Month: October 2022

《Synthesis of 4-Aryl-1,7-naphthyridine-2(1H)-thiones by the Electrocyclic Reaction of 4-(1-Arylalk-1-enyl)-3-isothiocyanatopyridines Generated in situ from the Corresponding Isocyanides》 was written by Kobayashi, Kazuhiro; Kozuki, Taketoshi; Suzuki, Teruhiko. Quality Control of 2,2-Dimehtyl-N-pyridin-3-yl-propionamide And the article was included in Helvetica Chimica Acta on April 17 ,2012. The article conveys some information:

A convenient synthesis for 4-substituted and 3,4-disubstituted 1,7-naphthyridine-2(1H)-thiones has been developed. The method is based on the electrocyclic reaction of 4-(1-arylalk-1-enyl)-3-isothiocyanatopyridines, generated in situ by the treatment of the resp. isocyanides with S8 in the presence of a catalytic amount of selenium. The isocyanides can be easily prepared from com. available pyridin-3-amine by conventional organic reactions. In the experiment, the researchers used many compounds, for example, 2,2-Dimehtyl-N-pyridin-3-yl-propionamide(cas: 70298-88-3Quality Control of 2,2-Dimehtyl-N-pyridin-3-yl-propionamide)

2,2-Dimehtyl-N-pyridin-3-yl-propionamide(cas: 70298-88-3) belongs to anime. Primary amines having a tertiary alkyl group (R3CNH2) are difficult to prepare with most methods but are made industrially by the Ritter reaction. In this method a tertiary alcohol reacts with hydrogen cyanide (HCN) in the presence of a concentrated strong acid; a formamide, RNH―CHO, is formed first, which then undergoes hydrolysis.Quality Control of 2,2-Dimehtyl-N-pyridin-3-yl-propionamide

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

《Systematic evaluation of textural properties, activation temperature and gas uptake of Cu2(pzdc)2L [L = dipyridyl-based ligands] porous coordination pillared-layer networks》 was published in Dalton Transactions in 2012. These research results belong to Garcia-Ricard, Omar J.; Silva-Martinez, Juan C.; Hernandez-Maldonado, Arturo J.. Category: amides-buliding-blocks The article mentions the following:

In situ high temperature x-ray diffraction, nitrogen porosimetry and gas adsorption at room temperature were used to elucidate the effect of the degassing or activation temperature on the long-range and micropore textural properties of a series of coordination polymers with pillared-layer structures. Ramp-and-soak TGA performed at selected activation temperatures were used to verify the thermal stability of a CPL-n series [Cu2(pzdc)2L; H2pzdc = pyrazine-2,3-dicarboxylic acid; L = 4,4′-azopyridine (apy) for CPL-4, 1,2-bis(4-pyridyl)ethylene (bpe) for CPL-5, N-(4-pyridyl)isonicotinamide (pia) for CPL-6, and 1,2-bis(4-pyridyl)glycol (dpyg) for CPL-7]. Although the activation temperatures were far below the decomposition point of the complexes, these resulted in significant and unique changes in micropore surface area and volume, even for CPL-4, -5 and -6, which contained pillar ligands with similar dimensions and similar structural long-range order. For the case of CPL-7, however, the framework appeared to be non-porous at any given activation temperature Pure component equilibrium adsorption data gathered for CO2, CH4, and N2 were used to elucidate the CPL-n materials potential for storage and separations at room temperature All of the materials exhibited considerable selectivity toward CO2, particularly at moderate pressures. Meanwhile, CO2 isosteric heats of adsorption indicated that the pore functionalities arising from the pillar ligands provided similar interactions with the adsorbate in the cases of CPL-4 and -5. For CPL-6, the presence of the carbonyl (C:O) group appeared to enhance interactions with CO2 at low loadings. After reading the article, we found that the author used N-(Pyridin-4-yl)isonicotinamide(cas: 64479-78-3Category: amides-buliding-blocks)

N-(Pyridin-4-yl)isonicotinamide(cas: 64479-78-3) belongs to amides. The solubilities of amides and esters are roughly comparable. Typically amides are less soluble than comparable amines and carboxylic acids since these compounds can both donate and accept hydrogen bonds.Category: amides-buliding-blocks

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

Formula: C11H22N2O4On May 20, 2022 ,《Exploration of Methanomethylophilus alvus pyrrolysyl-tRNA synthetase activity in yeast》 appeared in ACS Synthetic Biology. The author of the article were Stieglitz, Jessica T.; Lahiri, Priyanka; Stout, Matthew I.; Van Deventer, James A.. The article conveys some information:

Archaeal pyrrolysyl-tRNA synthetases (PylRSs) have been used to genetically encode over 200 distinct noncanonical amino acids (ncAAs) in proteins in Escherichia coli and mammalian cells. This vastly expands the range of chem. functionality accessible within proteins produced in these organisms. Despite these clear successes, explorations of PylRS function in yeast remain limited. In this work, we demonstrate that the Methanomethylophilus alvus PylRS (MaPylRS) and its cognate tRNACUAMaPyl support the incorporation of ncAAs into proteins produced in Saccharomyces cerevisiae using stop codon suppression methodologies. Addnl., we prepared three MaPylRS mutants originally engineered in E. coli and determined that all three were active with one or more ncAAs, although with low efficiencies of ncAA incorporation in comparison to the parent MaPylRS. Alongside MaPylRS variants, we evaluated the activity of previously reported Methanosarcina mazei, Methanosarcina barkeri, and chimeric M. mazei and M. barkeri PylRSs. Using S. cerevisiae RJY100 and pairing these PylRSs with the M. mazei tRNACUA, we did not observe any detectable stop codon suppression activity under the same conditions that produced moderately efficient ncAA incorporation with MaPylRS. The addition of MaPylRS/tRNACUAMaPyl to the orthogonal translation machinery toolkit in S. cerevisiae potentially opens the door to hundreds of ncAAs that have not previously been genetically encodable using other aminoacyl-tRNA synthetase/tRNA pairs. Extending the scope of ncAA incorporation in yeast could powerfully advance chem. and biol. research for applications ranging from basic biol. discovery to enzyme engineering and therapeutic protein lead discovery. The experimental process involved the reaction of H-Lys(Boc)-OH(cas: 2418-95-3Formula: C11H22N2O4)

H-Lys(Boc)-OH(cas: 2418-95-3) belongs to amino acids. Amino acids are not generally considered to be electrochemically active because products of the oxidation accumulate on the electrode surface and prevent it from participating in any further electrochemical processes.Formula: C11H22N2O4

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

Reference of H-Lys(Boc)-OHOn May 17, 2019 ,《Genetic incorporation of noncanonical amino acids using two mutually orthogonal quadruplet codons》 appeared in ACS Synthetic Biology. The author of the article were Hankore, Erome Daniel; Zhang, Linyi; Chen, Yan; Liu, Kun; Niu, Wei; Guo, Jiantao. The article conveys some information:

Genetic incorporation of noncanonical amino acids has emerged as a powerful tool for the study of protein structure and function. While the three triplet nonsense codons have been widely explored, quadruplet codons have attracted attention for the potential of creating addnl. blank codons for noncanonical amino acid mutagenesis. Here we demonstrated for the first time that two orthogonal quadruplet codons could be used to simultaneously encode two different noncanonical amino acids within a single protein in bacterial cells. To achieve this, we fine-tuned the interaction between aminoacyl-tRNA synthetase and tRNA, which afforded up to 21-fold improvement in quadruplet codon decoding efficiency. This work represents a significant step toward the use of multiple quadruplet codons for noncanonical amino acid mutagenesis. Simultaneous incorporation of two or more noncanonical amino acids is of significant importance for biol. applications that can benefit from multiple unique functional groups, such as fluorescence resonance energy transfer and NMR studies, and ultimately for the synthesis of completely unnatural biopolymers as new biomaterials. After reading the article, we found that the author used H-Lys(Boc)-OH(cas: 2418-95-3Reference of H-Lys(Boc)-OH)

H-Lys(Boc)-OH(cas: 2418-95-3) belongs to amino acids. Amino acids are not generally considered to be electrochemically active because products of the oxidation accumulate on the electrode surface and prevent it from participating in any further electrochemical processes.Reference of H-Lys(Boc)-OH

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

Electric Literature of C9H7ClF3NOOn March 10, 2015, Gantenbein, Markus; Hellstern, Manuel; Le Pleux, Loic; Neuburger, Markus; Mayor, Marcel published an article in Chemistry of Materials. The article was 《New 4,4′-Bis(9-carbazolyl)-Biphenyl Derivatives with Locked Carbazole-Biphenyl Junctions: High-Triplet State Energy Materials》. The article mentions the following:

We synthesized a series of 4,4′-bis(9-carbazolyl)-biphenyl (CBP) derivatives, using Me groups as spatially demanding groups, locking the angle between the carbazole subunit and the biphenyl backbone as potential matrix material for blue organic light-emitting diodes (OLEDs). The locked rotation was achieved by four Me groups either in positions 1 and 8 of the carbazole subunit (1) or in positions 3, 5, 3′, and 5′ of the biphenyl subunit (2), and the fixed spatial arrangement was confirmed by X-ray anal. The phys. properties of CBP derivatives based on parent structure 2 were further tailored by electron-withdrawing CF3 groups in positions 3 and 6 (3) or positions 2 and 7 of the carbazole subunits (4) or alternatively by electron-donating CH3O groups in positions 2 and 7 (5) of the same building blocks. Increased triplet energies (ET) compared to that of the parent compound CBP were found for all synthesized CBP derivatives 1-5. Enhanced glass transition temperatures ranging between 129 and 202 °C further corroborate the application potential of these derivatives for matrix material in blue OLEDs. In the experiment, the researchers used N-(2-Chloro-4-(trifluoromethyl)phenyl)acetamide(cas: 247170-19-0Electric Literature of C9H7ClF3NO)

N-(2-Chloro-4-(trifluoromethyl)phenyl)acetamide(cas: 247170-19-0) belongs to anime. Examples of direct uses of amines and their salts are as corrosion inhibitors in boilers and in lubricating oils (morpholine), as antioxidants for rubber and roofing asphalt (diarylamines), as stabilizers for cellulose nitrate explosives (diphenylamine), as protectants against damage from gamma radiation (diarylamines), as developers in photography (aromatic diamines), as flotation agents in mining, as anticling and waterproofing agents for textiles, as fabric softeners, in paper coating, and for solubilizing herbicides.Electric Literature of C9H7ClF3NO

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

Related Products of 64479-78-3On March 8, 2012, Li, Rongshi; Martin, Mathew P.; Liu, Yan; Wang, Binglin; Patel, Ronil A.; Zhu, Jin-Yi; Sun, Nan; Pireddu, Roberta; Lawrence, Nicholas J.; Li, Jiannong; Haura, Eric B.; Sung, Shen-Shu; Guida, Wayne C.; Schonbrunn, Ernst; Sebti, Said M. published an article in Journal of Medicinal Chemistry. The article was 《Fragment-Based and Structure-Guided Discovery and Optimization of Rho Kinase Inhibitors》. The article mentions the following:

Using high concentration biochem. assays and fragment-based screening assisted by structure-guided design, we discovered a novel class of Rho-kinase inhibitors. Compound 18 (I) was equipotent for ROCK1 (IC50 = 650 nM) and ROCK2 (IC50 = 670 nM), whereas compound 24 was more selective for ROCK2 (IC50 = 100 nM) over ROCK1 (IC50 = 1690 nM). The crystal structure of the compound 18-ROCK1 complex revealed that 18 is a type 1 inhibitor that binds the hinge region in the ATP binding site. Compounds 18 and 24 inhibited potently the phosphorylation of the ROCK substrate MLC2 in intact human breast cancer cells. In the experiment, the researchers used N-(Pyridin-4-yl)isonicotinamide(cas: 64479-78-3Related Products of 64479-78-3)

N-(Pyridin-4-yl)isonicotinamide(cas: 64479-78-3) belongs to amides.Related Products of 64479-78-3 The solubilities of amides and esters are roughly comparable. Typically amides are less soluble than comparable amines and carboxylic acids since these compounds can both donate and accept hydrogen bonds.

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

Formula: C13H26N2O4On September 15, 2019 ,《Preparation and biological evaluation of soluble tetrapeptide epoxyketone proteasome inhibitors》 was published in Bioorganic & Medicinal Chemistry. The article was written by Lei, Meng; Zhang, Haoyang; Miao, Hang; Du, Xiao; Zhou, Hui; Wang, Jia; Wang, Xueyuan; Feng, Huayun; Shi, Jingmiao; Liu, Zhaogang; Shen, Jian; Zhu, Yongqiang. The article contains the following contents:

A series of novel tetrapeptidyl epoxyketone inhibitors of 20S proteasome was designed and synthesized. To fully understand the SAR, various groups at R1, R2, R3, R4 and R5 positions, including aromatic and aliphatic substituents were designed, synthesized and biol. assayed. Based on the enzymic results, seven compounds were selected to evaluate their cellular activities and soluble compound (I) showed strong potency against human multiple myeloma (MM) cell lines. Microsomal stability results indicated that compound I was more stable in mice, rat and human microsomes than marketed carfilzomib. The in vivo activities of this compound were evaluated with the xenograft mice models of MM cell lines ARH77 and RPMI-8226 with luciferase expression and the T/C value of the two models were 49.5% and 37.6%, resp. To evaluate the potential cardiovascular toxicity, inhibition of hERG ion channel in HEK293 cells by compound I and carfilzomib was carried out. The results indicated that I had no binding affinity for the hERG ion channel while carfilzomib could bind it with IC50 of 92.1 μM. The experimental part of the paper was very detailed, including the reaction process of (S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamide(cas: 87694-50-6Formula: C13H26N2O4)

(S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamide(cas: 87694-50-6) belongs to amides.Formula: C13H26N2O4 The solubilities of amides and esters are roughly comparable. Typically amides are less soluble than comparable amines and carboxylic acids since these compounds can both donate and accept hydrogen bonds.

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

In 1999,Journal of Molecular Modeling included an article by Wang, Jiansuo; Lai, Luhua; Tang, Youqi. HPLC of Formula: 4746-61-6. The article was titled 《Data mining of toxic chemicals: structure patterns and QSAR》. The information in the text is summarized as follows:

The authors take a two-step strategy to explore non-congeneric toxic chems. from the database RTECS: the screening of structure patterns and the generation of a detailed relationship between structure and activity. An efficient similarity comparison is proposed to screen chem. patterns for further QSAR anal. Then CoMFA study is carried out on one structure pattern as an example of the implementation, and the result shows that QSAR studies of structure patterns can provide an estimate of the activity as well as a detailed relationship between activity and structure. From the performance of overall procedure, such a stepwise scheme is demonstrated to be feasible and effective to mine a database of toxic chems.2-Hydroxy-N-phenylacetamide(cas: 4746-61-6HPLC of Formula: 4746-61-6) was used in this study.

2-Hydroxy-N-phenylacetamide(cas: 4746-61-6) belongs to amides. Because of the greater electronegativity of oxygen, the carbonyl (C=O) is a stronger dipole than the N–C dipole.HPLC of Formula: 4746-61-6 The presence of a C=O dipole and, to a lesser extent a N–C dipole, allows amides to act as H-bond acceptors. In primary and secondary amides, the presence of N–H dipoles allows amides to function as H-bond donors as well.

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

In 2020,Advanced Functional Materials included an article by Feng, Jiale; Yang, Lupeng; Romanov, Alexander S.; Ratanapreechachai, Jirawit; Reponen, Antti-Pekka M.; Jones, Saul T. E.; Linnolahti, Mikko; Hele, Timothy J. H.; Koehler, Anna; Baessler, Heinz; Bochmann, Manfred; Credgington, Dan. Quality Control of N-(2-Chloro-4-(trifluoromethyl)phenyl)acetamide. The article was titled 《Environmental Control of Triplet Emission in Donor-Bridge-Acceptor Organometallics》. The information in the text is summarized as follows:

Carbene-metal-amides (CMAs) are a promising family of donor-bridge-acceptor mol. charge-transfer (CT) emitters for organic light-emitting diodes. A universal approach is demonstrated to tune the energy of their CT emission. A blueshift of ≤210 meV is achievable in solid state via dilution in a polar host matrix. The origin of this shift has 2 components: constraint of thermally-activated triplet diffusion, and electrostatic interactions between guest and polar host. This allows the emission of mid-green CMA archetypes to be tuned to sky blue without chem. modifications. Monte-Carlo simulations based on a Marcus-type transfer integral reproduce the concentration- and temperature-dependent triplet diffusion process, revealing a substantial shift in the ensemble d. of states in polar hosts. In Au-bridged CMAs, this shift does not lead to a significant change in luminescence lifetime, thermal activation energy, reorganization energy, or intersystem crossing rate. These discoveries offer new insight into coupling between the singlet and triplet manifolds in CMA materials, revealing a dominant interaction between states of CT character. The same approach is employed using materials which were chem. modified to alter the energy of their CT state directly, shifting the emission of sky-blue chromophores into the practical blue range. In the experiment, the researchers used N-(2-Chloro-4-(trifluoromethyl)phenyl)acetamide(cas: 247170-19-0Quality Control of N-(2-Chloro-4-(trifluoromethyl)phenyl)acetamide)

N-(2-Chloro-4-(trifluoromethyl)phenyl)acetamide(cas: 247170-19-0) belongs to anime. Primary amines having a tertiary alkyl group (R3CNH2) are difficult to prepare with most methods but are made industrially by the Ritter reaction. In this method a tertiary alcohol reacts with hydrogen cyanide (HCN) in the presence of a concentrated strong acid; a formamide, RNH―CHO, is formed first, which then undergoes hydrolysis.Quality Control of N-(2-Chloro-4-(trifluoromethyl)phenyl)acetamide

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

Kaloudi, Aikaterini; Kanellopoulos, Panagiotis; Radolf, Thorsten; Chepurny, Oleg G.; Rouchota, Maritina; Loudos, George; Andreae, Fritz; Holz, George G.; Nock, Berthold Artur; Maina, Theodosia published their research in Molecular Pharmaceutics on August 3 ,2020. The article was titled 《[99mTc]Tc-DGA1, a Promising CCK2R-Antagonist-Based Tracer for Tumor Diagnosis with Single-Photon Emission Computed Tomography》.Reference of H-Lys(Boc)-OH The article contains the following contents:

Radiolabeled gastrin analogs have been proposed for theranostics of cholecystokinin subtype 2 receptor (CCK2R)-pos. cancer. Peptide radioligands based on other receptor antagonists have displayed superior pharmacokinetics and higher biosafety than agonists. Here, we present DGA1, a derivative of the nonpeptidic CCK2R antagonist Z-360 carrying an acyclic tetraamine, for [99mTc]Tc labeling. Preclin. comparison of [99mTc]Tc-DGA1 with [99mTc]Tc-DG2 (CCK2R-agonist reference) was conducted in HEK293-CCK2R/CCK2i4svR cells and mice models, qualifying [99mTc]Tc-DGA1 for further study in patients with CCK2R-pos. tumors and single-photon emission computed tomog./CT. In the experiment, the researchers used H-Lys(Boc)-OH(cas: 2418-95-3Reference of H-Lys(Boc)-OH)

H-Lys(Boc)-OH(cas: 2418-95-3) belongs to amino acids. In addition to subunits of proteins, amino acids have many other functions as well, including osmoregulation (proline), neurotransmitters (gamma-aminobutyric acid), metabolic intermediates (ornithine and citrulline), and inhibitors (dehydroproline).Reference of H-Lys(Boc)-OH

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