Category: 566169-93-5

In an article, published in an article, once mentioned the application of 566169-93-5, Name is 2-(4-(Methylamino)phenyl)benzo[d]thiazol-6-ol,molecular formula is C14H12N2OS, is a conventional compound. this article was the specific content is as follows.Application In Synthesis of 2-(4-(Methylamino)phenyl)benzo[d]thiazol-6-ol

The Amyloid beta protein binding specificity to [be] high, high permeability of the blood-brain barrier, brain senile plaques in storage properties, whereas, in the remaining portion except the old brain plaques characteristic hardly boron carrier compound. [Solving means] a flavone derivatives, chromone derivatives, coumarin derivatives, orlon derivatives, chalcone derivative, benzothiazole derivative in the stilbene derivative, beta-Amyloid-associated disease or pathological -10 boron atom in each derivative compounds for boron neutron capture therapy applications to Amyloid protein. [Drawing] no (by machine translation)

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Thiazole | C3H447NS – PubChem,
Thiazole | chemical compound | Britannica

Electric Literature of 566169-93-5. Let’s face it, organic chemistry can seem difficult to learn. Especially from a beginner’s point of view. Like 566169-93-5, Name is 2-(4-(Methylamino)phenyl)benzo[d]thiazol-6-ol. In a document type is Article, introducing its new discovery.

Novel dibenzothiazole derivatives were synthesized and evaluated as amyloid-imaging agents. In vitro quantitative binding studies using AD brain tissue homogenates showed that the dibenzothiazole derivatives displayed high binding affinities with Ki values in the nanomolar range (6.8-36 nM). These derivatives are relatively lipophilic with partition coefficients (logP oct) in the range of 1.25-3.05. Preliminary structure-activity relationship studies indicated dibenzothiazole derivatives bearing electron-donating groups exhibited higher binding affinities than those bearing electron-withdrawing groups. A lead compound was selected for its high binding affinity and radiolabeled with [125I] through direct radioiodination using sodium [125I] iodide in the presence of Chloramine T. The radioligand (4-[2,6?]dibenzothiazolyl-2?-yl-2-[125I]-phenylamine) displayed moderate lipophilicity (logP oct, 2.70), very good brain uptake (3.71 ± 0.63% ID/g at 2 min after iv injection in mice), and rapid washout from normal brains (0.78% and 0.43% ID/g at 30 and 60 min, respectively). These studies indicated that lipophilic dibenzothiazole derivatives represent a promising pharmacophore for the development of novel amyloid-imaging agents for potential application in Alzheimer’s disease and related neurodegenerative disorders.

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Thiazole | C3H454NS – PubChem,
Thiazole | chemical compound | Britannica

566169-93-5, Name is 2-(4-(Methylamino)phenyl)benzo[d]thiazol-6-ol, molecular formula is C14H12N2OS, belongs to thiazole compound, is a common compound. In a patnet, once mentioned the new application about 566169-93-5, Safety of 2-(4-(Methylamino)phenyl)benzo[d]thiazol-6-ol

Synthesis and monkey-PET study of (R)- and (S)-18F-labeled 2-arylbenzoheterocyclic derivatives as amyloid probes with distinctive in vivo kinetics

This study describes an effective strategy to improve pharmacokinetics of Abeta imaging agents, offering a novel class of (R)- and (S)-18F-labeled 2-arylbenzoheterocyclic derivatives which bear an additional chiral hydroxyl group on the side chain. These ligands displayed binding abilities toward Abeta aggregates with Ki values ranging from 3.2 to 195.6 nM. Chirality-related discrepancy was observed in biodistribution, and (S)-2-phenylbenzoxazole enantiomers exhibited vastly improved brain clearance with washout ratios higher than 20. Notably, (S)-[18F]28 possessed high binding potency (Ki = 7.6 nM) and exceptional brain kinetics (9.46% ID/g at 2 min, brain2min/brain60min = 27.8) that is superior to well-established [18F]AV45. The excellent pharmacokinetics and low nonspecific binding of (S)-[18F]28 were testified by dynamic PET/CT scans in monkey brains. In addition, (S)-[18F]28 clearly labeled Abeta plaques both in vitro and ex vivo. These results might qualify (S)-[18F]28 to detect Abeta plaques with high signal-to-noise ratio.

