Category: 19759-66-1

Children learn through play, and they learn more than adults might expect. Science experiments are a great way to spark their curiosity, get their minds active, and encourage them to do something that doesn’t involve a screen. 19759-66-1, C8H5N3S. A document type is Article, introducing its new discovery., name: 2-Aminobenzothiazole-6-carbonitrile

Human 17beta-hydroxysteroid dehydrogenase type 10 is a multifunctional protein involved in many enzymatic and structural processes within mitochondria. This enzyme was suggested to be involved in several neurological diseases, e.g., mental retardation, Parkinson?s disease, or Alzheimer?s disease, in which it was shown to interact with the amyloid-beta peptide. We prepared approximately 60 new compounds based on a benzothiazolyl scaffold and evaluated their inhibitory ability and mechanism of action. The most potent inhibitors contained 3-chloro and 4-hydroxy substitution on the phenyl ring moiety, a small substituent at position 6 on the benzothiazole moiety, and the two moieties were connected via a urea linker (4at, 4bb, and 4bg). These compounds exhibited IC50 values of 1?2 muM and showed an uncompetitive mechanism of action with respect to the substrate, acetoacetyl-CoA. These uncompetitive benzothiazolyl inhibitors of 17beta-hydroxysteroid dehydrogenase type 10 are promising compounds for potential drugs for neurodegenerative diseases that warrant further research and development.

Interested yet? Keep reading other articles of 19759-66-1!, name: 2-Aminobenzothiazole-6-carbonitrile

Reference：
Thiazole | C3H2251NS – PubChem,
Thiazole | chemical compound | Britannica

19759-66-1, Name is 2-Aminobenzothiazole-6-carbonitrile, molecular formula is C8H5N3S, belongs to thiazole compound, is a common compound. In a patnet, once mentioned the new application about 19759-66-1, Formula: C8H5N3S

Guanidinothiazolecarboxamides (GTCs) are a novel class of antitumor agents found to be systemically active against experimental pulmonary metastases of 3LL Lewis lung carcinoma.A series of substituted benzothiazole GTCs were found to produce enhancement of survival in this model by using 8 days of intraperitoneal dosing initiated 2 days after intravenous tumor challenge.Quantitative structure-activity relationships have been discovered in the GTC series with survival enhancement correlated to substituent parameters.Optimal correlations were found between the probit transform of the drug-induced increased lifespan (ILS) and field and ? parameters.Among the most effective analogues in this series was N-(5-fluorobenzothiazol-2-yl)-2-guanidinothiazole-4-carboxamide (19).

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Formula: C8H5N3S. In my other articles, you can also check out more blogs about 19759-66-1

Reference：
Thiazole | C3H2252NS – PubChem,
Thiazole | chemical compound | Britannica

A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 19759-66-1, Name is 2-Aminobenzothiazole-6-carbonitrile, molecular formula is C8H5N3S. In a Article，once mentioned of 19759-66-1, COA of Formula: C8H5N3S

The multistep synthesis of a series of new substituted-benzothiazoles as hydrochloride or quaternary salts is described. 6-Amidino substituted 2-aminobenzothiazoles (5, 6), N-methyl-2-(4-cyanostyryl)benzothiazolium iodide (8), cyano-substituted-2-styrylbenzothiazoles (9-11) and amidino and bis-amidino-substituted 2-styrylbenzothiazoles (12-17) were prepared. The crystal structure of amidino derivative (6) was determined by single crystal X-ray analysis. All new prepared compounds were tested on the cytostatic activities against malignant cell lines: (SW620, colon carcinoma; Hep2, laryngeal carcinoma; HBL, melanoma; HeLa, cervical carcinoma and WI38, human normal fibroblasts). The compounds exerted a different inhibitory effect, depended on concentration and type of the cells. The best inhibitory effect was achieved with compounds (12-15), with slight differences among them. All of them inhibited the growth of examined tumor cell lines and also normal fibroblasts. Other examined compounds exhibited a moderate inhibitory effect, depending on type of the cells. Majority of them inhibited the growth of HeLa cells and WI38.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data.COA of Formula: C8H5N3S, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 19759-66-1, in my other articles.

Reference：
Thiazole | C3H2239NS – PubChem,
Thiazole | chemical compound | Britannica

A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 19759-66-1, Name is 2-Aminobenzothiazole-6-carbonitrile, molecular formula is C8H5N3S. In a Article，once mentioned of 19759-66-1, SDS of cas: 19759-66-1

Combination of bioactive moieties with different heteroatom(s): Application of the Suzuki cross-coupling reaction

Two series of thiophene/benzothiophene-linked quinolinyl oxadiazoles condensed to the substituted N-benzothiazolyl acetamides have been synthesized via the Suzuki cross-coupling reaction. The ester derivative of 6-bromo-substituted quinoline was reacted via the Suzuki cross-coupling reaction with commercially available (benzo)thiophen-2-ylboronic acid at optimized temperature in 1,2-dimethoxy ethane and water in the presence of potassium carbonate and palladium tetrakis. The resulting derivatives were then hydrazinolized using 99% hydrazine hydrate followed by cyclization using carbon disulfide in ethanolic KOH to furnish the corresponding oxadiazoles, which were then condensed with various substituted 2-chloro-N-benzothiazolyl acetamides to produce the final scaffolds involving a unique combination of four heterocycles to be examined for their antimicrobial activity against two Gram-positive bacteria (Staphylococcus aureus and Bacillus cereus), three Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa, and Klebsiella pneumoniae), and two fungal species (Aspergillus niger and Candida albicans). The investigation of biological screening data revealed that the majority of the compounds tested have demonstrated excellent activity (minimum inhibitory concentrations; 6.25-50 mug/mL) against most of the microorganisms as compared with the standard and hence they warrant more consideration as prospective antimicrobial agents. New products (9a-10i) were characterized by physicochemical, elemental, and spectral (IR, 1H NMR, and 13C NMR) data.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.SDS of cas: 19759-66-1. In my other articles, you can also check out more blogs about 19759-66-1

Reference：
Thiazole | C3H2229NS – PubChem,
Thiazole | chemical compound | Britannica

A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 19759-66-1, Name is 2-Aminobenzothiazole-6-carbonitrile, molecular formula is C8H5N3S. In a Article，once mentioned of 19759-66-1, SDS of cas: 19759-66-1

Combination of bioactive moieties with different heteroatom(s): Application of the Suzuki cross-coupling reaction

Two series of thiophene/benzothiophene-linked quinolinyl oxadiazoles condensed to the substituted N-benzothiazolyl acetamides have been synthesized via the Suzuki cross-coupling reaction. The ester derivative of 6-bromo-substituted quinoline was reacted via the Suzuki cross-coupling reaction with commercially available (benzo)thiophen-2-ylboronic acid at optimized temperature in 1,2-dimethoxy ethane and water in the presence of potassium carbonate and palladium tetrakis. The resulting derivatives were then hydrazinolized using 99% hydrazine hydrate followed by cyclization using carbon disulfide in ethanolic KOH to furnish the corresponding oxadiazoles, which were then condensed with various substituted 2-chloro-N-benzothiazolyl acetamides to produce the final scaffolds involving a unique combination of four heterocycles to be examined for their antimicrobial activity against two Gram-positive bacteria (Staphylococcus aureus and Bacillus cereus), three Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa, and Klebsiella pneumoniae), and two fungal species (Aspergillus niger and Candida albicans). The investigation of biological screening data revealed that the majority of the compounds tested have demonstrated excellent activity (minimum inhibitory concentrations; 6.25-50 mug/mL) against most of the microorganisms as compared with the standard and hence they warrant more consideration as prospective antimicrobial agents. New products (9a-10i) were characterized by physicochemical, elemental, and spectral (IR, 1H NMR, and 13C NMR) data.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.SDS of cas: 19759-66-1. In my other articles, you can also check out more blogs about 19759-66-1

Reference：
Thiazole | C3H2229NS – PubChem,
Thiazole | chemical compound | Britannica

The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.19759-66-1, Name is 2-Aminobenzothiazole-6-carbonitrile, molecular formula is C8H5N3S. In a Patent£¬once mentioned of 19759-66-1, category: thiazole

The present invention relates to compounds having a structure of general formula (I), processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment of bacterial infections in humans and warm-blooded animals.

The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction.I hope my blog about 19759-66-1 is helpful to your research., category: thiazole

Reference£º
Thiazole | C3H2237NS – PubChem,
Thiazole | chemical compound | Britannica

Related Products of 19759-66-1, An article , which mentions 19759-66-1, molecular formula is C8H5N3S. The compound – 2-Aminobenzothiazole-6-carbonitrile played an important role in people’s production and life.

The glycogen synthase kinase 3 (GSK-3) is implicated in multiple cellular processes and has been linked to the pathogenesis of Alzheimer’s disease (AD). In the course of our research topic we synthesized a library of potent GSK-3 inhibitors. We utilized the urea scaffold present in the potent and highly selective GSK-3 inhibitor AR-A014418 (AstraZeneca). This moiety suits both (a) a convergent approach utilizing readily accessible building blocks and (b) a divergent approach based on a microwave heating assisted Suzuki coupling. We established a chromatography-free purification method to generate products with sufficient purity for the biological assays. The structure-activity relationship of the library provided the rationale for the synthesis of the benzothiazolylurea 66 (IC50 = 140 nM) and the pyridylurea 62 (IC 50 = 98 nM), which displayed two to threefold enhanced activity versus the reference compound 18 (AR-A014418: IC50 = 330 nM) in our assays.

The glycogen synthase kinase 3 (GSK-3) is implicated in multiple cellular processes and has been linked to the pathogenesis of Alzheimer’s disease (AD). In the course of our research topic we synthesized a library of potent GSK-3 inhibitors. We utilized the urea scaffold present in the potent and highly selective GSK-3 inhibitor AR-A014418 (AstraZeneca). This moiety suits both (a) a convergent approach utilizing readily accessible building blocks and (b) a divergent approach based on a microwave heating assisted Suzuki coupling. We established a chromatography-free purification method to generate products with sufficient purity for the biological assays. The structure-activity relationship of the library provided the rationale for the synthesis of the benzothiazolylurea 66 (IC50 = 140 nM) and the pyridylurea 62 (IC 50 = 98 nM), which displayed two to threefold enhanced activity versus the reference compound 18 (AR-A014418: IC50 = 330 nM) in our assays.

I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 19759-66-1, help many people in the next few years., Related Products of 19759-66-1

Reference£º
Thiazole | C3H2242NS – PubChem,
Thiazole | chemical compound | Britannica

Related Products of 19759-66-1, An article , which mentions 19759-66-1, molecular formula is C8H5N3S. The compound – 2-Aminobenzothiazole-6-carbonitrile played an important role in people’s production and life.

In the present work, we designed and synthesized new roflumilast analogues with preferential-selective PDE-4B inhibition activity and improved pharmacokinetic properties. The unsubstituted benzo[d]thiazol-2-yl and -6-yl benzamide derivatives (4a and 6a) showed both good potency and preferential selectivity for PDE-4B. More remarkably, 6c revealed 6 times preferential PDE-4B/4D selectivity with a significant increase of in vitro cAMP and good % inhibition of TNF-alpha concentration. In addition, the in vitro pharmacokinetics of 6c showed good metabolic stability with in vitro CLint (5.67 mL/min/kg) and moderate % plasma protein binding (53.71%). This was reflected onto increased in vivo exposure with a half-life greater than roflumilast by 3 folds (21 h) and a Cmax value of 113.958 ng/mL. Molecular docking attributed its good activity to its key binding interactions in PDE-4B active site with additional hydrogen bonding with amino acids lining the metal pocket. Summing up, 6c can be considered as suitable candidate for further investigation for the treatment of COPD.

In the present work, we designed and synthesized new roflumilast analogues with preferential-selective PDE-4B inhibition activity and improved pharmacokinetic properties. The unsubstituted benzo[d]thiazol-2-yl and -6-yl benzamide derivatives (4a and 6a) showed both good potency and preferential selectivity for PDE-4B. More remarkably, 6c revealed 6 times preferential PDE-4B/4D selectivity with a significant increase of in vitro cAMP and good % inhibition of TNF-alpha concentration. In addition, the in vitro pharmacokinetics of 6c showed good metabolic stability with in vitro CLint (5.67 mL/min/kg) and moderate % plasma protein binding (53.71%). This was reflected onto increased in vivo exposure with a half-life greater than roflumilast by 3 folds (21 h) and a Cmax value of 113.958 ng/mL. Molecular docking attributed its good activity to its key binding interactions in PDE-4B active site with additional hydrogen bonding with amino acids lining the metal pocket. Summing up, 6c can be considered as suitable candidate for further investigation for the treatment of COPD.

I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 19759-66-1, help many people in the next few years., Related Products of 19759-66-1

Reference£º
Thiazole | C3H2248NS – PubChem,
Thiazole | chemical compound | Britannica

Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments.Introducing a new discovery about 19759-66-1, Name is 2-Aminobenzothiazole-6-carbonitrile, SDS of cas: 19759-66-1.

A copper-catalyzed aerobic oxidative reaction between aromatics or heteroaromatics with KSCN is developed by using O2 as the oxidant. The combination of Cu(OTf)2, N,N,N?,N?-tetramethylethylenediamine (TMEDA) and BF3¡¤Et2O provides an efficient catalytic system, affording substituted thiocyanation products and 2-aminobenzothiazoles in excellent yields. The reaction also possesses a good functional group tolerance for both strong electron-withdrawing and electron-donating groups.

A copper-catalyzed aerobic oxidative reaction between aromatics or heteroaromatics with KSCN is developed by using O2 as the oxidant. The combination of Cu(OTf)2, N,N,N?,N?-tetramethylethylenediamine (TMEDA) and BF3¡¤Et2O provides an efficient catalytic system, affording substituted thiocyanation products and 2-aminobenzothiazoles in excellent yields. The reaction also possesses a good functional group tolerance for both strong electron-withdrawing and electron-donating groups.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.SDS of cas: 19759-66-1. In my other articles, you can also check out more blogs about 19759-66-1

Reference£º
Thiazole | C3H2270NS – PubChem,
Thiazole | chemical compound | Britannica

Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments.Introducing a new discovery about 19759-66-1, Name is 2-Aminobenzothiazole-6-carbonitrile, SDS of cas: 19759-66-1.

The present invention is directed to a compound of formula (I), 1racemic-diastereomeric mixtures thereof, optical isomers thereof, prodrugs thereof, isotopes thereof or pharmaceutically-acceptable salts of said compound, isomers, prodrugs and isotopes, wherein the variables are defined herein. The compounds of this invention are useful as inhibitors of serine/threonine and tyrosine kinases. In particular, compounds of this invention are useful as inhibitors of tyrosine kinases that are important in hyperproliferative diseases, especially in cancer and in the process of angiogenesis.

The present invention is directed to a compound of formula (I), 1racemic-diastereomeric mixtures thereof, optical isomers thereof, prodrugs thereof, isotopes thereof or pharmaceutically-acceptable salts of said compound, isomers, prodrugs and isotopes, wherein the variables are defined herein. The compounds of this invention are useful as inhibitors of serine/threonine and tyrosine kinases. In particular, compounds of this invention are useful as inhibitors of tyrosine kinases that are important in hyperproliferative diseases, especially in cancer and in the process of angiogenesis.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.SDS of cas: 19759-66-1. In my other articles, you can also check out more blogs about 19759-66-1

Reference£º
Thiazole | C3H2238NS – PubChem,
Thiazole | chemical compound | Britannica