Ilhan, Zehra Esra et al. published their research in Neurobiology of Disease in 2022 |CAS: 585-88-6

The Article related to carbamazepine lamotrigine topiramate antiseizure agent gut bacteria epilepsy, anaerobic metabolism, antiepileptic drugs, drug formulations, epilepsy, intestinal epithelial cells, microbiome, parabens, pharmaco-resistance, seizures, toxicity and other aspects.Electric Literature of 585-88-6

On June 1, 2022, Ilhan, Zehra Esra; Brochard, Vincent; Lapaque, Nicolas; Auvin, Stephane; Lepage, Patricia published an article.Electric Literature of 585-88-6 The title of the article was Exposure to anti-seizure medications impact growth of gut bacterial species and subsequent host response. And the article contained the following:

Anti-seizure medications (ASMs) are the first line of treatment for seizure control in children with epilepsy. Cumulative evidence suggests an imbalanced gut microbiota in refractory epilepsy patients. We systematically investigated the differential antimicrobial impacts of nine ASM active ingredients, seven common excipients of ASMs, and four syrup formulations on core early-life gut microbiota strains. Addnl., we evaluated the toxicity and gene expression profiles of HT-29 colon epithelial cells when exposed to active ingredients with or without bacterial supernatants. The physicochem. structure of ASM active ingredients and bacterial phylogeny were found to be related to ASM toxicity. Carbamazepine, lamotrigine, and topiramate reduced the growth of more than ten strains along with syrup excipient propyl-paraben. Various artificial sweeteners present in ASM formulations stimulated the growth of gut bacterial strains. The active ingredients that were more toxic to bacterial strains also exhibited toxicity towards HT-29 cells, yet Bifidobacterium longum supernatant reduced cytotoxic effects of carbamazepine and lamotrigine. Akkermansia muciniphila or mixed community supernatants reduced the expression of drug resistance genes in HT-29 cell lines. In summary, our results indicate that several ASM active ingredients and their excipients regulate the growth of gut bacterial strains in a species-specific manner. Interactions between ASMs and gut epithelial cells might be modulated by gut microbial metabolites. The experimental process involved the reaction of SweetPearlR P300 DC Maltitol(cas: 585-88-6).Electric Literature of 585-88-6

The Article related to carbamazepine lamotrigine topiramate antiseizure agent gut bacteria epilepsy, anaerobic metabolism, antiepileptic drugs, drug formulations, epilepsy, intestinal epithelial cells, microbiome, parabens, pharmaco-resistance, seizures, toxicity and other aspects.Electric Literature of 585-88-6

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Yuan, Li-Ming et al. published their research in Chirality in 2017 |CAS: 32462-30-9

The Article related to chiral separation enantioselectivity cellulose sodium alginate hydroxypropyl beta cyclodextrin, cellulose, chiral separation, enantioselective membrane, hydroxypropyl-β-cyclodextrin, optical resolution mechanism of membrane, sodium alginate and other aspects.Computed Properties of 32462-30-9

Yuan, Li-Ming; Ma, Wei; Xu, Mei; Zhao, Hui-Lin; Li, Yuan-Yuan; Wang, Rui-Lin; Duan, Ai-Hong; Ai, Ping; Chen, Xue-Xian published an article in 2017, the title of the article was Optical resolution and mechanism using enantioselective cellulose, sodium alginate and hydroxypropyl-β-cyclodextrin membranes.Computed Properties of 32462-30-9 And the article contains the following content:

Chiral solid membranes of cellulose, sodium alginate, and hydroxypropyl-β-cyclodextrin were prepared for chiral dialysis separations After optimizing the membrane material concentrations, the membrane preparation conditions and the feed concentrations, enantiomeric excesses of 89.1%, 42.6%, and 59.1% were obtained for mandelic acid on the cellulose membrane, p-hydroxy phenylglycine on the sodium alginate membrane, and p-hydroxy phenylglycine on the hydroxypropyl-β-cyclodextrin membrane, resp. To study the optical resolution mechanism, chiral discrimination by membrane adsorption, solid phase extraction, membrane chromatog., high-pressure liquid chromatog. ultrafiltration were performed. All of the exptl. results showed that the first adsorbed enantiomer was not the enantiomer that first permeated the membrane. The crystal structures of mandelic acid and p-hydroxy phenylglycine are the racematic compounds We suggest that the chiral separation mechanism of the solid membrane is “adsorption – association – diffusion,” which is able to explain the optical resolution of the enantioselective membrane. This is also the first report in which solid membranes of sodium alginate and hydroxypropyl-β-cyclodextrin were used in the chiral separation of p-hydroxy phenylglycine. The experimental process involved the reaction of H-Phg(4-OH)-OH(cas: 32462-30-9).Computed Properties of 32462-30-9

The Article related to chiral separation enantioselectivity cellulose sodium alginate hydroxypropyl beta cyclodextrin, cellulose, chiral separation, enantioselective membrane, hydroxypropyl-β-cyclodextrin, optical resolution mechanism of membrane, sodium alginate and other aspects.Computed Properties of 32462-30-9

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Johansson, Rolf et al. published their patent in 2008 |CAS: 87674-15-5

The Article related to pyrimidinone pyridinylethylthio hydroxymethylalkylamino thiazolo derivative preparation nervous system disease, pyridinylethylthio hydroxymethylalkylamino thiazolopyrimidinone derivative preparation atherosclerosis multiple sclerosis asthma and other aspects.Synthetic Route of 87674-15-5

On April 3, 2008, Johansson, Rolf; Karlstroem, Sofia; Kers, Annika; Nordvall, Gunnar; Rein, Tobias; Slivo, Can published a patent.Synthetic Route of 87674-15-5 The title of the patent was Preparation of [(pyridinyl)ethyl]thio[(hydroxymethyl)alkyl]amino[1,3]thiazolo[4,5-d]pyrimidinone derivatives for use as therapeutic agents. And the patent contained the following:

Title compounds I [R1 = Me or CF3; R2 = halo, CN, or alkyl; R3 and R4 independently = H or Me; n = 0 to 2], and their pharmaceutically acceptable salts, are prepared and disclosed as therapeutic agents. Thus, e.g., II was prepared by oxidation of (2R)-2-[[5-[[(1S)-1-(5-chloropyridin-2-yl)ethyl]thio]-2-methoxy[1,3]thiazolo[4,5-d]pyrimidin-7-yl]amino]-4-methylpentan-1-ol (preparation given). Select I were evaluated in recombinant human fractalkine hCX3CR1 binding assay, e.g., II demonstrated a Ki value of 5.8 (nM). Title compounds I are disclosed as therapeutic agents of neurodegenerative disorders, demyelinating disease, cardio- and cerebrovascular atherosclerotic disorders, peripheral artery disease, rheumatoid arthritis, pulmonary diseases such as COPD, asthma or pain. The experimental process involved the reaction of 1-(3-Fluoropyridin-4-yl)ethanol(cas: 87674-15-5).Synthetic Route of 87674-15-5

The Article related to pyrimidinone pyridinylethylthio hydroxymethylalkylamino thiazolo derivative preparation nervous system disease, pyridinylethylthio hydroxymethylalkylamino thiazolopyrimidinone derivative preparation atherosclerosis multiple sclerosis asthma and other aspects.Synthetic Route of 87674-15-5

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Velikorodov, A. V. et al. published their research in Russian Journal of Organic Chemistry in 2021 |CAS: 96-76-4

The Article related to disubstituted indene dione preparation, phenylcarbamate ninhydrin sulfuric acid condensation, indenobenzofuran preparation, ninhydrin phenol acetic acid condensation, benzodiazocine preparation, ethylenediamine indenobenzofuran condensation and other aspects.HPLC of Formula: 96-76-4

On April 30, 2021, Velikorodov, A. V.; Stepkina, N. N.; Osipova, V. P.; Zukhairaeva, A. S.; Shustova, E. A. published an article.HPLC of Formula: 96-76-4 The title of the article was Synthesis of New Functionally Substituted Indenes, Benzofurans and 2,5-Benzodiazocin-1(2H)-ones. And the article contained the following:

The synthesis of new functionally substituted 1H-indene-1,3(2H)-diones, such as I [R = pyridin-2-yl, morpholin-4-yl] indenobenzofurans II [R1 = 1-adamantyl, t-Bu; R2 = Me, t-Bu] and 2,5-benzodiazocines III [R3 = H, t-Bu, NHCO2Me, 1-adamantyl; R4 = H, NHCO2Me; R5 = H, Me, t-Bu, NHCO2Me] was described. The condensations of ninhydrin in concentrated sulfuric acid with 2-(morpholin-4-yl)ethyl and 2-(pyridin-2-yl)ethyl phenylcarbamates at 20°C and with 2,6-di-tert-butylphenol while gradually raising temperature from 0 to 20°C gave corresponding 2,2-disubstituted 1H-indene-1,3(2H)-diones such as I in 62-89% yields. The indeno[1,2-b]benzofuran derivatives II were obtained with high yields (96-98%) by heating ninhydrin with 2-(1-adamantyl)-4-methylphenol and 2,4-di(tert-butyl)phenol, resp., in glacial acetic acid at 60°C. Benzofurans containing an adamantyl, tert-Bu, or carbamate fragment reacted with 99% ethylenediamine at 20°C to afford 80-85% of new 2,5-benzodiazocine derivatives III. The experimental process involved the reaction of 2,4-Di-tert-butylphenol(cas: 96-76-4).HPLC of Formula: 96-76-4

The Article related to disubstituted indene dione preparation, phenylcarbamate ninhydrin sulfuric acid condensation, indenobenzofuran preparation, ninhydrin phenol acetic acid condensation, benzodiazocine preparation, ethylenediamine indenobenzofuran condensation and other aspects.HPLC of Formula: 96-76-4

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Etoga, Jean-Louis G. et al. published their research in Bioorganic & Medicinal Chemistry Letters in 2010 |CAS: 32462-30-9

The Article related to glutamate uptake vglut inhibitor amino acid preparation, vesicular glutamate transporter inhibiting structure activity amino acid, phenylglycine aminothiophene sulfonic acid analog preparation, amino acid hydrolysis sulfonation sulfuric acid and other aspects.Recommanded Product: 32462-30-9

On April 15, 2010, Etoga, Jean-Louis G.; Ahmed, S. Kaleem; Patel, Sarjubhai; Bridges, Richard J.; Thompson, Charles M. published an article.Recommanded Product: 32462-30-9 The title of the article was Conformationally-restricted amino acid analogues bearing a distal sulfonic acid show selective inhibition of system Xc- over the vesicular glutamate transporter. And the article contained the following:

A panel of amino acid analogs and conformationally-restricted amino acids bearing a sulfonic acid were synthesized and tested for their ability to preferentially inhibit the obligate cysteine-glutamate transporter system X-c vs. the vesicular glutamate transporter (VGLUT). Several promising candidate mols. were identified: R/S-4-[4′-carboxyphenyl]-phenylglycine, a biphenyl substituted analog of 4-carboxyphenylglycine and 2-thiopheneglycine-5-sulfonic acid both of which reduced glutamate uptake at system X-c – by 70-75% while having modest to no effect on glutamate uptake at VGLUT. The experimental process involved the reaction of H-Phg(4-OH)-OH(cas: 32462-30-9).Recommanded Product: 32462-30-9

The Article related to glutamate uptake vglut inhibitor amino acid preparation, vesicular glutamate transporter inhibiting structure activity amino acid, phenylglycine aminothiophene sulfonic acid analog preparation, amino acid hydrolysis sulfonation sulfuric acid and other aspects.Recommanded Product: 32462-30-9

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

The Article related to copper iron manganese alkoxo butyldiethanolamine pivalate complex preparation magnetism, oxidation catalyst copper iron manganese alkoxo butyldiethanolamine pivalate, crystal structure copper iron manganese alkoxo butyldiethanolamine pivalate and other aspects.Product Details of 2160-93-2

Nesterova, Oksana V.; Nesterov, Dmytro S.; Vranovicova, Beata; Boca, Roman; Pombeiro, Armando J. L. published an article in 2018, the title of the article was Heterometallic CuIIFeIII and CuIIMnIII alkoxo-bridged complexes revealing a rare hexanuclear M6(μ-X)7(μ3-X)2 molecular core.Product Details of 2160-93-2 And the article contains the following content:

The novel hexanuclear complexes [Cu4Fe2(OH)(Piv)4(tBuDea)4Cl]·0.5CH3CN (1) and [Cu4Mn2(OH)(Piv)4(tBuDea)4Cl] (2) were prepared through one-pot self-assembly reactions of copper powder and iron(II) or manganese(II) chloride with N-tert-butyldiethanolamine (H2tBuDea) and pivalic acid (HPiv) in acetonitrile. Crystallog. studies revealed the uncommon mol. core type M6(μ-X)7(μ3-X)2 in 1 and 2, which can be viewed as a combination of two trimetallic M3(μ-X)2(μ3-X) fragments joined by three bridging atoms. The anal. and classification of the hexanuclear complexes having a M3(μ-X)2(μ3-X) moiety as a core forming fragment using data from the Cambridge Structural Database (CSD) were performed. Variable-temperature (1.8-300 K) magnetic susceptibility measurements of 1 showed a decrease of the effective magnetic moment value at low temperature, indicative of antiferromagnetic coupling between the magnetic centers (JFe-Cu/hc = -6.9 cm-1, JCu-Cu/hc = -4.1 cm-1, JFe-Fe/hc = -24.2 cm-1). Complex 1 acts as a catalyst in the reaction of mild oxidation of cyclohexane with H2O2, showing the yields of products, cyclohexanol and cyclohexanone, up to 17% using pyrazinecarboxylic acid as a promoter. In the oxidation of cis-1,2-dimethylcyclohexane with m-chloroperoxybenzoic acid (m-CPBA), 70% of retention of stereoconfiguration was observed for tertiary alcs. Compound 1 also catalyzes the amidation of cyclohexane with benzamide. In all three catalytic reactions the byproducts were investigated in detail and discussed. The experimental process involved the reaction of 2,2′-(tert-Butylazanediyl)diethanol(cas: 2160-93-2).Product Details of 2160-93-2

The Article related to copper iron manganese alkoxo butyldiethanolamine pivalate complex preparation magnetism, oxidation catalyst copper iron manganese alkoxo butyldiethanolamine pivalate, crystal structure copper iron manganese alkoxo butyldiethanolamine pivalate and other aspects.Product Details of 2160-93-2

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Pagano, Sandro et al. published their research in Chemistry – A European Journal in 2009 |CAS: 78-26-2

The Article related to europium cyanate urea complex preparation structure thermal decomposition, strontium cyanate urea complex preparation thermal decomposition, luminescence europium cyanate urea complex, crystal structure europium strontium cyanate urea complex and other aspects.Safety of 2-Methyl-2-propylpropane-1,3-diol

Pagano, Sandro; Montana, Giuseppe; Wickleder, Claudia; Schnick, Wolfgang published an article in 2009, the title of the article was Urea Route to Homoleptic Cyanates-Characterization and Luminescence Properties of [M(OCN)2(urea)] and M(OCN)2 with M = Sr, Eu.Safety of 2-Methyl-2-propylpropane-1,3-diol And the article contains the following content:

A novel approach for the synthesis of urea complexes and homoleptic cyanates of alk. earth metals and Eu is described. The compounds were fully characterized, including their magnetism and temperature-dependent luminescence properties. A novel approach for the synthesis of urea complexes and homoleptic cyanates of alk. earth metals and Eu is described. Direct reaction of urea with elemental Sr or Eu in closed ampuls at temperatures >120° yields [M(OCN)2(urea)] with M = Sr, Eu. According to single-crystal x-ray diffraction, the isotypic complexes exhibit a layer structure ([Eu(OCN)2(urea)]: space group P21/c, a 7.826(2), b 7.130(1), c 12.916(3) Å, β 99.76(3)°, Z = 4). Also, they were characterized by vibrational spectroscopy, thermal anal., magnetic measurements, and photoluminescence studies. Thermal treatment of [M(OCN)2(urea)] to 160-240° affords evaporation of urea and the subsequent formation of solvent-free homoleptic cyanates of Sr and Eu. The crystal structures of Sr(OCN)2 and Eu(OCN)2 were determined from x-ray powder diffraction data and refined by the Rietveld method. Both compounds crystallize in the orthorhombic space group Fddd and adopt the Sr(N3)2 type structure (Sr(OCN)2: a 6.1510(4), b 11.268(1), c 11.848(1) Å; Eu(OCN)2: a 6.1514(6), b 11.2863(12), c 11.8201(12) Å). The cyanates are stable up to 450°. Above 500° β-Sr(CN)2 and Eu2O2(CN)2 are formed. Excitation and emission spectra of [Eu(OCN)2(urea)], [Sr(OCN)2(urea)]:Eu2+, Eu(OCN)2, Sr(OCN)2:Eu2+ at different temperatures are reported. A strong green emission for all examined Eu-containing compounds due to a 4f6 5d1-4f7 transition is observed at low temperatures The luminescence properties are discussed in detail and are comparable to those of thiocyanates. Compared to the latter, a blue shift of the emission bands is observed due to the higher ionicity. The experimental process involved the reaction of 2-Methyl-2-propylpropane-1,3-diol(cas: 78-26-2).Safety of 2-Methyl-2-propylpropane-1,3-diol

The Article related to europium cyanate urea complex preparation structure thermal decomposition, strontium cyanate urea complex preparation thermal decomposition, luminescence europium cyanate urea complex, crystal structure europium strontium cyanate urea complex and other aspects.Safety of 2-Methyl-2-propylpropane-1,3-diol

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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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Friis, Ulrik F. et al. published their research in Contact Dermatitis in 2013 |CAS: 4719-04-4

The Article related to allergic contact dermatitis allergen occupational allergy, allergens, exposure analysis, occupational, occupational allergic contact dermatitis, occupational contact allergy, systematic exposure assessment, systematic stepwise exposure assessment and other aspects.Related Products of 4719-04-4

On September 30, 2013, Friis, Ulrik F.; Menne, Torkil; Flyvholm, Mari-Ann; Bonde, Jens Peter E.; Johansen, Jeanne D. published an article.Related Products of 4719-04-4 The title of the article was Occupational allergic contact dermatitis diagnosed by a systematic stepwise exposure assessment of allergens in the work environment. And the article contained the following:

Background. Information on the presence of contact allergens and irritants is crucial for the diagnosis of occupational contact dermatitis. Ingredient lists and Material Safety Datasheets (MSDSs) may be incomplete. Objectives. To evaluate the workability of a systematic exposure assessment in consecutive patients with suspected occupational contact dermatitis, and to study how it could potentially aid correct diagnostic classification. Methods. A tool for systematic stepwise assessment of exposures in the work environment was developed, consisting of six steps spanning medical history and workplace visits. The program included 228 consecutive patients diagnosed with occupational contact dermatitis: all patients underwent a clin. examination, the stepwise exposure assessment, and extensive patch and prick testing. Results. Of the participants. 48.2% were classified as having occupational allergic contact dermatitis. The diagnosis was made at the stepwise exposure assessment for 50.0% of patients at Step 1 (medical history) and for 34.5% at Step 2 (ingredient labeling/MSDS). We found 132 different occupational allergens of relevance to the patients’ eczema of these, 78.0% were allergens not included in the European baseline series. Conclusions. Systematic stepwise exposure assessment provides information that results in the identification of occupational allergies caused by allergens not included in the European baseline series in a substantial number of patients. The experimental process involved the reaction of 2,2′,2”-(1,3,5-Triazinane-1,3,5-triyl)triethanol(cas: 4719-04-4).Related Products of 4719-04-4

The Article related to allergic contact dermatitis allergen occupational allergy, allergens, exposure analysis, occupational, occupational allergic contact dermatitis, occupational contact allergy, systematic exposure assessment, systematic stepwise exposure assessment and other aspects.Related Products of 4719-04-4

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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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