Month: November 2022

Alsharif, Zakeyah A. published the artcileModular synthesis of thiazoline and thiazole derivatives by using a cascade protocol, Computed Properties of 64559-06-4, the publication is RSC Advances (2017), 7(52), 32647-32651, database is CAplus and MEDLINE.

The first synthetic protocol by which both thiazolines I (R = Me, allylamino, pyridin-2-yl, (E)-2-[(4-chlorophenyl)methylidene]hydrazin-1-yl, etc.) and thiazoles II [R¹ = 4-chlorophenyl, 4-trifluoromethylphenyl, benzylamino, (4-carboxyphenyl)aminyl] can be prepared has been reported. Novel mols. I and II are efficiently synthesized by using readily available and inexpensive substrates. The reaction conditions are mild and pure products were obtained without work-up and column purification

RSC Advances 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, Computed Properties of 64559-06-4.

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

El-Battrawy, Ibrahim published the artcileImpact of sacubitril/valsartan on cardiac arrest event rate. Letter regarding the article ‘Prospective ARNI vs. ACE inhibitor trial to DetermIne Superiority in reducing heart failure Events after Myocardial Infarction (PARADISE-MI): design and baseline characteristics’, Product Details of C24H29N5O3, the publication is European Journal of Heart Failure (2022), 24(7), 1324, database is CAplus and MEDLINE.

A polemic in response to Jering et al is given. The article by Jering et al.1 published in this Journal presented an interesting study concept. The study group aimed to study the impact of sacubitril/valsartan treatment in comparison with ramipril on cardiovascular outcome in patients with acute myocardial infarction. Patients are included if left ventricular ejection fraction ≤40% and/or in case of pulmonary congestion.

European Journal of Heart Failure published new progress about 137862-53-4. 137862-53-4 belongs to amides-buliding-blocks, auxiliary class GPCR/G Protein,Angiotensin Receptor, name is (S)-2-(N-((2′-(1H-Tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid, and the molecular formula is C24H29N5O3, Product Details of C24H29N5O3.

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

Hibino, Masaki published the artcileCationic guanine: positively charged nucleobase with improved DNA affinity inhibits self-duplex formation, Synthetic Route of 186046-83-3, the publication is Chemical Communications (Cambridge, United Kingdom) (2020), 56(17), 2546-2549, database is CAplus and MEDLINE.

Oligonucleotides represent powerful DNA-recognition tools, but the formation of undesirable “self-duplexes” becomes more probable with increasing DNA affinity. Herein, we have developed a modified nucleobase with “self-avoiding” properties. Facile methylation of guanine yields a cationic N⁷-methylguanine, which suppresses the formation of self-duplexes while improving DNA affinity through electrostatic interaction.

Chemical Communications (Cambridge, United Kingdom) published new progress about 186046-83-3. 186046-83-3 belongs to amides-buliding-blocks, auxiliary class Purine,Carboxylic acid,Amine,Benzene,Amide,Others,PNA,, name is 2-(N-(2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)ethyl)-2-(2-(((benzhydryloxy)carbonyl)amino)-6-oxo-5H-purin-9(6H)-yl)acetamido)acetic acid, and the molecular formula is C40H35N7O8, Synthetic Route of 186046-83-3.

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

Malnes, Daniel published the artcileOccurrence and mass flows of contaminants of emerging concern (CECs) in Sweden’s three largest lakes and associated rivers, HPLC of Formula: 137862-53-4, the publication is Chemosphere (2022), 133825, database is CAplus and MEDLINE.

Contaminants of emerging concern (CECs) are a concern in aquatic environments due to possible adverse effects on the environment and humans. This study assessed the occurrence and mass flows of CECs in Sweden’s three largest lakes and 24 associated rivers. The occurrence and distribution of 105 CECs was investigated, comprising 71 pharmaceuticals, 13 perfluoroalkyl substances (PFASs), eight industrial chems., four personal care products (PCPs), three parabens, two pesticides, and four other CECs (mostly anthropogenic markers). This is the first systematic study of CECs in Sweden’s main lakes and one of the first to report environmental concentrations of the industrial chems. tri-Bu citrate acetate and 2,2′-dimorpholinyldiethyl-ether. The ∑CEC concentration was generally higher in river water (31-5200 ng/L; median 440 ng/L) than in lake water (36-900 ng/L; median 190 ng/L). At urban lake sites, seasonal variations were observed for PCPs and parabens, and also for antihistamines, antidiabetics, antineoplastic agents, antibiotics, and fungicides. The median mass CEC load in river water was 180 g/day (range 4.0-4300 g/day), with a total mass load of 5000 g/day to Lake Vanern, 510 g/day to Lake Vattern, and 5600 g/day to Lake Malaren. All three lakes are used as drinking water reservoirs, so further investigations of the impact of CECs on the ecosystem and human health are needed.

Chemosphere published new progress about 137862-53-4. 137862-53-4 belongs to amides-buliding-blocks, auxiliary class GPCR/G Protein,Angiotensin Receptor, name is (S)-2-(N-((2′-(1H-Tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid, and the molecular formula is C24H29N5O3, HPLC of Formula: 137862-53-4.

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

Nihal, Minakshi published the artcileSIRT1 is upregulated in cutaneous T-cell lymphoma, and its inhibition induces growth arrest and apoptosis, Application In Synthesis of 380315-80-0, the publication is Cell Cycle (2014), 13(4), 632-640, database is CAplus and MEDLINE.

Silent information regulator type-1 (SIRT1) is the best-studied member of the Sirtuin (Sir2) family of nicotinamide dinucleotide (NAD)-dependent class III histone deacetylases (HDACs), but has not yet been explored in cutaneous T-cell lymphoma (CTCL). We analyzed five CTCL cell lines and lesional tissues using flow cytometry, immunostaining, immunoblotting, cell death, viability, and apoptosis assays, small-mol. inhibitors, and shRNA knockdown. We found strong SIRT1 expression among CTCL lines relative to normal lymphocytes. CTCL cells in lesional tissues also expressed SIRT1 strongly. SIRT1 knockdown resulted in reduced cellular metabolism and proliferation, increased apoptosis, and PARP cleavage products. Tenovin-1, which reversibly inhibits class III HDACs (SIRT1 and SIRT2), reduced SIRT enzymic activity and SIRT1 expression and led to increased apoptosis. These alterations were accompanied by increased forkhead box O3 (FoxO3) in several cell lines and increased nuclear p53, as well as acetylated p53 in wtp53 MyLa CTCL line. A combination of class I/II and class III HDACIs (vorinostat and tenovin-1) produced significantly greater growth inhibition, cell death via apoptosis, as well as superior p53 promoter upregulation in wtp53 MyLa cells as compared with either agent alone. This occurred in a partially p53-dependent manner, as these effects were blunted by p53 knockdown. Our results indicate that SIRT1 is strongly expressed in CTCL. Its inhibition results in reduced growth and increased apoptosis of CTCL cells. Furthermore, our findings suggest that some CTCL patients, such as those with wtp53, might benefit more from treatment with a combination of different classes of HDACIs than with a single agent.

Cell Cycle published new progress about 380315-80-0. 380315-80-0 belongs to amides-buliding-blocks, auxiliary class Apoptosis,p53, name is N-((4-Acetamidophenyl)carbamothioyl)-4-(tert-butyl)benzamide, and the molecular formula is C20H23N3O2S, Application In Synthesis of 380315-80-0.

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

Chen, Long published the artcileCombining p53 stabilizers with metformin induces synergistic apoptosis through regulation of energy metabolism in castration-resistant prostate cancer, Computed Properties of 380315-80-0, the publication is Cell Cycle (2016), 15(6), 840-849, database is CAplus and MEDLINE.

Since altered energy metabolism is a hallmark of cancer, many drugs targeting metabolic pathways are in active clin. trials. The tumor suppressor p53 is often inactivated in cancer, either through downregulation of protein or loss-of-function mutations. As such, stabilization of p53 is considered as one promising approach to treat those cancers carrying wild type (WT) p53. Herein, SIRT1 inhibitor Tenovin-1 and polo-like kinase 1 (Plk1) inhibitor BI2536 were used to stabilize p53. We found that both Tennovin-1 and BI2536 increased the anti-neoplastic activity of metformin, an inhibitor of oxidative phosphorylation, in a p53 dependent manner. Since p53 has also been shown to regulate metabolic pathways, we further analyzed glycolysis and oxidative phosphorylation upon drug treatments. We showed that both Tennovin-1 and BI2536 rescued metformin-induced glycolysis and that both Tennovin-1 and BI2536 potentiated metformin-associated inhibition of oxidative phosphorylation. Of significance, castration-resistant prostate cancer (CRPC) C4-2 cells show a much more robust response to the combination treatment than the parental androgen-dependent prostate cancer LNCaP cells, indicating that targeting energy metabolism with metformin plus p53 stabilizers might be a valid approach to treat CRPC carrying WT p53.

Cell Cycle published new progress about 380315-80-0. 380315-80-0 belongs to amides-buliding-blocks, auxiliary class Apoptosis,p53, name is N-((4-Acetamidophenyl)carbamothioyl)-4-(tert-butyl)benzamide, and the molecular formula is C20H23N3O2S, Computed Properties of 380315-80-0.

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

Brun, Omar published the artcileSelective derivatization of N-terminal cysteines using cyclopentenediones, HPLC of Formula: 186046-83-3, the publication is Organic Letters (2016), 18(19), 4836-4839, database is CAplus and MEDLINE.

The outcome of the Michael-type reaction between thiols and 2,2-disubstituted cyclopentenediones (CPDs) varies depending on the thiol. Stable compounds with two fused rings were formed upon reaction with 1,2-aminothiols (such as N-terminal cysteines in peptides). Other thiols gave reversibly Michael-type adducts that were in equilibrium with the starting materials. This differential reactivity allows differently placed cysteines to be distinguished and has been exploited to prepare bioconjugates incorporating two or three different moieties.

Organic Letters published new progress about 186046-83-3. 186046-83-3 belongs to amides-buliding-blocks, auxiliary class Purine,Carboxylic acid,Amine,Benzene,Amide,Others,PNA,, name is 2-(N-(2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)ethyl)-2-(2-(((benzhydryloxy)carbonyl)amino)-6-oxo-5H-purin-9(6H)-yl)acetamido)acetic acid, and the molecular formula is C40H35N7O8, HPLC of Formula: 186046-83-3.

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

Seuring, Jan published the artcileFirst Example of a Universal and Cost-Effective Approach: Polymers with Tunable Upper Critical Solution Temperature in Water and Electrolyte Solution, Category: amides-buliding-blocks, the publication is Macromolecules (Washington, DC, United States) (2012), 45(9), 3910-3918, database is CAplus.

We present a powerful universal and versatile approach for the synthesis of polymers that show a UCST in water. Up to now only a few polymers were known that show an upper critical solution temperature (UCST) in water. This study establishes general requirements to obtain polymers with a UCST in water as well as electrolyte solution It is demonstrated that old homo- and copolymer systems like poly(methacrylamide) and poly(acrylamide-co-acrylonitrile) can exhibit a UCST in water and how polymers with a tunable UCST can be synthesized by copolymerization of acrylamide and acrylonitrile, monomers that are industrially produced on large scales. Controlled increase of the UCST by copolymerization of acrylamide with varying amounts of acrylonitrile was shown, and it could be varied between 6 and 60 °C. The hysteresis between the cloud point upon cooling and heating was very small with only 1-2 °C in most cases. The cloud points in pure water were similar to the cloud points measured in phosphate buffered saline. Also, it is possible to prepare highly concentrated thermo-responsive polymer solutions without gel formation.

Macromolecules (Washington, DC, United States) published new progress about 2479-62-1. 2479-62-1 belongs to amides-buliding-blocks, auxiliary class Monomers,Acrylamide Monomers, name is N-(2-Amino-2-oxoethyl)acrylamide, and the molecular formula is C17H18N2O6, Category: amides-buliding-blocks.

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

Liu, Fangyao published the artcileThermoresponsive Gold Nanoparticles with Positive UCST-Type Thermoresponsivity, Synthetic Route of 2479-62-1, the publication is Macromolecular Chemistry and Physics (2015), 216(4), 460-465, database is CAplus.

Trithiocarbonate end-functionalized poly(N-acryloylglycinamide) (PNAGA), synthesized via reversible addition-fragmentation transfer (RAFT) polymerization of different mol. weights, is grafted onto gold nanoparticles (AuNPs) by ligand exchange in phosphate-buffered saline. The PNAGA-grafted AuNPs display upper critical solution temperature (UCST)-type transitions: stable colloidal distribution and aggregation above and below the cloud points, resp. Cloud points of PNAGA are not affected by the grafting procedure, and PNAGA@AuNPs show similar cloud points as that of the trithiocarbonate end-functionalized free-PNAGAs used for grafting. The UCST-type phase transition is reversible for many cycles. The reversible control of the phase transition is proved by turbidity measurements and UV-vis spectroscopy, as well as by transmission electron microscopy (TEM).

Macromolecular Chemistry and Physics published new progress about 2479-62-1. 2479-62-1 belongs to amides-buliding-blocks, auxiliary class Monomers,Acrylamide Monomers, name is N-(2-Amino-2-oxoethyl)acrylamide, and the molecular formula is C5H8N2O2, Synthetic Route of 2479-62-1.

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

Losasso, Valeria published the artcileSmall molecules enhance the potency of natural antimicrobial peptides, Formula: C6H6N2O, the publication is Biophysical Journal (2022), 121(3), 491-501, database is CAplus and MEDLINE.

The skin-associated microbiome plays an important role in general well-being and in a variety of treatable skin conditions. In this regard, endogenous antimicrobial peptides have both a direct and indirect role in determining the composition of the microbiota. We demonstrate here that certain small mol. species can amplify the antimicrobial potency of naturally occurring antimicrobial peptides. In this study, we have used niacinamide, a form of vitamin B3 naturally found in foods and widely used in cosmetic skincare products, and two of its structural analogs, to investigate their cooperativity with the human antimicrobial peptide LL37 on the bacterium Staphylococcus aureus. We observed a clear synergistic effect of niacinamide and, to some extent, N-methylnicotinamide, whereas isonicotinamide showed no significant cooperativity with LL37. Adaptively biased mol. dynamics simulations using simplified model membrane substrates and single peptides revealed that these mols. partition into the headgroup region of an anionic bilayer used to mimic the bacterial membrane. The simulated effects on the phys. properties of the simulated model membrane are well correlated with exptl. activity observed in real biol. assays despite the simplicity of the model. In contrast, these mols. have little effect on zwitterionic bilayers that mimic a mammalian membrane. We conclude that niacinamide and N-methylnicotinamide can therefore potentiate the activity of host peptides by modulating the phys. properties of the bacterial membrane, and to a lesser extent through direct interactions with the peptide. The level of cooperativity is strongly dependent on the detailed chem. of the additive, suggesting an opportunity to fine-tune the behavior of host peptides.

Biophysical Journal 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, Formula: C6H6N2O.

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