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Introduction Curcumin is a neuroprotective compound that inhibits the formation of amyloid oligomers and fibrils and binds to beta-amyloid plaques in Alzheimer’s disease (AD). We aimed to synthesize an 18F-labeled curcumin derivate ([18F]4) and to characterize its positron emission tomography (PET) tracer-binding properties to beta-amyloid plaques in a transgenic APP23 mouse model of AD. Methods We utilized facile one-pot synthesis of [18F]4 using nucleophilic 18F-fluorination and click chemistry. Binding of [18F]4 to beta-amyloid plaques in the transgenic APP23 mouse brain cryosections was studied in vitro using heterologous competitive binding against PIB. [18F]4 uptake was studied ex vivo in rodents and in vivo using PET/computed tomography of transgenic APP23 and wild-type control mice. Results The radiochemical yield of [18F]4 was 21 ± 11%, the specific activity exceeded 1 TBq/mumol, and the radiochemical purity exceeded 99.3% at the end of synthesis. In vitro studies of [18F]4 with the transgenic APP23 mouse revealed high beta-amyloid plaque binding. In vivo and ex vivo studies demonstrated that [18F]4 has fast clearance from the blood, moderate metabolism but low blood-brain barrier (BBB) penetration. Conclusions [ 18F]4 was synthesized in high yield and excellent quality. In vitro studies, metabolite profile, and fast clearance from the blood indicated a promising tracer for Abeta imaging. However, [18F]4 has low in vivo BBB penetration and thus further studies are needed to reveal the reason for this and to possibly overcome this issue.

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Reference:
Thiazole | C3H461NS – PubChem,
Thiazole | chemical compound | Britannica

Sep 2021 News New explortion of 2-(4-(Methylamino)phenyl)benzo[d]thiazol-6-ol

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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 Article,once mentioned of 566169-93-5, Recommanded Product: 566169-93-5

Alzheimer’s disease (AD) is a complex brain disorder that still remains ill defined. In order to understand the significance of binding of different clinical in vivo imaging ligands to the polymorphic pathological features of AD brain, the molecular characteristics of the ligand interacting with its specific binding site need to be defined. Herein, we observed that tritiated Pittsburgh Compound B (3H-PIB) can be displaced from synthetic Abeta(1-40) and Abeta(1-42) fibrils and from the PIB binding complex purified from human AD brain (ADPBC) by molecules containing a chalcone structural scaffold. We evaluated how substitution on the chalcone scaffold alters its ability to displace 3H-PIB from the synthetic fibrils and ADPBC. By comparing unsubstituted core chalcone scaffolds along with the effects of bromine and methyl substitution at various positions, we found that attaching a hydroxyl group on the ring adjacent to the carbonyl group (ring I) of the parent member of the chalcone family generally improved the binding affinity of chalcones toward ADPBC and synthetic fibrils F40 and F42. Furthermore, any substitution on ring I at the ortho-position of the carbonyl group greatly decreases the binding affinity of the chalcones, potentially as a result of steric hindrance. Together with the finding that neither our chalcones nor PIB interact with the Congo Red/X-34 binding site, these molecules provide new tools to selectively probe the PIB binding site that is found in human AD brain, but not in brains of AD pathology animal models. Our chalcone derivatives also provide important information on the effects of fibril polymorphism on ligand binding.

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Thiazole | C3H483NS – PubChem,
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09/9/2021 News Simple exploration of 2-(4-(Methylamino)phenyl)benzo[d]thiazol-6-ol

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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 Patent,once mentioned of 566169-93-5, Application In Synthesis of 2-(4-(Methylamino)phenyl)benzo[d]thiazol-6-ol

A method of identifying a patient as prodromal to a disease associated with amyloid deposition by imaging techniques is provided. In addition, a method of identifying amyloid deposition diseases in patients who present with a dementing disorder of questionable etiology by imaging techniques is provided. The methods discloses substances which are used for imaging and generating data which can be used to determine progress of an asymptomatic patient to a disease associated with amyloid deposition. or to identify amyloid deposition diseases in patients who present with a dementing disorder of questionable etiology.

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Thiazole | C3H491NS – PubChem,
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Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Formula: C14H12N2OS. In my other articles, you can also check out more blogs about 566169-93-5

Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments.Introducing a new discovery about 566169-93-5, Name is 2-(4-(Methylamino)phenyl)benzo[d]thiazol-6-ol, Formula: C14H12N2OS.

