Tag: 297.3533

Vree, T. B. et al. published their research in European Journal of Clinical Pharmacology in 1981 | CAS: 127-76-4

N-(4-(N-(Thiazol-2-yl)sulfamoyl)phenyl)acetamide (cas: 127-76-4) belongs to thiazole derivatives. Thiazoles in peptides or their ability to bind proteins, DNA and RNA has led to many synthetic studies and new applications. Electrophilic attack at nitrogen depends on the presence of electron density at nitrogen as well as the position and nature of substituent linked to the thiazole ring.Computed Properties of C11H11N3O3S2

Pharmacokinetics and mechanism of renal excretion of short acting sulfonamides and N4-acetylsulfonamide derivatives in man. Structural requirements of sulfonamides for active tubular secretion was written by Vree, T. B.;Hekster, Y. A.;Damsma, J. E.;Tijhuis, M.;Friesen, W. T.. And the article was included in European Journal of Clinical Pharmacology in 1981.Computed Properties of C11H11N3O3S2 This article mentions the following:

The pharmacokinetics of short acting sulfonamides and a series of N4-acetylsulfonamides was investigated. Sulfonamides with a S atom 2 at. bond distances from the N1-atom are excreted by active tubular secretion, e.g. sulfamethizole  [144-82-1], sulfaethidole  [94-19-9], and sulfathiazole  [72-14-0]. When the S atom is replaced by an O or N, active renal excretion no longer occurs. N4-Acetylsulfonamides are excreted by active tubular secretion. The renal clearance value of the N4-acetylsulfonamides are not influenced by the substituent at the N1 position. Two groups of N4-acetylsulfonamides can be distinguished. One has a T1/2 of 4-6 h and a renal clearance value of 20-60 mL/min and the second has a T1/2 of 10-20 h and a renal clearance of <10 mL/min. N4-Acetylsulfonamides are deacetylated ∼5%. In the experiment, the researchers used many compounds, for example, N-(4-(N-(Thiazol-2-yl)sulfamoyl)phenyl)acetamide (cas: 127-76-4Computed Properties of C11H11N3O3S2).

N-(4-(N-(Thiazol-2-yl)sulfamoyl)phenyl)acetamide (cas: 127-76-4) belongs to thiazole derivatives. Thiazoles in peptides or their ability to bind proteins, DNA and RNA has led to many synthetic studies and new applications. Electrophilic attack at nitrogen depends on the presence of electron density at nitrogen as well as the position and nature of substituent linked to the thiazole ring.Computed Properties of C11H11N3O3S2

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Vree, T. B. et al. published their research in European Journal of Clinical Pharmacology in 1981 | CAS: 127-76-4

N-(4-(N-(Thiazol-2-yl)sulfamoyl)phenyl)acetamide (cas: 127-76-4) belongs to thiazole derivatives. Thiazoles in peptides or their ability to bind proteins, DNA and RNA has led to many synthetic studies and new applications. Electrophilic attack at nitrogen depends on the presence of electron density at nitrogen as well as the position and nature of substituent linked to the thiazole ring.Computed Properties of C11H11N3O3S2

Pharmacokinetics and mechanism of renal excretion of short acting sulfonamides and N4-acetylsulfonamide derivatives in man. Structural requirements of sulfonamides for active tubular secretion was written by Vree, T. B.;Hekster, Y. A.;Damsma, J. E.;Tijhuis, M.;Friesen, W. T.. And the article was included in European Journal of Clinical Pharmacology in 1981.Computed Properties of C11H11N3O3S2 This article mentions the following:

The pharmacokinetics of short acting sulfonamides and a series of N4-acetylsulfonamides was investigated. Sulfonamides with a S atom 2 at. bond distances from the N1-atom are excreted by active tubular secretion, e.g. sulfamethizole  [144-82-1], sulfaethidole  [94-19-9], and sulfathiazole  [72-14-0]. When the S atom is replaced by an O or N, active renal excretion no longer occurs. N4-Acetylsulfonamides are excreted by active tubular secretion. The renal clearance value of the N4-acetylsulfonamides are not influenced by the substituent at the N1 position. Two groups of N4-acetylsulfonamides can be distinguished. One has a T1/2 of 4-6 h and a renal clearance value of 20-60 mL/min and the second has a T1/2 of 10-20 h and a renal clearance of <10 mL/min. N4-Acetylsulfonamides are deacetylated ∼5%. In the experiment, the researchers used many compounds, for example, N-(4-(N-(Thiazol-2-yl)sulfamoyl)phenyl)acetamide (cas: 127-76-4Computed Properties of C11H11N3O3S2).

N-(4-(N-(Thiazol-2-yl)sulfamoyl)phenyl)acetamide (cas: 127-76-4) belongs to thiazole derivatives. Thiazoles in peptides or their ability to bind proteins, DNA and RNA has led to many synthetic studies and new applications. Electrophilic attack at nitrogen depends on the presence of electron density at nitrogen as well as the position and nature of substituent linked to the thiazole ring.Computed Properties of C11H11N3O3S2

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Nelson, P. A. et al. published their research in Xenobiotica in 1987 | CAS: 127-76-4

N-(4-(N-(Thiazol-2-yl)sulfamoyl)phenyl)acetamide (cas: 127-76-4) belongs to thiazole derivatives. The thiazole ring is notable as a component of the vitamin thiamine (B1).Various laboratory methods exist for the organic synthesis of thiazoles. For example, 2,4-dimethylthiazole is synthesized from thioacetamide and chloroacetone.SDS of cas: 127-76-4

The effect of nitrite on 14C-sulfathiazole (4-amino-N-2-thiazolyl[U14C]benzenesulfonamide) metabolism in the rat was written by Nelson, P. A.;Paulson, G. D.;Feil, V. J.. And the article was included in Xenobiotica in 1987.SDS of cas: 127-76-4 This article mentions the following:

Rats given a meal containing 613 p.p.m. of 14C-sulfathiazole excreted less 14C-activity in urine and more 14C-activity in feces as nitrite in the meal was increased (0, 10, 100, or 1000 p.p.m.). As nitrite in the meal was increased from 0 to 1000 p.p.m. the total 14C-residues in the gastrointestinal tract 6 h after dosing increased, but decreased in other tissues. High nitrite in the meal resulted in increased methanol insoluble 14C-activity in the gastrointestinal tract but had little or no effect on the methanol-insoluble activity in liver and blood. Conversion of 14C-sulfathiazole to 14C-desaminosulfathiazole in the rat was greatly increased by nitrite in the meal. In the experiment, the researchers used many compounds, for example, N-(4-(N-(Thiazol-2-yl)sulfamoyl)phenyl)acetamide (cas: 127-76-4SDS of cas: 127-76-4).

N-(4-(N-(Thiazol-2-yl)sulfamoyl)phenyl)acetamide (cas: 127-76-4) belongs to thiazole derivatives. The thiazole ring is notable as a component of the vitamin thiamine (B1).Various laboratory methods exist for the organic synthesis of thiazoles. For example, 2,4-dimethylthiazole is synthesized from thioacetamide and chloroacetone.SDS of cas: 127-76-4

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Magon, Arlene M. et al. published their research in Journal of Laboratory and Clinical Medicine in 1981 | CAS: 127-76-4

N-(4-(N-(Thiazol-2-yl)sulfamoyl)phenyl)acetamide (cas: 127-76-4) belongs to thiazole derivatives. Thiazole is a five-membered, unsaturated, planar, 蟺-excessive heteroaromatic containing one sulfur atom and one pyridine-type nitrogen atom at position 3 of the cyclic ring system. The pyridine-type nitrogen in the thiazole ring deactivates the ring for electrophilic substitution reactions, which is further reduced in acid due to protonation of the thiazole ring.HPLC of Formula: 127-76-4

