Tag: 200-300

On June 26, 2014, Parmee, Emma R.; Xu, Jiayi published a patent.Safety of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate The title of the patent was Preparation of novel 2-pyridinecarboxamide derivatives as glucokinase activators useful in treating diseases. And the patent contained the following:

The title compounds I [R1, R2 = (un)substituted 6-10 membered aryl, 5-10 membered heteroaryl, 5-7 membered cycloalkyl, or 5-7 membered aliphatic heterocyclic group; ring A = (un)substituted 5-7 membered monocyclic or 9-10 membered bicyclic heteroaryl group in which the carbon atom attached to the amide nitrogen atom contained in formula I forms C:N together with the nitrogen atom in the ring; L = alkyl, alkoxyalkyl, alkoxy, etc.; T = CO2R, COR3R4, P(O)(OR5)2; R, R3-R5 = H or alkyl] that are effective as glucokinase activating agents, and useful for treating or preventing type 2 diabetes and similar conditions, were prepared E.g., a multi-step synthesis of II, starting from 6-chloro-3-fluoropyridine-2-carboxylic acid, was described. The GK activation capability of the exemplified compounds I was determined (data given). Pharmaceutical compositions and methods of treatment were also included. The experimental process involved the reaction of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate(cas: 859522-19-3).Safety of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate

The Article related to pyridinecarboxamide preparation glucokinase activator antidiabetic antiobesity, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Safety of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate

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

On November 26, 2015, Lin, Songnian; Parmee, Emma R.; Xu, Jiayi published a patent.Application In Synthesis of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate The title of the patent was Novel 2-pyridinecarboxamide derivatives, compositions containing such compounds, and methods of treatment. And the patent contained the following:

Novel pyridine-2-carboxamide derivatives of formula I and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are effective as glucokinase activating agents. Pharmaceutical compositions and methods of treatment are also included. The present invention relates to novel pyridine-2-carboxamide derivatives and salts thereof which are effective as glucokinase activating agents. Moreover, it relates to compositions containing such compounds, and methods of treatment. The experimental process involved the reaction of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate(cas: 859522-19-3).Application In Synthesis of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate

The Article related to pyridinecarboxamide preparation glucokinase activator antidiabetic antiobesity, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Application In Synthesis of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate

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

On August 1, 2020, Goya-Jorge, Elizabeth; Abdmouleh, Fatma; Carpio, Laureano E.; Giner, Rosa M.; Sylla-Iyarreta Veitia, Maite published an article.Computed Properties of 92-36-4 The title of the article was Discovery of 2-aryl and 2-pyridinylbenzothiazoles endowed with antimicrobial and aryl hydrocarbon receptor agonistic activities. And the article contained the following:

Benzothiazole is a privileged scaffold in medicinal chem. present in diverse bioactive compounds with multiple pharmacol. applications such as analgesic, anticonvulsant, antidiabetic, anti-inflammatory, anticancer and radioactive amyloidal imagining agents. We reported in this work the study of sixteen functionalized 2-aryl and 2-pyridinylbenzothiazoles as antimicrobial agents and as aryl hydrocarbon receptor (AhR) modulators. The antimicrobial activity against Gram-pos. (S. aureus and M. luteus) and Gram-neg. (P. aeruginosa, S. enterica and E. coli) pathogens yielded MIC ranging from 3.13 to 50μg/mL and against the yeast C. albicans, the benzothiazoles displayed MIC from 12.5 to 100μg/mL. All compounds showed promising antibiofilm activity against S. aureus and P. aeruginosa. The arylbenzothiazole 12 displayed the greatest biofilm eradication in S. aureus (74%) subsequently verified by fluorescence microscopy. The ability of benzothiazoles to modulate AhR expression was evaluated in a cell-based reporter gene assay. Six benzothiazoles (7, 8-10, 12, 13) induced a significant AhR-mediated transcription and interestingly compound 12 was also the strongest AhR-agonist identified. Structure-activity relationships are suggested herein for the AhR-agonism and antibiofilm activities. Furthermore, in silico predictions revealed a good ADMET profile and druglikeness for the arylbenzothiazole 12 as well as binding similarities to AhR compared with the endogenous agonist FICZ. 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 aryl pyridinylbenzothiazole hydrocarbon receptor antimicrobial agonistic activity, agonism, ah receptor, antibacterial, antibiofilm, antifungal, benzothiazole, Pharmacology: Effects Of Antimicrobials and Parasiticides and other aspects.Computed Properties of 92-36-4

