Month: October 2022

Mohi El-Deen, Eman M.; Anwar, Manal M.; El-Gwaad, Amina A. Abd; Karam, Eman A.; El-Ashrey, Mohamed K.; Kassab, Rafika R. published an article in 2022, the title of the article was Novel Pyridothienopyrimidine Derivatives: Design, Synthesis and Biological Evaluation as Antimicrobial and Anticancer Agents.COA of Formula: C2H4ClNO And the article contains the following content:

The growing risk of antimicrobial resistance besides the continuous increase in the number of cancer patients represents a great threat to global health, which requires intensified efforts to discover new bioactive compounds to use as antimicrobial and anticancer agents. Thus, a new set of pyridothienopyrimidine derivatives 2a,b-9a,b was synthesized via cyclization reactions of 3-amino-thieno[2,3-b]pyridine-2-carboxamides 1a,b with different reagents. All new compounds were evaluated against five bacterial and five fungal strains. Many of the target compounds showed significant antimicrobial activity. In addition, the new derivatives were further subjected to cytotoxicity evaluation against HepG-2 and MCF-7 cancer cell lines. The most potent cytotoxic candidates (3a, 4a, 5a, 6b, 8b and 9b) were examined as EGFR kinase inhibitors. Mol. docking study was also performed to explore the binding modes of these derivatives at the active site of EGFR-PK. Compounds 3a, 5a and 9b displayed broad spectrum antimicrobial activity with MIC ranges of 4-16 μg/mL and potent cytotoxic activity with IC50 ranges of 1.17-2.79 μM. In addition, they provided suppressing activity against EGFR with IC50 ranges of 7.27-17.29 nM, higher than that of erlotinib, IC50 = 27.01 nM. The experimental process involved the reaction of 2-Chloroacetamide(cas: 79-07-2).COA of Formula: C2H4ClNO

The Article related to pyridothienopyrimidine derivative biol evaluation antimicrobial anticancer agent, egfr-pk inhibition, hepg-2 cells, mcf-7 cells, antimicrobial activity, cyclization reactions, molecular docking, pyridothienopyrimidines, thieno[2,3-b]pyridine and other aspects.COA of Formula: C2H4ClNO

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

On February 20, 2020, Klann, Kevin; Tascher, Georg; Muench, Christian published an article.Application In Synthesis of 2-Chloroacetamide The title of the article was Functional Translatome Proteomics Reveal Converging and Dose-Dependent Regulation by mTORC1 and eIF2α. And the article contained the following:

Regulation of translation is essential during stress. However, the precise sets of proteins regulated by the key translational stress responses-the integrated stress response (ISR) and mTORC1-remain elusive. We developed multiplexed enhanced protein dynamics (mePROD) proteomics, adding signal amplification to dynamic-SILAC and multiplexing, to enable measuring acute changes in protein synthesis. Treating cells with ISR/mTORC1-modulating stressors, we showed extensive translatome modulation with ∼20% of proteins synthesized at highly reduced rates. Comparing translation-deficient sub-proteomes revealed an extensive overlap demonstrating that target specificity is achieved on protein level and not by pathway activation. Titrating cap-dependent translation inhibition confirmed that synthesis of individual proteins is controlled by intrinsic properties responding to global translation attenuation. This study reports a highly sensitive method to measure relative translation at the nascent chain level and provides insight into how the ISR and mTORC1, two key cellular pathways, regulate the translatome to guide cellular survival upon stress. The experimental process involved the reaction of 2-Chloroacetamide(cas: 79-07-2).Application In Synthesis of 2-Chloroacetamide

The Article related to proteomics translatome mtorc1 eif2alpha protein dynamics integrated stress response, silac, tmt, cap-dependent translation, integrated stress response, mtor, proteomics, pulse labeling, stress response, translation, unfolded protein response and other aspects.Application In Synthesis of 2-Chloroacetamide

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

On August 16, 2021, Kuskov, Andrey; Selina, Oxana; Kulikov, Pavel; Imatdinov, Ilnaz; Balysheva, Vera; Kryukov, Alexander; Shtilman, Mikhail; Markvicheva, Elena published an article.Recommanded Product: 2-Chloroacetamide The title of the article was Amphiphilic Poly(N-Vinylpyrrolidone) Nanoparticles Loaded with DNA Plasmids Encoding Gn and Gc Glycoproteins of the Rift Valley Fever Virus: Preparation and In Vivo Evaluation. And the article contained the following:

The aim of the study was to develop amphiphilic poly(N-vinylpyrrolidone) (PVP) nanoparticles (NPs) loaded with DNA plasmids encoding Gn and Gc glycoproteins of the Rift Valley fever virus (RVFV) and to study the humoral response in vivo. DNA plasmids were protected from extracellular nucleases by loading in NPs from PVP derivatives modified with amino acids β-alanine (Ala7-PVPOD4000) or glycine (Gly7.5-PVP-OD4000) fabricated by the original self-assembly technique. The obtained NPs were administered in mice and the enhancement of humoral response compared to this one in case of immunization with native DNA plasmids was demonstrated. The NPs loaded with DNA plasmids are promising for the fabrication of various DNA particulate vaccines. The experimental process involved the reaction of 2-Chloroacetamide(cas: 79-07-2).Recommanded Product: 2-Chloroacetamide

The Article related to alanine glycine modified polyvinylpyrrolidone nanoparticle fabrication self assembly cytotoxicity, dna vaccines, gn and gc glycoproteins, rift valley fever virus, amphiphilic polymers, humoral response, nanoparticles, poly(n-vinylpyrrolidone) and other aspects.Recommanded Product: 2-Chloroacetamide

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

On December 7, 2018, Baghdady, Yehia Z.; Schug, Kevin A. published an article.Electric Literature of 27115-50-0 The title of the article was A novel diagnostic in situ derivatization kit for the simultaneous determination of 14 biomarkers of exposure to benzene, toluene, ethyl benzene and xylenes in human urine by isotope dilution liquid chromatography tandem mass spectrometry and kit optimization using response surface methodology. And the article contained the following:

Metabolite profiling can be used as a diagnostic measure for both short and long term co-exposure by individuals to benzene, toluene, ethylbenzene and xylenes (BTEX). A novel one pot derivatization in situ kit (OPDISK) was developed and optimized using a multivariate approach based on central composite design. The OPDISK was designed to simultaneously derivatize, in a urine sample matrix, a series of fourteen carboxylic acid and phenol-bearing urinary metabolites of BTEX to enhance their chromatog. anal. and sensitivity for detection by liquid chromatog. – electrospray ionization – tandem mass spectrometry (LC-ESI-MS/MS). Using the reagent kit, the less responsive functional units on the mols. were converted to permanently pos.-charged functional units. The kit was composed of three components, 2-fluoro-1-methylpyridinium p-toluenesulfonate (FMP), 3-carbinol-1-methylpyridinium iodide (CMP) and triethylamine (TEA) as a basic catalyst and, only after diluting a urine sample 20-fold with acetonitrile, was applied under mild conditions of room temperature and short reaction time of 20 min. The derivatized biomarkers were then directly analyzed using isotope dilution LC-ESI-MS/MS. The method was sensitive (limit of detection on column ranged from 1.4 pg to 3.1 ng), accurate (mean accuracy from 85% to 114%), and precise (mean coefficient of variation from 1% to 14%). The method results indicated a good linearity (R2 ≥0.990) for all metabolites. ClinChek urine control samples were used successfully to demonstrate the accuracy of the method. The experimental process involved the reaction of 2-(4-Methylbenzamido)acetic acid(cas: 27115-50-0).Electric Literature of 27115-50-0

The Article related to benzene toluene ethylbenzene xylene exposure biomarker determination urine, btex exposure biomarker determination human urine lc ms opdisk, btex, biomarkers, central composite design, in situ derivatization, metabolites, occupational exposure and other aspects.Electric Literature of 27115-50-0

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

On October 15, 2015, Mueller, Thomas Ernst; Guertler, Christoph; Basu, Susmit; Leitner, Walter published a patent.Application of 5455-98-1 The title of the patent was Method for the production of oxazolidinone compounds. And the patent contained the following:

The present invention relates to a method for the production of oxazolidinone compounds, comprising the step of slowly reacting an isocyanate compound with an epoxide compound in the presence of a Lewis acid catalyst. The invention further relates to an oxazolidinone compound, obtainable by a method according to the invention, with a color as determined according to ASTM D1209-05 (2011) of ≤200 and a molar ratio of the oxazolidinone compound to isocyanurate byproduct o/i of ≥85/15. Lastly, the invention relates to an oligomeric or polymeric oxazolidinone compound, obtainable by a method according to the invention using an isocyanate compound with two or more NCO groups per mol. and an epoxide compound with two or more epoxy groups per mol., comprising at least two units derived from the isocyanate compound and at least two units derived from the epoxide compound, with a color as determined according to ASTM D1209-05 (2011) of ≤200. The experimental process involved the reaction of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione(cas: 5455-98-1).Application of 5455-98-1

The Article related to oxazolidinone derivative manufacture epoxide isocyanate reaction lewis acid catalyst, diepoxide diisocyanate copolymer manufacture lewis acid catalyst, discoloration prevention oxazolidinone derivative manufacture lewis acid reaction catalyst and other aspects.Application of 5455-98-1

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

On May 22, 2014, Mueller, Thomas Ernst; Guertler, Christoph; Basu, Susmit; Leitner, Walter published a patent.Formula: C11H9NO3 The title of the patent was Production of low and high molecular weight oxazolidinone compounds. And the patent contained the following:

The invention relates to a method for the production of oxazolidinone compounds, comprising the step of slowly reacting an isocyanate compound with an epoxide compound in the presence of a Lewis acid catalyst. The invention further relates to an oxazolidinone compound, obtainable by a method according to the invention, with a color as determined according to ASTM D1209 – 05 (2011) of ≤200 and a molar ratio of the oxazolidinone compound to isocyanurate byproduct o/i of ≥85/15. Lastly, the invention relates to an oligomeric or polymeric oxazolidinone compound, obtainable by a method according to the invention using an isocyanate compound with two or more NCO groups per mol. and an epoxide compound with two or more epoxy groups per mol., comprising at least two units derived from the isocyanate compound and at least two units derived from the epoxide compound, with a color as determined according to ASTM D1209 – 05 (2011) of ≤200. The experimental process involved the reaction of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione(cas: 5455-98-1).Formula: C11H9NO3

The Article related to oxazolidinone derivative manufacture epoxide isocyanate reaction lewis acid catalyst, diepoxide diisocyanate copolymer manufacture lewis acid catalyst, discoloration prevention oxazolidinone derivative manufacture lewis acid reaction catalyst and other aspects.Formula: C11H9NO3

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

On April 1, 2020, Liu, Lulu; Liu, Renshuai; Yang, Xinying; Hou, Xuben; Fang, Hao published an article.Application of 97-09-6 The title of the article was Design, synthesis and biological evaluation of tyrosine derivatives as Mcl-1 inhibitors. And the article contained the following:

The upregulation of the protein myeloid cell leukemia-1 (Mcl-1) is closely associated with various human cancers, which can result in the evasion of apoptosis and a low survival rate. Therefore, developing Mcl-1 inhibitors has become a promising paradigm for cancer therapy. Herein, we designed and synthesized a novel series of tyrosine derivatives, among which compounds (I) (R1 = 3,5-di-Me-4-Cl-Ph, X = H, R2 = OBut, n = 2; R1 = 3,5-di-Me-4-Cl-Ph, X = H, R2 = Ph, n = 1; R1 = naphthyl, X = Br, R2 = 4-Me-benzyl, n = 1) exhibited very high binding affinity to Mcl-1 with Ki values of 0.18, 0.27 and 0.23μM, resp. Interestingly, compound I (R1 = 3,5-di-Me-4-Cl-Ph, X = H, R2 = Ph, n = 1) showed not only potent activity against Mcl-1 but also considerable selectivity over Bcl-2 and Bcl-xL, which was rationalized by mol. docking and fragment-centric topog. mapping (FCTM). It is worth noting that compounds I (R1 = 3,5-di-Me-4-Cl-Ph, X = H, R2 = OBut, n = 2; R1 = 3,5-di-Me-4-Cl-Ph, X = H, R2 = Ph, n = 1; R1 = naphthyl, X = Br, R2 = 4-Me-benzyl, n = 1) displayed potent antiproliferative activity against several cancer cell lines and could induce apoptosis of KM3 and HepG2 cells in a dose-dependent manner. The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Application of 97-09-6

The Article related to peptidomimetic tyrosine synthesis drug design apoptosis, mol docking mcl1 inhibitor peptidomimetic, tyrosine methyl ester bromoalkane condensation benzenesulfonamide amidation coupling, apoptosis, cancer, mcl-1 inhibitors, tyrosine derivatives and other aspects.Application of 97-09-6

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

On October 18, 2021, Uzal-Varela, Rocio; Valencia, Laura; Lalli, Daniela; Maneiro, Marcelino; Esteban-Gomez, David; Platas-Iglesias, Carlos; Botta, Mauro; Rodriguez-Rodriguez, Aurora published an article.Application of 79-07-2 The title of the article was Understanding the Effect of the Electron Spin Relaxation on the Relaxivities of Mn(II) Complexes with Triazacyclononane Derivatives. And the article contained the following:

Investigating the relaxation of water 1H nuclei induced by paramagnetic Mn(II) complexes is important to understand the mechanisms that control the efficiency of contrast agents used in diagnostic magnetic resonance imaging (MRI). Herein, a series of potentially hexadentate triazacyclononane (TACN) derivatives containing different pendant arms were designed to explore the relaxation of the electron spin in the corresponding Mn(II) complexes using a combination of 1H NMR relaxometry and theor. calculations These ligands include 1,4,7-triazacyclononane-1,4,7-triacetic acid (H3NOTA) and three derivatives in which an acetate group is replaced by sulfonamide (H3NO2ASAm), amide (H2NO2AM) or pyridyl (H2NO2APy) pendants, resp. The analog of H3NOTA containing three propionate pendant arms (H3NOTPrA) was also investigated. The x-ray structure of the derivative containing two acetate groups and a sulfonamide pendant arm [Mn(NO2ASAm)]- evidenced six-coordination of the ligand to the metal ion, with the coordination polyhedron being close to a trigonal prism. The relaxivities of all complexes at 20 MHz and 25° (1.1-1.3 mM-1 s-1) are typical of systems that lack water mols. coordinated to the metal ion. The nuclear magnetic relaxation profiles evidence significant differences in the relaxivities of the complexes at low fields (<1 MHz), which are associated with different spin relaxation rates. The zero field splitting (ZFS) parameters calculated using DFT and CASSCF methods show that electronic relaxation is relatively insensitive to the nature of the donor atoms. However, the twist angle of the two tripodal faces that delineate the coordination polyhedron, defined by the N atoms of the TACN unit (lower face) and the donor atoms of the pendant arms (upper face), has an important effect in the ZFS parameters. A twist angle close to the ideal value for an octahedral coordination (60°), such as that in [Mn(NOTPrA)]-, leads to a small ZFS energy, whereas this value increases as the coordination polyhedron approaches to a trigonal prism. The experimental process involved the reaction of 2-Chloroacetamide(cas: 79-07-2).Application of 79-07-2

The Article related to amido pyridyl triazacyclononanetriacetate manganese complex preparation spin relaxation relaxivity, crystal mol structure manganese trifluoromethylphenylsulfonamido triazacyclononane complex, electrochem redox triazacyclononane manganese complex and other aspects.Application of 79-07-2

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

On May 14, 1996, Roucoux, Alain; Thieffry, Laurent; Carpentier, Jean-Francois; Devocelle, Marc; Meliet, Catherine; Agbossou, Francine; Mortreux, Andre; Welch, Alan J. published an article.Recommanded Product: 65645-88-7 The title of the article was Amidophosphine-Phosphinites: Synthesis and Use in Rhodium-Based Asymmetric Hydrogenation of Activated Keto Compounds. Crystal Structure of Bis[(μ-chloro)((S)-2-((diphenylphosphino)oxy)-2-phenyl- N-(diphenylphosphino)-N-methylacetamide)rhodium(I)]. And the article contained the following:

Amidophosphine-phosphinite ligands (AMPP) derived from (S)-N-benzylmandelamide ((S)-R,R’-benzylmandelNOP (S)-1 (R = R’ = phenyl) and (S)-7 (R = Ph, R’ = cyclopentyl)), (S)-N-methylmandelamide ((S)-R,R’-methylmandelNOP (S)-2 (R = R’ = phenyl) and (S)-8 (R = Ph, R’ = cyclopentyl)), (S)-N-methyllactamide ((S)-R,R’-methyllactaNOP (S)-3 (R = R’ = phenyl) and (S)-9 (R = Ph, R’ = cyclopentyl)), and (S)-2-(hydroxymethyl)-2-pyrrolidinone ((S)-R,R’-oxoProNOP (S)-4-6 and (S)-10 (R, R’ = Ph, cyclohexyl, cyclopentyl)) have been prepared in high yields (60-94%) and reacted with rhodium precursors to prepare neutral “Rh{AMPP}” complexes of general formula [Rh{AMPP}X]2, where X = Cl, I, OCOCH3, OCOCF3, and OCOC3F7. The crystal structure of [Rh{(S)-Ph,Ph-methylmandelNOP}Cl]2 (12) has been determined The rhodium atom has a cis square-planar coordination, and the seven-membered chelate ring has a boat conformation with the nitrogen atom in the mean plane RhP2. Complexes have been used as catalyst precursors for the asym. hydrogenation of dihydro-4,4-dimethyl-2,3-furandione (27) and N-benzylbenzoylformamide (29) giving the corresponding optically active hydroxy compounds in high yields and low to high enantiomeric excesses (28-98.7% ee and 13-87% ee, resp.). Catalytic activities (turnover frequency at 50% conversion at room temperature up to 3300 h-1) as well as the enantioselectivities depended strongly on the nature of the substituents on phosphorus as well as on the nature of the non chiral ligands. Catalyst precursor [Rh{(S)-Cp,Cp-oxoProNOP}OCOCF3]2 afforded (R)-pantolactone in 98.7% ee. The experimental process involved the reaction of (S)-2-Hydroxy-N-methyl-2-phenylacetamide(cas: 65645-88-7).Recommanded Product: 65645-88-7

The Article related to amidophosphine phosphinite preparation reaction rhodium complex, asym hydrogenation catalyst rhodium amidophosphine phosphinite, mandelamide lactamide phosphino preparation reaction rhodium, crystal mol structure amidophosphine phosphinite rhodium and other aspects.Recommanded Product: 65645-88-7

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

On January 31, 2020, Doellinger, Joerg; Schneider, Andy; Hoeller, Marcell; Lasch, Peter published an article.Application of 79-07-2 The title of the article was Sample preparation by easy extraction and digestion (SPEED) – a universal, rapid, and detergent-free protocol for proteomics based on acid extraction. And the article contained the following:

The main challenge of bottom-up proteomic sample preparation is to extract proteomes in a manner that enables efficient protein digestion for subsequent mass spectrometric anal. Today’s sample preparation strategies are commonly conceptualized around the removal of detergents, which are essential for extraction but strongly interfere with digestion and LC-MS. These multi-step preparations contribute to a lack of reproducibility as they are prone to losses, biases and contaminations, while being time-consuming and labor-intensive. We report a detergent-free method, named Sample Preparation by Easy Extraction and Digestion (SPEED), which consists of three mandatory steps, acidification, neutralization and digestion. SPEED is a universal method for peptide generation from various sources and is easily applicable even for lysis-resistant sample types as pure trifluoroacetic acid (TFA) is used for highly efficient protein extraction by complete sample dissolution The protocol is highly reproducible, virtually loss-less, enables very rapid sample processing and is superior to the detergent/chaotropic agent-based methods FASP, ISD-Urea and SP3 for quant. proteomics. SPEED holds the potential to dramatically simplify and standardize sample preparation while improving the depth of proteome coverage especially for challenging samples. The experimental process involved the reaction of 2-Chloroacetamide(cas: 79-07-2).Application of 79-07-2

The Article related to escherichia staphylococcus hela proteomics acid extraction speed, tfa, automation, bacteria, detergent-free, digestion, label-free quantification, lysis, mass spectrometry, microbiome, pathogens, protein denaturation, proteomics, sample preparation and other aspects.Application of 79-07-2

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