902086-40-2Relevant academic research and scientific papers
Benzothiazole amphiphiles promote the formation of dendritic spines in primary hippocampal neurons
Cifelli, Jessica L.,Dozier, Lara,Chung, Tim S.,Patrick, Gentry N.,Yang, Jerry
, p. 11981 - 11992 (2016)
The majority of excitatory synapses in the brain exist on dendritic spines. Accordingly, the regulation of dendritic spine density in the hippocampus is thought to play a central role in learning and memory. The development of novel methods to control spine density could, therefore, have important implications for treatment of a host of neurodegenerative and developmental cognitive disorders. Herein, we report the design and evaluation of a new class of benzothiazole amphiphiles that exhibit a dosedependent response leading to an increase in dendritic spine density in primary hippocampal neurons. Cell exposure studies reveal that the increase in spine density can persist for days in the presence of these compounds, but returns to normal spine density levels within 24 h when the compounds are removed, demonstrating the capability to reversibly control spinogenic activity. Time-lapse imaging of dissociated hippocampal neuronal cultures shows that these compounds promote a net increase in spine density through the formation of new spines. Biochemical studies support that promotion of spine formation by these compounds is accompanied by Ras activation. These spinogenic molecules were also capable of inhibiting a suspected mechanism for dendritic spine loss induced by Alzheimer-related aggregated amyloid-? peptides in primary neurons. Evaluation of this new group of spinogenic agents reveals that they also exhibit relatively low toxicity at concentrations displaying activity. Collectively, these results suggest that small molecules that promote spine formation could be potentially useful for ameliorating cognitive deficiencies associated with spine loss in neurodegenerative diseases such as Alzheimer disease, and may also find use as general cognitive enhancers.
4-benzo five-membered ring-phenyl sulfonium salt compound as well as preparation method and application thereof
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Paragraph 0114-0117; 0144-0147, (2021/02/10)
The invention discloses a 4-benzo five-membered ring-phenyl sulfonium salt compound as well as a preparation method and application thereof, and relates to a 4-benzo five-membered ring-phenyl sulfonium salt derivative shown as a formula (I), a photocuring composition and a preparation method of the 4-benzo five-membered ring-phenyl sulfonium salt derivative shown as the formula (I). Compared witha 4-styryl phenyl sulfonium salt, the 4-benzo five-membered ring-phenyl sulfonium salt derivative shown in the formula (I) has better molecular photoinitiation efficiency and simpler synthesis steps,and is expected to become a photoinitiator for industrial production and application of UV-Vis-LED excitable photocureable photocureable coatings or printing ink.
I2/TBHP-Mediated tandem cyclization and oxidation reaction: Facile access to 2-substituted thiazoles and benzothiazoles
Liu, Li,Tan, Chen,Fan, Rong,Wang, Zihan,Du, Hongguang,Xu, Kun,Tan, Jiajing
supporting information, p. 252 - 256 (2019/01/10)
The efficient synthesis of 2-substituted thiazoles and benzothiazoles has been accomplished employing readily available cysteine esters and 2-aminobenzenethiols as N and S sources. The reaction proceeds under an I2/TBHP system and involves a on
USE OF BENZOTHIAZOLE AMPHIPHILES FOR TREATING TRAUMATIC BRAIN INJURY
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Paragraph 0155; 0162, (2019/01/16)
The present invention is directed to methods of reducing symptoms of traumatic brain injury in patients by administering a therapeutically effective amount of a benzothiazole amphiphile compound to a patient suffering from a traumatic brain injury within 0 to 72 hours of incurring the injury.
Selective Construction of 2-Substituted Benzothiazoles from o-Iodoaniline Derivatives S8 and N-Tosylhydrazones
Huang, Yubing,Zhou, Peiqi,Wu, Wanqing,Jiang, Huanfeng
, p. 2460 - 2466 (2018/02/23)
Selective construction of 2-substituted benzothiazoles from o-iodoaniline derivatives S8 and N-tosylhydrazone via a copper-promoted [3 + 1 + 1]-type cyclization reaction has been realized. In the protocol, the carbon atom on N-tosylhydrazone could be regulated to construct benzothiazole by changing the reaction system. Furthermore, the transformation has achieved the construction of multiple carbon-heteroatom bonds.
BENZOTHIAZOLE AMPHIPHILES
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Paragraph 0240, (2017/08/01)
Disclosed herein, inter alia, are compounds and methods for increasing spine density in a neuron, and for treatment of neuronal diseases and cancer.
An efficient desulfitative C-C cross coupling of fused thiazolidine-2-thione with boronic acids and boronic acid pinacol esters: Formation of fused thiazoles
Rajaguru, Kandasamy,Mariappan, Arumugam,Manjusri, Ramachandran,Muthusubramanian, Shanmugam,Bhuvanesh, Nattamai
, p. 86832 - 86839 (2015/11/03)
An efficient Pd(0)-catalyzed Cu(i)-mediated desulfitative C-C cross-coupling of benzo-fused thiazolidine-2-thione with boronic acids under neutral Liebeskind-Srogl conditions is described. The desulfitative cross coupling of boronic acid pinacol esters has also been demonstrated with fused thiazolidine-2-thione under basic conditions to afford fused thiazoles with good to excellent yields.
Synthesis of benzothiazoles through copper-catalyzed one-pot three-component reactions with use of sodium hydrosulfide as a sulfur surrogate
Park, Namjin,Heo, Yumi,Kumar, Manian Rajesh,Kim, Yong,Song, Kwang Ho,Lee, Sunwoo
experimental part, p. 1984 - 1993 (2012/05/05)
Copper-catalyzed one-pot three-component reactions of 2-iodoanilines, aldehydes, and NaSH·n H2O afford benzothiazoles in good yields. When CuCl was employed as a catalyst in the absence of a ligand, a variety of aromatic aldehydes and substituted 2-iodoanilines reacted with NaSH·n H2O to produce the corresponding 2-arylbenzothiazoles in 70-98 % yields. The copper catalyst plays a key role in C-S bond formation between NaSH·n H2O and the aryl iodide that was formed from the condensation of 2-iodoaniline and aldehyde. It was found that NaSH·n H2O functions as a sulfur surrogate and oxidant in the formation of benzothiazole. 2-Iodoanilines, aldehydes, and NaSH·n H2O afford benzothiazoles in a one-pot reaction in the presence of a copper catalyst. The desired products can be obtainedin moderate to good yields. The copper catalyst plays a key role in C-S bond formation between aryl iodides and NaSH·n H2O. Copyright
