Tag: 100-200

The author of 《Enzymatic degradation of fluorinated Poly(ε-caprolactone) (PCL) block copolymer films with improved hydrophobicity》 were Liu, Qun; Wang, Haipeng; Chen, Lei; Li, Wulong; Zong, Yakun; Sun, Yi; Li, Zhanxiong. And the article was published in Polymer Degradation and Stability in 2019. COA of Formula: C6H15NO The author mentioned the following in the article:

Fluorinated Poly(ε-caprolactone) (PCL) block copolymers PCL-PTFOA(2 h), PCL-PTFOA(4 h), PCL-PTFOA(6 h), PCL-PTFOA(8 h) were prepared via esterification by using poly(1H,1H,2H,2H-perfluorooctylacrylate) (PTFOA) with different mol. weights as reactants. It was found that PCL-PTFOA(6 h) and PCL-PTFOA(8 h) possessed the similar mol. weight via GPC anal. PCL and fluorinated PCL block copolymers films were prepared by solution casting method. The structure and properties of film surface of the fluorinated PCL block copolymers were analyzed by energy dispersive X-ray spectrometer (EDS), scanning electron microscope (SEM), Differential scanning calorimetry (DSC), water contact angles (WCAs) and the surface free energy. The results showed that the fluorinated PCL films possessed improved hydrophobicity because of the microphase separation between fluoropolymer chain and PCL chain. The enzymic degradation of PCL, PCL-PTFOA(2 h), PCL-PTFOA(4 h) and PCL-PTFOA(6 h) films were performed at 37 °C in a phosphate buffer solution (PBS, 0.1 M, with a pH of 7.2-7.4) with lipase and analyzed by weight loss, SEM and EDS. It was found that the introduction of fluorine-containing segment reduced the rate of enzymic degradation of the copolymer film in the early period, while increased the finally weight loss rate with a prolonged time. In addition, the enzymic degradation rate of PCL-PTFOA(2 h) film and PCL-PTFOA(4 h) film was faster than that of PCL-PTFOA(6 h) film. The experimental part of the paper was very detailed, including the reaction process of 6-Aminohexan-1-ol(cas: 4048-33-3COA of Formula: C6H15NO)

6-Aminohexan-1-ol(cas: 4048-33-3) may be used along with glutaric acid to generate poly(ester amide)s with excellent film- and fiber forming properties. It can undergo cyclization over copper supported on γ-alumina and magnesia to form hexahydro-1H-azepine.COA of Formula: C6H15NO

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In 2019,Medicinal Chemistry Research included an article by Khan, Ayesha; Khan, Ajmal; Farooq, Umar; Taha, Muhammad; Shah, Syed Adnan Ali; Halim, Sobia Ahsan; Akram, Arfa; Khan, Mohammed Ziauddin; Jan, Abdul Khaliq; Al-Harrasi, Ahmed. Quality Control of 3,5-Dihydroxybenzaldehyde. The article was titled 《Oxindole-based chalcones: synthesis and their activity against glycation of proteins》. The information in the text is summarized as follows:

Diabetes mellitus, a metabolic disorder, is characterized by a substantial hyperglycemia. Prevalence of hyperglycemia for longer period of time can cause nonenzymic condensation of sugar in blood with amino group of protein and give rise to advanced glycation end products (AGEs). AGEs play a major role in the onset of late diabetic complications including diabetic retinopathy, nephropathy, neuropathy and cardiovascular diseases. There is a need to establish potential therapeutic regimens that can effectively inhibit the formation of AGEs. To this end a series of novel oxindole-based chalcones have been investigated for their antiglycation potential. Analogs 1 (IC50 = 155.22 ± 2.98 μM), 3 (IC50 = 195.95 ± 0.43 μM), 4 (IC50 = 289.47 ± 2.47 μM), 5 (IC50 = 222.44 ± 4.03 μM), 7 (IC50 = 251.27 ± 2.80 μM), and 20 (224.23 ± 1.93 μM) showed potent inhibitory activity against glycation compared to the reference Rutin (IC50 = 294.5 ± 1.5 μM). These results reveal that multiple hydroxyl substituents and their position on the aromatic ring play a key role in inhibitory effect due to their hydrogen bonding potential. The study also reveals the influence of substituents on the binding capabilities and in turn inhibitory potential of different analogs.3,5-Dihydroxybenzaldehyde(cas: 26153-38-8Quality Control of 3,5-Dihydroxybenzaldehyde) was used in this study.

3,5-Dihydroxybenzaldehyde(cas: 26153-38-8) is used as a building block in the synthesis of more complex structures. It is also used in the synthesis of terbutaline, which is an important bronchodilator.Quality Control of 3,5-Dihydroxybenzaldehyde

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In 2019,Chemistry – A European Journal included an article by Zheng, Lu; Zhan, Yulin; Ye, Lin; Zheng, Dan; Wang, Ying; Zhang, Kun; Jiang, Hua. SDS of cas: 126456-43-7. The article was titled 《Chiral Induction and Remote Chiral Communication in Quinoline Oligoamide Foldamers for Determination of Enantiomeric Excess and Absolute Configuration of Chiral Amines and Their Derivatives》. The information in the text is summarized as follows:

Two pentameric foldamers, Q5 (I) and Q5C-S (II), containing a C-F bond were synthesized based on quinoline oligamide foldamers for the measurement of enantiomeric excess and for the determination of absolute configuration of chiral amines, diamines, amino alcs., and α-amino acid esters. Chiral induction of Q5 was triggered in situ when the chiral analytes reacted with the C-F bond in Q5 by a N-nucleophilic substitution reaction, leading to a linear correlation between the CD amplitude at the region of quinoline chromophores and the ee values of the chiral analytes, which can be used for the ee determination of chiral analytes. Furthermore, the CD intensity of Q5C-S containing a chiral motif at its C-terminus enhances via remote, favorable chiral communication when the chiral induction was triggered in situ by chiral analytes at the N-terminus matches the original helicity of Q5C-S, but decreases via remote, conflicted chiral communication when the chiral induction is triggered in situ by chiral mols. at the N-terminus mismatches the original one. The system can thus be used for determination of the absolute configuration of chiral analytes, given that the chirality of the chiral motif at the C-terminus of Q5C-S is known. In the experimental materials used by the author, we found (1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol(cas: 126456-43-7SDS of cas: 126456-43-7)

(1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol(cas: 126456-43-7) belongs to anime. Amines have a free lone pair with which they can coordinate to metal centers. Amine–metal bonds are weaker because amines are incapable of backbonding, but they are still important for sensing applications.While stronger than hydrogen bonds, amine–metal bonds are still weaker than both covalent and ionic bonds.SDS of cas: 126456-43-7

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In 2019,Advanced Synthesis & Catalysis included an article by Oh, Hyunseok; Park, Areum; Jeong, Kyu-Sung; Han, Soo Bong; Lee, Hyuk. COA of Formula: C6H12O. The article was titled 《Copper-Catalyzed 1,2-Bistrifluoromethylation of Terminal Alkenes》. The information in the text is summarized as follows:

The catalytic 1,2-bistrifluoromethylations of alkenes catalyzed by Copper (Cu) have been reported. Two CF3 sources have been used, namely Umemoto’s reagent and (trifluoromethyl)trimethylsilane (TMSCF3). Each reagent plays a unique role during this transformation; Umemoto’s reagent generates CF3 radicals, while TMSCF3 is used to form CF3 anions. Copper (I) bromide (CuBr) exhibited the best catalytic activity for this reaction. CuBr oxidizes the alkyl radical, which is produced by the addition of CF3 radical to the alkenes R(CH2)nCH2=CH2 (Ar = 4-acetamidophenoxy, 3-methylphenoxy, phthalimido, (4-methylbenzene)sulfonamido, 4-formylphenoxy, etc.; n = 1, 2, 3, 4) to the corresponding alkyl cation, which then reacts with the CF3 anion from TMSCF3 to produce the desired products R(CH2)nCH(CF3)CH2CF3. This reaction tolerates a diverse set of substrates bearing functional groups such as amides, esters, ethers, ketones, protected amines, tertiary amines, and phthalimides, hence making this transformation to be widely applicable to a wide variety of substrates. After reading the article, we found that the author used 5-Hexen-1-ol(cas: 821-41-0COA of Formula: C6H12O)

5-Hexen-1-ol(cas: 821-41-0) is a volatile organic compound. Further, it is used to prepare 6-bromo-hex-1-ene by reaction with phosphorus tribromide.COA of Formula: C6H12O

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In 2018,Jiang, Fen; Guo, An-ping; Xu, Jia-chen; You, Qi-Dong; Xu, Xiao-Li published 《Discovery of a Potent Grp94 Selective Inhibitor with Anti-Inflammatory Efficacy in a Mouse Model of Ulcerative Colitis》.Journal of Medicinal Chemistry published the findings.Product Details of 27489-62-9 The information in the text is summarized as follows:

As the endoplasmic reticulum paralog of Hsp90, Grp94 chaperones a small set of client proteins associated with some diseases, including cancer, primary open-angle glaucoma, and inflammatory disorders. Grp94-selective inhibition has been a potential therapeutic strategy for these diseases. In this study, inspired by the conclusion that ligand-induced “”Phe199 shift”” effect is the structural basis of Grp94-selective inhibition, a series of novel Grp94 selective inhibitors incorporating “”benzamide”” moiety were developed, among which compound I manifested the most potent Grp94 inhibitory activity with an IC50 value of 2 nM and over 1000-fold selectivity to Grp94 against Hsp90α. In a DSS-induced mouse model of ulcerative colitis (UC), compound I exhibited significant anti-inflammatory efficacy. This work provides a potent Grp94 selective inhibitor as probe compound for the biol. study of Grp94 and represents the first study that confirms the potential therapeutic efficacy of Grp94-selective inhibitors against UC. In the experiment, the researchers used trans-4-Aminocyclohexanol(cas: 27489-62-9Product Details of 27489-62-9)

trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. The methylamines occur in small amounts in some plants. Many polyfunctional amines (i.e., those having other functional groups in the molecule) occur as alkaloids in plants—for example, mescaline, 2-(3,4,5-trimethoxyphenyl)ethylamine; the cyclic amines nicotine, atropine, morphine, and cocaine; and the quaternary salt choline, N-(2-hydroxyethyl)trimethylammonium chloride, which is present in nerve synapses and in plant and animal cells.Product Details of 27489-62-9

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In 2013,Zhang, Lei; Villalobos, Anabella; Beck, Elizabeth M.; Bocan, Thomas; Chappie, Thomas A.; Chen, Laigao; Grimwood, Sarah; Heck, Steven D.; Helal, Christopher J.; Hou, Xinjun; Humphrey, John M.; Lu, Jiemin; Skaddan, Marc B.; McCarthy, Timothy J.; Verhoest, Patrick R.; Wager, Travis T.; Zasadny, Kenneth published 《Design and Selection Parameters to Accelerate the Discovery of Novel Central Nervous System Positron Emission Tomography (PET) Ligands and Their Application in the Development of a Novel Phosphodiesterase 2A PET Ligand》.Journal of Medicinal Chemistry published the findings.Synthetic Route of C3H8ClNO The information in the text is summarized as follows:

To accelerate the discovery of novel small mol. central nervous system (CNS) positron emission tomog. (PET) ligands, we aimed to define a property space that would facilitate ligand design and prioritization, thereby providing a higher probability of success for novel PET ligand development. Toward this end, we built a database consisting of 62 PET ligands that have successfully reached the clinic and 15 radioligands that failed in late-stage development as neg. controls. A systematic anal. of these ligands identified a set of preferred parameters for physicochem. properties, brain permeability, and nonspecific binding (NSB). These preferred parameters have subsequently been applied to several programs and have led to the successful development of novel PET ligands with reduced resources and timelines. This strategy is illustrated here by the discovery of the novel phosphodiesterase 2A (PDE2A) PET ligand 4-(3-[18F]fluoroazetidin-1-yl)-7-methyl-5-{1-methyl-5-[4-(trifluoromethyl)phenyl]-1H-pyrazol-4-yl}imidazo[5,1-f][1,2,4]triazine, [18F]PF-05270430 (5). In addition to this study using Azetidin-3-ol hydrochloride, there are many other studies that have used Azetidin-3-ol hydrochloride(cas: 18621-18-6Synthetic Route of C3H8ClNO) was used in this study.

Azetidin-3-ol hydrochloride(cas:18621-18-6) is one of azetidine.Azetidines (azacyclobutanes) constitute a well-known class of heterocyclic compounds. Azetidine scaffold has been discovered in several natural products.Synthetic Route of C3H8ClNO Several pharmacologically important synthetic compounds also contain azetidine ring. Because of inherent ring strain, the synthesis of azetidines is a challenging endeavor.

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In 1990,Archibald, T. G.; Baum, K.; Garver, L. C. published 《Synthesis of N-nitroazetidines》.Synthetic Communications published the findings.Recommanded Product: Azetidin-3-ol hydrochloride The information in the text is summarized as follows:

Direct nitrolysis of 3-substituted azetidine hydrochlorides with acetyl nitrate gives cyclic nitramines I (R = ONO2, O3SMe, CO2H). In the experiment, the researchers used Azetidin-3-ol hydrochloride(cas: 18621-18-6Recommanded Product: Azetidin-3-ol hydrochloride)

Azetidin-3-ol hydrochloride(cas:18621-18-6) is one of azetidine.Azetidines (azacyclobutanes) constitute a well-known class of heterocyclic compounds. Azetidine scaffold has been discovered in several natural products.Recommanded Product: Azetidin-3-ol hydrochloride Several pharmacologically important synthetic compounds also contain azetidine ring. Because of inherent ring strain, the synthesis of azetidines is a challenging endeavor.

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Alcohol – Wikipedia,
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On February 29, 2012, Koide, Haruki; Narasaki, Ritsuko; Hasegawa, Keiko; Nishimura, Naoko; Hasumi, Keiji published an article.Related Products of 32462-30-9 The title of the article was A new series of the SMTP plasminogen modulator with a phenylglycine-based side chain. And the article contained the following:

Our previous studies established fermentation conditions that enable efficient production of an SMTP (Stachybotrys microspora tripenyl phenols) congener through feeding of a precursor amine to S. microspora. In this study, we isolated five new SMTP congeners with a phenylglycine-based side chain to investigate structure-activity relationships further. This paper deals with the isolation and characterization of these congeners. A culture fed with an optically active precursor afforded single major product (SMTP-43, -43D, -44, or -44D), whereas a culture fed with racemic 3-hydroxy-D,L-phenylglycine gave two major products, which were separable each other on reversed-phase HPLC. SMTP-43, which had an L-2-phenylglycine moiety as the N-linked side chain, was potent in enhancing plasminogen activation. The experimental process involved the reaction of H-Phg(4-OH)-OH(cas: 32462-30-9).Related Products of 32462-30-9

The Article related to stachybotrys microspora tripenyl phenol fermentation plasminogen modulator sar, Pharmacology: Structure-Activity and other aspects.Related Products of 32462-30-9

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On January 1, 2010, Wang, Haofan; Byun, Youngjoo; Barinka, Cyril; Pullambhatla, Mrudula; Bhang, Hyo-eun C.; Fox, James J.; Lubkowski, Jacek; Mease, Ronnie C.; Pomper, Martin G. published an article.Synthetic Route of 32462-30-9 The title of the article was Bioisosterism of urea-based GCPII inhibitors: Synthesis and structure-activity relationship studies. And the article contained the following:

We report a strategy based on bioisosterism to improve the physicochem. properties of existing hydrophilic, urea-based GCPII inhibitors. Comprehensive structure-activity relation studies of the P1′ site of ZJ-43- and DCIBzL-based compounds identified several glutamate-free inhibitors with Ki values below 20 nM. Among them, compound 32d (Ki = 11 nM) exhibited selective uptake in GCPII-expressing tumors by SPECT-CT imaging in mice. A novel conformational change of amino acids in the S1′ pharmacophore pocket was observed in the x-ray crystal structure of GCPII complexed with 32d. The experimental process involved the reaction of H-Phg(4-OH)-OH(cas: 32462-30-9).Synthetic Route of 32462-30-9

The Article related to gcpii inhibitor urea derivative bioisosterism preparation structure activity, Pharmacology: Structure-Activity and other aspects.Synthetic Route of 32462-30-9

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On May 28, 2015, Duan, Wenwen; Li, Jin; Inks, Elizabeth S.; Chou, C. James; Jia, Yuping; Chu, Xiaojing; Li, Xiaoyang; Xu, Wenfang; Zhang, Yingjie published an article.Computed Properties of 78-26-2 The title of the article was Design, Synthesis, and Antitumor Evaluation of Novel Histone Deacetylase Inhibitors Equipped with a Phenylsulfonylfuroxan Module as a Nitric Oxide Donor. And the article contained the following:

On the basis of the strategy of creating multifunctional drugs, a novel series of phenylsulfonylfuroxan-based hydroxamates with histone deacetylase (HDAC) inhibitory and nitric oxide (NO) donating activities were designed, synthesized, and evaluated. The most potent NO donor-HDAC inhibitor (HDACI) hybrid, 5c, exhibited a much greater in vitro antiproliferative activity against the human erythroleukemia (HEL) cell line than that of the approved drug SAHA (Vorinostat), and its antiproliferative activity was diminished by the NO scavenger Hb in a dose-dependent manner. Further mechanism studies revealed that 5c strongly induced cellular apoptosis and G1 phase arrest in HEL cells. Animal experiment identified 5c as an orally active agent with potent antitumor activity in a HEL cell xenograft model. Interestingly, although compound 5c was remarkably HDAC6-selective at the mol. level, it exhibited pan-HDAC inhibition in a western blot assay, which is likely due to class I HDACs inhibition caused by NO release at the cellular level. The experimental process involved the reaction of 2-Methyl-2-propylpropane-1,3-diol(cas: 78-26-2).Computed Properties of 78-26-2

The Article related to phenylsulfonyl furoxan hydroxamate preparation histone deacetylase no cancer, Pharmacology: Structure-Activity and other aspects.Computed Properties of 78-26-2

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