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

On February 24, 2015, Sheik, Daniel A.; Brooks, Lauren; Frantzen, Kristen; Dewhurst, Stephen; Yang, Jerry published an article.Quality Control of 2-(4-Aminophenyl)-6-methylbenzothiazole The title of the article was Inhibition of the Enhancement of Infection of Human Immunodeficiency Virus by Semen-Derived Enhancer of Virus Infection Using Amyloid-Targeting Polymeric Nanoparticles. And the article contained the following:

The semen-derived enhancer of virus infection (SEVI) is a natural amyloid material that has been shown to substantially increase viral attachment and infectivity of HIV in cells. The authors previously reported that synthetic monomeric and oligomeric amyloid-targeting mols. could form protein-resistive coatings on SEVI and inhibit SEVI- and semen-mediated enhancement of HIV infectivity. While oligomeric amyloid-binding compounds showed substantial improvement in apparent binding to SEVI compared to monomeric compounds, the authors observed only a modest correlation between apparent binding to SEVI and activity for reducing SEVI-mediated HIV infection. Here, the authors synthesized amyloid-binding polyacrylate-based polymers and polymeric nanoparticles of comparable size to HIV virus particles (∼150 nm) to assess the effect of sterics on the inhibition of SEVI-mediated enhancement of HIV infectivity. The authors show that these polymeric materials exhibit excellent capability to reduce SEVI-mediated enhancement of HIV infection, with the nanoparticles exhibiting the greatest activity (IC50 value of ∼4 μg/mL, or 59 nM based on polymer) of any SEVI-neutralizing agent reported to date. The results support that the improved activity of these nanomaterials is likely due to their increased size (diameters = 80-200 nm) compared to amyloid-targeting small mols. and that steric interactions may play as important a role as binding affinity in inhibiting viral infection mediated by SEVI amyloids. In contrast to the previously reported SEVI-neutralizing, amyloid-targeting mols. (which required concentrations at least 100-fold above the Kd to observe activity), the approx. 1:1 ratio of apparent Kd to IC50 for activity of these polymeric materials suggests the majority of polymer mols. that are bound to SEVI contribute to the inhibition of HIV infectivity enhanced by SEVI. Such size-related effects on phys. inhibition of protein-protein interactions may open further opportunities for the use of targeted nanomaterials in disease intervention. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Quality Control of 2-(4-Aminophenyl)-6-methylbenzothiazole

The Article related to hiv infection sevi amyloid targeting polyacrylate nanoparticle preparation antiaids, hiv, sevi, acrylate, nanoparticles, polymer, steric inhibition, Pharmacology: Effects Of Antimicrobials and Parasiticides and other aspects.Quality Control of 2-(4-Aminophenyl)-6-methylbenzothiazole

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

Ukrainets, I. V.; Bereznyakova, N. L.; Kolesnik, O. V.; Turov, O. V. published an article in 2007, the title of the article was Synthesis, spectral characteristics and biological properties of 1-furfuryl-4-hydroxy-2-oxo-1,2,5,6,7,8-hexahydroquinoline-3-carboxylic acid anilides and heterylamides.Name: 2-(4-Aminophenyl)-6-methylbenzothiazole And the article contains the following content:

With the purpose of determination of regularities of their structure-antituberculosis activity relationship, the synthesis of 1-furfuryl-4-hydroxy-2-oxo-1,2,5,6,7,8-hexahydroquinoline-3-carboxylic acids N-R-amides has been carried out. The peculiarities of the NMR spectra of the compounds synthesized and the results of studying of their antimycobacterial activity are discussed. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Name: 2-(4-Aminophenyl)-6-methylbenzothiazole

The Article related to structure tuberculostatic furfuryl hexahydroquinoline carboxylate preparation, Pharmacology: Effects Of Antimicrobials and Parasiticides and other aspects.Name: 2-(4-Aminophenyl)-6-methylbenzothiazole

