Category: 35203-88-4

Shingare, M. S. published the artcileSynthesis of sulfonamides derived from 2-acetamido-4-(3′-chlorosulfonyl-4′-aryl)thiazoles, Quality Control of 35203-88-4, the main research area is thiazole amino sulfamoylphenyl; chlorosulfonation arylthiazole; sulfonamide; phenylsulfonamide; aminothiazole.

Chlorosulfonation of 2-acetamido-4-arylthiazoles yielded 2-acetamido-4-(3-chlorosulfonyl-4-substituted aryl)thiazoles, which were converted into the corresponding sulfonamides I (R = Me, Cl, Br) and N-substituted phenyl-sulfonamides II (R1 = H, Me, Cl, OMe, OEt, Br). II were hydrolysed to the resp. 2-aminothiazoles. The position of sulfonamido group in I was confirmed by NMR spectra and chem. methods.

Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry published new progress about thiazole amino sulfamoylphenyl; chlorosulfonation arylthiazole; sulfonamide; phenylsulfonamide; aminothiazole. 35203-88-4 belongs to class amides-buliding-blocks, name is 3-Acetylbenzenesulfonamide, and the molecular formula is C8H9NO3S, Quality Control of 35203-88-4.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Altomare, Cosimo published the artcileDetermination of lipophilicity and hydrogen-bond donor acidity of bioactive sulfonyl-containing compounds by reversed-phase HPLC and centrifugal partition chromatography and their application to structure-activity relations, Safety of 3-Acetylbenzenesulfonamide, the main research area is lipophilicity hydrogen acidity benzenesulfonamide aminodiphenylsulfone QSAR; structure lipophilicity hydrogen acidity benzenesulfonamide aminodiphenylsulfone.

The lipophilic character of two large series of substituted benzenesulfonamides (BzSA)and 4-aminodiphenylsulfones (4-ADS) has been assessed by two chromatog. methods, i.e. reversed-phase HPLC using a relatively novel octadecylpolyvinyl packing and centrifugal counter-current chromatog. (CPC). The octadecylpolyvinyl stationary phase proved an interesting alternative to the more common octadecylsilane type stationary phase for obtaining retention parameters correlated to partition coefficients (i.e. log P). The CPC method, being far less time-consuming and markedly more precise than the classical shake-flask method, offers a promising alternative to measuring partition coefficients The parameter Δlog Poct-hep, i.e. log Poctanol minus log Pheptane, was also examined for both congeneric series and was indicative of a similar H-bonding capacity for the SO2NH2 and 4-NH2-C6H4-SO2 groups. QSAR analyses of carbonic anhydrase inhibition by BzSA and antimycobacterial activity of 4-ADS show the capacity of the new lipophilicity parameters to express the hydrophobic component of the drug-enzyme interactions and to reveal a possible role of H-bond donor capacity in governing the antimycobacterial activity of 4-ADS.

Journal of Pharmacy and Pharmacology published new progress about Acidity. 35203-88-4 belongs to class amides-buliding-blocks, name is 3-Acetylbenzenesulfonamide, and the molecular formula is C8H9NO3S, Safety of 3-Acetylbenzenesulfonamide.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Altomare, C. published the artcileLipophilicity measurements of benzenesulfonamide inhibitors of carbonic anhydrase by reversed-phase HPLC, Computed Properties of 35203-88-4, the main research area is lipophilicity benzenesulfonamide HPLC; carbonic anhydrase inhibitor benzenesulfonamide QSAR.

The lipophilicity of 33 meta and para substituted benzenesulfonamides was studied by reversed-phase HPLC using MeOH-H2O or MeCO-H2O as the mobile phases and μ Bondapak C18 as the stationary phase. A linear relation between the capacity factor (log k’) and the volume fraction of the organic modifier (θ) was established for each solute. The extrapolation of the retention to φ = 0 (0% of organic modifier) 0% organic modifier) permitted the elimination of any selective and specific effects of organic modifier, to calculate log kw and finally to derive τw for each substituent. The Hansch’s π hydrophobic parameter was linearly correlated to τw (r = 0.953), but no improvement in the correlation equation was observed when τw values obtained by adding silanol masking amines to the mobile phase were used. By introducing an indicator variable which takes into account the possibility of the substituent to make hydrogen bonding, a slight but significant improvement was instead observed The replacement of π with τw in the regression equation obtained in a recent QSAR study on carbonic anhydrase inhibition by benzenesulfonamide gives rise to a correlation equation with comparable statistical significance.

International Journal of Pharmaceutics published new progress about Lipophilicity. 35203-88-4 belongs to class amides-buliding-blocks, name is 3-Acetylbenzenesulfonamide, and the molecular formula is C8H9NO3S, Computed Properties of 35203-88-4.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Jacobs, Jeffrey W. published the artcileDiscovery of Tenapanor: A First-in-Class Minimally Systemic Inhibitor of Intestinal Na+/H+ Exchanger Isoform 3, SDS of cas: 35203-88-4, the main research area is tenapanor inhibitor intestine sodium hydrogen exchanger isoform 3 NHE3.

We present herein the design, synthesis, and optimization of gut-restricted inhibitors of Na+/H+ exchanger isoform 3 (NHE3). NHE3 is predominantly expressed in the kidney and gastrointestinal tract where it acts as the major absorptive sodium transporter. We desired minimally systemic agents that would block sodium absorption in the gastrointestinal tract but avoid exposure in the kidney. Starting with a relatively low-potency highly bioavailable hit compound (1), potent and minimally absorbed NHE3 inhibitors were designed, culminating with the discovery of tenapanor (28). Tenapanor has been approved by the U.S. Food and Drug Administration (FDA) for the treatment of irritable bowel syndrome with constipation in adults.

ACS Medicinal Chemistry Letters published new progress about Digestive tract. 35203-88-4 belongs to class amides-buliding-blocks, name is 3-Acetylbenzenesulfonamide, and the molecular formula is C8H9NO3S, SDS of cas: 35203-88-4.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Galley, W. C. published the artcileKinetics of triplet-triplet energy transfer and intramolecular distances in enzyme-inhibitor complexes, Formula: C8H9NO3S, the main research area is kinetics energy transfer bimol; enzyme inhibitor complex conformation; mol distance energy transfer.

The kinetics of triplet-triplet energy transfer and donor-acceptor geometries were used to estimate mol. distances in bimol. systems and to measure variability within enzyme-inhibitor complexes. The average distance from the center of the energy donor (m-acetylbenzene sulfonamide) to that of ≥1 tryptophan residue in bovine, human B, and human C forms of carbonic anhydrase were estimated as 10.1, <9.5, and 10.4 Å, resp. The use of kinetics of triplet energy transfer is recommended for studying bimol. conformations. Nature (London, United Kingdom) published new progress about Energy transfer. 35203-88-4 belongs to class amides-buliding-blocks, name is 3-Acetylbenzenesulfonamide, and the molecular formula is C8H9NO3S, Formula: C8H9NO3S.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

McCarville, Michael published the artcilePhosphorescent probes for proteins, Quality Control of 35203-88-4, the main research area is carbonic anhydrase inhibitor phosphorescent; tryptophan energy transfer; protein phosphorescent probes.

Use of bound phosphorescent chromophores to study protein structure was investigated. Carbonic anhydrase inhibitors with 3 different arrangements of singlet and triplet energy levels relative to those of tryptophan were used to determine their ability to transfer triplet energy. Ligands representing each of the 3 energy level arrangements were found to exhibit triplet-triplet energy transfer with a tryptophan residue at the active site of carbonic anhydrase. This greatly increases the number of ligands which may be useful as phosphorescent probes and is a potential source of data for determining the position of the ligand in the binding site.

Biochimica et Biophysica Acta, Protein Structure published new progress about Energy transfer. 35203-88-4 belongs to class amides-buliding-blocks, name is 3-Acetylbenzenesulfonamide, and the molecular formula is C8H9NO3S, Quality Control of 35203-88-4.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Fujikura, Takashi published the artcileStudies on benzenesulfonamide derivatives with α- and β-adrenergic antagonistic and antihypertensive activities, Computed Properties of 35203-88-4, the main research area is benzenesulfonamide sympatholytic antihypertensive preparation; aminoethylbenzenesulfonamide phenylmethylpropyl; phenoxyethylaminoethylbenzenesulfonamide; structure activity benzenesulfonamide aminohydroxyethyl.

New α- and β-adrenergic blockers, benzenesulfonamide derivatives I (R = H, halo, MeO, Me, Pr, MeS, MeSO2; R1 = H, MeO) and II (R2 = Me, MeO, OH; R3 = H, OH, MeO, EtO) were prepared from acetylbenzenesulfonamides. All the target compounds have two asym. centers and therefore consist of two diastereomers. I (R = 2-Me, R1 = 2-MeO) (III) and II (R2 = Me, R3 = 2-MeO) (IV) showed potent α- and β-blocking activities and they were each separated into two diastereomers (III-A and III-B, and IV-A and IV-B) and one isomer had mainly β-blocking activity and the other isomer had mainly α-blocking activity. In addition, several compounds showing relatively strong α- and β-blocking activities were also examined for antihypertensive activity and III and IV were more potent than labetalol. Structure-activity relationships were discussed.

Chemical & Pharmaceutical Bulletin published new progress about Antihypertensives. 35203-88-4 belongs to class amides-buliding-blocks, name is 3-Acetylbenzenesulfonamide, and the molecular formula is C8H9NO3S, Computed Properties of 35203-88-4.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Carotti, Angelo published the artcileInhibition of carbonic anhydrase by substituted benzenesulfonamides. A reinvestigation by QSAR and molecular graphics analysis, Computed Properties of 35203-88-4, the main research area is carbonic anhydrase inhibitor benzenesulfonamide QSAR.

The inhibition of bovine carbonic anhydrase B by an appropriately designed set of m- and p-substituted benzenesulfonamides (I, R = H, halo, alkoxy, aryl, etc.) was studied. From the results the following quant. structure-activity relationship was derived: log 1/Ki = 0.95σ + 0.54π – 0.35B5,3 + 6.29. In this equation Ki is the inhibition constant, σ is the Hammett constant, π is the hydrophobic parameter and B5,3 is the sterimol steric parameter for the m-substituents. Using this equation, a new congener was designed and synthesized and the Ki for a new congener intended to maximize the inhibitory potency (1/Ki) was predicted. The interactions involved in the enzyme-inhibitors binding as suggested by the correlation equation, have been tentatively interpreted using computer built 3-D mol. models based on the published X-ray crystallog. coordinates of the free and inhibitor-bound carbonic anhydrase. The results from our analyses have been compared with those obtained in some previous QSAR analyses.

Quantitative Structure-Activity Relationships published new progress about Arenesulfonamides Role: USES (Uses). 35203-88-4 belongs to class amides-buliding-blocks, name is 3-Acetylbenzenesulfonamide, and the molecular formula is C8H9NO3S, Computed Properties of 35203-88-4.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Dong, Yi published the artcileRhodium(III)-catalyzed sulfonamide directed ortho C-H carbenoid functionalization via metal carbene migratory insertion, HPLC of Formula: 35203-88-4, the main research area is diazoacetate arylsulfonyl acetamide preparation rhodium catalyst regioselective migratory insertion; acetylsulfamoyl arylacetate preparation.

A rhodium(III)-catalyzed sulfonamide directed ortho C-H carbenoid functionalization was developed with good yields. This method was attractive due to its broad substrate scope and enabled derivation of diverse biol. active sulfonamide structures and late-stage modification of sulfa drugs.

Chemical Communications (Cambridge, United Kingdom) published new progress about 1,3-Dicarbonyl compounds Role: RCT (Reactant), RACT (Reactant or Reagent). 35203-88-4 belongs to class amides-buliding-blocks, name is 3-Acetylbenzenesulfonamide, and the molecular formula is C8H9NO3S, HPLC of Formula: 35203-88-4.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Cash, Gordon G. published the artcilePrediction of inhibitory potencies of arenesulfonamides toward carbonic anhydrase using easily calculated molecular connectivity indices, Safety of 3-Acetylbenzenesulfonamide, the main research area is carbonic anhydrase inhibitor arenesulfonamide QSAR.

Previous literature reports described the correlation of arenesulfonamide inhibitory potency toward carbonic anhydrase with a quantum mech. descriptor, namely, the total charge on the sulfonamide oxygens, and an indicator variable. The present paper attempts to correlate the same inhibitory potency data with the much more easily calculated mol. connectivity indexes (MCIs) for the same set of compounds A good (r = 0.91) two-variable correlation was found for an subset, from which compounds with a certain structural characteristic had been excluded. This result is consistent with many previous reports that MCIs do well in predicting relative biol. activities of a homologous series of compounds but less well for groups of compounds that differ at several sites.

Structural Chemistry published new progress about QSAR (quantitative structure-activity relationship). 35203-88-4 belongs to class amides-buliding-blocks, name is 3-Acetylbenzenesulfonamide, and the molecular formula is C8H9NO3S, Safety of 3-Acetylbenzenesulfonamide.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics