Tag: 300-400

On February 14, 2019, Zablocki, Mary-Margaret; Guerin, David J.; Ng, Pui Yee; Wang, Zhongguo; Shelekhin, Tatiana; Caravella, Justin; Li, Hongbin; Ioannidis, Stephanos published a patent.Electric Literature of 227940-70-7 The title of the patent was Heteroaryl carboxamide derivatives as ubiquitin-specific protease inhibitors and their preparation. And the patent contained the following:

The invention relates to compounds of formula I, their use as modulators, such as inhibitors, of at least one pathway chosen from USP28 and USP25, pharmaceutical compositions comprising the inhibitors and methods of using the inhibitors in the treatment of cancers, among other ailments. Compounds of formula I, wherein X is CRARB and O; RA and RB are independently H, halo, hydroxy, etc.; R1 is 6 – 12 membered (un)substituted fused and (un)substituted nonfused heteroaryls, R2 is N-linked (un)substituted 4 – 12 membered heterocyclyls, (un)substituted C-linked 4 – 12 membered heterocyclyls and (un)substituted O-linked 4 – 12 member heterocyclyl; R3 is independently H, C1-6 alkyl, C1-6 alkoxy, etc.; n is 0, 1, 2 and 3; R4 is H, C1-6 alkyl, C1-6 alkoxy, etc.; R5 is H, deuterium and Me; Y1, Y2 and Y3 are independently CR3 and N; and pharmaceutically acceptable salts thereof, are claimed. Compound II was prepared using a multistep procedure (procedure given). Compound II was evaluated for its USP28 and USP25 inhibitory activities giving an IC50 of 0.05-2 μM and 0.2-2 μM, resp. Compounds of the invention were evaluated for their inhibitory activity (data given). The experimental process involved the reaction of tert-Butyl 7-benzyl-9-oxo-3,7-diazabicyclo[3.3.1]nonane-3-carboxylate(cas: 227940-70-7).Electric Literature of 227940-70-7

The Article related to heteroaryl carboxamide preparation usp28 usp25 modulator inhibitor cancer, Heterocyclic Compounds (One Hetero Atom): Benzopyrans (Including Coumarins, Isocoumarins, Chromones, Benzopyrones, Dibenzopyrans, and Other Arenopyrans) and other aspects.Electric Literature of 227940-70-7

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

On May 20, 2022, Kasu, Yasar Arfat T.; Arva, Akshaya; Johnson, Jess; Sajan, Christin; Manzano, Jasmin; Hennes, Andrew; Haynes, Jacy; Brower, Christopher S. published an article.Electric Literature of 79642-50-5 The title of the article was BAG6 prevents the aggregation of neurodegeneration-associated fragments of TDP43. And the article contained the following:

Neurodegeneration is associated with the aggregation of proteins bearing solvent-exposed hydrophobicity as a result of their misfolding and/or proteolytic cleavage. An understanding of the cellular protein quality control mechanisms which prevent protein aggregation is fundamental to understanding the etiol. of neurodegeneration. By examining the metabolism of disease-linked C-terminal fragments of the TAR DNA-binding protein 43 (TDP43), we found that the Bcl-2 associated athanogene 6 (BAG6) functions as a sensor of proteolytic fragments bearing exposed hydrophobicity and prevents their intracellular aggregation. In addition, BAG6 facilitates the ubiquitylation of TDP43 fragments by recruiting the Ub-ligase, Ring finger protein 126 (RNF126). Authenticating its role in preventing aggregation, we found that TDP43 fragments form intracellular aggregates in the absence of BAG6. Finally, we found that BAG6 could interact with and solubilize addnl. neurodegeneration-associated proteolytic fragments. Therefore, BAG6 plays a general role in preventing intracellular aggregation associated with neurodegeneration. The experimental process involved the reaction of Bis(2,5-dioxopyrrolidin-1-yl) glutarate(cas: 79642-50-5).Electric Literature of 79642-50-5

