Tag: 300-400

Identification of Anti-Mycobacterial Biofilm Agents Based on the 2-Aminoimidazole Scaffold was written by Nguyen, T. Vu;Minrovic, Bradley M.;Melander, Roberta J.;Melander, Christian. And the article was included in ChemMedChem in 2019.Reference of 87694-53-9 This article mentions the following:

Tuberculosis (TB) remains a significant global health problem for which new therapeutic options are sorely needed. The ability of the causative agent, Mycobacterium tuberculosis, to reside within host macrophages and form biofilm-like communities contributes to the persistent and drug-tolerant nature of the disease. Compounds that can prevent or reverse the biofilm-like phenotype have the potential to serve alongside TB antibiotics to overcome this tolerance, and decrease treatment duration. Using Mycobacterium smegmatis as a surrogate organism, the authors report the identification of two new 2-aminoimidazole compounds that inhibit and disperse mycobacterial biofilms, work synergistically with isoniazid and rifampicin to eradicate preformed M. smegmatis biofilms in vitro, are nontoxic toward Galleria mellonella, and exhibit stability in mouse plasma. In the experiment, the researchers used many compounds, for example, (S)-tert-Butyl (1-(methoxy(methyl)amino)-1-oxo-3-phenylpropan-2-yl)carbamate (cas: 87694-53-9Reference of 87694-53-9).

(S)-tert-Butyl (1-(methoxy(methyl)amino)-1-oxo-3-phenylpropan-2-yl)carbamate (cas: 87694-53-9) belongs to esters. Esters perform as high-grade solvents for a broad array of plastics, plasticizers, resins, and lacquers, and are one of the largest classes of synthetic lubricants on the commercial market. Polyesters are important plastics, with monomers linked by ester moieties. Because of their lack of hydrogen-bond-donating ability, esters do not self-associate. Consequently, esters are more volatile than carboxylic acids of similar molecular weight.Reference of 87694-53-9

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Strong inhibition of cholera toxin B subunit by affordable, polymer-based multivalent inhibitors was written by Haksar, Diksha;de Poel, Eyleen;van Ufford, Linda Quarles;Bhatia, Sumati;Haag, Rainer;Beekman, Jeffrey;Pieters, Roland J.. And the article was included in Bioconjugate Chemistry in 2019.Reference of 4163-60-4 This article mentions the following:

Cholera is a potentially fatal bacterial infection that affects a large number of people in developing countries. It is caused by the cholera toxin (CT), an AB₅ toxin secreted by Vibrio cholera. The toxin comprises a toxic A-subunit and a pentameric B-subunit that bind to the intestinal cell surface. Several monovalent and multivalent inhibitors of the toxin have been synthesized but are too complicated and expensive for practical use in developing countries. Meta-nitrophenyl 浼?galactoside (MNPG) is a known promising ligand for CT, and here mono- and multivalent compounds based on MNPG were synthesized. We present the synthesis of MNPG in greatly improved yields and its use while linked to a multivalent scaffold. We used economical polymers as multivalent scaffolds, namely, polyacrylamide, dextran, and hyperbranched polyglycerols (hPGs). Copper-catalyzed alkyne azide cycloaddition reaction (CuAAC) produced the inhibitors that were tested in an ELISA-type assay and an intestinal organoid swelling inhibition assay. The inhibitory properties varied widely depending on the type of polymer, and the most potent conjugates showed IC₅₀ values in the nanomolar range. In the experiment, the researchers used many compounds, for example, (2S,3R,4S,5S,6R)-6-(Acetoxymethyl)tetrahydro-2H-pyran-2,3,4,5-tetrayl tetraacetate (cas: 4163-60-4Reference of 4163-60-4).

(2S,3R,4S,5S,6R)-6-(Acetoxymethyl)tetrahydro-2H-pyran-2,3,4,5-tetrayl tetraacetate (cas: 4163-60-4) belongs to esters. Esters perform as high-grade solvents for a broad array of plastics, plasticizers, resins, and lacquers, and are one of the largest classes of synthetic lubricants on the commercial market. Esterification is the general name for a chemical reaction in which two reactants (typically an alcohol and an acid) form an ester as the reaction product. Esters are common in organic chemistry and biological materials.Reference of 4163-60-4

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Glycan targeted polymeric antibiotic prodrugs for alveolar macrophage infections was written by Chen, Jasmin;Su, Fang-Yi;Das, Debobrato;Srinivasan, Selvi;Son, Hye-Nam;Lee, Brian;Radella, Frank II;Whittington, Dale;Monroe-Jones, Taylor;West, T. Eoin;Convertine, Anthony J.;Skerrett, Shawn J.;Stayton, Patrick S.;Ratner, Daniel M.. And the article was included in Biomaterials in 2019.Reference of 4163-60-4 This article mentions the following:

Alveolar macrophages resident in the lung are prominent phagocytic effector cells of the pulmonary innate immune response, and paradoxically, are attractive harbors for pathogens. Consequently, facultative intracellular bacteria, such as Francisella tularensis, can cause severe systemic disease and sepsis, with high morbidity and mortality associated with pulmonary infection. Current clin. treatment, which involves exhaustive oral or i.v. antibiotic therapy, has limitations such as systemic toxicity and off-target effects. Pulmonary administration represents a promising alternative to systemic dosing for delivering antibiotics directly to the lung. Here, we present synthesized mannosylated ciprofloxacin polymeric prodrugs for efficient pulmonary delivery, targeting, and subsequent internalization by alveolar macrophages. We demonstrate significant improvement in efficacy against intracellular infections in an otherwise uniformly lethal airborne Francisella murine model (F. novicida). When administered to the lungs of mice in a prophylactic regimen, the mannosylated ciprofloxacin polymeric prodrugs led to 50% survival. In a treatment regimen that was concurrent with infection, the survival of mice increased to 87.5%. Free ciprofloxacin antibiotic was ineffective in both cases. This significant difference in antibacterial efficacy demonstrates the impact of this delivery platform based on improved physiochem., pharmacokinetic, and pharmacodynamic properties of ciprofloxacin administered via our glycan polymeric prodrug. This modular platform provides a route for overcoming the limitations of free drug and increasing efficacy in treatment of intracellular infection. In the experiment, the researchers used many compounds, for example, (2S,3R,4S,5S,6R)-6-(Acetoxymethyl)tetrahydro-2H-pyran-2,3,4,5-tetrayl tetraacetate (cas: 4163-60-4Reference of 4163-60-4).

(2S,3R,4S,5S,6R)-6-(Acetoxymethyl)tetrahydro-2H-pyran-2,3,4,5-tetrayl tetraacetate (cas: 4163-60-4) belongs to esters. Carboxylic acid esters of low molecular weight are colourless, volatile liquids with pleasant odours, slightly soluble in water. Esters are more polar than ethers but less polar than alcohols. They participate in hydrogen bonds as hydrogen-bond acceptors, but cannot act as hydrogen-bond donors, unlike their parent alcohols. This ability to participate in hydrogen bonding confers some water-solubility.Reference of 4163-60-4

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Quantitative analysis of Phthalate Esters by in-situ thermal desorption atmospheric pressure photoionization mass spectrometry using a dopant as the internal standard was written by Wang, Weimin;Jiang, Dandan;Jin, Liuyu;Wang, Pingping;Xu, Fuxing;Li, Haiyang;Ding, Chuan-Fan. And the article was included in International Journal of Mass Spectrometry in 2022.Formula: C20H26O4 This article mentions the following:

Phthalate Esters (PAEs) are a group of chems. widely used in plastic products, and they are also known as endocrine disruptors that can adversely affect the hormonal balance in humans. Since many food-contacting items, such as lunch boxes, fresh keeping film, disposable cups, are made of plastic, the PAEs can easily enter the human body through the polluted foods or drinks. Traditional anal. techniques involve laborious sample pretreatment and low-throughput anal., so it is necessary to develop techniques that can rapidly and quant. detect these compounds In this article, a miniaturized ion trap mass spectrometer (ITMS) was established firstly, then, an in-situ thermal desorption atm. pressure photoionization (in-situ TD-APPI) was designed, and the dopant was explored using for improving the sensitivity and as internal standard (IS) simultaneously in the anal. process. The in-situ TD-APPI presents good performance: (1) More than 20 times improvement in sensitivity compared with Nano-ESI for PAEs; (2) 12 kinds of phthalates were quantified with using acetone as the IS, and the LODs and LOQs ranges were found to be 0.02-1 娓璯/mL and 0.02-100 娓璯/mL, resp. The technique was also applied to the quantification of mixed solutions, and the results were validated by LC/MS. Finally, six categories of food-contacting items containing PAEs were analyzed with superficial content (ng/cm²) ranging from 0 to 6.20 ng/cm². These results demonstrate the potential of rapid quantification of anal. of PAEs in practical plastic food-contacting items by in-situ TD-APPI. In the experiment, the researchers used many compounds, for example, Dicyclohexyl phthalate (cas: 84-61-7Formula: C20H26O4).

Dicyclohexyl phthalate (cas: 84-61-7) belongs to esters. Esters are also usually derived from carboxylic acids. It may also be obtained by reaction of acid anhydride or acid halides with alcohols or by the reaction of salts of carboxylic acids with alkyl halides. Esters are more polar than ethers but less polar than alcohols. They participate in hydrogen bonds as hydrogen-bond acceptors, but cannot act as hydrogen-bond donors, unlike their parent alcohols. This ability to participate in hydrogen bonding confers some water-solubility.Formula: C20H26O4

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Synthesis and calpain inhibitory activity of 浼?ketoamides with 2,3-methanoleucine stereoisomers at the P₂ position was written by Donkor, Isaac O.;Zheng, Xiaozhang;Miller, Duane D.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2000.Related Products of 87694-53-9 This article mentions the following:

A series of novel ketoamides I, (Ph = phenyl) incorporating all four 2,3-methanoleucine stereoisomers at the P₂ position, was synthesized. The compounds displayed a wide variation in K_i values for inhibition of calpain I depending on the configuration of the P₂ methanoleucine residue. However, similar variation in cathepsin B inhibition was not observed suggesting that the S₂ pocket of calpain I is more stereosensitive than that of cathepsin B. In the experiment, the researchers used many compounds, for example, (S)-tert-Butyl (1-(methoxy(methyl)amino)-1-oxo-3-phenylpropan-2-yl)carbamate (cas: 87694-53-9Related Products of 87694-53-9).

(S)-tert-Butyl (1-(methoxy(methyl)amino)-1-oxo-3-phenylpropan-2-yl)carbamate (cas: 87694-53-9) belongs to esters. Esters are widespread in nature and are widely used in industry. In nature, fats are in general triesters derived from glycerol and fatty acids. Esters are responsible for the aroma of many fruits, including apples, durians, pears, bananas, pineapples, and strawberries. Because of their lack of hydrogen-bond-donating ability, esters do not self-associate. Consequently, esters are more volatile than carboxylic acids of similar molecular weight.Related Products of 87694-53-9

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Effects of Glycosylation and D-Amino Acid Substitution on the Antitumor and Antibacterial Activities of Bee Venom Peptide HYL was written by Wu, Ming-hao;Ai, Su;Chen, Qing;Chen, Xiang-yan;Li, Hong-jin;Li, Yu-lei;Zhao, Xia. And the article was included in Bioconjugate Chemistry in 2020.Application In Synthesis of (2S,3R,4S,5S,6R)-6-(Acetoxymethyl)tetrahydro-2H-pyran-2,3,4,5-tetrayl tetraacetate This article mentions the following:

Glycosylation is a promising strategy for modulating the physicochem. properties of peptides. However, the influence of glycosylation on the biol. activities of peptides remains unknown. Here, we chose the bee venom peptide HYL as a model peptide and 12 different monosaccharides as model sugars to study the effects of glycosylation site, number, and monosaccharide structure on the biochem. properties, activities, and cellular selectivities of HYL derivatives Some analogs of HYL showed improvement not only in cell selectivity and proteolytic stability but also in antitumor and antimicrobial activity. Moreover, we found that the helicity of glycopeptides can affect its antitumor activity and proteolytic stability, and the 浼?linked D-monosaccharides can effectively improve the antitumor activity of HYL. Therefore, it is possible to design peptides with improved properties by varying the number, structure, and position of monosaccharides. What’s more, the glycopeptides HYL-31 and HYL-33 show a promising prospect for antitumor and antimicrobial drugs development, resp. In addition, we found that the D-lysine substitution strategy can significantly improve the proteolytic stability of HYL. Our new approach provides a reference or guidance for the research of novel antitumor and antimicrobial peptide drugs. In the experiment, the researchers used many compounds, for example, (2S,3R,4S,5S,6R)-6-(Acetoxymethyl)tetrahydro-2H-pyran-2,3,4,5-tetrayl tetraacetate (cas: 4163-60-4Application In Synthesis of (2S,3R,4S,5S,6R)-6-(Acetoxymethyl)tetrahydro-2H-pyran-2,3,4,5-tetrayl tetraacetate).

(2S,3R,4S,5S,6R)-6-(Acetoxymethyl)tetrahydro-2H-pyran-2,3,4,5-tetrayl tetraacetate (cas: 4163-60-4) belongs to esters. Esters are widespread in nature and are widely used in industry. In nature, fats are in general triesters derived from glycerol and fatty acids. Esters are responsible for the aroma of many fruits. Acyl chlorides and acid anhydrides alcoholysis is another way to produce esters. Acyl chlorides and acid anhydrides react with alcohols to produce esters. Anydrous conditions are recommended since both acyl chlorides and acid anhydrides react with water.Application In Synthesis of (2S,3R,4S,5S,6R)-6-(Acetoxymethyl)tetrahydro-2H-pyran-2,3,4,5-tetrayl tetraacetate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Prediction of infinite-dilution activity coefficients with neural collaborative filtering was written by Tan, Tian;Cheng, Hongye;Chen, Guzhong;Song, Zhen;Qi, Zhiwen. And the article was included in AIChE Journal in 2022.Related Products of 84-61-7 This article mentions the following:

Accurate prediction of infinite dilution activity coefficient (绾?sup>閳?/sup>) for phase equilibrium and process design is crucial. In this work, an exptl. 绾?sup>閳?/sup> dataset containing 295 solutes and 407 solvents (21,048 points) is obtained through data integrating, cleaning, and filtering. The dataset is arranged as a sparse matrix with solutes and solvents as columns and rows, resp. Neural collaborative filtering (NCF), a modern matrix completion technique based on deep learning, is proposed to fully fill in the 绾?sup>閳?/sup> matrix. Ten-fold cross-validation is performed on the collected dataset to test the effectiveness of the proposed NCF, proving that NCF outperforms the state-of-the-art phys. model and previous machine learning model. The completed 绾?sup>閳?/sup> matrix makes solvent screening and extension of UNIFAC parameters possible. Taking two typical hard-to-sep. systems (benzene/cyclohexane and Me cyclopentane/n-hexane mixtures) as examples, the NCF-developed database provides high-throughput screening for separation systems in terms of solvent selectivity and capacity. In the experiment, the researchers used many compounds, for example, Dicyclohexyl phthalate (cas: 84-61-7Related Products of 84-61-7).

Dicyclohexyl phthalate (cas: 84-61-7) belongs to esters. Esters are widespread in nature and are widely used in industry. In nature, fats are in general triesters derived from glycerol and fatty acids. Esters are responsible for the aroma of many fruits. Cyclic esters are called lactones, regardless of whether they are derived from an organic or inorganic acid. One example of an organic lactone is 绾?valerolactone.Related Products of 84-61-7

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Extraction of phthalic acid esters from soft drinks and infusions by dispersive liquid-liquid microextraction based on the solidification of the floating organic drop using a menthol-based natural deep eutectic solvent was written by Ortega-Zamora, Cecilia;Jimenez-Skrzypek, Gabriel;Gonzalez-Salamo, Javier;Hernandez-Borges, Javier. And the article was included in Journal of Chromatography A in 2021.Application of 84-61-7 This article mentions the following:

In this work, a natural deep eutectic solvent (NADES) consisting of L-menthol and acetic acid in a 1:1 molar ratio has been applied as extraction solvent for the dispersive liquid-liquid microextraction based on the solidification of the floating organic drop (DLLME-SFO) of a group of nine phthalic acid esters (di-Pr phthalate, DPP; Bu benzyl phthalate, BBP; di-Bu phthalate, DBP; dicyclohexyl phthalate, DCHP; diisopentyl phthalate, DIPP; di-n-pentyl phthalate, DNPP; di(2-ethylhexyl) phthalate, DEHP; diisononyl phthalate, DINP; and diisodecyl phthalate, DIDP) from three common infusions (chamomile, pennyroyal mint, and linden teas) and three soft drinks (green tea, tonic, and lime and lemon drink), using dihexyl phthalate (DHP) and di-n-octyl phthalate (DNOP) as internal standards After the DLLME-SFO procedure, analyses were carried out by high-performance liquid chromatog. with UV detection. Method calibration showed good linearity for all the analytes and matrixes, with determination coefficients (R2) higher than 0.9910. Relative recovery values were between 71 and 125%, with relative standard deviation values in the range 1-22% for the six types of samples, while the limits of quantification of the method were in the range 4.3-51.1娓璯/L for infusions and in the range 3.5-33.3娓璯/L for soft drinks. Several samples purchased in different local supermarkets were analyzed, finding DPP, DBP, DIPP, DEHP and DINP, although only DPP, DBP and DEHP could be quantified in some of them. In the experiment, the researchers used many compounds, for example, Dicyclohexyl phthalate (cas: 84-61-7Application of 84-61-7).

Dicyclohexyl phthalate (cas: 84-61-7) belongs to esters. Esters are also usually derived from carboxylic acids. It may also be obtained by reaction of acid anhydride or acid halides with alcohols or by the reaction of salts of carboxylic acids with alkyl halides. Esters contain a carbonyl center, which gives rise to 120鎺?C閳ユ弲閳ユ彊 and O閳ユ弲閳ユ彊 angles. Unlike amides, esters are structurally flexible functional groups because rotation about the C閳ユ彊閳ユ弲 bonds has a low barrier. Their flexibility and low polarity is manifested in their physical properties; they tend to be less rigid (lower melting point) and more volatile (lower boiling point) than the corresponding amides. Application of 84-61-7

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

An expedient conversion of 浼?amino acids into Weinreb amides using COMU as a coupling agent was written by Tyrrell, Elizabeth;Brawn, Peter;Carew, Mark;Greenwood, Iain. And the article was included in Tetrahedron Letters in 2011.Product Details of 87694-53-9 This article mentions the following:

The use of COMU, as a non-hazardous partner, in the coupling of N-Boc 浼?amino acids with N-methoxy-N-methylamine to afford the corresponding Weinreb amides is discussed. From a practical point of view the reaction can be monitored visually by virtue of the color change associated with the conversion of substrates (yellow) into the products (orange). As the byproducts of the reaction are conveniently water-soluble, the products are isolated relatively pure and with minimal racemization. These factors coupled with the short reaction time make this a very useful procedure. In the experiment, the researchers used many compounds, for example, (S)-tert-Butyl (1-(methoxy(methyl)amino)-1-oxo-3-phenylpropan-2-yl)carbamate (cas: 87694-53-9Product Details of 87694-53-9).

(S)-tert-Butyl (1-(methoxy(methyl)amino)-1-oxo-3-phenylpropan-2-yl)carbamate (cas: 87694-53-9) belongs to esters. Carboxylic acid esters of low molecular weight are colourless, volatile liquids with pleasant odours, slightly soluble in water. Liquid esters of low volatility serve as softening agents for resins and plastics. Esters also include many industrially important polymers. Polymethyl methacrylate is a glass substitute sold under the names Lucite and Plexiglas; polyethylene terephthalate is used as a film (Mylar) and as textile fibres sold as Terylene, Fortrel, and Dacron.Product Details of 87694-53-9

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

浼?Ketoamide Phe-Pro isostere as a new core structure for the inhibition of HIV protease was written by Munoz, Benito;Giam, Chou-Zen;Wong, Chi-Huey. And the article was included in Bioorganic & Medicinal Chemistry in 1994.Name: (S)-tert-Butyl (1-(methoxy(methyl)amino)-1-oxo-3-phenylpropan-2-yl)carbamate This article mentions the following:

Studies on the inhibition of HIV-1 protease utilizing a core isostere with replacement of the scissile bond for an 浼?amino-ketone have resulted in the development of an 浼?keto-amide isosteric replacement of the Phe-Pro scissile amide bond. The simple dipeptide isostere I was a promising new core structure for the development of the enzyme inhibitors. I exhibited K_i = 6 娓璏 against HIV-1 protease, compared to 230 娓璏 and >50 娓璏 for the corresponding phosphinic acid and hydroxyethylamine isosteres. In the experiment, the researchers used many compounds, for example, (S)-tert-Butyl (1-(methoxy(methyl)amino)-1-oxo-3-phenylpropan-2-yl)carbamate (cas: 87694-53-9Name: (S)-tert-Butyl (1-(methoxy(methyl)amino)-1-oxo-3-phenylpropan-2-yl)carbamate).

(S)-tert-Butyl (1-(methoxy(methyl)amino)-1-oxo-3-phenylpropan-2-yl)carbamate (cas: 87694-53-9) belongs to esters. Esters are widespread in nature and are widely used in industry. In nature, fats are in general triesters derived from glycerol and fatty acids. Esters are responsible for the aroma of many fruits. Esters contain a carbonyl center, which gives rise to 120鎺?C閳ユ弲閳ユ彊 and O閳ユ弲閳ユ彊 angles. Unlike amides, esters are structurally flexible functional groups because rotation about the C閳ユ彊閳ユ弲 bonds has a low barrier. Their flexibility and low polarity is manifested in their physical properties; they tend to be less rigid (lower melting point) and more volatile (lower boiling point) than the corresponding amides. Name: (S)-tert-Butyl (1-(methoxy(methyl)amino)-1-oxo-3-phenylpropan-2-yl)carbamate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics