Tag: 200-300

On July 17, 2008, Murray, Anthony; Lau, Jesper; Vedsoe, Per published a patent.Quality Control of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate The title of the patent was Preparation of arylureidothiazolylthioalkanoates as glucokinase activators. And the patent contained the following:

Title compounds [I; R = CH2CO2H, CH2CMe2CO2H, CMe2CO2H; R1 = substituted (heteroaryl-fused) Ph], were prepared for treatment of diabetes, hyperglycemia, obesity, syndrome X, dyslipidemia, and impaired glucose tolerance (no data). Thus, cyclopentylmethyl(2,5-difluorophenyl)amine (preparation given), Et 3-(2-aminothiazol-5-ylsulfanyl)-2,2-dimethylpropionate (preparation given), carbonyldiimidazole, and DMAP were stirred together in THF at 40-50° to give the desired urea ester, which was saponified with aqueous NaOH in THF/MeOH to give [2-[3-cyclopentylmethyl-3-(2,5-difluorophenyl)ureido]thiazol-5-ylsulfanyl]acetic acid. The experimental process involved the reaction of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate(cas: 859522-19-3).Quality Control of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate

The Article related to arylcyclopentylmethylureidothiazolylthioalkanoate preparation glucokinase activator, diabetes hyperglycemia obesity dyslipidemia treatment thiazolylthioalkanoate ureido aryl cyclopentylmethyl and other aspects.Quality Control of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate

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

On March 20, 2012, Murray, Anthony; Lau, Jesper; Vedsoe, Per published a patent.Synthetic Route of 859522-19-3 The title of the patent was Urea glucokinase activators. And the patent contained the following:

This application relates to novel urea glucokinase activators and use of the compounds of the invention for preparation of a medicament for the treatment of various diseases, e.g. for the treatment of type 2 diabetes. Further encompassed is a pharmaceutical composition comprising a compound according to the invention and a process for preparing such. The experimental process involved the reaction of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate(cas: 859522-19-3).Synthetic Route of 859522-19-3

The Article related to arylcyclopentylmethylureidothiazolylthioalkanoate preparation glucokinase activator, diabetes hyperglycemia obesity dyslipidemia treatment thiazolylthioalkanoate ureido aryl cyclopentylmethyl and other aspects.Synthetic Route of 859522-19-3

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

Hussein, Awaz Jamil; Azeez, Hashim Jalal published an article in 2013, the title of the article was Synthesis and antimicrobial activity of some new thiazolidin-4-one derivatives of 4-(6-methylbenzo[d]thiazol-2-yl)benzamine.COA of Formula: C14H12N2S And the article contains the following content:

A number of derivatives of 2-(substituted phenyl)-3-(4-(6-methylbenzo[d]thiazol-2-yl)phenyl)thiazolidin-4-one were synthesized from the reaction of 4-(6-methylbenzo[d]thiazol-2-yl)benzenamine with different substituted benzaldehydes followed by cyclocondensation reaction of the prepared imines with 2-mercaptoacetic acid in high yields. Furthermore, the structures of the newly synthesized compounds were confirmed by FT-IR, 13C-NMR, 13C-DEPT, and 1H-NMR spectral data. The imines and thiazolidin-4-one derivatives were evaluated for their antibacterial activity against Escherichia coli as gram neg. and Staphylococcus aureus as gram pos., the results have shown significant activity against both types of bacteria. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).COA of Formula: C14H12N2S

The Article related to benzothiazolylaniline aryl aldehyde condensation, schiff base preparation antibacterial cyclization mercaptoacetate, aryl benzothiazolylphenyl thiazolidinone preparation antibacterial and other aspects.COA of Formula: C14H12N2S

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

On July 31, 2009, Yotnoi, Bunlawee; Limtrakul, Jumras; Prior, Timothy; Rujiwatra, Apinpus published an article.Recommanded Product: 2-(4-Aminophenyl)-6-methylbenzothiazole The title of the article was Preparation and Characterization of Bis(μ-1,2-diaminoethane)cobalt(II) Hexavanadate: A Layered Polyoxovanadate Pillared by a Cobalt Coordination Complex. And the article contained the following:

The first example of polyoxovanadate layered framework with a cobalt coordination complex as a pillaring unit, CoII(μ-C2N2H8)2[VIV4VV2O14], was readily synthesized under hydrothermal conditions. The structure can be solved and refined in monoclinic P21/n with a 9.143(3), b 6.5034(11), c 15.874(4) Å, β = 101.90(2), V = 923.6(4) Å3 and Z = 2. The crystal structure comprises two-dimensional {VIV4VV2O14}2- layers extending parallel to [101], constructed from tetrahedral {VVO4} and square pyramidal {VIVO5} building units. Adjacent layers are linked through the octahedral {CoIIO2(μ-C2N2H8)2} pillars, within which the CoII resides on an inversion center. The structure displays N-H···O and C-H···O hydrogen bonding between the ethylenediamine and vanadium oxide layers. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Recommanded Product: 2-(4-Aminophenyl)-6-methylbenzothiazole

The Article related to cobalt diaminoethane bridge layered polyoxovanadate pillared complex hydrothermal preparation, crystal structure cobalt diaminoethane bridge layered polyoxovanadate pillared complex and other aspects.Recommanded Product: 2-(4-Aminophenyl)-6-methylbenzothiazole

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

On December 1, 2015, Maracic, Silvija; Kraljevic, Tatjana Gazivoda; Paljetak, Hana Cipcic; Peric, Mihaela; Matijasic, Mario; Verbanac, Donatella; Cetina, Mario; Raic-Malic, Silvana published an article.Safety of 2-(4-Aminophenyl)-6-methylbenzothiazole The title of the article was 1,2,3-Triazole pharmacophore-based benzofused nitrogen/sulfur heterocycles with potential anti-Moraxella catarrhalis activity. And the article contained the following:

Versatile 1,2,3-triazole pharmacophore-based benzofused heterocycles containing halogen-substituted aromatic, 7-substituted coumarin or penciclovir-like subunit were designed and synthesized to evaluate their antibacterial activities against selected Gram-pos. and Gram-neg. bacteria. Hybridization approach using environmentally friendly Cu(I)-catalyzed click reaction under microwave irradiation was adopted in the synthesis of regioselective 1,4-disubstituted 1,2,3-triazole tethered heterocycles, while post-N-alkylation of NH-1,2,3-triazoles afforded both 2,4- and 1,4-disubstituted 1,2,3-triazole regioisomers. Several compounds revealed fluorescence in the violet region of the visible spectrum with a strong influence of Ph spacer in 25-30 on both wavelength and emission intensity. Fusion of selected subunits led to new hybrid architecture, benzothiazole-1,2,3-triazolecoumarin derivative I that demonstrated extremely narrow spectrum activity towards fastidious Gram-neg. bacteria Moraxella catarrhalis. Selected hybrids showed the potency against Moraxella catarrhalis (MIC ≤ 0.25 μg/mL) comparable to that of reference antibiotic azithromycin, which suggested that further investigations are necessary to optimize this potential hit compound as a new anti-Moraxella catarrhalis agent. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Safety of 2-(4-Aminophenyl)-6-methylbenzothiazole

The Article related to moraxella catarrhalis antibacterial triazole heterocycle preparation, 1,2,3-triazole, antibacterial activity, coumarin, fluorescence, hybridization approach, moraxella catarrhalis and other aspects.Safety of 2-(4-Aminophenyl)-6-methylbenzothiazole

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

On October 31, 2020, Goya-Jorge, Elizabeth; Giner, Rosa M.; Sylla-Iyarreta Veitia, Maite; Gozalbes, Rafael; Barigye, Stephen J. published an article.Electric Literature of 92-36-4 The title of the article was Predictive modeling of aryl hydrocarbon receptor (AhR) agonism. And the article contained the following:

The aryl hydrocarbon receptor (AhR) plays a key role in the regulation of gene expression in metabolic machinery and detoxification systems. In the recent years, this receptor has attracted interest as a therapeutic target for immunol., oncogenic and inflammatory conditions. In the present report, in silico and in vitro approaches were combined to study the activation of the AhR. To this end, a large database of chem. compounds with known AhR agonistic activity was employed to build 5 classifiers based on the Adaboost (AdB), Gradient Boosting (GB), Random Forest (RF), Multilayer Perceptron (MLP) and Support Vector Machine (SVM) algorithms, resp. The built classifiers were examined, following a 10-fold external validation procedure, demonstrating adequate robustness and predictivity. These models were integrated into a majority vote based ensemble, subsequently used to screen an inhouse library of compounds from which 40 compounds were selected for prospective in vitro exptl. validation. The general correspondence between the ensemble predictions and the in vitro results suggests that the constructed ensemble may be useful in predicting the AhR agonistic activity, both in a toxicol. and pharmacol. context. A preliminary structure-activity anal. of the evaluated compounds revealed that all structures bearing a benzothiazole moiety induced AhR expression while diverse activity profiles were exhibited by phenolic derivatives The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Electric Literature of 92-36-4

The Article related to aryl hydrocarbon receptor agonism benzothiazole b hesperetin apigenin, agonistic activity, aryl hydrocarbon receptor, benzothiazoles, computational modeling, coumarins, flavonoids, polyphenols, qsar, triterpenes and other aspects.Electric Literature of 92-36-4

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

On February 28, 2014, Song, Jung Min; DiBattista, Amanda Marie; Sung, You Me; Ahn, Joo Myung; Turner, R. Scott; Yang, Jerry; Pak, Daniel T. S.; Lee, Hey-Kyoung; Hoe, Hyang-Sook published an article.HPLC of Formula: 92-36-4 The title of the article was A tetra(ethylene glycol) derivative of benzothiazole aniline ameliorates dendritic spine density and cognitive function in a mouse model of Alzheimer’s disease. And the article contained the following:

We recently reported that the tetra(ethylene glycol) derivative of benzothiazole aniline, BTA-EG4, acts as an amyloid-binding small mol. that promotes dendritic spine d. and cognitive function in wild-type mice. This raised the possibility that BTA-EG4 may benefit the functional decline seen in Alzheimer’s disease (AD). In the present study, we directly tested whether BTA-EG4 improves dendritic spine d. and cognitive function in a well-established mouse model of AD carrying mutations in APP, PS1 and tau (APPswe;PS1M146V;tauP301L, 3xTg AD mice). We found that daily injections of BTA-EG4 for 2 wk improved dendritic spine d. and cognitive function of 3xTg AD mice in an age-dependent manner. Specifically, BTA-EG4 promoted both dendritic spine d. and morphol. alterations in cortical layers II/III and in the hippocampus at 6-10 mo of age compared to vehicle-injected mice. However, at 13-16 mo of age, only cortical spine d. was improved without changes in spine morphol. The changes in dendritic spine d. correlated with Ras activity, such that 6-10 mo old BTA-EG4 injected 3xTg AD mice had increased Ras activity in the cortex and hippocampus, while 13-16 mo old mice only trended toward an increase in Ras activity in the cortex. Finally, BTA-EG4 injected 3xTg AD mice at 6-10 mo of age showed improved learning and memory; however, only minimal improvement was observed at 13-16 mo of age. This behavioral improvement corresponds to a decrease in soluble Aβ 40 levels. Taken together, these findings suggest that BTA-EG4 may be beneficial in ameliorating the synaptic loss seen in early AD. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).HPLC of Formula: 92-36-4

The Article related to tetraethylene glycol derivative bta dendritic spine alzheimers disease neuroprotectant, cognition cortex, 3xtg ad mice, ad, alzheimer’s disease, aβ, bta-eg(4), dendritic spine, ras signaling, amyloid-β and other aspects.HPLC of Formula: 92-36-4

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

On February 29, 2016, Lee, Nathanael J.; Song, Jung Min; Cho, Hyun-Ji; Sung, You Me; Lee, Taehee; Chung, Andrew; Hong, Sung-Ha; Cifelli, Jessica L.; Rubinshtein, Mark; Habib, Lila K.; Capule, Christina C.; Turner, R. Scott; Pak, Daniel T. S.; Yang, Jerry; Hoe, Hyang-Sook published an article.Product Details of 92-36-4 The title of the article was Hexa (ethylene glycol) derivative of benzothiazole aniline promotes dendritic spine formation through the RasGRF1-Ras dependent pathway. And the article contained the following:

The authors’ recent study demonstrated that an amyloid-β binding mol., BTA-EG4, increases dendritic spine number via Ras-mediated signaling. To potentially optimize the potency of the BTA compounds, the authors synthesized and evaluated an amyloid-β binding analog of BTA-EG4 with increased solubility in aqueous solution, BTA-EG6. The authors initially examined the effects of BTA-EG6 on dendritic spine formation and found that BTA-EG6-treated primary hippocampal neurons had significantly increased dendritic spine number compared to control treatment. In addition, BTA-EG6 significantly increased the surface level of AMPA receptors. Upon investigation into the mol. mechanism by which BTA-EG6 promotes dendritic spine formation, the authors found that BTA-EG6 may exert its effects on spinogenesis via RasGRF1-ERK signaling, with potential involvement of other spinogenesis-related proteins such as Cdc42 and CDK5. Taken together, the authors’ data suggest that BTA-EG6 boosts spine and synapse number, which may have a beneficial effect of enhancing neuronal and synaptic function in the normal healthy brain. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Product Details of 92-36-4

The Article related to bta eg6 preparation dendritic spine rasgrf1 erk signaling, hexaethylene glycol benzothiazole aniline derivative preparation dendritic spine, bta-eg6, dendritic spine, rap signaling, ras signaling and other aspects.Product Details of 92-36-4

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

Tomoshige, Shusuke; Nomura, Sayaka; Ohgane, Kenji; Hashimoto, Yuichi; Ishikawa, Minoru published an article in 2017, the title of the article was Discovery of Small Molecules that Induce the Degradation of Huntingtin.Computed Properties of 92-36-4 And the article contains the following content:

Huntington’s disease (HD) is an autosomal dominant neurodegenerative disorder caused by the aggregation of mutant huntingtin (mHtt), and removal of toxic mHtt is expected to be an effective therapeutic approach. The authors designed two small hybrid mols. by linking a ligand for ubiquitin ligase (cellular inhibitor of apoptosis protein 1; cIAP1) with probes for mHtt aggregates, anticipating that these compounds would recruit cIAP1 to mHtt and induce selective degradation by the ubiquitin-proteasome system. The synthesized compounds reduced mHtt levels in HD patient fibroblasts and appear to be promising candidates for the development of a treatment for HD. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Computed Properties of 92-36-4

The Article related to huntington disease treatment huntingtin protein ciap1 hybrid mol preparation, bestatin hybrid preparation ciap1 mhtt interaction inhibitor huntington disease, huntington’s disease, drug design, medicinal chemistry, protein degradation, small-molecule protein degraders and other aspects.Computed Properties of 92-36-4

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

On July 11, 2013, Meltzer-Mats, Ella; Babai-Shani, Gali; Pasternak, Lily; Uritsky, Neta; Getter, Tamar; Viskind, Olga; Eckel, Jurgen; Cerasi, Erol; Senderowitz, Hanoch; Sasson, Shlomo; Gruzman, Arie published an article.Related Products of 92-36-4 The title of the article was Synthesis and Mechanism of Hypoglycemic Activity of Benzothiazole Derivatives. And the article contained the following:

AMP activated protein kinase (AMPK) has emerged as a major potential target for novel antidiabetic drugs. We studied the structure of 2-chloro-5-((Z)-((E)-5-((5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl)methylene)-4-oxothiazolidin-2-ylidene)amino)benzoic acid (PT-1), which attenuates the autoinhibition of the enzyme AMPK, for the design and synthesis of different benzothiazoles with potential antidiabetic activity. We synthesized several structurally related benzothiazole derivatives that increased the rate of glucose uptake in L6 myotubes in an AMPK-dependent manner. One compound, 2-(benzo[d]thiazol-2-ylmethylthio)-6-ethoxybenzo[d]thiazole , augmented the rate of glucose uptake up to 2.5-fold compared with vehicle-treated cells and up to 1.1-fold compared to PT-1. Concomitantly, it elevated the abundance of GLUT4 in the plasma membrane of the myotubes and activated AMPK. S.c. administration of 2-(benzo[d]thiazol-2-ylmethylthio)-6-ethoxybenzo[d]thiazole to hyperglycemic Kuo Kondo rats carrying the Ay-yellow obese gene (KKAy) mice lowered blood glucose levels toward the normoglycemic range. In accord with its activity, compound 2-(benzo[d]thiazol-2-ylmethylthio)-6-ethoxybenzo[d]thiazole showed a high fit value to a pharmacophore model derived from the PT-1. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Related Products of 92-36-4

The Article related to denzothiazole derivative preparation hypoglycemic mechanism ampk antidiabetic target diabetes, plasma glut4 myotube ampk antidiabetic denzothiazole derivative preparation diabetes, mol modeling pharmacophore model food intake denzothiazole derivative preparation and other aspects.Related Products of 92-36-4

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