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

Yang, S.; Liu, Q.-X.; Zeng, W.-J.; Zou, Y.; Wang, Z.-G.; Zhu, H.-L. published an article in 2004, the title of the article was Crystal structure of bis[N-(2-(2-hydroxyethylamino)ethyl)salicylideneimine]cadmium(II) dihydrate, Cd(C11H17N2O2)2·2H2O.Recommanded Product: 92-36-4 And the article contains the following content:

The title compound is monoclinic, space group P21/n, a 9.236(4), b 21.102(9), c 12.987(6) Å, β 97.638(6)°, Z = 4, Rgt(F) = 0.039, wRref(F2) = 0.117, T = 298 K. At. coordinates are given. The title compound is an electronically neutral cadmium(II) complex with two lattice water mols. The central cadmium atom is six-coordinated by four nitrogen atoms and two oxygen atoms from two Schiff base ligands. The three diagonal angles of the cadmium octahedron are 167.O(1)°, 152.4(1)°, and 154.5(1)°, resp., indicating a strongly distorted octahedral coordination of the cadmium atom. The two aromatic rings in each complex are nearly perpendicular to each other with a dihedral angle of 98.2(2)°. N(4), O(2), O(4) and O(5) atoms contribute to the formation of hydrogen bonds. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Recommanded Product: 92-36-4

The Article related to crystal structure cadmium hydroxyethylaminoethylsalicylideneimine hydrate, mol structure cadmium hydroxyethylaminoethylsalicylideneimine hydrate, Crystallography and Liquid Crystals: Crystal Structure and other aspects.Recommanded Product: 92-36-4

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

On June 30, 2003, Mosier, Philip D.; Jurs, Peter C.; Custer, Laura L.; Durham, Stephen K.; Pearl, Greg M. published an article.SDS of cas: 92-36-4 The title of the article was Predicting the Genotoxicity of Thiophene Derivatives from Molecular Structure. And the article contained the following:

We report several binary classification models that directly link the genetic toxicity of a series of 140 thiophene derivatives with information derived from the compounds’ mol. structure. Genetic toxicity was measured using an SOS Chromotest. IMAX (maximal SOS induction factor) values were recorded for each of the 140 compounds both in the presence and in the absence of S9 rat liver homogenate. Compounds were classified as genotoxic if IMAX ≥ 1.5 in either test or nongenotoxic if IMAX < 1.5 for both tests. The mol. structures were represented by numerical descriptors that encoded the topol., geometric, electronic, and polar surface area properties of the thiophene derivatives The classification models used were linear discriminant anal. (LDA), k-nearest neighbor classification (k-NN), and the probabilistic neural network (PNN). These were used in conjunction with either a genetic algorithm or a generalized simulated annealing to find optimal subsets of descriptors for each classifier. The quality of the resulting models was determined by the number of misclassified compounds, with preference given to models that produced fewer false neg. classifications. Model sizes ranged from seven descriptors for LDA to three descriptors for k-NN and PNN. Very good classification results were obtained with all three classifiers. Classification rates for the LDA, k-NN, and PNN models were 80, 85, and 85%, resp., for the prediction set compounds Addnl., a consensus model was generated that incorporated all three of the basic model types. This consensus model correctly predicted the genotoxicity of 95% of the prediction set compounds The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).SDS of cas: 92-36-4

The Article related to genotoxicity thiophene derivative structure activity relationship, Toxicology: Chemicals (Household, Industrial, General) and other aspects.SDS of cas: 92-36-4

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

Li, Yang; Du, Zhi; Liu, Xinping; Ma, Mengmeng; Yu, Dongqin; Lu, Yao; Ren, Jinsong; Qu, Xiaogang published an article in 2019, the title of the article was Near-Infrared Activated Black Phosphorus as a Nontoxic Photo-Oxidant for Alzheimer’s Amyloid-β Peptide.Name: 2-(4-Aminophenyl)-6-methylbenzothiazole And the article contains the following content:

The inhibition of amyloid-β (Aβ) aggregation by photo-oxygenation has become an effective way of treating Alzheimer’s disease (AD). New near-IR (NIR) activated treatment agents, which not only possess high photo-oxygenation efficiency, but also show low biotoxicity, are urgently needed. Herein, for the first time, it is demonstrated that NIR activated black phosphorus (BP) could serve as an effective nontoxic photo-oxidant for amyloid-β peptide in vitro and in vivo. The nanoplatform BP@BTA (BTA: one of thioflavin-T derivatives) possesses high affinity to the Aβ peptide due to specific amyloid selectivity of BTA. Importantly, under NIR light, BP@BTA can significantly generate a high quantum yield of singlet oxygen (1O2) to oxygenate Aβ, thereby resulting in inhibiting the aggregation and attenuating Aβ-induced cytotoxicity. In addition, BP could finally degrade into nontoxic phosphate, which guarantees the biosafety. Using transgenic Caenorhabditis elegans CL2006 as AD model, the results demonstrate that the 1O2-generation system could dramatically promote life-span extension of CL2006 strain by decreasing the neurotoxicity of Aβ. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Name: 2-(4-Aminophenyl)-6-methylbenzothiazole

The Article related to nearir black phosphorus photooxidant alzheimer’s amyloid, alzheimer’s disease, amyloid-β, black phosphorus, nontoxic photo-oxidants, photo-oxygenation, singlet oxygen, Radiation Biochemistry: Disease Diagnosis and Therapy and other aspects.Name: 2-(4-Aminophenyl)-6-methylbenzothiazole

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

On July 20, 2007, Kim, Mi Kyoung; Choo, Il Han; Lee, Hyo Sun; Woo, Jong Inn; Chong, Youhoon published an article.Safety of 2-(4-Aminophenyl)-6-methylbenzothiazole The title of the article was 3D-QSAR of PET agents for imaging β-amyloid in Alzheimer’s disease. And the article contained the following:

The accumulation of excess senile plaques (β-amyloid, Aβ-plaques) in the brain is strongly associated with the pathogenesis of Alzheimer’s disease (AD). While there are no definitive treatments available to affect a cure of AD, much recent interest has been given to the development of antiamyloid therapies aimed at halting and reversing Aβ-deposition and, thus, monitoring of the therapeutic efficacy would greatly benefit from methods for the in vivo detection and quantification of Aβ-deposits in the brain. A 3D-QSAR model was constructed with several PET ligands such as Thioflavin-T analogs and stilbene derivatives using CoMFA (Comparative Mol. Field Anal.) and CoMSIA (Comparative Mol. Similarity Indexes Anal.). The 3D-QSAR model could be applied to predict binding affinity of the structurally related compounds against Aβ-plaques. 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 beta amyloid pet imaging agent qsar model, thioflavin stilbene derivative amyloid plaque imaging qsar, Radiation Biochemistry: Disease Diagnosis and Therapy and other aspects.Safety of 2-(4-Aminophenyl)-6-methylbenzothiazole

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

On June 15, 2004, Chen, Yen Ting; Seto, Christopher T. published an article.Electric Literature of 92-36-4 The title of the article was Parallel synthesis of a library of bidentate protein tyrosine phosphatase inhibitors based on the α-ketoacid motif. And the article contained the following:

Protein tyrosine phosphatases (PTPases) regulate intracellular signal transduction pathways by controlling the level of tyrosine phosphorylation in cells. These enzymes play an important role in a variety of diseases including type II diabetes and infection by the bacterium Yersinia pestis, which is the causative agent of bubonic plague. This report describes the synthesis, using parallel solution-phase methods, of a library of 104 potential inhibitors of PTPases. The library members are based on the bis(aryl α-ketocarboxylic acid) motif that incorporates a carboxylic acid on the central benzene linker. This carboxylic acid was coupled with a variety of different aromatic amines through an amide linkage. The aromatic component of the resulting amides is designed to make contacts with residues that surround the active site of the PTPase. The library was screened against the Yersinia PTPase and PTP1B. Based upon the screening results, four members of the library were selected for further study. These four compounds were evaluated against the Yersinia PTPase, PTP1B, TCPTP, CD45, and LAR. Compound 14 has an IC50 value of 590 nM against PTP1B and is a reversible competitive inhibitor. This affinity represents a greater than 120-fold increase in potency over compound 2, the parent structure upon which the library was based. A second inhibitor, compound 12, has an IC50 value of 240 nM against the Yersinia PTPase. In general, the selectivity of the inhibitors for PTP1B was good compared to LAR, but modest when compared to TCPTP and CD45. 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 combinatorial library protein tyrosine phosphatase inhibitor alpha ketoacid, Enzymes: Substrates-Cofactors-Inhibitors-Activators-Coenzymes-Products and other aspects.Electric Literature of 92-36-4

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