November 2022 - Page 60 of 223 - Amides-buliding-blocks

Chen, Jia-Shiong’s team published research in Scientific Reports in 12 | CAS: 169590-42-5

Scientific Reports published new progress about 169590-42-5. 169590-42-5 belongs to amides-buliding-blocks, auxiliary class Sulfamide,Immunology/Inflammation,COX, name is 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, and the molecular formula is C17H14F3N3O2S, Application of 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide.

Chen, Jia-Shiong published the artcileCC-01 (chidamide plus celecoxib) modifies the tumor immune microenvironment and reduces tumor progression combined with immune checkpoint inhibitor, Application of 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, the publication is Scientific Reports (2022), 12(1), 1100, database is CAplus and MEDLINE.

Immune checkpoint inhibitors (ICIs) have shown clin. benefit in solid tumors, with modest rates of clin. response. Hence, improved therapeutic approaches need to be investigated. Herein, we assessed a combination of chidamide plus celecoxib (called CC-01) combined with programmed cell death protein 1 (PD-1) blockade in a CT26 model as potent tumor microenvironment (TME) regulator. The antitumor activity was assessed by measuring tumor size, overall response rate, and survival rate. Immune profiling of tumor-infiltrating lymphocytes was performed by flow cytometry. Tumor tissues were assessed by chip assay to predict the possible pathway. Tumor size was significantly reduced in mice treated with CC-01 combined with or without anti-PD-1 antibody, however the triple combination therapy consistently demonstrated that it significantly increased both the ORR and survival rate in term of clin. applications. In the combination group, immune landscape profiling revealed decreased populations of immunosuppressive regulatory T cells, myeloid-derived suppressor cells, and tumor-associated macrophages. Anal. of the mouse tumor chip data using Gene Ontol. enrichment anal. of biol. processes revealed that the triple combination upregulated genes associated with responses to interferon-gamma. Our results demonstrated that CC-01 possessed potent TME regulatory properties, augmenting the antitumor effect when combined with ICIs. This antitumor effect was achieved by altering the immune landscape in TILs (tumor-infiltrating lymphocytes) and was associated with immune cell activation in the TME. Furthermore, CC-01 demonstrated potent anticancer immune response activity, mainly reducing the number and function of several immunosuppressive cells. The combination of CC-01 with an ICI will further enhance the anticancer effect and boost the immune response rate. Collectively, our results support the clin. evaluation of CC-01 in combination with ICIs in several advanced cancers.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Hussain, Muhammad Asif’s team published research in Journal of Industrial and Engineering Chemistry (Amsterdam, Netherlands) in 99 | CAS: 1453-82-3

Journal of Industrial and Engineering Chemistry (Amsterdam, Netherlands) published new progress about 1453-82-3. 1453-82-3 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is Isonicotinamide, and the molecular formula is C6H6N2O, HPLC of Formula: 1453-82-3.

Hussain, Muhammad Asif published the artcileAn efficient hydration of nitriles with ruthenium-supported heterogeneous catalyst in water under moderate conditions, HPLC of Formula: 1453-82-3, the publication is Journal of Industrial and Engineering Chemistry (Amsterdam, Netherlands) (2021), 187-195, database is CAplus.

A facile eco-friendly heterogeneous catalytic system has been developed for amide synthesis that further utilized in pharmaceutical and organic chem. The Ru/MnO₂ catalyst has shown outstanding and unprecedented activity for a wide range of aliphatic and benzylic nitriles in green solvent water at 60°C. The system has also exhibited a remarkable tolerance for selective hydration of heteroatom (e.g. nitrogen, oxygen and sulfur atoms) containing nitriles. Pharmaceutically important nicotinamides and pyrazinamide has been synthesized by hydration of the heteroat. nitriles with appreciable yields and selectivities. Moreover, the Ru/MnO₂ catalyst has employed water as a benign solvent, with more than 30,000 TONs and reusability five times after isolation from the reaction mixture by centrifugation and easy workup that established a path for green environmental and technol. acceptable protocol.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Drsata, J.’s team published research in Cesko-Slovenska Farmacie in 37 | CAS: 64559-06-4

Cesko-Slovenska Farmacie published new progress about 64559-06-4. 64559-06-4 belongs to amides-buliding-blocks, auxiliary class Amine,Benzene,Amide,Ether, name is 3-Methoxybenzothioamide, and the molecular formula is C8H9NOS, Formula: C8H9NOS.

Drsata, J. published the artcileBiological side-effects of potential antituberculotic agents. XIII. Use of serum aspartate aminotransferase for the examination of organ toxicity of thiobenzamides, Formula: C8H9NOS, the publication is Cesko-Slovenska Farmacie (1988), 37(6), 243-5, database is CAplus and MEDLINE.

Ten title compounds (I; R¹ = H, 4-Br, 3-Cl, 4-Cl, 3-Me, 4-Me, 3-MeO, 4-MeO, 4-NMe₂; R² = H, 4-Cl) were screened for hepatotoxicity as indicated by blood serum levels of aspartate aminotransferase (AST). An equation is derived relating the values of Hammett’s constants for I and log AST. The hepatotoxicity of I decreases with an increase in the value of Hammett’s constant

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Willis, Julian C. W.’s team published research in Nature Chemistry in 10 | CAS: 2418-95-3

Nature Chemistry published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C18H15N3O3, Formula: C11H22N2O4.

Willis, Julian C. W. published the artcileMutually orthogonal pyrrolysyl-tRNA synthetase/tRNA pairs, Formula: C11H22N2O4, the publication is Nature Chemistry (2018), 10(8), 831-837, database is CAplus and MEDLINE.

Genetically encoding distinct non-canonical amino acids (ncAAs) into proteins synthesized in cells requires mutually orthogonal aminoacyl-tRNA synthetase (aaRS)/tRNA pairs. The pyrrolysyl-tRNA synthetase/^PyltRNA pair from Methanosarcina mazei (Mm) has been engineered to incorporate diverse ncAAs and is commonly considered an ideal pair for genetic code expansion. However, finding new aaRS/tRNA pairs that share the advantages of the MmPylRS/Mm^PyltRNA pair and are orthogonal to both endogenous aaRS/tRNA pairs and the MmPylRS/Mm^PyltRNA pair has proved challenging. Here we demonstrate that several ΔNPylRS/^PyltRNA_CUA pairs, in which PylRS lacks an N-terminal domain, are active, orthogonal and efficiently incorporate ncAAs in Escherichia coli. We create new PylRS/^PyltRNA pairs that are mutually orthogonal to the MmPylRS/Mm^PyltRNA pair and show that transplanting mutations that reprogram the ncAA specificity of MmPylRS into the new PylRS reprograms its substrate specificity. Finally, we show that distinct PylRS/^PyltRNA-derived pairs can function in the same cell, decode distinct codons and incorporate distinct ncAAs.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Shcherbakov, Nikolay V.’s team published research in Journal of Organic Chemistry in 86 | CAS: 2451-91-4

Journal of Organic Chemistry published new progress about 2451-91-4. 2451-91-4 belongs to amides-buliding-blocks, auxiliary class Nitrile,Amine,Benzene, name is N,N-Dibenzylcyanamide, and the molecular formula is C14H18BNO2, Safety of N,N-Dibenzylcyanamide.

Shcherbakov, Nikolay V. published the artcileRedox-Neutral and Atom-Economic Route to β-Carbolines via Gold-Catalyzed [4 + 2] Cycloaddition of Indolylynamides and Cyanamides, Safety of N,N-Dibenzylcyanamide, the publication is Journal of Organic Chemistry (2021), 86(24), 17804-17815, database is CAplus and MEDLINE.

Gold(I)-catalyzed [4 + 2] cycloaddition of indolylynamides I (R = Ts, Boc; R¹ = R² = H BnO; R³ = tosyl, mesyl, brosyl, etc.; R⁴ = Me, cyclopropyl, benzyl, etc.; R³R⁴ = -C(O)O(CH₂)₂-) and cyanamides (aminonitriles) R⁵CN [R⁵ = diethylamino, methylphenylamino, pyrrolidino, etc.] is an efficient redox-neutral and atom-economic route to diversely substituted 1,3-diamino-α-carbolines II. The protocol operates under mild conditions (Ph₃PAuNTf₂ 5 mol%, DCE, 60°C) with a good tolerance to functional groups (23 examples and yields up to 98%). The obtained α-carboline systems represent a versatile synthetic platform with modifiable substituents for successive functionalizations. Control experiments indicate the crucial role of both the nature of reactants and the identity of employed catalysts in the developed cycloaddition

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Hintermann, Samuel’s team published research in Bioorganic & Medicinal Chemistry Letters in 17 | CAS: 100377-32-0

Bioorganic & Medicinal Chemistry Letters published new progress about 100377-32-0. 100377-32-0 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is N-Methoxy-N-methylisonicotinamide, and the molecular formula is C8H10N2O2, Application In Synthesis of 100377-32-0.

Hintermann, Samuel published the artcileIdentification of a series of highly potent activators of the Nurr1 signaling pathway, Application In Synthesis of 100377-32-0, the publication is Bioorganic & Medicinal Chemistry Letters (2007), 17(1), 193-196, database is CAplus and MEDLINE.

The nuclear receptor Nurr1 (NR4A2) is critically involved in the development and maintenance of midbrain dopaminergic neurons and is believed to function independently of endogenous activation. The hit identification and SAR studies leading to isoxazolo-pyridinone 7e (I), a highly potent, brain penetrable activator of the Nurr1 signaling pathway, are described.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Nechaev, Ilya V.’s team published research in Journal of Organic Chemistry in 86 | CAS: 1453-82-3

Journal of Organic Chemistry published new progress about 1453-82-3. 1453-82-3 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is Isonicotinamide, and the molecular formula is C6H6N2O, Related Products of amides-buliding-blocks.

Nechaev, Ilya V. published the artcileThree-Component Reaction of 3,3-Difluorocyclopropenes, s-Tetrazines, and (benzo) Pyridines, Related Products of amides-buliding-blocks, the publication is Journal of Organic Chemistry (2021), 86(1), 1037-1052, database is CAplus and MEDLINE.

A new three-component reaction leading to 1-α-(pyridyl-2-[1,2,4]triazolyl)-2-alkyl-ethanones has been discovered while studying the reactivity of monosubstituted 3,3-difluorocyclopropenes in an inverse electronic demand Diels-Alder (IEDDA) cycloaddition-cycloreversion sequence with s-tetrazines. The reaction involving the above-mentioned reactants and (benzo)pyridine as a third component results in a complex transformation proceeding in mild conditions in a stoichiometric ratio of reactants and has high functional group tolerance (phenols, amides, ethers, carboxylic acids, ketones, and acrylic esters). As a result, simple pyridines are selectively functionalized at the α-position in good isolated yields. The reaction mechanism includes a rare azaphilic [4 + 2]-cycloaddition step between s-tetrazine and intermediate 1-hydroxyindolizine, suggested after byproduct identification and tracked with a deuterium label. To date, it is only the third known example of skewed azaphilic cycloaddition of tetrazine. The reaction is truly three-component and cannot be effectively performed stepwise.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Coppi, Elisabetta’s team published research in Biochemical Pharmacology (Amsterdam, Netherlands) in 177 | CAS: 264622-53-9

Biochemical Pharmacology (Amsterdam, Netherlands) published new progress about 264622-53-9. 264622-53-9 belongs to amides-buliding-blocks, auxiliary class GPCR/G Protein,Adenosine Receptor, name is N-(4-Acetylphenyl)-2-(4-(2,6-dioxo-1,3-dipropyl-2,3,6,9-tetrahydro-1H-purin-8-yl)phenoxy)acetamide, and the molecular formula is C27H29N5O5, Related Products of amides-buliding-blocks.

Coppi, Elisabetta published the artcileAdenosine A_2B receptors inhibit K⁺ currents and cell differentiation in cultured oligodendrocyte precursor cells and modulate sphingosine-1-phosphate signaling pathway, Related Products of amides-buliding-blocks, the publication is Biochemical Pharmacology (Amsterdam, Netherlands) (2020), 113956, database is CAplus and MEDLINE.

Oligodendrocytes are the only myelinating cells in the brain and differentiate from their progenitors (OPCs) throughout adult life. However, this process fails in demyelinating pathologies. Adenosine is emerging as an important player in OPC differentiation and we recently demonstrated that adenosine A_2A receptors inhibit cell maturation by reducing voltage-dependent K⁺ currents. No data are available to date about the A_2B receptor (A_2BR) subtype. The bioactive lipid mediator sphingosine-1-phosphate (S1P) and its receptors (S1P_1-5) are also crucial modulators of OPC development. An interaction between this pathway and the A_2BR is reported in peripheral cells. We studied the role of A_2BRs in modulating K⁺ currents and cell differentiation in OPC cultures and we investigated a possible interplay with S1P signaling. Our data indicate that the A_2BR agonist BAY60-6583 and its new analog P453 inhibit K⁺ currents in cultured OPC and the effect was prevented by the A_2BR antagonist MRS1706, by K⁺ channel blockers and was differently modulated by the S1P analog FTY720-P. An acute (10 min) exposure of OPCs to BAY60-6583 also increased the phosphorylated form of sphingosine kinase 1 (SphK1). A chronic (7 days) treatment with the same agonist decreased OPC differentiation whereas SphK1/2 inhibition exerted the opposite effect. Furthermore, A_2BR was overexpressed during OPC differentiation, an effect prevented by the pan SphK1/2 inhibitor VPC69047. Finally, A_2BR silenced cells showed increased cell maturation, decreased SphK1 expression and enhanced S1P lyase levels. We conclude that A_2BRs inhibit K⁺ currents and cell differentiation and pos. modulate S1P synthesis in cultured OPCs.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Pappa, Kalliopi I. et al. published their research in Scientific Reports in 2021 | CAS: 1094-61-7

((2R,3S,4R,5R)-5-(3-Carbamoylpyridin-1-ium-1-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl hydrogen phosphate (cas: 1094-61-7) belongs to amides. Because of the greater electronegativity of oxygen, the carbonyl (C=O) is a stronger dipole than the N–C dipole. The presence of a C=O dipole and, to a lesser extent a N–C dipole, allows amides to act as H-bond acceptors. Amides are not in general accessible by the direct condensation of amines with carboxylic acids for two reasons: first, both components are readily deactivated by a transfer of a proton from the acid to the amine and second, the hydroxy unit on the carbonyl of the acid is a relatively poor leaving group. Nevertheless, the formation of five- and six-membered rings is often surprisingly simple provided that other factors can be brought into play to assist in the condensation.Category: amides-buliding-blocks

Metabolic rewiring is associated with HPV-specific profiles in cervical cancer cell lines was written by Pappa, Kalliopi I.;Daskalakis, George;Anagnou, Nicholas P.. And the article was included in Scientific Reports in 2021.Category: amides-buliding-blocks The following contents are mentioned in the article:

Both HPV-pos. and HPV-neg. cervical cancers are associated with aberrant metabolism, although the oncogenic drivers remain elusive. Here we show the assessment of the metabolomic profiles of four distinct cervical cell lines, a normal and three cancer cell lines, one HPV-neg. (C33A) and two HPV-pos. (SiHa HPV16+, HeLa HPV18+), employing an ultra performance liquid chromatog. and a high resolution mass spectrometry. Out of the total 462 metabolites, 248 to 326 exhibited statistically significant differences, while Random Forests anal. identified unique mols. for each cell line. The two HPV+ cell lines exhibited features of Warburg metabolism, consistent with the role of the HPV E6 protein. SiHa and HeLa cells displayed purine salvage pathway activity, while C33A cells revealed synthesis of cytidine, via a novel mechanism. These data document a highly dynamic HPV-specific rewiring of metabolic pathways occurring in cervical cancer. Therefore, this approach can eventually provide novel mechanistic insights into cervical carcinogenesis. This study involved multiple reactions and reactants, such as ((2R,3S,4R,5R)-5-(3-Carbamoylpyridin-1-ium-1-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl hydrogen phosphate (cas: 1094-61-7Category: amides-buliding-blocks).

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

Mattonai, Marco et al. published their research in Microchemical Journal in 2020 | CAS: 18836-52-7

(2E,4E)-N-Isobutyldeca-2,4-dienamide (cas: 18836-52-7) belongs to amides. In primary and secondary amides, the presence of N–H dipoles allows amides to function as H-bond donors as well. Thus amides can participate in hydrogen bonding with water and other protic solvents; the oxygen atom can accept hydrogen bonds from water and the N–H hydrogen atoms can donate H-bonds. Amides can be recrystallised from large quantities of water, ethanol, ethanol/ether, aqueous ethanol, chloroform/toluene, chloroform or acetic acid. The likely impurities are the parent acids or the alkyl esters from which they have been made. The former can be removed by thorough washing with aqueous ammonia followed by recrystallisation, whereas elimination of the latter is by trituration or recrystallisation from an organic solvent.Application In Synthesis of (2E,4E)-N-Isobutyldeca-2,4-dienamide

Characterization of volatile and non-volatile fractions of spices using evolved gas analysis and multi-shot analytical pyrolysis was written by Mattonai, Marco;Watanabe, Atsushi;Ribechini, Erika. And the article was included in Microchemical Journal in 2020.Application In Synthesis of (2E,4E)-N-Isobutyldeca-2,4-dienamide The following contents are mentioned in the article:

In the present work, evolved gas anal.-mass spectrometry (EGA-MS) and anal. pyrolysis coupled with gas chromatog./mass spectrometry (Py-GC/MS) were used to characterize both the volatile and non-volatile fractions of six com. available spices. Anal. of spices is usually performed through the study of their headspace composition by solid phase microextraction (SPME). In this new approach, EGA-MS was used to establish thermal degradation regions, and Py-GC/MS was used to obtain compositional information on each region sep. using double-shot pyrolysis. This study demonstrates that EGA-MS and Py-GC/MS provide the same advantages of solid-phase micro extraction and increase the range of detectable products by performing high-temperature desorption and degradation of the non-volatile fraction of spices. Our approach provided both qual. and semi-quant. data that could be used in the future to improve authentication studies by considering the results not only of headspace composition, but also on the pyrolytic behavior of the lignocellulosic matrix. This study involved multiple reactions and reactants, such as (2E,4E)-N-Isobutyldeca-2,4-dienamide (cas: 18836-52-7Application In Synthesis of (2E,4E)-N-Isobutyldeca-2,4-dienamide).

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