Interactions of glucose 6-phosphate dehydrogenase deficiency with drug acetylation and hydroxylation reactions was written by Magon, Arlene M.;Leipzig, Rosanne M.;Zannoni, Vincent G.;Brewer, George J.. And the article was included in Journal of Laboratory and Clinical Medicine in 1981.HPLC of Formula: 127-76-4 This article mentions the following:

It is hypothesized that the bimodal distribution of hemolytic response by glucose 6-phosphate dehydrogenase (G6PD) [9001-40-5]-deficient individuals to particular drugs such as sulfones may be due to the genetically determined acetylation rate of those drugs. Since metabolism, e.g., hydroxylation, may be required for these drugs to become hemolytic, genetically and environmentally determined variation in hydroxylation of a drug may also contribute to this variability in hemolytic response. To test the possibilities that acetylation and hydroxylation alter the hemolytic potential of these drugs, G6PD-deficient and normal red cells were incubated with mouse liver microsomes at 2 states of hydroxylase activity (uninduced and induced), an NADPH-generating system, and acetylated or unacetylated drug. GSH depletion was then measured in the cells as an indicator of prelytic cell damage. In the presence of induced (high hydroxylase activity) microsomes, promizole [473-30-3] or DDS [80-08-0] in unacetylated form caused the highest level of GSH depletion in G6PD-deficient red cells. Acetylation protected against GSH depletion. The specificity of the hydroxylation reaction in producing marked GSH depletion was shown by the protective effect of a specific hydroxylation inhibitor. Thus, G6PD-deficient, genetically slow acetylators, having high microsomal activity, would be most susceptible to promizole- or DDS-induced hemolysis, compared to other metabolic phenotypes. In addition, the bimodality in hemolytic response to promizole probably corresponds to the bimodal distribution of acetylator phenotype in the population. In the experiment, the researchers used many compounds, for example, N-(4-(N-(Thiazol-2-yl)sulfamoyl)phenyl)acetamide (cas: 127-76-4HPLC of Formula: 127-76-4).

N-(4-(N-(Thiazol-2-yl)sulfamoyl)phenyl)acetamide (cas: 127-76-4) belongs to thiazole derivatives. Thiazole is a five-membered, unsaturated, planar, 蟺-excessive heteroaromatic containing one sulfur atom and one pyridine-type nitrogen atom at position 3 of the cyclic ring system. The pyridine-type nitrogen in the thiazole ring deactivates the ring for electrophilic substitution reactions, which is further reduced in acid due to protonation of the thiazole ring.HPLC of Formula: 127-76-4

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Sapozhnikova, N. V. et al. published their research in Zhurnal Prikladnoi Khimii (Sankt-Peterburg, Russian Federation) in 1944 | CAS: 127-76-4

N-(4-(N-(Thiazol-2-yl)sulfamoyl)phenyl)acetamide (cas: 127-76-4) belongs to thiazole derivatives. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities. Various laboratory methods exist for the organic synthesis of thiazoles. Prominent is the Hantzsch thiazole synthesis is a reaction between haloketones and thioamides.Reference of 127-76-4

Solubility of several sulfanilamide compounds in water and in water-alcohol mixtures was written by Sapozhnikova, N. V.;Postovskii, I. Ya.. And the article was included in Zhurnal Prikladnoi Khimii (Sankt-Peterburg, Russian Federation) in 1944.Reference of 127-76-4 This article mentions the following:

The solubilities in water of sulfanilamide, sulfaguanidine, sulfapyridine, sulfamethylthiazole, sulfathiazole, sulfamethyldiazine and their Ac derivatives were determined at 20-39掳. N’-heterocyclic derivatives have poor water solubility Heats of solution range from 9500 to 10, 600 cal./mol. All compounds, except diacetylsulfanilamide have maximum solubility in EtOH-water mixtures of 67-76% EtOH. Solubilities in water up to 100掳 are given in graphical form. In the experiment, the researchers used many compounds, for example, N-(4-(N-(Thiazol-2-yl)sulfamoyl)phenyl)acetamide (cas: 127-76-4Reference of 127-76-4).

N-(4-(N-(Thiazol-2-yl)sulfamoyl)phenyl)acetamide (cas: 127-76-4) belongs to thiazole derivatives. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities. Various laboratory methods exist for the organic synthesis of thiazoles. Prominent is the Hantzsch thiazole synthesis is a reaction between haloketones and thioamides.Reference of 127-76-4

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Uno, Toyozo et al. published their research in Yakugaku Zasshi in 1960 | CAS: 127-76-4

N-(4-(N-(Thiazol-2-yl)sulfamoyl)phenyl)acetamide (cas: 127-76-4) belongs to thiazole derivatives. Thiazole is a five-membered, unsaturated, planar, 蟺-excessive heteroaromatic containing one sulfur atom and one pyridine-type nitrogen atom at position 3 of the cyclic ring system.Various laboratory methods exist for the organic synthesis of thiazoles. For example, 2,4-dimethylthiazole is synthesized from thioacetamide and chloroacetone.Synthetic Route of C11H11N3O3S2

Metabolism of sulfathiazole. I. Excreted substance in human urine after administration of sulfathiazole was written by Uno, Toyozo;Ueda, Michihiro. And the article was included in Yakugaku Zasshi in 1960.Synthetic Route of C11H11N3O3S2 This article mentions the following:

The urine during oral administration of sulfathiazole (I) was examined by paper chromatography, using neutral, acid, and alk. developing solvents and by paper electrophoresis. I, acetylsulfathiazole (II), sulfathiazole N4-sulfonate, sulfathiazole N4-glucuronide, and an unknown substance (III) were detected. These products, except the III, were compared with authentic samples. In another experiment I, II, and an unknown glucuronic acid conjugate were isolated but no other substances. A new and simple apparatus for two-dimensional, ascending paper chromatography was devised, in which the filter paper was wrapped in a plastic sheet. In the experiment, the researchers used many compounds, for example, N-(4-(N-(Thiazol-2-yl)sulfamoyl)phenyl)acetamide (cas: 127-76-4Synthetic Route of C11H11N3O3S2).

N-(4-(N-(Thiazol-2-yl)sulfamoyl)phenyl)acetamide (cas: 127-76-4) belongs to thiazole derivatives. Thiazole is a five-membered, unsaturated, planar, 蟺-excessive heteroaromatic containing one sulfur atom and one pyridine-type nitrogen atom at position 3 of the cyclic ring system.Various laboratory methods exist for the organic synthesis of thiazoles. For example, 2,4-dimethylthiazole is synthesized from thioacetamide and chloroacetone.Synthetic Route of C11H11N3O3S2

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Bellen, Z. et al. published their research in Chemia Analityczna (Warsaw, Poland) in 1956 | CAS: 127-76-4

N-(4-(N-(Thiazol-2-yl)sulfamoyl)phenyl)acetamide (cas: 127-76-4) belongs to thiazole derivatives. Thiazoles frequently appear in peptide studies. Thiazoles can also be used as protected formyl groups, which can be released in later stages of complex natural product synthesis. Thiazole is a versatile building block for the construction and lead generation of new drug discoveries. Numerous diazole-based compounds are in clinical use as anticancer, antileukemic, antiinflammatory, antiviral, antifungal, antirheumatic, immunomodulator, and antiparasitic agents.Product Details of 127-76-4

Determination of 2-[bis-(N-acetylsulfanilyl)]aminothiazole in the commercial product was written by Bellen, Z.;Mroczkowska, Z.. And the article was included in Chemia Analityczna (Warsaw, Poland) in 1956.Product Details of 127-76-4 This article mentions the following:

The method consists of ammonolysis of the product by heating with concentrated NH3 and EtOH and by double evaporation of EtOH and NH3. Acetyl sulfathiazole is determined by potentiometric titration in H2OMe2CO mixture (4:1) with standard NaOH solution The determination of impurities in the sample is analogous. The results are tabulated and given in graphs. The method gave good results for pure as well as for com. samples. In the experiment, the researchers used many compounds, for example, N-(4-(N-(Thiazol-2-yl)sulfamoyl)phenyl)acetamide (cas: 127-76-4Product Details of 127-76-4).