The Article related to aggregation bag6 neurodegeneration proteolytic fragment ubiquitylation tdp43 rnf126, biological sciences, cell biology, molecular biology, molecular neuroscience, neuroscience and other aspects.Electric Literature of 79642-50-5

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Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On February 28, 2022, MacKeown, Henry; Magi, Emanuele; Di Carro, Marina; Benedetti, Barbara published an article.Application of 6197-30-4 The title of the article was Unravelling the role of membrane pore size in polar organic chemical integrative samplers (POCIS) to broaden the polarity range of sampled analytes. And the article contained the following:

Polar organic chem. integrative samplers (POCIS) are widely used in their standard configuration for sampling contaminants in water bodies. A wider polyethersulfone (PES) membrane pore size was employed in POCIS exposed in a static calibration experiment to investigate the uptake of 21 emerging contaminants ranging from hydrophilic (perfluoroalkyl compounds, xanthines, an artificial sweetener) to more hydrophobic compounds (pharmaceuticals, estrogens, UV filters). Compared to standard POCIS with 0.1-μm pore size PES membranes, the POCIS with 5-μm pore size PES membranes did not increase sampling rates for compounds of relatively low and mid-hydrophobicity. However, the uptake of more hydrophobic and anionic compounds, which either poorly diffuse through or are retained within the standard 0.1-μm PES membrane, showed a marked increase. This led to the first ever recorded sampling rates for triclosan (0.249 L day-1) and two UV filters (0.075-0.123 L day-1). Based on these results, more attention should be placed on the choice of the appropriate membrane for each POCIS application. The most suitable configuration depends on the studied compound physico-chem. characteristics-such as the polarity and the compound membrane-to-sorbent partitioning coefficient-but also on the site conditions (deployment time, fouling, flow variations, et.). The experimental process involved the reaction of 2-Ethylhexyl 2-cyano-3,3-diphenylacrylate(cas: 6197-30-4).Application of 6197-30-4

The Article related to polar organic chem integrative sampler membrane pore size polarity, emerging contaminants, liquid chromatography-mass spectrometry, membrane pore size, pocis, water monitoring and other aspects.Application of 6197-30-4

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Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On March 1, 2020, Labille, Jerome; Slomberg, Danielle; Catalano, Riccardo; Robert, Samuel; Apers-Tremelo, Marie-Laure; Boudenne, Jean-Luc; Manasfi, Tarek; Radakovitch, Olivier published an article.Product Details of 6197-30-4 The title of the article was Assessing UV filter inputs into beach waters during recreational activity: A field study of three French Mediterranean beaches from consumer survey to water analysis. And the article contained the following:

In order to assess the release of UV filters from the sunscreen used by beachgoers into seawater within the bathing zone, a field campaign was carried out during the summer of 2017 at three beaches in Marseille, along the French Mediterranean coast. A social survey analyzed beachgoer attendance, the quantities and types of suncare products used and the bathing frequencies, while the bathing water was analyzed spatially and temporally so as to quantify both mineral and organic UV filters directly released and recovered. During the peak recreational time at the three beaches, both mineral and organic UV filters were detected in higher concentrations in the bathing area than offshore. In general, higher concentrations were recovered in the water top surface layer than in the water column, giving resp. 100-900 and 20-50μg/L for TiO2, 10-15 and 1-3μg/L for ZnO, 40-420 and 30-150 ng/L for octocrylene, and 10-15 and 10-350 ng/L for avobenzone. More than 75% of the 471 interviewees reported bathing every time they go to the beach, with 68% using a suncare product 2.6 times on average From these data we estimated that an average mass of 52 kg/day or 1.4 t/mo of suncare products are possibly released into bathing water for a beach attended by 3000 people daily. The mass ratio of UV filters in such products typically ranges from 0.03 to 0.1, allowing us to propose theor. maximum concentrations in the beach water. Our recovery of measured UV filter concentrations in seawater compared to the theor. concentrations revealed two distinct scenarios for the mineral and organic filters. While up to 49% of the mineral filters used by beachgoers may be released into the seawater, the organic filters were minimally recovered in the environment, most likely due to internalization through the skin barrier or partial photodegradation The experimental process involved the reaction of 2-Ethylhexyl 2-cyano-3,3-diphenylacrylate(cas: 6197-30-4).Product Details of 6197-30-4

The Article related to uv filter sunscreen beach seawater pollution french mediterranean, environmental social issue, marine contamination, nanomaterial fate, sunscreen, titanium dioxide, uv filter and other aspects.Product Details of 6197-30-4

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

On October 1, 2021, Law, Japhet Cheuk-Fung; Huang, Yanran; Chow, Chi-Hang; Lam, Tsz-Ki; Leung, Kelvin Sze-Yin published an article.Reference of 2-Ethylhexyl 2-cyano-3,3-diphenylacrylate The title of the article was Comparative physicochemical properties and toxicity of organic UV filters and their photocatalytic transformation products. And the article contained the following:

Transformation products (TPs) of micropollutants contaminating our water resources have become an emerging issue due to the potential threats they pose to environmental and human health. This study investigated the transformation chem., toxicity, physicochem. properties and environmental behavior resulting from photocatalytic transformation of organic UV filters as model micropollutants. 3-Benzylidene camphor (3-BC), 4-hydroxybenzophenone (4-HB) and octocrylene (OC) were effectively degraded by UV-A/TiO2 treatment, with TPs identified and characterized with high resolution mass spectrometry. Nitrated-TPs were observed to be formed in the presence of nitrite and nitrate for 3-BC and 4-HB, suggesting that the transformation process could be altered by components in the water matrix. Vibrio fischeri bioluminescence inhibition assay revealed an increase in toxicity of TPs derived from photocatalytic treatment, with quant. structure-activity relationship model (ECOSAR) predicted an enhanced toxicity of individual TPs′ after transformation. Assessment of physicochem. properties and environmental behavior suggested that TPs as compared to parent organic UV filters, may represent even greater hazards due to their increased water solubility, persistence and mobility – in addition to retaining the parent organic UV filter′s toxicity. The results provide important information relevant to the potential risks for the selected organic UV filters, and their corresponding transformation products. The experimental process involved the reaction of 2-Ethylhexyl 2-cyano-3,3-diphenylacrylate(cas: 6197-30-4).Reference of 2-Ethylhexyl 2-cyano-3,3-diphenylacrylate

The Article related to physicochem property toxicity organic uv filter photocatalytic transformation, environmental fate, micropollutants, mobility, persistence, sunscreens, transformation pathway and other aspects.Reference of 2-Ethylhexyl 2-cyano-3,3-diphenylacrylate

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

On May 17, 2019, Qiu, Xing; Sun, Ning; Kong, Ying; Li, Yan; Yang, Xiaobao; Jiang, Biao published an article.Recommanded Product: 882518-89-0 The title of the article was Chemoselective Synthesis of Lenalidomide-Based PROTAC Library Using Alkylation Reaction. And the article contained the following:

Using DIPEA as base in N-methyl-2-pyrrolidinone (NMP), lenalidomide underwent regioselective alkylation with bromoesters and Boc-protected bromoamines followed by deprotection to yield lenalidomide derivatives as a library of potential PROTAC reagents. One of the products was coupled to the known BET binding agent JQ1 to yield I; I degraded BET protein in cells and effectively inhibited cancer cell proliferation. The experimental process involved the reaction of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate(cas: 882518-89-0).Recommanded Product: 882518-89-0

The Article related to protac library lenalidomide regioselective preparation, regioselective alkylation lenalidomide bromoamine bromoester, bet degradation antitumor activity jq1 lenalidomide conjugate and other aspects.Recommanded Product: 882518-89-0

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

On February 22, 2020, Seyer, Alexandra; Mlynek, Franz; Himmelsbach, Markus; Buchberger, Wolfgang; Klampfl, Christian W. published an article.Computed Properties of 6197-30-4 The title of the article was Investigations on the uptake and transformation of sunscreen ingredients in duckweed (Lemna gibba) and Cyperus alternifolius using high-performance liquid chromatography drift-tube ion-mobility quadrupole time-of-flight mass spectrometry. And the article contained the following:

The uptake, translocation and transformation of three UV-blockers commonly employed in sunscreens, namely avobenzone, octocrylene and octisalate from water by Lemna gibba and Cyperus alternifolius was investigated. Reversed phase high performance liquid chromatog. coupled to drift-tube ion-mobility quadrupole time-of-flight mass spectrometry was used for analyzing the extracts from the selected plants after incubation with the UV-blockers for one week. For avobenzone several transformation products resulting from hydroxylation, demethylation and oxidation of the parent mol. could be identified by measuring accurate mass, performing MS/MS experiments and by determining their drift-tube collision cross sections employing nitrogen as drift gas. In addition, the plants were subjected to two com. available sunscreens, providing similar results to those obtained for the standard solutions of the UV-blockers. Finally, a kinetic study on the uptake and transformation of avobenzone, octocrylene and octisalate was conducted over a period of 216 h, revealing that the UV-filters were mostly present in their parent form and only to a smaller part converted into transformation products. The experimental process involved the reaction of 2-Ethylhexyl 2-cyano-3,3-diphenylacrylate(cas: 6197-30-4).Computed Properties of 6197-30-4

The Article related to lemna cyperus sunscreen uptake transformation, drift-tube ion mobility-mass spectrometry, environmental analysis, personal care products, plant metabolism, sunscreen, uv-filters and other aspects.Computed Properties of 6197-30-4

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

On December 15, 2020, Muniz-Gonzalez, Ana-Belen; Martinez-Guitarte, Jose-Luis published an article.Name: 2-Ethylhexyl 2-cyano-3,3-diphenylacrylate The title of the article was Unveiling complex responses at the molecular level: Transcriptional alterations by mixtures of bisphenol A, octocrylene, and 2′-ethylhexyl 4- (dimethylamino)benzoate on Chironomus riparius. And the article contained the following:

Living organisms are exposed to mixtures of pollutants in the wild. Inland aquatic ecosystems contain many compounds from different sources that pollute the water column and the sediment. However, majority of toxicol. research is focused on the effects of single exposures to toxicants. Furthermore, studies have been principally oriented toward ecol. relevant effects of intoxication, and lack an anal. of the cellular and mol. mechanisms involved in the response to toxicants. Effects of single, binary, and ternary mixtures of three compounds, bisphenol A, octocrylene, and 2′-ethylhexyl 4- (dimethylamino)benzoate, were assessed using a Real-Time PCR array. Forty genes, and addnl. six reference genes, were included in the array. The genes were selected based on their association with hormone responses, detoxification mechanisms, the stress response, DNA repair, and the immune system. The study was performed on Chironomus riparius, a benthic dipteran with an essential role in the food web. Transcriptional responses were assessed both 24 and 96 h post-exposure, to determinate short- and medium-term cellular responses. Individual fourth instar larvae were exposed to 0.1 and 1 mg/L of each of the toxic compounds and compound mixtures A weak response was detected at 24 h, which was stronger in larvae exposed to mixtures than to individual toxicants. The response at 96 h was complex and principally involved genes related to the endocrine system, detoxification mechanisms, and the stress response. Furthermore, exposure to mixtures of compounds altered the expression patterns of an increased number of genes than did individual compound exposures, which suggested complex interactions between compounds affected the regulation of transcriptional activity. The results obtained highlight the importance of analyzing the mechanisms involved in the response to mixtures of compounds over extended periods and offer new insights into the basis of the physiol. responses to pollution. The experimental process involved the reaction of 2-Ethylhexyl 2-cyano-3,3-diphenylacrylate(cas: 6197-30-4).Name: 2-Ethylhexyl 2-cyano-3,3-diphenylacrylate

The Article related to chironomus riparius endocrine disrupting chem toxicity transcriptional alteration, aquatic insect, chironomids, invertebrates, mixture toxicity, multi-stress, transcriptional alterations and other aspects.Name: 2-Ethylhexyl 2-cyano-3,3-diphenylacrylate

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

On May 31, 2022, Herzum, Astrid; Cozzani, Emanuele; Parodi, Aurora; Gallo, Rosella published an article.Application of 6197-30-4 The title of the article was Ketoprofen-induced photoallergic consort contact dermatitis: A difficult diagnosis. And the article contained the following:

Consort contact dermatitis is an allergic or photoallergic dermatitis caused by sensitizers conveyed by a partner or companion via direct interpersonal skin contact or indirect contact through shared objects. We describe a patient who experienced severe bouts of photoallergic contact dermatitis as a result of an indirect contact with topical ketoprofen used by her mother. A 34-yr-old lady was referred with a 7-yr history of vesicobullous eruptions recurrent on different body sites, presently in remission. The history was suggestive of recurrent acute allergic contact dermatitis induced by a strong allergen but the patient denied direct contact with any likely trigger including cosmetics and topical medicaments. A meticulous search for indirect contact with renowned potent haptens eventually revealed that the patient′s mother used topical ketoprofen and accompanied her daughter to the beach where they happened to use the same lounge chair. The allergens were applied in duplicate on the upper back; one set was irradiated on day (D) 2 with UVA radiation at the dose of 5 J/cm2. The patient′s dermatitis never recurred after her mother discontinued topical ketoprofen. The experimental process involved the reaction of 2-Ethylhexyl 2-cyano-3,3-diphenylacrylate(cas: 6197-30-4).Application of 6197-30-4

The Article related to difficult diagnosis ketoprofen photoallergic consort contact dermatitis, allergic contact dermatitis, case report, consort dermatitis, ketoprofen, patch test, photo-contact dermatitis and other aspects.Application of 6197-30-4

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

On April 3, 2015, Dikshit, Dinesh Kumar; Kumar, K. S. Anil; Dikshit, Madhu; Barthwal, Manoj Kumar; Misra, Ankita; Jain, Manish published a patent.Safety of tert-Butyl 7-benzyl-9-oxo-3,7-diazabicyclo[3.3.1]nonane-3-carboxylate The title of the patent was Preparation of 3,7-diazabicyclo[3.3.1]nonane carboxamides as antithrombotic agents. And the patent contained the following:

The present invention relates to the 3,7-diazabicyclo[3.3.1]nonane carboxamides of formula I as anti-thrombotic (anti-platelet) agents and process for preparation thereof. The invention also relates to use of these moieties as inhibitors of collagen induced platelet adhesion and aggregation mediated through collagen receptors both in vitro and in vivo. Compounds of formula I wherein R’ is II and III; R is alkyl, acyl, tosyl, etc; R” is halo, cyano, lower alkyl, etc.; R1 is H and lower alkyl; R2 is lower alkyl and aryl; R3 is tert-butyloxycarbonyl and benzyloxycarbonyl groups; are claimed. Example compound IV was prepared by acylation of N-Bocbispidine with N-benzylpyroglutamic acid. The invention compounds were evaluated for their antithrombotic activity (some data given). The experimental process involved the reaction of tert-Butyl 7-benzyl-9-oxo-3,7-diazabicyclo[3.3.1]nonane-3-carboxylate(cas: 227940-70-7).Safety of tert-Butyl 7-benzyl-9-oxo-3,7-diazabicyclo[3.3.1]nonane-3-carboxylate

The Article related to preparation pyroglutamyldiazabicyclononane carboxamide antithrombotic, collagen induced platelet adhesion aggregation inhibitor preparation pyroglutamyldiazabicyclononane carboxamide and other aspects.Safety of tert-Butyl 7-benzyl-9-oxo-3,7-diazabicyclo[3.3.1]nonane-3-carboxylate

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