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Reference：
Thiazole | C3H427NS – PubChem,
Thiazole | chemical compound | Britannica

In an article, published in an article, once mentioned the application of 566169-93-5, Name is 2-(4-(Methylamino)phenyl)benzo[d]thiazol-6-ol,molecular formula is C14H12N2OS, is a conventional compound. this article was the specific content is as follows.category: thiazole

2-Phenylbenzothiazole conjugated with cyclopentadienyl tricarbonyl [CpM(CO)3] (M = Re, 99mTc) complexes as potential imaging probes for beta-amyloid plaques

Technetium-99m-labeled cyclopentadienyl tricarbonyl complexes conjugated with the 2-phenylbenzothiazole binding motif were synthesized. The rhenium surrogates 20, 21, 22 and 23 were demonstrated to have moderate to high affinities for Abeta1-42 aggregates with Ki values of 142, 76, 64 and 24 nM, respectively. During the fluorescence staining of brain sections of transgenic mice and patients with Alzheimer’s disease, these rhenium complexes demonstrated perfect and intense labeling of Abeta plaques. Moreover, in in vitro autoradiography, 99mTc-labeled complexes clearly detected beta-amyloid plaques on sections of brain tissue from transgenic mice, which confirmed the sufficient affinity of these tracers for Abeta plaques. However, these compounds did not show desirable properties in vivo, especially showing poor brain uptake (below 0.5% ID g-1), which will hinder the further development of these tracers as brain imaging agents. Nonetheless, it is encouraging that these 99mTc-labeled complexes designed by a conjugate approach displayed sufficient affinities for Abeta plaques. This journal is

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Thiazole | C3H448NS – PubChem,
Thiazole | chemical compound | Britannica

Related Products of 566169-93-5, Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 566169-93-5, Name is 2-(4-(Methylamino)phenyl)benzo[d]thiazol-6-ol, molecular formula is C14H12N2OS. In a Article，once mentioned of 566169-93-5

Bis(arylvinyl)pyrazines, -pyrimidines, and -pyridazines As imaging agents for tau fibrils and beta-Amyloid plaques in alzheimers disease models

The in vivo diagnosis of Alzheimers disease (AD) is of high socioeconomic interest and remains a demanding field of research. The biopathological hallmarks of the disease are extracellular plaques consisting of aggregated beta-amyloid peptides (Abeta) and tau protein derived intracellular tangles. Here we report the synthesis and evaluation of fluorescent pyrazine, pyrimidine,and pyridazine derivatives in vitro and in vivo aiming at a tau-based diagnosis of AD. The probes were pre-evaluated on human brain tissue by fluorescence microscopy and were found to label all known disease-related alterations at high contrast and specificity. To quantify the binding affinity, a new thiazine red displacement assay was developed and selected candidates were toxicologically profiled. The application in transgenic mouse models demonstrated bioavailability and brain permeability for one compound. In the course of histological testing, we discovered an AD-related deposition of tau aggregates in the Bowmans glands of the olfactory epithelium, which holds potential for an endoscopic diagnosis of AD in the olfactory system.

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Thiazole | C3H444NS – PubChem,
Thiazole | chemical compound | Britannica

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Maillard reaction of 18F-FDG with biological amines results in the formation of 18F-fluorodeoxyglycosylamines (18F-FDGly) as pseudo-Amadori products. To increase in vivo stability, we report the reductive amination of FDGly to provide reduced fluorodeoxyglucamines (FDGlu). 18F-Fluorodeoxyglucamines (18F-FDGlu), resulting from linking 18F-FDG (hydrophilic) to lipophilic molecules containing amine group may be useful as positron emission tomography (PET) imaging agents. Two amine derivatives, 7-chloro-8-hydroxy-3-methyl-l-(3?-aminophenyl)-2,3,4,5-tetrahydro-lH-3-benzazepine (SCH 38548 for dopamine D1 receptors) and BTA-0 (for Abeta amyloid) were reacted with FDG under reductive amination conditions to yield stable products, FDGluSCH and FDGluBTA. FDGluSCH had high binding affinity to rat brain dopamine D1 receptors with a Ki of 19.5 nM while FDGluBTA had micromolar affinity for human frontal cortex Abeta plaques. 18F-FDGluSCH was prepared in low to modest radiochemical yields and preliminary results showed binding to the rat striatum in brain slices. In vivo stability of 18F-FDGluSCH needs to be determined. Our results suggest that 18F-FDG is a useful ‘radioactive synthon’ for PET radiotracer development. Its usefulness will have to be determined on the basis of the structure-activity relationship of the target molecule.

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Thiazole | C3H458NS – PubChem,
Thiazole | chemical compound | Britannica

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Amyloid nitroxyl radical (nitroxide) ligands were used to detect amyloid-beta fibrils, the main constituents of senile plaques in Alzheimer’s disease, using anisotropic ESR spectra, and were found to affect the aggregation process due to the radical functionality. These compounds have great potential as novel and multifunctional probes, combining spin labels, spin probes, and fluorescence probes.

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Thiazole | C3H480NS – 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. 566169-93-5, Name is 2-(4-(Methylamino)phenyl)benzo[d]thiazol-6-ol, molecular formula is C14H12N2OS. In a Review£¬once mentioned of 566169-93-5, Quality Control of: 2-(4-(Methylamino)phenyl)benzo[d]thiazol-6-ol

Alzheimer’s disease (AD), the most common form of dementia, is a progressive and fatal neurodegenerative disorder. The neuropathological hallmarks of AD generally revealed on postmortem brain tissue are the extracellular neuritic plaque deposits and intracellular neurofibrillary tangles. Significant evidence supports the pivotal role of beta-amyloid peptides in the pathogenesis of AD. Therefore, The ability to image beta-amyloid plaques in brain with noninvasive techniques such as positron emission tomography (PET) or single-photon emission computed tomography (SPECT) may not only aid in presymptomatic identification of AD patients and differential diagnosis of patients with dementia, but also monitoring the effectiveness of anti-amyloid therapeutic strategies. For these reasons, development of beta-amyloid plaquespecific imaging agents has been extensively pursued and reported. This review summarizes the current status of 18F-labeled radioligand development for PET imaging of beta-amyloid plaques. [18F]FDDNP is the first PET radioligand that demonstrated differential uptake and retention in the brain of AD patients, while a low signal-to-noise ratio in PET studies was indicated. At this time, [18F]3′-F-PIB (flutemetamol), [18F]AV-1 (florbetaben), [18F]AZD4694, and [18F]MK-3328 are undergoing phase II and III clinical trial. [18F]AV-45 (florbetapir) has recently been approved by FDA for use in patients being evaluated for Alzheimer’s disease and other causes of cognitive decline. Several other 18F-labeled radioligands based upon imidazo[1,2-a]pyridine, benzothiazole, stilbene, benzofuran, and benzoxazole core structures have also been synthesized and evaluated.

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Thiazole | C3H481NS – PubChem,
Thiazole | chemical compound | Britannica

Synthetic Route of 566169-93-5, Chemistry can be defined as the study of matter and the changes it undergoes. You¡¯ll sometimes hear it called the central science because it is the connection between physics and all the other sciences, starting with biology.566169-93-5, Name is 2-(4-(Methylamino)phenyl)benzo[d]thiazol-6-ol, molecular formula is C14H12N2OS. In a patent, introducing its new discovery.

Objective: Amyloid-beta plaques and neurofibrillary tangles composed of tau protein are the neuropathological hallmarks of Alzheimer?s disease. In recent years, marked progress has been made in Alzheimer?s disease research using tau ligands for positron emission tomography (PET). However, the issue of off-target binding, that is, the binding of ligands to regions without tau pathology, remains unresolved. Tissues with melanin-containing cells (MCCs) have been suggested as binding targets for tau ligands. In the present study, we characterized the MCC-binding properties of representative tau PET ligands. Methods: Autoradiographic studies of [18F]AV-1451 and [18F]THK5351 were conducted using postmortem human midbrain sections. Saturation-binding assays of [18F]AV-1451 and [18F]THK5351 were performed with B16F10 melanoma cells. The blocking effects of 25 compounds against [18F]THK5351 binding to B16F10 cells were used to investigate the relationship between chemical structure and MCC binding. Results: Autoradiography demonstrated specific binding of the radioligands in the substantia nigra. [18F]AV-1451 and [18F]THK5351 exhibited saturable binding to melanoma cells ([18F]AV-1451: Kd = 669 ¡À 196?nM, Bmax = 622 ¡À 269?pmol/mg protein; [18F]THK5351: Kd = 441 ¡À 126?nM, Bmax = 559 ¡À 75.5?pmol/mg protein). In blocking studies with melanoma cells, compounds bearing multiple aromatic rings and an aminopyridine group, including tau ligands such as AV-1451, PBB3, and a lead compound of MK-6240, exhibited the inhibition of [18F]THK5351 binding comparable to self-blocking by THK5351 (> 70% at 10?muM). Conclusions: These studies suggest that the binding properties of [18F]AV-1451 and [18F]THK5351 are sufficient to expect highlighting of tissues with a high density of MCCs. The findings of the present study should aid the development of neuroimaging ligands that do not bind to MCC.

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Thiazole | C3H453NS – 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.566169-93-5, Name is 2-(4-(Methylamino)phenyl)benzo[d]thiazol-6-ol, molecular formula is C14H12N2OS. In a Review£¬once mentioned of 566169-93-5, Product Details of 566169-93-5

Two of the main pathological hallmarks of Alzheimer’s disease (AD) are neuritic plaques and neurofibrillary tangles. Significant evidence supports a critical and probable causative role of beta amyloid (Abeta) plaque formation. Since neuroprotective treatments are typically most effective at early stages of injury, the detection and measurement of Abeta load in living brain should be performed at early and perhaps even presymptomatic stages of AD. Two primary targets of molecular imaging research with positron emission tomography (PET) are to develop surrogate markers (radioligands) for assessing disease progression and for monitoring the efficacy of developmental therapeutics. Here, we review the current status of radioligand development for PET imaging of Abeta aggregates. General structure-activity relationships have emerged, including the identification of at least three different ligand binding sites in various Abeta aggregates and recognition of the general structural requirements for ligand binding at each site. Also a few radioligands applicable to imaging Abeta plaques in living human brain with positron emission tomography (PET) have emerged, including [11C]PIB, [11C]SB-13 and [18F]FDDNP.

Two of the main pathological hallmarks of Alzheimer’s disease (AD) are neuritic plaques and neurofibrillary tangles. Significant evidence supports a critical and probable causative role of beta amyloid (Abeta) plaque formation. Since neuroprotective treatments are typically most effective at early stages of injury, the detection and measurement of Abeta load in living brain should be performed at early and perhaps even presymptomatic stages of AD. Two primary targets of molecular imaging research with positron emission tomography (PET) are to develop surrogate markers (radioligands) for assessing disease progression and for monitoring the efficacy of developmental therapeutics. Here, we review the current status of radioligand development for PET imaging of Abeta aggregates. General structure-activity relationships have emerged, including the identification of at least three different ligand binding sites in various Abeta aggregates and recognition of the general structural requirements for ligand binding at each site. Also a few radioligands applicable to imaging Abeta plaques in living human brain with positron emission tomography (PET) have emerged, including [11C]PIB, [11C]SB-13 and [18F]FDDNP.

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Thiazole | C3H419NS – PubChem,
Thiazole | chemical compound | Britannica