N-(4-(N-(Thiazol-2-yl)sulfamoyl)phenyl)acetamide (cas: 127-76-4) belongs to thiazole derivatives. Thiazoles frequently appear in peptide studies. Thiazoles can also be used as protected formyl groups, which can be released in later stages of complex natural product synthesis. Thiazole is a versatile building block for the construction and lead generation of new drug discoveries. Numerous diazole-based compounds are in clinical use as anticancer, antileukemic, antiinflammatory, antiviral, antifungal, antirheumatic, immunomodulator, and antiparasitic agents.Product Details of 127-76-4

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Nelson, P. A. et al. published their research in Xenobiotica in 1987 | CAS: 127-76-4

N-(4-(N-(Thiazol-2-yl)sulfamoyl)phenyl)acetamide (cas: 127-76-4) belongs to thiazole derivatives. The thiazole ring is notable as a component of the vitamin thiamine (B1).Various laboratory methods exist for the organic synthesis of thiazoles. For example, 2,4-dimethylthiazole is synthesized from thioacetamide and chloroacetone.SDS of cas: 127-76-4

The effect of nitrite on 14C-sulfathiazole (4-amino-N-2-thiazolyl[U14C]benzenesulfonamide) metabolism in the rat was written by Nelson, P. A.;Paulson, G. D.;Feil, V. J.. And the article was included in Xenobiotica in 1987.SDS of cas: 127-76-4 This article mentions the following:

Rats given a meal containing 613 p.p.m. of 14C-sulfathiazole excreted less 14C-activity in urine and more 14C-activity in feces as nitrite in the meal was increased (0, 10, 100, or 1000 p.p.m.). As nitrite in the meal was increased from 0 to 1000 p.p.m. the total 14C-residues in the gastrointestinal tract 6 h after dosing increased, but decreased in other tissues. High nitrite in the meal resulted in increased methanol insoluble 14C-activity in the gastrointestinal tract but had little or no effect on the methanol-insoluble activity in liver and blood. Conversion of 14C-sulfathiazole to 14C-desaminosulfathiazole in the rat was greatly increased by nitrite in the meal. In the experiment, the researchers used many compounds, for example, N-(4-(N-(Thiazol-2-yl)sulfamoyl)phenyl)acetamide (cas: 127-76-4SDS of cas: 127-76-4).

N-(4-(N-(Thiazol-2-yl)sulfamoyl)phenyl)acetamide (cas: 127-76-4) belongs to thiazole derivatives. The thiazole ring is notable as a component of the vitamin thiamine (B1).Various laboratory methods exist for the organic synthesis of thiazoles. For example, 2,4-dimethylthiazole is synthesized from thioacetamide and chloroacetone.SDS of cas: 127-76-4

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Magon, Arlene M. et al. published their research in Journal of Laboratory and Clinical Medicine in 1981 | CAS: 127-76-4

N-(4-(N-(Thiazol-2-yl)sulfamoyl)phenyl)acetamide (cas: 127-76-4) belongs to thiazole derivatives. Thiazole is a five-membered, unsaturated, planar, π-excessive heteroaromatic containing one sulfur atom and one pyridine-type nitrogen atom at position 3 of the cyclic ring system. The pyridine-type nitrogen in the thiazole ring deactivates the ring for electrophilic substitution reactions, which is further reduced in acid due to protonation of the thiazole ring.HPLC of Formula: 127-76-4

Interactions of glucose 6-phosphate dehydrogenase deficiency with drug acetylation and hydroxylation reactions was written by Magon, Arlene M.;Leipzig, Rosanne M.;Zannoni, Vincent G.;Brewer, George J.. And the article was included in Journal of Laboratory and Clinical Medicine in 1981.HPLC of Formula: 127-76-4 This article mentions the following:

It is hypothesized that the bimodal distribution of hemolytic response by glucose 6-phosphate dehydrogenase (G6PD) [9001-40-5]-deficient individuals to particular drugs such as sulfones may be due to the genetically determined acetylation rate of those drugs. Since metabolism, e.g., hydroxylation, may be required for these drugs to become hemolytic, genetically and environmentally determined variation in hydroxylation of a drug may also contribute to this variability in hemolytic response. To test the possibilities that acetylation and hydroxylation alter the hemolytic potential of these drugs, G6PD-deficient and normal red cells were incubated with mouse liver microsomes at 2 states of hydroxylase activity (uninduced and induced), an NADPH-generating system, and acetylated or unacetylated drug. GSH depletion was then measured in the cells as an indicator of prelytic cell damage. In the presence of induced (high hydroxylase activity) microsomes, promizole [473-30-3] or DDS [80-08-0] in unacetylated form caused the highest level of GSH depletion in G6PD-deficient red cells. Acetylation protected against GSH depletion. The specificity of the hydroxylation reaction in producing marked GSH depletion was shown by the protective effect of a specific hydroxylation inhibitor. Thus, G6PD-deficient, genetically slow acetylators, having high microsomal activity, would be most susceptible to promizole- or DDS-induced hemolysis, compared to other metabolic phenotypes. In addition, the bimodality in hemolytic response to promizole probably corresponds to the bimodal distribution of acetylator phenotype in the population. In the experiment, the researchers used many compounds, for example, N-(4-(N-(Thiazol-2-yl)sulfamoyl)phenyl)acetamide (cas: 127-76-4HPLC of Formula: 127-76-4).

N-(4-(N-(Thiazol-2-yl)sulfamoyl)phenyl)acetamide (cas: 127-76-4) belongs to thiazole derivatives. Thiazole is a five-membered, unsaturated, planar, π-excessive heteroaromatic containing one sulfur atom and one pyridine-type nitrogen atom at position 3 of the cyclic ring system. The pyridine-type nitrogen in the thiazole ring deactivates the ring for electrophilic substitution reactions, which is further reduced in acid due to protonation of the thiazole ring.HPLC of Formula: 127-76-4

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Sapozhnikova, N. V. et al. published their research in Zhurnal Prikladnoi Khimii (Sankt-Peterburg, Russian Federation) in 1944 | CAS: 127-76-4

N-(4-(N-(Thiazol-2-yl)sulfamoyl)phenyl)acetamide (cas: 127-76-4) belongs to thiazole derivatives. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities. Various laboratory methods exist for the organic synthesis of thiazoles. Prominent is the Hantzsch thiazole synthesis is a reaction between haloketones and thioamides.Reference of 127-76-4

Solubility of several sulfanilamide compounds in water and in water-alcohol mixtures was written by Sapozhnikova, N. V.;Postovskii, I. Ya.. And the article was included in Zhurnal Prikladnoi Khimii (Sankt-Peterburg, Russian Federation) in 1944.Reference of 127-76-4 This article mentions the following:

The solubilities in water of sulfanilamide, sulfaguanidine, sulfapyridine, sulfamethylthiazole, sulfathiazole, sulfamethyldiazine and their Ac derivatives were determined at 20-39°. N’-heterocyclic derivatives have poor water solubility Heats of solution range from 9500 to 10, 600 cal./mol. All compounds, except diacetylsulfanilamide have maximum solubility in EtOH-water mixtures of 67-76% EtOH. Solubilities in water up to 100° are given in graphical form. In the experiment, the researchers used many compounds, for example, N-(4-(N-(Thiazol-2-yl)sulfamoyl)phenyl)acetamide (cas: 127-76-4Reference of 127-76-4).

N-(4-(N-(Thiazol-2-yl)sulfamoyl)phenyl)acetamide (cas: 127-76-4) belongs to thiazole derivatives. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities. Various laboratory methods exist for the organic synthesis of thiazoles. Prominent is the Hantzsch thiazole synthesis is a reaction between haloketones and thioamides.Reference of 127-76-4

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica