Shi, Ya-Jing et al. published their research in Inorganica Chimica Acta in 2018 |CAS: 32462-30-9

The Article related to zinc hydroxyphenylglycine bipyridine polymer preparation homochiral luminescence cd spectra, thermal stability zinc hydroxyphenylglycine bipyridine polymer, crystal structure zinc hydroxyphenylglycine bipyridine polymer and other aspects.Safety of H-Phg(4-OH)-OH

On February 24, 2018, Shi, Ya-Jing; Song, Hui-Hua published an article.Safety of H-Phg(4-OH)-OH The title of the article was Three enantiomeric pairs of zinc(II) homochiral coordination compounds based on D-(-)- and L-(+)-4-Hydroxyphenylglycine: Synthesis, structures and luminescent properties. And the article contained the following:

Three enantiomeric pairs of novel homochiral coordination compounds (HCCs) with the formula {[Zn(D-hpg)(4,4′-bipy)(H2O)]·(NO3)}n 1-D, {[Zn(L-hpg)(4,4′-bipy)(H2O)]·(NO3)}n 1-L, {[Zn(D-hpg)(4,4′-bipy)(H2O)]·(ClO4)}n 2-D, {[Zn(L-hpg)(4,4′-bipy)(H2O)]·(ClO4)}n 2-L, [Zn(D-hpg)2(4,4′-bipy)]·(4,4′-bipy)·2H2O 3-D, [Zn(L-hpg)2(4,4′-bipy)]·(4,4′-bipy)·2H2O 3-L (D-Hhpg = D-(-)-4-Hydroxyphenylglycine, L-Hhpg = L-(+)-4-Hydroxyphenylglycine, 4,4′-bipy = 4,4′-bipyridine) have been synthesized and characterized by single-crystal X-ray diffraction, elemental anal., IR spectroscopy, thermal anal. and powder X-ray diffraction. Compounds 1 and 2 are isostructural 2D layer structures with NO-3 or ClO-4 anions between the layers. While compound 3 features a 0D structure without counter anions. Compounds 1-D and 2-D both contain 1D right-hand helical chains via D-Hhpg ligand, while 1-L and 2-L both contain 1D left-hand helical chains via L-Hhpg ligand. It’s worth noting that 3-D forms left-hand supramol. double helical chains, while 3-L forms right-hand supramol. double helical chains. Compounds 1-3 are further extended into 3D supramol. architectures through hydrogen-bonding interactions. CD and luminescent properties of compounds 1-3 were investigated at room temperature Our results highlight that chiral ligands have an important effect on regulating the chirality/helicity of complexes and the frameworks can be controlled via applying different zinc salts and adjusting the pH values. The experimental process involved the reaction of H-Phg(4-OH)-OH(cas: 32462-30-9).Safety of H-Phg(4-OH)-OH

The Article related to zinc hydroxyphenylglycine bipyridine polymer preparation homochiral luminescence cd spectra, thermal stability zinc hydroxyphenylglycine bipyridine polymer, crystal structure zinc hydroxyphenylglycine bipyridine polymer and other aspects.Safety of H-Phg(4-OH)-OH

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Wang, Yixuan et al. published their research in Food Chemistry in 2022 |CAS: 621-37-4

The Article related to elaeagnus bifidobacterium fruit juice antioxidant secondary metabolites metabolomics, antioxidant activity, elaeagnus angustifolia var. orientalis(l.)kuntze, material transformation, widely-targeted metabolomic analysis and other aspects.Synthetic Route of 621-37-4

On April 16, 2022, Wang, Yixuan; Li, Hui; Li, Xiaozhen; Wang, Chenxi; Li, Qianhong; Xu, Meng; Guan, Xiangluo; Lan, Zhenghui; Ni, Yongqing; Zhang, Yan published an article.Synthetic Route of 621-37-4 The title of the article was Widely targeted metabolomics analysis of enriched secondary metabolites and determination of their corresponding antioxidant activities in Elaeagnus angustifolia var. orientalis (L.)Kuntze fruit juice enhanced by Bifidobacterium animalis subsp. Lactis HN-3 fermentation. And the article contained the following:

Elaeagnus angustifolia var. orientalis (L.)Kuntze fruit contains a large number of naturally occurring mols. present as glycoside, methylated, and Me ester conjugates, which should be hydolyzed or transformed to become bioactive forms. For this purpose, Bifidobacterium animalis subsp. lactis HN-3 was selected to ferment Elaeagnus angustifolia var. orientalis (L.)Kuntze fruit juice (EOJ). After fermentation, the total phenolic content (TPC) and antioxidant capacity of the EOJ increased significantly compared to the non-fermented EOJ. Using widely-targeted metabolomics anal., polyphenolic compounds involved in the flavonoid biosynthetic pathway were determined to be up-regulated in the fermented EOJ. In addition, the metabolites generated by 8 deglycosidation, 5 demethylation, 5 hydrogenation, and 28 other reactions were detected in higher concentrations in the fermented EOJ compared to the non-fermented EOJ. Interestingly, these up-regulated metabolites have higher antioxidant and other biol. activities than their metabolic precursors, which provide a theor. basis for the development of Bifidobacterium-fermented plant products with stronger functional activities. The experimental process involved the reaction of 3-Hydroxyphenylacetic acid(cas: 621-37-4).Synthetic Route of 621-37-4

The Article related to elaeagnus bifidobacterium fruit juice antioxidant secondary metabolites metabolomics, antioxidant activity, elaeagnus angustifolia var. orientalis(l.)kuntze, material transformation, widely-targeted metabolomic analysis and other aspects.Synthetic Route of 621-37-4

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Stoller, Sven et al. published their research in Angewandte Chemie, International Edition in 2011 |CAS: 32462-30-9

The Article related to topp nitroxide amino acid preparation epr distance peptide, tetramethyldioxooxylpiperazinyl phenylglycine preparation epr distance peptide, nitroxide labeled phenylglycine preparation determination distance peptide epr and other aspects.COA of Formula: C8H9NO3

Stoller, Sven; Sicoli, Giuseppe; Baranova, Tatiana Y.; Bennati, Marina; Diederichsen, Ulf published an article in 2011, the title of the article was TOPP-A Novel Nitroxide-Labeled Amino Acid for EPR Distance Measurements.COA of Formula: C8H9NO3 And the article contains the following content:

We report the synthesis of a novel, rigid nitroxide-labeled amino acid 4-(3,3,5,5-tetramethyl-2,6-dioxo-4-oxylpiperazin-1-yl)-L-phenylglycine (TOPP, I) that does not produce perturbation of the secondary structure, thus, providing a promising tool for structural studies of peptides and proteins. The design of the TOPP amino acid is based on the alignment of the nitroxide with the Cα-Cβ amino acid bond on one axis and the synthetic applicability with respect to racemization at Cα during amino acid and peptide oligomer synthesis. The present study illustrates the straightforward assignment of a spin-spin distance measured by pulsed EPR which is in contrast to the different and ambiguous result obtained with the commonly used MTSSL label. Furthermore, the predicted reduced mobility of the TOPP spin label represents a potential advantage for its incorporation into transmembrane peptides for the structure determination of peptide arrangements at an at. scale. The experimental process involved the reaction of H-Phg(4-OH)-OH(cas: 32462-30-9).COA of Formula: C8H9NO3

The Article related to topp nitroxide amino acid preparation epr distance peptide, tetramethyldioxooxylpiperazinyl phenylglycine preparation epr distance peptide, nitroxide labeled phenylglycine preparation determination distance peptide epr and other aspects.COA of Formula: C8H9NO3

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Heussner, Kirsten et al. published their research in European Journal of Inorganic Chemistry in 2011 |CAS: 2160-93-2

The Article related to heptamolybdate octamolybdate polymolybdate amphiphilic butyldiethanolammonium preparation crystal supramol structure, crystal structure heptamolybdate octamolybdate polymolybdate amphiphilic butyldiethanolammonium salt and other aspects.Category: alcohols-buliding-blocks

Heussner, Kirsten; Grabau, Mathias; Forster, Johannes; Streb, Carsten published an article in 2011, the title of the article was Can Hydrophobic Interactions Influence Supramolecular Aggregation in Self-Assembled Organic-Inorganic Hybrid Structures?.Category: alcohols-buliding-blocks And the article contains the following content:

This study aims to provide insights into the ability of amphiphilic cations to influence the assembly of hybrid organic-inorganic crystal lattices using hydrophobic interactions. To study the hypothesis, a prototype amphiphilic cation, tert-butyldiethanolammonium, was employed together with molybdenum oxide clusters of increasing size and charge in the self-assembly of type I hybrid systems. The molybdate clusters were used as model inorganic building blocks as they can be formed in situ and their size and charge can be adjusted by pH control. Using this strategy, three hybrid structures were obtained and characterized using single-crystal x-ray diffraction, theor. bond valence sum calculations, elemental anal., FTIR spectroscopy, TG and theor. Hirshfeld anal. Heptamolybdate Na5[tBuNH(C2H4OH)2][Mo7O24]·ca. 14H2O (1) was isolated, which features sodium-linked dimeric cluster species and isolated octadecanuclear sodium clusters. Octamolybdate [tBuNH(C2H4OH)2]4[Mo8O26]·ca. 4H2O (2) was isolated, containing the octanuclear β-[Mo8O26]4- cluster. At low pH levels (below pH 2), [tBuNH(C2H4OH)2]14[Mo36O112(H2O)16][Mo36O112(H2O)14{tBuNH(C2H4OH)2}2]·ca. 36H2O (3) was obtained, which is based on a 36-center molybdenum oxide cluster. Crystallog. anal. of the assemblies showed that the formation of hydrophobic regions within the crystal lattice is affected by the size of the inorganic building blocks employed. In 1 and 2, the hydrophobic tert-Bu groups of the amphiphilic cations aggregate into hydrophobic assemblies. In contrast, the structural arrangement in 3 is dominated by the large inorganic cluster and the organic cations are incorporated as isolated units. This behavior is further supported by theor. Hirshfeld surface anal. of the organic counterions, which suggests that, with increasing cluster size, the contribution of long-range, hydrophobic intermol. interactions decreases, which is in line with the crystallog. anal. for 1-3. The experimental process involved the reaction of 2,2′-(tert-Butylazanediyl)diethanol(cas: 2160-93-2).Category: alcohols-buliding-blocks

The Article related to heptamolybdate octamolybdate polymolybdate amphiphilic butyldiethanolammonium preparation crystal supramol structure, crystal structure heptamolybdate octamolybdate polymolybdate amphiphilic butyldiethanolammonium salt and other aspects.Category: alcohols-buliding-blocks

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Vicker, Nigel et al. published their patent in 2009 |CAS: 386704-04-7

The Article related to adamantyl ketone derivative preparation 11 beta hydroxysteroid dehydrogenase inhibitor, phenyl ketone derivative preparation 11 beta hsd1 inhibitor, benzyl ketone preparation 11 beta hydroxysteroid dehydrogenase type i and other aspects.Category: alcohols-buliding-blocks

On September 3, 2009, Vicker, Nigel; Su, Xiangdong; Pradaux-Caggiano, Fabienne; Potter, Barry Victor Lloyd published a patent.Category: alcohols-buliding-blocks The title of the patent was Adamantyl, phenyl, and benzyl ketone derivatives as inhibitors of 11β-hydroxysteroid dehydrogenase type I useful in the treatment of diseases and preparation and pharmaceutical compositions thereof. And the patent contained the following:

Title compounds I and their pharmaceutical compositions are prepared and disclosed as inhibitors of 11β-hydroxysteroid dehydrogenase type I (11β-HSD1) useful in the treatment of diseases. Compounds I [X and Z independently = (un)saturated C1-3 carbon chain; Y = S, SO, SO2, CH=CH, CH2CH2, or O; R1 = 1-adamantyl, 2,4,6-trimethylphenyl, 1-(4-chlorophenyl)C3-6 cycloalkyl, or 2-(4-chlorophenyl)propan-2-yl; R2 = (un)substituted 5- to 6- membered N-containing heteroaryl; with the provision that when R1 = 1-adamantyl and X-Y-Z = CH2S, CH2SO, or CH2SO2, then R2 ≠ 1-methylimidazol-2-yl; or when R1 = 1-adamantyl and X-Y-Z = CH2O, then R2 ≠ 2-methylpyridinyl] are claimed. For example, compound II was prepared via substitution of 2-bromo-1-[1-(4-chlorophenyl)cyclopropyl]ethanone with 2-mercapto-1-methylimidazole. Select I were assayed for 11β-HSD1 inhibition and compound II was found to possess >60% inhibition at 1 μM concentration The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Category: alcohols-buliding-blocks

The Article related to adamantyl ketone derivative preparation 11 beta hydroxysteroid dehydrogenase inhibitor, phenyl ketone derivative preparation 11 beta hsd1 inhibitor, benzyl ketone preparation 11 beta hydroxysteroid dehydrogenase type i and other aspects.Category: alcohols-buliding-blocks

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Schultz, Rose Ann et al. published their research in Journal of the American Chemical Society in 1985 |CAS: 2160-93-2

The Article related to azacrown ether cation binding preparation, nitrogen pivot lariat ether cation binding, crown ether cation binding preparation, inclusion compound monoazacrown ether cation, diethanolamine cyclization glycol dimesylate and other aspects.Computed Properties of 2160-93-2

On November 13, 1985, Schultz, Rose Ann; White, Banita D.; Dishong, Dennis M.; Arnold, Kristin A.; Gokel, George W. published an article.Computed Properties of 2160-93-2 The title of the article was 12-, 15-, and 18-Membered-ring nitrogen-pivot lariat ethers: syntheses, properties, and sodium and ammonium cation binding properties. And the article contained the following:

N-pivot lariat ethers of varying ring sizes can be prepared by cyclization of an amine or substituted diol. 12-Membered ethers I [R = PhCH2, 2-, 4-MeOC6H4, 2-MeOC6H4CH2, HO(CH2)3, Me2NCH2CH2, MeOCH2CH2; n = 1] were prepared by the method of M. Calverley and J. Dale (1982); this involves cyclo-bis-dialkylation of an amine with 1,11-diiodo-3,6,9-trioxaundecane. I (R = 2-O2NC6H4CH2, 3,6-dioxaheptyl, 3,6,9-trioxadecyl, 3,6,9,12-tetraoxatridecyl, 11-allyloxy-3,6,9-trioxaundecyl; n = 1) did not form in high yield by this method or were more conveniently prepared by alkylation of I (R = H, n = 1). The latter was prepared from I (R = PhCH2, n = 1) by hydrogenolysis. Monoaza-15-crown-5 derivatives I (R = allyl, Bu, Me3C, PhCH2, MeOCH2CH2, 3,6-dioxaheptyl, 3,6,9,12,15,18,21,24-octaoxapentacosyl, 2-MeOC6H4, 4-MeOC6H4, 2-MeOC6H4CH2; n = 2) were prepared by cyclizing RN(CH2CH2OH)2 with R1(OCH2CH2)3OR1 (R1 = MeSO2, 4-MeC6H4SO2). I (R = Me, 2-O2NC6H4CH2, 4-O2NC6H4CH2, Me3CO2CCH2, n =2) were prepared by the alkylation of I (R = H, n = 2) which was prepared by hydrogenolysis I (R = PhCH2, n = 2). Monoaza-18-crown-6 derivatives I (R = H, Me, PhCH2, MeOCH2CH2, 3,6-dioxaheptyl, 3,6,9-trioxadecyl, 3,6,9,12-tetraoxatridecyl, 3,6,9,12,15-pentaoxahexadecyl, 3,6,9,12,15,18,21,24-octaoxapentacosyl, 2-MeOC6H4; n = 3) were analogously prepared Studies involving NH4 cation binding show that the interaction of ring and side-chain with the cation is intramol. in MeOH solution; the Na cation binds similarly. X-ray crystal structure evidence confirms this for the solid state in the I (R = 2-MeOCH2CH2, n = 3)·KI complex. The strongest binding for Na occurs when 6 O are present, regardless of ring size, which suggests that a flexible macrocycle is directed by the cation to envelop and solvate in the geometry most appropriate for the cation. The experimental process involved the reaction of 2,2′-(tert-Butylazanediyl)diethanol(cas: 2160-93-2).Computed Properties of 2160-93-2

The Article related to azacrown ether cation binding preparation, nitrogen pivot lariat ether cation binding, crown ether cation binding preparation, inclusion compound monoazacrown ether cation, diethanolamine cyclization glycol dimesylate and other aspects.Computed Properties of 2160-93-2

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Young, Robert N. et al. published their patent in 1990 |CAS: 42900-89-0

The Article related to arylstyrylquinoline diacid preparation leukotriene antagonist, cytoprotection arylstyrylquinoline diacid, eye antiinflammatory arylstyrylquinoline diacid, antiasthmatic arylstyrylquinoline diacid, srsa inhibitor arylstyrylquinoline diacid preparation and other aspects.Recommanded Product: Isochroman-3-ol

On November 28, 1990, Young, Robert N.; Gauthier, Jacques Yves; Zamboni, Robert; Belley, Michel L. published a patent.Recommanded Product: Isochroman-3-ol The title of the patent was Preparation of diarylstyrylquinoline diacids as leukotriene antagonists. And the patent contained the following:

Title compounds I [R1 = 7-Cl, 7-MeO, 6-F3C, 7-F3C, 6-MeSO2, H, 6,7-Cl2; Y = CH:CH, CH2CH2, CH2O, CHMeCH2; A = HO2C(CH2)2S, Me2NCO(CH2)2S, 3-(HO2C)C6H4S, Me3CNHCO(CH2)2S, 4-carboxy-2-pyridyl, [(1-adamantylamino)carbonylethyl]thio, 1-tetrazol-5-ylmethylthio, etc.; B = 2-(HO2C)C6H4CH2CH2, 3-(HO2C)C6H4, 5-carboxy-2-thiophenyl, HO2CCH2CHMe(CH2)2, 6-carboxy-2-pyridyl, 2-(Me3CNHCO)C6H4S, 3-[(1-tetrazol-5-yl)methyl]phenyl, etc.] and their salts, useful as inhibitors of leukotriene biosynthesis, antiasthmatic, antiallergic, antiinflammatory, and cytoprotective agents (no data, assays described), are prepared I may also be used to treat erosive gastritis, inflammatory bowel disease, prevention of SRA-release (no data). To a suspension of [(7-chloroquinolin-2-yl)methyl]triphenylphosphonium bromide in THF was added BuLi, the reaction mixture was stirred at -78° and Me 2-[3-[2-(methoxycarbonyl)ethylthio]-3-(3-formylphenyl)propyl]benzoate [preparation from 3-(BrCH2)C6H4CN given] added, the mixture warmed to room temperature to give I [R1 = 7-Cl; Y = CH:CH; A = HO2C(CH2)2S; B = 2-(HO2C)C6H4CH2CH2] (II) as the di-Me ester, which in THF and MeOH was saponified to give II.2Na salt. A capsule, injectable suspension and tablet formulations comprising I are given. Pharmaceutical composition of I may comprise an addnl. active ingredient such as nonsteroidal antiinflammatory drug, peripheral analgesic, cyclooxygenase inhibitor, etc. The experimental process involved the reaction of Isochroman-3-ol(cas: 42900-89-0).Recommanded Product: Isochroman-3-ol

The Article related to arylstyrylquinoline diacid preparation leukotriene antagonist, cytoprotection arylstyrylquinoline diacid, eye antiinflammatory arylstyrylquinoline diacid, antiasthmatic arylstyrylquinoline diacid, srsa inhibitor arylstyrylquinoline diacid preparation and other aspects.Recommanded Product: Isochroman-3-ol

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Nesterova, Oksana V. et al. published their research in Inorganic Chemistry in 2018 |CAS: 2160-93-2

The Article related to epr magnetic susceptibility copper n substituted diethanolamine complex, oxidative dehydrogenation cyclohexane amidation copper n substituted diethanolamine complex, crystal structure dinuclear copper n substituted diethanolamine complex preparation and other aspects.Synthetic Route of 2160-93-2

On October 1, 2018, Nesterova, Oksana V.; Nesterov, Dmytro S.; Jezierska, Julia; Pombeiro, Armando J. L.; Ozarowski, Andrew published an article.Synthetic Route of 2160-93-2 The title of the article was Copper(II) Complexes with Bulky N-Substituted Diethanolamines: High-Field Electron Paramagnetic Resonance, Magnetic, and Catalytic Studies in Oxidative Cyclohexane Amidation. And the article contained the following:

The novel coordination compounds [Cu2(HtBuDea)2(OAc)2] (1) and [Cu2(HBuDea)2Cl2]·nH2O (2) have been prepared through the reaction of the resp. copper(II) salts with N-tert-butyldiethanolamine (H2tBuDea, for 1) or N-butyldiethanolamine (H2BuDea, for 2) in methanol solution Crystallog. anal. reveals that, in spite of the common binuclear {Cu2(μ-O)2} core, the supramol. structures of the complexes are drastically different. In 1 binuclear mols. are linked together by H-bonds into 1D chains, while in 2 the neighboring pairs of binuclear mols. are H-bonded, forming tetranuclear aggregates. Variable-temperature (1.8-300 K) magnetic susceptibility measurements of 1 and 2 show a dominant antiferromagnetic behavior. Both complexes were also studied by HF-EPR spectroscopy. While the interaction between Cu(II) centers in 1 can be described by a single coupling constant J = 130.1(3) cm-1 (using H = JS1S2), the crystallog. different {Cu2(μ-O)2} pairs in 2 are expected exchange from ferro- to antiferromagnetic behavior (with J ranging from -32 to 110 cm-1, according to DFT calculations). Complexes 1 and 2 act as catalysts in the amidation of cyclohexane with benzamide, employing tBuOOtBu as oxidant. The maximum achieved conversion of benzamide (20%, after 24 h reaction time) was observed in the 1/tBuOOtBu system. In the cases of tBuOO(O)CPh or tBuOOH oxidants, no significant amidation product was observed, while for tBuOO(O)CPh, the oxidative dehydrogenation of cyclohexane occurred, giving cyclohexene, to afford the allylic ester (cyclohex-2-en-1-yl benzoate) as the main reaction product. The experimental process involved the reaction of 2,2′-(tert-Butylazanediyl)diethanol(cas: 2160-93-2).Synthetic Route of 2160-93-2

The Article related to epr magnetic susceptibility copper n substituted diethanolamine complex, oxidative dehydrogenation cyclohexane amidation copper n substituted diethanolamine complex, crystal structure dinuclear copper n substituted diethanolamine complex preparation and other aspects.Synthetic Route of 2160-93-2

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Ghosh, Arun K. et al. published their patent in 2009 |CAS: 386704-04-7

The Article related to thiazolylpyrrolidinecarbonylbenzamide preparation selective secretase inhibitor, alzheimer disease treatment thiazolylpyrrolidinecarbonylbenzamide preparation, hydroxyaminobutanylthiazolylpyrrolidinecarbonylbenzamide preparation secretase inhibitor and other aspects.Formula: C7H6F3NO

On April 2, 2009, Ghosh, Arun K.; Liu, Chunfeng; Devasamudram, Thippeswamy; Lei, Hui; Swanson, Lisa M.; Ankala, Sudha V.; Lilly, John C.; Bilcer, Geoffrey M. published a patent.Formula: C7H6F3NO The title of the patent was Preparation of (3-hydroxy-4-amino-butan-2-yl)-3-[2-(thiazol-2-yl)pyrrolidine-1-carbonyl]benzamide derivatives and related compounds as selective beta-secretase inhibitors. And the patent contained the following:

The title compounds [I; A1 = each (un)substituted cycloalkyl, heterocycloalkyl, aryl, or heteroaryl; A2 = each cycloalkylene, heterocycloalkylene, arylene, or heteroarylene; X = CH2, O, (un)substituted NH, or S(O)w; or where X is CH or N, and is the attachment point for R6 or R7; L1, L5 = a bond, (un)substituted NH, S(O)q, (un)substituted alkylene; L4 = a bond, C(O), (un)substituted NH, S(O)q, (un)substituted alkylene; R2, R3 = S(O)2R11, C(O)R12, each (un)substituted NH2, alkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl, aryl, aralkyl, heteroaryl, or heteroaralkyl; R4, R5 = H, halogen, NO2, each (un)substituted OH, NH2, alkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl, aryl, aralkyl, heteroaryl, or heteroaralkyl, S(O)nR11, C(O)R12; R6, R7 = H, halogen, NO2, each (un)substituted OH, NH2, alkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl, aryl, aralkyl, heteroaryl, or heteroaralkyl, S(O)nR11, C(O)R12; R11 = H, each (un)substituted alkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl, aryl, aralkyl, heteroaryl, or heteroaralkyl; R12 = H, each (un)substituted NH2, OH, alkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl, aryl, aralkyl, heteroaryl, or heteroaralkyl; m = 0-2] or pharmaceutically acceptable salts or solvates thereof were prepared The present invention provides novel β-secretase inhibitors which are capable of selectively reducing memapsin 2 catalytic activity relative to memapsin 1 catalytic activity or cathepsin D by greater than ∼5 or ∼10-fold. It also provides methods for their use, including methods of treating of Alzheimer’s disease. Thus, to 330 mg (R)-3-methyl-5-[2-(4-methylthiazol-2-yl)pyrrolidine-1-carbonyl]benzoic acid in CH2Cl2 at room temperature, 269 mg 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride and 162 mg HOBT were added, stirred at room temperature for 20 min, cooled to 0°, treated with a solution of (2R,3S)-3-amino-4-phenyl-1-[3-(trifluoromethyl)benzylamino]butan-2-ol and 2 mL diisopropylethylamine in CH2Cl2, and stirred at room temperature for 16 h to yield 60% N-[(2S,3R)-3-hydroxy-1-phenyl-4-[[3-(trifluoromethyl)benzyl]amino]butan-2-yl]-3-methyl-5-[[(R)-2-(4-methylthiazol-2-yl)pyrrolidin-1-yl]carbonyl]benzamide (II). II showed Ki of 7.09, 1,079.9, and 825.73 nM, for inhibiting memapsin 2 (β-secretase), cathepsin D, memapsin 1 (β-secretase 2), resp., and showed IC50 of 23 nM against memapsin 2 (β-secretase). The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Formula: C7H6F3NO

The Article related to thiazolylpyrrolidinecarbonylbenzamide preparation selective secretase inhibitor, alzheimer disease treatment thiazolylpyrrolidinecarbonylbenzamide preparation, hydroxyaminobutanylthiazolylpyrrolidinecarbonylbenzamide preparation secretase inhibitor and other aspects.Formula: C7H6F3NO

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Yan, Jun et al. published their research in Science of the Total Environment in 2022 |CAS: 621-37-4

The Article related to gut microbiota disorder intestinal barrier damage toxicity microparticle nanoparticle, titanium dioxide pyroglutamic phenylacetic acid juvenile, biomarker, correlation, fecal transplant, gut microbiome, tio(2) microparticle, tio(2) nanoparticle and other aspects.Safety of 3-Hydroxyphenylacetic acid

On May 15, 2022, Yan, Jun; Chen, Qi; Tian, Lei; Li, Kang; Lai, Wenqing; Bian, Liping; Han, Jie; Jia, Rui; Liu, Xiaohua; Xi, Zhuge published an article.Safety of 3-Hydroxyphenylacetic acid The title of the article was Intestinal toxicity of micro- and nano-particles of foodborne titanium dioxide in juvenile mice: Disorders of gut microbiota-host co-metabolites and intestinal barrier damage. And the article contained the following:

The wide use of TiO2 particles in food and the high exposure risk to children have prompted research into the health risks of TiO2. We used the microbiome and targeted metabolomics to explore the potential mechanism of intestinal toxicity of foodborne TiO2 micro-/nanoparticles after oral exposure for 28 days in juvenile mice. Results showed that the gut microbiota-including the abundance of Bacteroides, Bifidobacterium, Lactobacillus, and Prevotella-changed dynamically during exposure. The organic inflammatory response was activated, and lipopolysaccharide levels increased. Intestinal toxicity manifested as increased mucosal permeability, impaired intestinal barrier, immune damage, and pathol. changes. The expression of antimicrobial peptides, occludin, and ZO-1 significantly reduced, while that of JNK2 and Src/pSrc increased. Compared with micro-TiO2 particles, the nano-TiO2 particles had strong toxicity. Fecal microbiota transplant confirmed the key role of gut microbiota in intestinal toxicity. The levels of gut microbiota-host co-metabolites, including pyroglutamic acid, L-glutamic acid, phenylacetic acid, and 3-hydroxyphenylacetic acid, changed significantly. Significant changes were observed in the glutathione and propanoate metabolic pathways. There was a significant correlation between the changes in gut microbiota, metabolites, and intestinal cytokine levels. These, together with the intestinal barrier damage signaling pathway, constitute the network mechanism of the intestinal toxicity of TiO2 particles. The experimental process involved the reaction of 3-Hydroxyphenylacetic acid(cas: 621-37-4).Safety of 3-Hydroxyphenylacetic acid

The Article related to gut microbiota disorder intestinal barrier damage toxicity microparticle nanoparticle, titanium dioxide pyroglutamic phenylacetic acid juvenile, biomarker, correlation, fecal transplant, gut microbiome, tio(2) microparticle, tio(2) nanoparticle and other aspects.Safety of 3-Hydroxyphenylacetic acid

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