This work focuses on the development of specific substrates for estrogen sulfotransferase (SULT1E1) to produce molecular imaging probes for this enzyme. SULT1E1 is a key enzyme in estrogen homeostasis, playing a central role in the prevention and development of human disease. In vitro sulfation assays showed alkyl and aryl substitutions to a fused heterocyclic system modeled after beta-naphthol (betaN), based on compounds that interact with the estrogen receptor, rendered several molecules with enhanced specificity for SULT1E1 over SULT1A1*1, SULT1A1*2, SULT1A3, and SULT2A1. Several 6-hydroxy-2-arylbenzothiazoles tested demonstrated excellent affinity – V max/Km ratios – and specificity for SULT1E1. Km values ranged from 0.12-2.36 muM. A strong correlation was observed between polarity of the 4?-sustituent on the 2-aryl moiety (Hammett sigmap) and the log(Vmax/Km) (r = 0.964). Substrate sensitivity is influenced by the acidity of the 6-phenolic group demonstrated by correlating its 1H NMR chemical shift (deltaOH) with the log(V max/Km) (r = 0.963). Acidity is mediated by the electron withdrawing capacity of the 4?-substituent outlined by the correlation of the C-2 13C NMR chemical shift (deltaC2) with the log(Vmax/Km) (r = 0.987). 2-[4-(Methylamino)phenyl]-6- hydroxybenzothiazole (2b) was radiolabeled with carbon-11 (11C-(2b)) and used in vivo for microPET scanning and tissue metabolite identification. High PET signal was paralleled with the presence of radiolabeled 11C-(2b)-6-O-sulfate and the SULT1E1 protein detected by western blot. Because this and other members of this family presenting specificity for SULT1E1 can be labeled with carbon-11 or fluorine-18, in vivo assays of SULT1E1 functional activity are now feasible in humans.

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Thiazole | C3H424NS – PubChem,
Thiazole | chemical compound | Britannica

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The present invention is directed to a method of using radiolabeled ethylene glycol (n = 1) (EG) or polyethylene glycol (n = from 2 to 10) (PEG) as a labeling group moiety on compounds that can be useful for imaging tissues. Specifically, the EG or PEG moiety preferably contains a radiofluorine (18F), and is covalently bonded to a ligand (L). The L portion of the molecule can be any molecule appropriate for covalently bonding with the radiolabeled EG or PEG moiety and subsequent use as an imaging agent. In particular, the imaging agent is preferably an agent suitable for administering to a mammal and detecting by PET or SPECT imaging.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data.Safety of 2-(4-(Methylamino)phenyl)benzo[d]thiazol-6-ol, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 566169-93-5, in my other articles.

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Thiazole | C3H441NS – PubChem,
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The important role of 2-(4-(Methylamino)phenyl)benzo[d]thiazol-6-ol

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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 Patent,once mentioned of 566169-93-5, Recommanded Product: 2-(4-(Methylamino)phenyl)benzo[d]thiazol-6-ol

This invention relates to novel thioflavin derivatives, methods of using the derivatives in, for example, in vivo imaging of patients having neuritic plaques, pharmaceutical compositions comprising the thioflavin derivatives and method of synthesizing the compounds. The compounds find particular use in the diagnosis and treatment of patients having diseases where accumulation of neuritic plaques are prevalent. The disease states or maladies include but are not limited to Alzheimer’s disease, familial Alzheimer’s disease, Down’s Syndrome and homozygotes for the apolipoprotein E4 allele.

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Reference:
Thiazole | C3H428NS – PubChem,
Thiazole | chemical compound | Britannica

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In vivo imaging of beta-amyloid plaques in the brain may lead to the early diagnosis of Alzheimer’s disease (AD) and monitoring of the progression and effectiveness of treatment. In the present study, we report on the development of two potential PET probes, [18F]FPYBF-2 ([ 18F]10) and [18F]FPHBF-2 ([18F]21), for imaging of beta-amyloid plaques in AD brain. In experiments in vitro, 10 and 21 displayed high affinity for Abeta(1-42) aggregates (Ki = 2.41 and 3.85 nM, respectively). In biodistribution experiments using normal mice, they displayed high uptake in the brain (7.38 and 8.18%-ID/g at 2 min postinjection, respectively), and the radioactivity washed out from the brain rapidly (3.15 and 3.87%-ID/g at 60 min postinjection, respectively), which is highly desirable for beta-amyloid imaging agents. In vivo, they clearly labeled beta-amyloid plaques in Tg2576 mice. Furthermore, the specific labeling of beta-amyloid plaques by 10 and 21 was observed in autoradiographs of sections of autopsied AD brain. These new fluorinated benzofuran derivatives are promising PET probes for imaging cerebral beta-amyloid plaques.

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Thiazole | C3H462NS – PubChem,
Thiazole | chemical compound | Britannica

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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 Article,once mentioned of 566169-93-5, category: thiazole

In this study, six novel benzothiazole derivatives based on the bithiophene structure were developed as potential beta-amyloid probes. In vitro binding studies using Abeta aggregates showed that all of them demonstrated high binding affinities with Ki values ranged from 0.11 to 4.64 nM. In vitro fluorescent staining results showed that these compounds can intensely stained Abeta plaques within brain sections of APP/PS1 transgenic mice, animal model for AD. Two radioiodinated compounds [125I]-2-(5?-iodo-2,2?-bithiophen-5-yl)-6-methoxybenzo[d]thiazole [125I]10 and [125I]-2-(2,2?-bithiophen-5-yl)-6-iodobenzo[d]thiazole [125I]13 were successfully prepared through an iododestannylation reaction. Furthermore, in vitro autoradiography of the AD model mice brain sections showed that both [125I]10 and [125I]13 labeled the Abeta plaques specifically with low background. In vivo biodistribution studies in normal mice indicated that [125I]13 exhibited high brain uptake (3.42% ID/g at 2 min) and rapid clearance from the brain (0.53% ID/g at 60 min), while [125I]10 showed lower brain uptake (0.87% ID/g at 2 min). In conclusion, these preliminary results of this study suggest that the novel radioiodinated benzothiazole derivative [125I]13 may be a candidate as an in vivo imaging agent for detecting beta-amyloid plaques in the brain of AD patients.

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Thiazole | C3H464NS – PubChem,
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Discovery of 2-(4-(Methylamino)phenyl)benzo[d]thiazol-6-ol

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Related Products 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.

The development of radioligands to image beta-amyloid (Abeta) plaques and neurofibrillary tangles (NFTs) in vivo in the aging human brain is an important and active area of radiopharmaceutical design. When used in combination with positron emission tomography (PET) or single photon emission computed tomography (SPECT), amyloid-imaging tracers could facilitate the evaluation of the efficacy of anti-amyloid therapies currently under intense development by many major pharmaceutical companies throughout the world. Amyloid-imaging agents could also serve as surrogate markers in early diagnosis and neuropathogenesis studies of Alzheimer’s disease and other aging-related neurodegenerative disorders. In this review article, the design and biological evaluation of amyloid-imaging agents are discussed. The structures of these agents vary from large proteins and peptides such as radiolabeled Abeta peptides and monoclonal antibodies to small molecules derived from Congo red, Chrysamine-G, thioflavin-T, and Acridine Orange. In vitro studies indicate that amyloid plaques contain multiple binding sites that can accommodate structurally diverse compounds, providing flexibility for radiopharmaceutical design of amyloid imaging agents. Compared to large biomolecules, small molecule radiotracers are often readily accessible through chemical synthesis and can display superior brain permeability. Several small molecule amyloid-imaging radioligands display high binding affinities to Abeta and sufficient brain penetration for imaging studies. Recent studies demonstrate the feasibility of imaging amyloid plaques in vivo in human subjects with PET. Imaging NFTs, separately or in concert with Abeta plaques, is not as far advanced as imaging Abeta plaques and remains to be fully characterized and demonstrated.

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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 Patent,once mentioned of 566169-93-5, Recommanded Product: 566169-93-5

This invention provides compounds and methods of imaging amyloid deposits using radiolabeled compounds. This invention also provides a method of inhibiting the aggregation of amyloid proteins to form amyloid plaques or deposits, a method of determining a therapeutic compound’s ability to inhibit aggregation of amyloid protein, and a method of delivering a therapeutic agent to amyloid deposits.

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Reference:
Thiazole | C3H430NS – PubChem,
Thiazole | chemical compound | Britannica