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Activation of HIF-1α and Nrf2 is a primary component of cellular response to oxidative stress, and activation of HIF-1α and Nrf2 provides neuroprotection in models of neurodegenerative disorders, including ischemic stroke, Alzheimer’s and Parkinson’s diseases. Screening a library of CNS-targeted drugs using novel reporters for HIF-1α and Nrf2 elevation in neuronal cells revealed histone deacetylase (HDAC) inhibitors as potential activators of these pathways. We report the identification of phenylhydroxamates as single agents exhibiting tripartite inhibition of HDAC6, inhibition of HIF-1 prolyl hydroxylase (PHD), and activation of Nrf2. Two superior tripartite agents, ING-6 and ING-66, showed neuroprotection against various cellular insults, associated with stabilization of both Nrf2 and HIF-1, and expression of their resp. target genes in vitro and in vivo. Discovery of the innate ability of phenylhydroxamate HDAC inhibitors to activate Nrf2 and HIF provides a novel route to multifunctional neuroprotective agents and cautions against HDAC6 selective inhibitors as chem. probes of specific HDAC isoform function.

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Name: 5-Fluoroindoline. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: 5-Fluoroindoline, is researched, Molecular C8H8FN, CAS is 2343-22-8, about Ruthenium-catalyzed C7 amidation of indoline C-H bonds with sulfonyl azides. Author is Pan, Changduo; Abdukader, Ablimit; Han, Jie; Cheng, Yixiang; Zhu, Chengjian.

A ruthenium-catalyzed direct C7 amidation of indoline C-H bonds with sulfonyl azides was developed. This procedure allows the synthesis of a variety of 7-amino-substituted indolines, which are useful in pharmaceutical. The good functional tolerances, as well as the mild conditions, are prominent feature of this method.

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Activation of HIF-1α and Nrf2 is a primary component of cellular response to oxidative stress, and activation of HIF-1α and Nrf2 provides neuroprotection in models of neurodegenerative disorders, including ischemic stroke, Alzheimer’s and Parkinson’s diseases. Screening a library of CNS-targeted drugs using novel reporters for HIF-1α and Nrf2 elevation in neuronal cells revealed histone deacetylase (HDAC) inhibitors as potential activators of these pathways. We report the identification of phenylhydroxamates as single agents exhibiting tripartite inhibition of HDAC6, inhibition of HIF-1 prolyl hydroxylase (PHD), and activation of Nrf2. Two superior tripartite agents, ING-6 and ING-66, showed neuroprotection against various cellular insults, associated with stabilization of both Nrf2 and HIF-1, and expression of their resp. target genes in vitro and in vivo. Discovery of the innate ability of phenylhydroxamate HDAC inhibitors to activate Nrf2 and HIF provides a novel route to multifunctional neuroprotective agents and cautions against HDAC6 selective inhibitors as chem. probes of specific HDAC isoform function.

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The reaction of an aromatic heterocycle with a proton is called a protonation. One of articles about this theory is 《Rh(III)-Catalyzed Carbocyclization of 3-(Indolin-1-yl)-3-oxopropanenitriles with Alkynes and Alkenes through C-H Activation》. Authors are Zhou, Tao; Wang, Yanwei; Li, Bin; Wang, Baiquan.The article about the compound:5-Fluoroindolinecas:2343-22-8,SMILESS:FC1=CC2=C(NCC2)C=C1).Recommanded Product: 2343-22-8. Through the article, more information about this compound (cas:2343-22-8) is conveyed.

Rh(III)-catalyzed carbocyclization reactions of 3-(indolin-1-yl)-3-oxopropanenitriles with alkynes and alkenes have been developed to form 1,7-fused indolines through C-H activation. These reactions have a broad range of substrates and high yields. Unsym. aryl-alkyl substituted alkynes proceeded smoothly with high regioselectivity. Electron-rich alkynes could undergo further oxidative coupling reaction to form polycyclic compounds For alkenes, 1,2-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-4-ones were formed via C(sp2)-H bond alkenylation and C(sp2)-H, C(sp3)-H oxidative coupling reactions.

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Chen, Qing-An; Chen, Zhiwei; Dong, Vy M. published an article about the compound: 5-Fluoroindoline( cas:2343-22-8,SMILESS:FC1=CC2=C(NCC2)C=C1 ).HPLC of Formula: 2343-22-8. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:2343-22-8) through the article.

The hydroamination of internal alkynes via tandem rhodium catalysis gives branched N-allylic indolines with high regio- and enantioselectivity. An acid switch provides access to the linear isomer in preference to the branched isomer by an isomerization mechanism. Mechanistic studies suggest formation of an allene intermediate, which undergoes hydroamination to generate allylic amines instead of the enamine or imine products typically observed in alkyne hydroaminations.

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Computed Properties of C8H8FN. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: 5-Fluoroindoline, is researched, Molecular C8H8FN, CAS is 2343-22-8, about 5-Hydroxytryptamine (5-HT3) receptor antagonists. 2. 1-Indolinecarboxamides. Author is Bermudez, Jose; Dabbs, Steven; Joiner, Karen A.; King, Frank D..

Indazole I is a potent and selective 5-HT3 receptor antagonist. A novel series of potent 5-HT3 receptor antagonists, 1-indoline- and 1-indolecarboxamides II [R = H , F, Cl, MeO, O2N; R1 = H, Me, Et, Ph; R2 = H, Me; R1R2 = (CH2)2, (CH2)4, (CH2)5; R3 = H, Me; n = 2,3] and III (R1 = H, Me, Et, Ph), resp., is described. The activity of II suggests that aromaticity of the 5-membered ring is not an essential requirement for potency provided that an in plane orientation of the CO group is favored. On the basis of this hypothesis indene IV was prepared In IV the in plane orientation of the CO group is maintained by conjugation with the aromatic ring through the sp2-hybridized C. IV is also a potent 5-HT3 receptor antagonist.

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Safety of 5-Fluoroindoline. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: 5-Fluoroindoline, is researched, Molecular C8H8FN, CAS is 2343-22-8, about The use of IR studies to investigate substituent effects: geometry changes in substituted anilines. Author is Butt, G. L.; Topsom, R. D..

The frequencies and intensities of the νNH mode of p-XC6H4NHMe (X = NMe2, OMe, F, Cl, Me, H, CO2Me, CN, NO2) were recorded. The frequencies followed σ values whereas the intensities correlated with σ- values, as a result of changing geometry in the mols. Results for 5-substituted indolines supported this explanation.

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So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Preobrazhenskaya, M. N.; Mukhanov, V. I.; Kostyuchenko, N. P.; Suvorov, N. N. researched the compound: 5-Fluoroindoline( cas:2343-22-8 ).SDS of cas: 2343-22-8.They published the article 《Glycosylindoles. XI. Synthesis of 1-β-D-ribopyranosides of 5- and 6-fluoroindole》 about this compound( cas:2343-22-8 ) in Zhurnal Organicheskoi Khimii. Keywords: ribopyranosylindole fluoro; conformation ribopyranoside indole. We’ll tell you more about this compound (cas:2343-22-8).

Treatment of 6-fluoroindoline with D-ribose, followed by acetylation gave 72% 6-fluoro derivative (I; R = Ac, X = 6-F) which was dehydrogenated by heating with 2,3-dichloro-5,6-dicyanoquinone to give 44% of the indole derivative (II; R = Ac, X = 6-F). Deacetylation of the latter with Na-OMe-MeOH gave 97% 1-β-D-ribopyranosyl-6-fluoroindole (II; R = H, X = 6-F). Analogously prepared were the 5-fluoro derivatives and the corresponding α-D-anomers. Conformations of the ribopyranosyl group were determined by PMR.

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Related Products of 2343-22-8. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: 5-Fluoroindoline, is researched, Molecular C8H8FN, CAS is 2343-22-8, about Dual-Active-Sites Design of Co@C Catalysts for Ultrahigh Selective Hydrogenation of N-Heteroarenes. Author is Zhang, Sai; Gan, Jie; Xia, Zhaoming; Chen, Xiao; Zou, Yong; Duan, Xuezhi; Qu, Yongquan.

Herein, a general yet powerful strategy to design and fabricate dual-active-sites Co@C core-shell nanoparticle for boosting selective hydrogenation of various N-heteroarenes was reported. It could break the limitation of scaling relation on traditional metal surfaces and thus afford unprecedentedly high selectivity, activity and stability. Combining kinetics anal. and DFT calculations with multiple techniques directly unveil that the critical porous carbon shell with a pore size of 0.53 nm not only allowed H2 diffusion to Co sites for activation and blocked accessibility of N-heteroarenes but also catalyzed hydrogenation of N-heteroarenes via hydrogen spillover from Co sites. In addition, the presence of surface/subsurface carbon at the Co sites showed high anti-sulfur poisoning and anti-oxidant capability. This work was valuable for guiding the design and manipulation of cost-effective and robust hydrogenation catalysts.

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So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Zhao, Fei; Masci, Domiziana; Ferla, Salvatore; Varricchio, Carmine; Brancale, Andrea; Colonna, Serena; Black, Gary W.; Turner, Nicholas J.; Castagnolo, Daniele researched the compound: 5-Fluoroindoline( cas:2343-22-8 ).HPLC of Formula: 2343-22-8.They published the article 《Monoamine Oxidase (MAO-N) Biocatalyzed Synthesis of Indoles from Indolines Prepared via Photocatalytic Cyclization/Arylative Dearomatization》 about this compound( cas:2343-22-8 ) in ACS Catalysis. Keywords: monoamine oxidase indole indoline photocatalytic cyclization dearomatization. We’ll tell you more about this compound (cas:2343-22-8).

The biocatalytic aromatization of indolines into indole derivatives exploiting monoamine oxidase (MAO-N) enzymes is presented. Indoline substrates were prepared via photocatalytic cyclization of arylaniline precursors or via arylative dearomatization of unsubstituted indoles and in turn chemoselectively aromatized by the MAO-N D11 whole cell biocatalyst. Computational docking studies of the indoline substrates in the MAO-N D11 catalytic site allowed for the rationalization of the biocatalytic mechanism and exptl. results of the biotransformation. This methodol. represents an efficient example of biocatalytic synthesis of indole derivatives and offers a facile approach to access these aromatic heterocycles under mild reaction conditions.

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