates, Sulfonyl Chlorides and Sulfonamides from Thioanisoles

New and high yielding procedures to convert thioanisoles into versatile sulfonyl chloride derivatives were developed by strategically taking advantage of the Pummerer reaction.

Antibacterial monic acid derivatives

A compound of the formula (I) STR1 wherein R is a group STR2 R1 is hydrogen, phenyl, C1-20 alkyl, C2-8 alkenyl or C2-8 alkynyl each of which may optionally be substituted; or C3-7 cycloalkyl, X is a divalent group --Y--C=C--, and Y is oxygen or sulphur, have antibacterial and/or antimycoplasmal activity.

Novel antibacterial amide compounds and process means for producing the same

Novel organic amide compounds which are N-[6-[(aminosulfonyl)phenyl]-1,2-dihydro-2-oxonicotinyl]penicillin and cephalosporin type compounds having broad spectrum antibacterial utility are provided by (a) reacting the free amino acid of the appropriate penicillin or cephalosporin or the acid salt or silylated derivative or complex thereof with a reactive derivative of the corresponing N-6-[(aminosulfonyl)phenyl]-1,2-dihydro-2-oxonicotinic acid or (b) reacting the free amino acid 6-aminopenicillanic acid, 7-aminocephalosporanic acid, 7-amino-3-methylceph-3-em-4-carboxylic acid or a related compound or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding D-N-[6-[(aminosulfonyl)phenyl]-1,2-dihydro-2-oxonicotinyl]-2-substituted glycine. Pharmaceutical compositions containing said compounds and methods for treating infections using said compositions are also disclosed.