Tag: 300-400

Discovery of a Novel Oral Glucocorticoid Receptor Modulator (AZD9567) with Improved Side Effect Profile was written by Ripa, Lena;Edman, Karl;Dearman, Matthew;Edenro, Goran;Hendrickx, Ramon;Ullah, Victoria;Chang, Hui-Fang;Lepistoe, Matti;Chapman, Dave;Geschwindner, Stefan;Wissler, Lisa;Svanberg, Petter;Lawitz, Karolina;Malmberg, Jesper;Nikitidis, Antonios;Olsson, Roine I.;Bird, James;Llinas, Antoni;Hegelund-Myrbaeck, Tove;Berger, Markus;Thorne, Philip;Harrison, Richard;Koehler, Christian;Drmota, Tomas. And the article was included in Journal of Medicinal Chemistry in 2018.Reference of 87694-53-9 This article mentions the following:

Synthetic glucocorticoids (GC) are essential for the treatment of a broad range of inflammatory diseases. However, their use is limited by target related adverse effects on, e.g., glucose homeostasis and bone metabolism Starting from a nonsteroidal GR ligand that is a full agonist in reporter gene assays, the authors exploited key functional triggers within the receptor, generating a range of structurally diverse partial agonists. Of these, only a narrow subset exhibited full anti-inflammatory efficacy and a significantly reduced impact on adverse effect markers in human cell assays compared to prednisolone. This led to the discovery of AZD9567 (15) with excellent in vivo efficacy when dosed orally in a rat model of joint inflammation. Compound 15 is currently being evaluated in clin. trials comparing the efficacy and side effect markers with those of prednisolone. 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. Many esters have the potential for conformational isomerism, but they tend to adopt an s-cis (or Z) conformation rather than the s-trans (or E) alternative, due to a combination of hyperconjugation and dipole minimization effects. The preference for the Z conformation is influenced by the nature of the substituents and solvent, if present. Lactones with small rings are restricted to the s-trans (i.e. E) conformation due to their cyclic structure.Reference of 87694-53-9

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

Surface roughness influences the protein corona formation of glycosylated nanoparticles and alter their cellular uptake was written by Piloni, Alberto;Wong, Chin Ken;Chen, Fan;Lord, Megan;Walther, Andreas;Stenzel, Martina H.. And the article was included in Nanoscale in 2019.SDS of cas: 4163-60-4 This article mentions the following:

Recently the role of protein absorption in nanoparticle drug delivery has gathered significant attention as the protein corona can significantly decide on the fate of nanoparticles in the body. Although it is known that the surface chem. will significantly influence the amount and type of bound protein, there is little known about the effect of surface roughness and surface topog. on the interaction. In this work, we show how patchy nanoparticles can noticeably reduce the adsorption of proteins compared to spherical nanoparticles with a smooth surface as demonstrated using six ABC triblock terpolymers based on glucose, mannose and galactose. As control, smooth nanoparticles were prepared from poly(2-D-sugar Et acrylate)-b-poly (Bu acrylate)-b-polystyrene (PSugEA-b-PBuA-b-PS). The patchy nanoparticles displayed significantly reduced protein absorption when exposed to serum-supplemented cell culture media, as observed using dynamic light scattering. Addnl., an enrichment of Hb was observed in the corona compared to the serum protein in solution The amount of albumin on the surface was observed to be dependent on the type of sugar with glucose resulting in the highest absorption. The protein corona led to cellular uptake that was unrelated to the underlying sugar, which was supposed to help targeting specific cell lines. This example demonstrated how the protein corona can override any attempts to target receptor expressing cells. 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: 4163-60-4SDS of cas: 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. Volatile esters with characteristic odours are used in synthetic flavours, perfumes, and cosmetics. Certain volatile esters are used as solvents for lacquers, paints, and varnishes. 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.SDS of cas: 4163-60-4

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

Evaluation of chemicals of environmental concern in crumb rubber and water leachates from several types of synthetic turf football pitches was written by Celeiro, Maria;Armada, Daniel;Ratola, Nuno;Dagnac, Thierry;de Boer, Jacob;Llompart, Maria. And the article was included in Chemosphere in 2021.Electric Literature of C20H26O4 This article mentions the following:

Nowadays concern exists about the safety for both football players and the environment of recycled tire rubber used as infill in synthetic turf football pitches. In this study 40 target compounds, including polycyclic aromatic hydrocarbons (PAHs), plasticizers, antioxidants and vulcanization agents were determined in 50 synthetic football pitches of diverse characteristics to estimate environmental risks. This is the first study of crumb rubber sport facilities in Portugal. Analyses were performed by ultrasound-assisted extraction followed by gas chromatog.-tandem mass spectrometry (UAE-GC-MS/MS). To evaluate the transfer of the target chems. from the crumb rubber to the runoff water, water leachates collected from several football pitches were analyzed by solid-phase microextraction (SPME-GC-MS/MS). In addition, lab-scale runoff simulation experiments were performed to assess whether a persistent inflow of the target compounds from the football pitches into the runoff water wcould exist. Results revealed the presence of most of the target PAHs in crumb rubber at total concentrations up to 57μg g-1, next to a high number of plasticizers and vulcanization agents. Runoff water collected from the football pitches contained up to 13 PAHs as well as other chems. of environmental concern. In addition, continuous leaching of chems. from the crumb rubber to the surrounding water was demonstrated. The transfer of target chems. into the runoff water poses a potential risk for the aquatic environment. In the experiment, the researchers used many compounds, for example, Dicyclohexyl phthalate (cas: 84-61-7Electric Literature of C20H26O4).

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, including apples, durians, pears, bananas, pineapples, and strawberries. Many esters have the potential for conformational isomerism, but they tend to adopt an s-cis (or Z) conformation rather than the s-trans (or E) alternative, due to a combination of hyperconjugation and dipole minimization effects. The preference for the Z conformation is influenced by the nature of the substituents and solvent, if present. Lactones with small rings are restricted to the s-trans (i.e. E) conformation due to their cyclic structure.Electric Literature of C20H26O4

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

Synthesis and antibacterial profiles of targeted triclosan derivatives was written by Howse, Gemma L.;Bovill, Richard A.;Stephens, Peter J.;Osborn, Helen M. I.. And the article was included in European Journal of Medicinal Chemistry in 2019.HPLC of Formula: 4163-60-4 This article mentions the following:

There is an ongoing urgent need for new targeted antibacterial compounds with novel mechanisms of action for the treatment of infections caused by bacteria that are resistant to currently available materials. Herein we report the synthesis and characterization of four α-D-glycopyranosides, e.g. I, and three β-D-glycopyranosides of the broad antibacterial agent triclosan, in generally good synthetic yields, and with excellent purity. Each triclosan glycoside was analyzed to determine its ability to inhibit the growth of a wide range of Gram-neg. and Gram-pos. organisms, including many of clin. significance. All of the triclosan glycosides that were synthesized demonstrated antibacterial activity against many of the organisms that were examined Two Bacillus strains could be identified from various strains of Bacillus and Staphylococcus after inoculation onto nutrient agar Number 2 with 0.25 μg/mL triclosan-α-D-glucopyranoside I. This glucoside may, therefore, be of use for the isolation and identification of the food-poisoning organism Bacillus cereus. 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: 4163-60-4HPLC of Formula: 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. 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.HPLC of Formula: 4163-60-4

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

Characteristics of dust-phase phthalates in dormitory, classroom, and home and non-dietary exposure in Beijing, China was written by Qu, Meinan;Wang, Lixin;Liu, Fang;Zhao, Yi;Shi, Xiangzhao;Li, Sijia. And the article was included in Environmental Science and Pollution Research in 2021.Related Products of 84-61-7 This article mentions the following:

The phthalate concentrations in dust from undergraduate dormitories, classrooms, and homes in Beijing, China, were measured in Apr. 2017. We analyzed the characteristics of phthalates in dust from three environments. In addition, we estimated the daily intake of phthalates via three pathways using Monte Carlo simulations. The detection frequency of eight phthalates in dust ranges from 74.5 to 100%. Di (2-ethylhexyl) phthalate (DEHP), di-Bu phthalate (DnBP), and di-iso-Bu phthalate (DiBP) are the most abundant phthalates. The median proportion of DEHP in dust is the highest, ranging from 67.1 to 72.9%. The PMF results indicated that two, four, and three types of phthalate sources exist in home, dormitory, and classroom, resp. The differences in the phthalate concentrations between sunny and shaded rooms and urban and suburban classrooms are insignificant, whereas that between male and female dormitories is significant. The total daily intake of DEHP, DnBP, and DiBP ranges from 97.3 to 336 ng/ (kg·day). The oral intake for DEHP in classrooms and the dermal intake of DnBP and DiBP in homes are the highest. The carcinogenic risk of DEHP to university students is the highest in classrooms and the total carcinogenic risk of the three environments is 4.70 x 10^-6. 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 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. 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 84-61-7

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

Synthesis and biological activities of amino acids functionalized α-GalCer analogues was written by Ma, Weiwei;Bi, Jingjing;Zhao, Chuanfang;Zhang, Zhiguo;Liu, Tongxin;Zhang, Guisheng. And the article was included in Bioorganic & Medicinal Chemistry in 2020.SDS of cas: 4163-60-4 This article mentions the following:

Invariant natural killer T-cells (iNKT-cells) are promising targets for manipulating the immune system, which can rapidly release a large amount of Th1 and Th2 cytokines upon the engagement of their T cell receptor with glycolipid antigens presented by CD1d. In this paper, we wish to report a novel series of α-GalCer analogs which were synthesized by incorporation of L-amino acid Me esters in the C-6′ position of glycolipid. The evaluation of these synthetic analogs for their capacities to stimulate iNKT-cells into producing Th1 and Th2 cytokines both in vitro and in vivo indicated that they were potent CD1d ligands and could stimulate murine spleen cells into a higher release of the Th1 cytokine IFN-γ in vitro. In vivo, Gly-α-GalCer (I) and Lys-α-GalCer (II) showed more Th1-biased responses than α-GalCer, especially II showed the highest selectivity for IFN-γ production (IFN-γ/IL-4 = 5.32) compared with I (IFN-γ/IL-4 = 2.5) in vivo. These novel α-GalCer analogs might be used as efficient X-ray crystallog. probes to reveal the relationship between glycolipids and CD1d proteins in α-GalCer/CD1d complexes and pave the way for developing new potent immunostimulating agents. 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: 4163-60-4SDS of cas: 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 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. 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.SDS of cas: 4163-60-4

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

Novel bis-cyclic guanidines as potent membrane-active antibacterial agents with therapeutic potential was written by Teng, Peng;Nimmagadda, Alekhya;Su, Ma;Hong, Yuzhu;Shen, Ning;Li, Chunpu;Tsai, Ling-Yu;Cao, Jessica;Li, Qi;Cai, Jianfeng. And the article was included in Chemical Communications (Cambridge, United Kingdom) in 2017.SDS of cas: 87694-53-9 This article mentions the following:

We designed a class of small dimeric cyclic guanidine derivatives which display potent antibacterial activity against both multidrug-resistant Gram-neg. and Gram-pos. bacteria. They could compromise bacterial membranes without developing resistance, inhibit biofilms formed by E. coli, and exhibit excellent in vivo activity in the MRSA-infected thigh burden mouse model. 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: 87694-53-9SDS of cas: 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. 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.SDS of cas: 87694-53-9

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

One pot synthesis of thio-glycosides via aziridine opening reactions was written by Hribernik, Nives;Tamburrini, Alice;Falletta, Ermelinda;Bernardi, Anna. And the article was included in Organic & Biomolecular Chemistry in 2021.Application of 4163-60-4 This article mentions the following:

A one-pot aziridine opening reaction by glycosyl thiols generated in situ from the corresponding anomeric thio-acetates affords thio-glycosides with a pseudo-disaccharide structure and an N-linked tether. The scope of the one-pot aziridine opening reaction was explored on a series of mono- and disaccharides, creating a class of pseudo-glycosidic compounds with potential for further functionalization. Unexpected anomerization of glycosyl thiols was observed under the reaction conditions and the influence of temperature, base and solvent on the isomerization was investigated. Single isomers were obtained in good to acceptable yields for mannose, rhamnose and sialic acid derivatives The class of thio-glycomimetics synthesized can potentially be recognized by various lectins, while presenting hydrolytic and enzymic stability. The nitrogen functionality incorporated in the glycomimetics can be exploited for further functionalization, including tethering to linkers, scaffolds or peptide residues. 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 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 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. 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.Application of 4163-60-4

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

Combining Inducible Lectin Expression and Magnetic Glyconanoparticles for the Selective Isolation of Bacteria from Mixed Populations was written by Petch, Joshua E.;Gurnani, Pratik;Yilmaz, Gokhan;Mastrotto, Francesca;Alexander, Cameron;Heeb, Stephan;Camara, Miguel;Mantovani, Giuseppe. And the article was included in ACS Applied Materials & Interfaces in 2021.Synthetic Route of C16H22O11 This article mentions the following:

The selective isolation of bacteria from mixed populations has been investigated in varied applications ranging from differential pathogen identification in medical diagnostics and food safety to the monitoring of microbial stress dynamics in industrial bioreactors. Selective isolation techniques are generally limited to the confinement of small populations in defined locations, may be unable to target specific bacteria, or rely on immunomagnetic separation, which is not universally applicable. In this proof-of-concept work, we describe a novel strategy combining inducible bacterial lectin expression with magnetic glyconanoparticles (MGNPs) as a platform technol. to enable selective bacterial isolation from cocultures. An inducible mutant of the type 1 fimbriae, displaying the mannose-specific lectin FimH, was constructed in Escherichia coli allowing for “on-demand” glycan-binding protein presentation following external chem. stimulation. Binding to glycopolymers was only observed upon fimbrial induction and was specific for mannosylated materials. A library of MGNPs was produced via the grafting of well-defined catechol-terminal glycopolymers prepared by reversible addition-fragmentation chain transfer (RAFT) polymerization to magnetic nanoparticles. Thermal anal. revealed high functionalization (â‰?5% polymer by weight). Delivery of MGNPs to cocultures of fluorescently labeled bacteria followed by magnetic extraction resulted in efficient depletion of type 1 fimbriated target cells from wild-type or afimbriate E. coli. Extraction efficiency was found to be dependent on the mol. weight of the glycopolymers utilized to engineer the nanoparticles, with MGNPs decorated with shorter Dopa-(ManAA)₅₀ mannosylated glycopolymers found to perform better than those assembled from a longer Dopa-(ManAA)₂₀₀ analog. The extraction efficiency of fimbriated E. coli was also improved when the counterpart strain did not harbor the genetic apparatus for the expression of the type 1 fimbriae. Overall, this work suggests that the modulation of the genetic apparatus encoding bacterial surface-associated lectins coupled with capture through MGNPs could be a versatile tool for the extraction of bacteria from mixed populations. 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: 4163-60-4Synthetic Route of C16H22O11).

(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, including apples, durians, pears, bananas, pineapples, and strawberries. 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.Synthetic Route of C16H22O11

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

Synthesis of new chiral peptide nucleic acid (PNA) monomers by a simplified reductive amination method was written by Falkiewicz, Bogdan;Kowalska, Katarzyna;Kolodziejczyk, Aleksandra S.;Wisniewski, Kaximierz;Lankiewicz, Leszek. And the article was included in Nucleosides & Nucleotides in 1999.Quality Control of (S)-tert-Butyl (1-(methoxy(methyl)amino)-1-oxo-3-phenylpropan-2-yl)carbamate This article mentions the following:

The aim of this work was the preparation of four new peptide nucleic acid (PNA) monomers, e.g. I [R = iso-Bu, CH₂Ph, (R)-CH(OCH₂Ph)CH₃, CH₂C₆H₄-4-OCH₂Ph; Boc = Me₃CO₂C] by reductive amination of N^α-Boc-protected chiral amino aldehydes, derived from Leu, Phe, Tyr(Bzl), and Thr(Bzl), with Me glycinate. To the crude 2-substituted Me N-(2-Boc-aminoethyl)glycinates obtained, thymin-1-ylacetic acid was coupled using TBTU procedure in a one-pot reaction. PNA monomers were isolated and characterized. 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: 87694-53-9Quality Control of (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. Volatile esters with characteristic odours are used in synthetic flavours, perfumes, and cosmetics. Certain volatile esters are used as solvents for lacquers, paints, and varnishes. Many esters have the potential for conformational isomerism, but they tend to adopt an s-cis (or Z) conformation rather than the s-trans (or E) alternative, due to a combination of hyperconjugation and dipole minimization effects. The preference for the Z conformation is influenced by the nature of the substituents and solvent, if present. Lactones with small rings are restricted to the s-trans (i.e. E) conformation due to their cyclic structure.Quality Control of (S)-tert-Butyl (1-(methoxy(methyl)amino)-1-oxo-3-phenylpropan-2-yl)carbamate

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