Category: 2743-40-0

Zhang, Zhaokuo; Yang, Ziwei; Wu, Yujing; Yuan, Zhen; Du, Jianlong; Li, Lijun published the artcile< Reduced amino acid Schiff base containing ruthenium(III) complexes: Synthesis, characterization, DNA interaction, and in vitro cytotoxicity>, Electric Literature of 2743-40-0, the main research area is amino acid Schiff base ruthenium complex DNA interaction cytotoxicity; DNA; cytotoxicity; ruthenium(III) complexes.

A number of reduced amino Schiff base ligands and corresponding ruthenium(III) complexes were designed and prepared based on the fact that amino acids not only possess multiple coordinate atoms but also improve the solubility of drugs in the body. The interaction of the complexes with calf thymus DNA was analyzed with spectroscopic methods of UV-visible absorption spectra, DNA competitive binding with ethidium bromide, CD spectra, and DNA melting experiments, and DNA viscosity measurements, indicating that the complexes bind to DNA primarily in the grooving mode. With respect to the ligands, the cytotoxicity in vitro of the complexes against Hela, A549, and MCF-7 cells was much enhanced, with most of the IC50 values less than 50μM or even comparable with those of cisplatin.

Journal of Biochemical and Molecular Toxicology published new progress about Amino acids Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 2743-40-0 belongs to class esters-buliding-blocks, and the molecular formula is C8H18ClNO2, Electric Literature of 2743-40-0.

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

Pramanick, Pranab K.; Zhou, Zhibing; Hou, Zhenlin; Ao, Yufei; Yao, Bo published the artcile< Native amine-directed site-selective C(sp3)-H arylation of primary aliphatic amines with aryl iodides>, Reference of 2743-40-0, the main research area is aliphatic amine preparation aryl iodide regioselective arylation; aralkyl amine preparation.

A simple and efficient method for site-selective C(sp3)-H arylation of primary aliphatic amines by aryl iodides were established. In the presence of only 5 mol% Pd(OAc)2, a wide range of aliphatic amines including O-benzyl and O-silyl amino alcs. were arylated at γ- or δ-positions by aryl iodides containing a broad scope of functional groups. The synthetic application of this method had also been demonstrated by large-scale synthesis, the synthesis of a fingolimod analog and the conjugation with natural D-menthol and fluorescent 1,8-naphthalimide.

Chinese Chemical Letters published new progress about Aliphatic amines Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 2743-40-0 belongs to class esters-buliding-blocks, and the molecular formula is C8H18ClNO2, Reference of 2743-40-0.

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

Lewis, Frank W.; Bird, Kathleen; Navarro, Jean-Philippe; El Fallah, Rawa; Brandel, Jeremy; Hubscher-Bruder, Veronique; Tsatsanis, Andrew; Duce, James A.; Tetard, David; Bourne, Samuel; Maina, Mahmoud; Pienaar, Ilse S. published the artcile< Synthesis, physicochemical characterization and neuroprotective evaluation of novel 1-hydroxypyrazin-2(1H)-one iron chelators in an in vitro cell model of Parkinson′s disease>, Recommanded Product: H-Leu-OEt.HCl, the main research area is Parkinson disease iron chelator physicochem property neuroprotective.

Iron dysregulation, dopamine depletion, cellular oxidative stress and α-synuclein protein mis-folding are key neuronal pathol. features seen in the progression of Parkinson′s disease. Iron chelators endowed with one or more therapeutic modes of action have long been suggested as disease modifying therapies for its treatment. In this study, novel 1-hydroxypyrazin-2(1H)-one iron chelators were synthesized and their physicochem. properties, iron chelation abilities, antioxidant capacities and neuroprotective effects in a cell culture model of Parkinson′s disease were evaluated. Physicochem. properties (log β, log D7.4, pL0.5) suggest that these ligands have a poorer ability to penetrate cell membranes and form weaker iron complexes than the closely related 1-hydroxypyridin-2(1H)-ones. Despite this, we show that levels of neuroprotection provided by these ligands against the catecholaminergic neurotoxin 6-hydroxydopamine in vitro were comparable to those seen previously with the 1-hydroxypyridin-2(1H)-ones and the clin. used iron chelator Deferiprone, with two of the ligands restoring cell viability to ≥89% compared to controls. Two of the ligands were endowed with addnl. phenol moieties in an attempt to derive multifunctional chelators with dual iron chelation/antioxidant activity. However, levels of neuroprotection with these ligands were no greater than ligands lacking this moiety, suggesting the neuroprotective properties of these ligands are due primarily to chelation and passivation of intracellular labile iron, preventing the generation of free radicals and reactive oxygen species that otherwise lead to the neuronal cell death seen in Parkinson′s disease.

Dalton Transactions published new progress about Antioxidants. 2743-40-0 belongs to class esters-buliding-blocks, and the molecular formula is C8H18ClNO2, Recommanded Product: H-Leu-OEt.HCl.

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

Chen, Yuan; Fu, Lulu; Sun, Baobao; Qian, Cheng; Wang, Ruibing; Jiang, Juli; Lin, Chen; Ma, Jing; Wang, Leyong published the artcile< Competitive Selection of Conformation Chirality of Water-Soluble Pillar[5]arene Induced by Amino Acid Derivatives>, Category: esters-buliding-blocks, the main research area is amino acid ethyl ester hydrochloride induced conformation chirality pillararene.

The competitive conformation chirality of dynamically racemic water-soluble pillar[5]arene WP5 can be induced by 19 different L-amino acid Et ester hydrochlorides. Among them, L-Arg-OEt and 18 other L-amino acid Et ester hydrochlorides can induce the opposite-handedness conformation of WP5. This was ascribed to the different binding models with a side-chain moiety or Et ester moiety of amino acids toward the cavity of WP5.

Organic Letters published new progress about Amino acid esters Role: PEP (Physical, Engineering or Chemical Process), PRP (Properties), RCT (Reactant), SPN (Synthetic Preparation), PROC (Process), RACT (Reactant or Reagent), PREP (Preparation) (hydrochlorides). 2743-40-0 belongs to class esters-buliding-blocks, and the molecular formula is C8H18ClNO2, Category: esters-buliding-blocks.

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

Ossowicz, Paula; Kardaleva, Proletina; Guncheva, Maya; Klebeko, Joanna; Swiatek, Ewelina; Janus, Ewa; Yancheva, Denitsa; Angelov, Ivan published the artcile< Ketoprofen-based ionic liquids: synthesis and interactions with bovine serum albumin>, Application In Synthesis of 2743-40-0, the main research area is ketoprofen based ionic liquid formulation bovine serum albumin; binding constants; bovine serum albumin; ionic liquids; ketoprofen; secondary structure.

The development of ionic liquids based on active pharmaceutical ingredients (API-ILs) is a possible solution to some of the problems of solid and/or hydrophobic drugs such as low solubility and bioavailability, polymorphism and an alternative route of administration could be suggested as compared to the classical drug. Here, we report for the first time the synthesis and detailed characterization of a series of ILs containing a cation amino acid esters and anion ketoprofen (KETO-ILs). The affinity and the binding mode of the KETO-ILs to bovine serum albumin (BSA) were assessed using fluorescence spectroscopy. All compounds bind in a distance not longer than 6.14 nm to the BSA fluorophores. The estimated binding constants (KA) are in order of 105 L mol-1, which is indicative of strong drug or IL-BSA interactions. With respect to the ketoprofen-BSA system, a stronger affinity of the ILs containing l-LeuOEt, l-ValOBu, and l-ValOEt cation towards BSA is clearly seen. Fourier transformed IR spectroscopy experiments have shown that all studied compounds induced a rearrangement of the protein mol. upon binding, which is consistent with the suggested static mechanism of BSA fluorescence quenching and formation of complexes between BSA and the drugs. All tested compounds were safe for macrophages.

Molecules published new progress about Bovine serum albumin Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 2743-40-0 belongs to class esters-buliding-blocks, and the molecular formula is C8H18ClNO2, Application In Synthesis of 2743-40-0.

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

Guerfi, Meriem; Berredjem, Malika; Bahadi, Rania; Djouad, Seif-Eddine; Bouzina, Abdeslem; Aissaoui, Mohamed published the artcile< An efficient synthesis, characterization, DFT study and molecular docking of novel sulfonylcycloureas>, Formula: C8H18ClNO2, the main research area is sulfonylcyclourea preparation DFT mol docking; sulfonamide ethyl bis chloroethyl carbamate cyclization.

Sulfonylcycloureas derivatives I (R = H, i-Bu, Bn, etc.) are novel heterocyclic compounds synthesized by condensation reaction of several sulfonamides derived from aminoesters with Et bis(2-chloroethyl)carbamate. Series of these desired products are obtained from good to excellent yields within 3-4 h in all cases. Mol. docking are used to study the anticancer activity of the most active compounds Mol. docking of the mol.s into the AKR1C1 crystal structure reveals the key interactions with the active site. The theor. calculations for the compounds I were performed using DFT/B3LYP/6-31 G (d,p) method. The optimized structural parameters, Frontier MOs (FMO’s) and global reactivity descriptors were determined The dipole moment (μ), polarizability (α) and first order hyperpolarizability (β) values of the title compound have been computed at the same level of theory on the finite field approach.

Journal of Molecular Structure published new progress about Amino acid esters Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 2743-40-0 belongs to class esters-buliding-blocks, and the molecular formula is C8H18ClNO2, Formula: C8H18ClNO2.

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

Cortes-Clerget, Margery; Lee, Nicholas R.; Lipshutz, Bruce H. published the artcile< Synthetic chemistry in water: Applications to peptide synthesis and nitro group reductions>, Safety of H-Leu-OEt.HCl, the main research area is peptide synthesis coupling water green chem solvent cosolvent; amine synthesis nitro group reduction carbonyl iron powder safety.

Amide bond formation and aromatic/heteroaromatic nitro-group reductions represent two of the most commonly used transformations in organic synthesis. Unfortunately, such processes can be especially wasteful and hence environmentally harmful, and may present safety hazards as well, given the reaction conditions involved. The two protocols herein describe alternative technologies that offer solutions to these issues. Polypeptides can now be made in water at ambient temperatures using small amounts of the designer surfactant TPGS-750-M, thereby eliminating the use of organic solvents as the reaction medium. Likewise, a safe, inexpensive and efficient procedure is outlined for nitro-group reductions, using industrial iron in the form of carbonyl iron powder (CIP), an inexpensive item of commerce. The peptide synthesis will typically take, overall, 3-4 h for a simple coupling and 8 h for a two-step deprotection/coupling process. The workup usually consists of a simple extraction and acidic/basic aqueous washings. The nitro reduction procedure will typically take 6-8 h to complete, including setup, reaction time and workup.

Nature Protocols published new progress about Amide group (amide bond). 2743-40-0 belongs to class esters-buliding-blocks, and the molecular formula is C8H18ClNO2, Safety of H-Leu-OEt.HCl.

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

Wang, Xinmou; Yu, Mo; Song, Hongjian; Liu, Yuxiu; Wang, Qingmin published the artcile< Radical Transformation of Aliphatic C-H Bonds to Oxime Ethers via Hydrogen Atom Transfer>, HPLC of Formula: 2743-40-0, the main research area is oxime ether preparation regioselective; alkane oxime radical transformation.

Herein, a strategy for conversion of aliphatic C-H bonds to oxime ethers via hydrogen atom transfer was described. In this strategy, the decatungstate anion and sulfate radical played complementary roles in the abstraction of hydrogen atoms from primary, secondary, and tertiary C-H bonds of alkanes. The easy accessibility of alkanes and the broad substrate scope, mild conditions, and excellent regioselectivity of these reactions made this strategy applicable for the transformation of raw materials to high-value chems.

Organic Letters published new progress about Alkanes Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 2743-40-0 belongs to class esters-buliding-blocks, and the molecular formula is C8H18ClNO2, HPLC of Formula: 2743-40-0.

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

Sherrill, Lavinia M.; Joya, Elva E.; Walker, AnnMarie; Roy, Anuradha; Alhammad, Yousef M.; Atobatele, Moriama; Wazir, Sarah; Abbas, George; Keane, Patrick; Zhuo, Junlin; Leung, Anthony K. L.; Johnson, David K.; Lehtio, Lari; Fehr, Anthony R.; Ferraris, Dana published the artcile< Design, synthesis and evaluation of inhibitors of the SARS-CoV-2 nsp3 macrodomain>, HPLC of Formula: 2743-40-0, the main research area is SARS CoV2 coronavirus nsp3 macrodomain inhibitor COVID19; ADP-ribosylation; COVID-19; Coronavirus; Nsp3 macrodomain inhibitors; SARS-CoV-2.

A series of amino acid based 7H-pyrrolo[2,3-d]pyrimidines were designed and synthesized to discern the structure activity relationships against the SARS-CoV-2 nsp3 macrodomain (Mac1), an ADP-ribosylhydrolase that is critical for coronavirus replication and pathogenesis. Structure activity studies identified compound 15c as a low-micromolar inhibitor of Mac1 in two ADP-ribose binding assays. This compound also demonstrated inhibition in an enzymic assay of Mac1 and displayed a thermal shift comparable to ADPr in the melting temperature of Mac1 supporting binding to the target protein. A structural model reproducibly predicted a binding mode where the pyrrolo pyrimidine forms a hydrogen bonding network with Asp22 and the amide backbone NH of Ile23 in the adenosine binding pocket and the carboxylate forms hydrogen bonds to the amide backbone of Phe157 and Asp156, part of the oxyanion subsite of Mac1. Compound 15c also demonstrated notable selectivity for coronavirus macrodomains when tested against a panel of ADP-ribose binding proteins. Together, this study identified several low MW, low 娓璏 Mac1 inhibitors to use as small mol. chem. probes for this potential anti-viral target and offers starting points for further optimization.

Bioorganic & Medicinal Chemistry published new progress about Anticoronaviral agents. 2743-40-0 belongs to class esters-buliding-blocks, and the molecular formula is C8H18ClNO2, HPLC of Formula: 2743-40-0.

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

Sherrill, Lavinia M.; Joya, Elva E.; Walker, AnnMarie; Roy, Anuradha; Alhammad, Yousef M.; Atobatele, Moriama; Wazir, Sarah; Abbas, George; Keane, Patrick; Zhuo, Junlin; Leung, Anthony K. L.; Johnson, David K.; Lehtio, Lari; Fehr, Anthony R.; Ferraris, Dana published the artcile< Design, synthesis and evaluation of inhibitors of the SARS-CoV-2 nsp3 macrodomain>, HPLC of Formula: 2743-40-0, the main research area is SARS CoV2 coronavirus nsp3 macrodomain inhibitor COVID19; ADP-ribosylation; COVID-19; Coronavirus; Nsp3 macrodomain inhibitors; SARS-CoV-2.

A series of amino acid based 7H-pyrrolo[2,3-d]pyrimidines were designed and synthesized to discern the structure activity relationships against the SARS-CoV-2 nsp3 macrodomain (Mac1), an ADP-ribosylhydrolase that is critical for coronavirus replication and pathogenesis. Structure activity studies identified compound 15c as a low-micromolar inhibitor of Mac1 in two ADP-ribose binding assays. This compound also demonstrated inhibition in an enzymic assay of Mac1 and displayed a thermal shift comparable to ADPr in the melting temperature of Mac1 supporting binding to the target protein. A structural model reproducibly predicted a binding mode where the pyrrolo pyrimidine forms a hydrogen bonding network with Asp22 and the amide backbone NH of Ile23 in the adenosine binding pocket and the carboxylate forms hydrogen bonds to the amide backbone of Phe157 and Asp156, part of the oxyanion subsite of Mac1. Compound 15c also demonstrated notable selectivity for coronavirus macrodomains when tested against a panel of ADP-ribose binding proteins. Together, this study identified several low MW, low 渭M Mac1 inhibitors to use as small mol. chem. probes for this potential anti-viral target and offers starting points for further optimization.

Bioorganic & Medicinal Chemistry published new progress about Anticoronaviral agents. 2743-40-0 belongs to class esters-buliding-blocks, and the molecular formula is C8H18ClNO2, HPLC of Formula: 2743-40-0.

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