Month: December 2022

Zhou, Min published the artcileSynthesis of poly-α/β-peptides with tunable sequence via the copolymerization on N-carboxyanhydride and N-thiocarboxyanhydride, Computed Properties of 2418-95-3, the publication is iScience (2021), 24(10), 103124, database is CAplus and MEDLINE.

The fascinating functions of proteins and peptides in biol. systems have attracted intense interest to explore their mimics using polymers, including polypeptides synthesized from polymerization The folding, structures and functions of proteins and polypeptides are largely dependent on their sequence. However, sequence-tunable polymerization for polypeptide synthesis is a long-lasting challenge. The application of polypeptides is also greatly hindered by their susceptibility to enzymic degradation Although poly-α/β-peptide has proven to be an effective strategy to address the stability issue, the synthesis of poly-α/β-peptide from polymerization is not available yet. Hereby, we demonstrate a living and controlled copolymerization on α-NCA and β-NTA to prepare sequence-tunable poly-α/β-peptides. This polymerization strategy shows a prominent solvent-driven characteristic, providing random-like copolymers of poly-α/β-peptides in THF and block-like copolymers of poly-α/β-peptides in a mixed solvent of CHCl₃/H₂O (95/5, volume/volume), and opens new avenues for sequence-tunable polymerization and enables facile synthesis of proteolysis tunable poly-α/β-peptides for diverse applications.

iScience 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 C14H26O2, Computed Properties of 2418-95-3.

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

Gilstrap, Lauren published the artcileSacubitril/valsartan vs ACEi/ARB at hospital discharge and 5-year survival in older patients with heart failure with reduced ejection fraction: A decision analysis approach, Product Details of C24H29N5O3, the publication is American Heart Journal (2022), 23-28, database is CAplus and MEDLINE.

In clin. trials, sacubitril/valsartan has demonstrated significant survival benefits compared to angiotensin converting enzyme inhibitors or angiotensin receptor blockers (ACEi/ARB). Whether older patients with heart failure with reduced ejection fraction (HFrEF) benefit as much, due to higher rates of comorbidities, frailty and drug discontinuation, is unknown. Using a cohort of Medicare beneficiaries hospitalized with HFrEF between 2016 and 2018, we determined all-cause mortality and HF-readmission rates among patients not given ACEi/ARB or sacubitril/valsartan at hospital discharge, by age. We then used risk reductions from the SOLVD, PARADIGM-HF and PIONEER-HF trials to estimate the benefits of ACEi/ARB and sacubitril/valsartan. We then incorporated age-specific estimates of drug discontinuation from Medicare. A Markov decision process model was used to simulate 5-yr survival and estimate number needed to treat, comparing discharge on ACEi/ARB vs sacubitril/valsartan by age. After accounting for drug discontinuation rates, which were surprisingly slightly higher among those discharged on ACEi/ARB (2.3%/mo vs 1.9%/mo), there was a small but significant survival advantage to discharge on sacubitril/valsartan over 5 years (+0.81 mo [95% CI 0.80, 0.81]). The benefit of sacubitril/valsartan over ACEi/ARB did not decrease with increasing age – the number needed to treat among 66 to 74-yr-old patients was 84 and among 85+ year-old patients was 67. Even after accounting for “real world” rates of drug discontinuation, discharge on sacubitril/valsartan after conferred a small, but significant, survival advantage which does not appear to wane with increasing age.

American Heart Journal 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

Zhang, Jinqi published the artcileStudy on the aluminum amides conversion of esters to amides, Safety of N,N-Diethylisonicotinamide, the publication is Nanjing Daxue Xuebao, Ziran Kexue (1996), 32(2), 242-245, database is CAplus.

A convenient method was used for directly converting esters to amides by using the reagents derived from the reaction of trimethylaluminum with ammonium chloride, primary amines hydrochloride or secondary amines hydrochloride at high yield in relatively short reaction time and at low temperature Reactions of aluminum amides with aromatic esters were extensively studied and the influence of different substituting groups on the reaction was discussed. It was concluded that, if an electron-donating group was attached to the nitrogen atom instead of hydrogen, the reactivity of the aluminum amide would be increased, and, if an electron-withdrawing group was attached to benzene ring, the electron-deficiency of carboyl carbon would be increased, the yield of amides would be also increased.

Nanjing Daxue Xuebao, Ziran Kexue published new progress about 530-40-5. 530-40-5 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is N,N-Diethylisonicotinamide, and the molecular formula is C10H11NO4, Safety of N,N-Diethylisonicotinamide.

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

Chen, Jian published the artcileNickel-Catalyzed Multicomponent Coupling: Synthesis of α-Chiral Ketones by Reductive Hydrocarbonylation of Alkenes, COA of Formula: C11H22N2O4, the publication is Journal of the American Chemical Society (2021), 143(35), 14089-14096, database is CAplus and MEDLINE.

A nickel-catalyzed, multicomponent regio- and enantioselective coupling via sequential hydroformylation and carbonylation from readily available starting materials has been developed. This modular multicomponent hydrofunctionalization strategy enables the straightforward reductive hydrocarbonylation of a broad range of unactivated alkenes to produce a wide variety of unsym. dialkyl ketones bearing a functionalized α-stereocenter, including enantioenriched chiral α-aryl ketones and α-amino ketones. It uses chiral bisoxazoline as a ligand, silane as a reductant, chloroformate as a safe CO source, and a racemic secondary benzyl chloride or an N-hydroxyphthalimide (NHP) ester of a protected α-amino acid as the alkylation reagent. The benign nature of this process renders this method suitable for late-stage functionalization of complex mols.

Journal of the American Chemical Society 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 C11H22N2O4, COA of Formula: C11H22N2O4.

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

Peng, Guibin published the artcileA two-step strategy for the preparation of anion-exchange membranes based on poly(vinylidenefluoride-co-hexafluoropropylene) for electrodialysis desalination, Related Products of amides-buliding-blocks, the publication is Polymer (2021), 123508, database is CAplus.

The development of a facile approach to fabricate anion exchange membranes (AEMs) with efficient ionic transport and desirable stabilities (mech. and dimensional) for various applications is meaningful. In this work, a two-step strategy for the preparation of AEMs with 3D network structure, via crosslinking reaction between 2-chloroacetamide (CAA) modified poly (vinylidene fluoride-co-hexafluoropropylene) (PVDF-HFP) and N,N,N’,N’-tetramethyl-1,4-diaminobutane (TMDAB) has been reported. The as-prepared AEMs with ion-exchange capacity (IEC) in the range of 1.38-1.84 mmol g^-1, exhibit the much lower water uptake (13.14-22.45%, 80°C) relative to the un-crosslinked AEM (35.89%, 80°C). In addition, due to the presence of fluorine-based 3D network structure, the as-prepared AEMs show much enhanced mech. and thermal stability in comparison with the un-crosslinked AEM. In the electrodialysis (ED) application, the optimized AEM shows the higher current efficiency (78.6%) and lower energy consumption (2.01 kWh kg^-1 NaCl) than those of com. AEM AEM-Type II (76.4%; 2.26 kWh kg^-1), resp., within 150 min of operation interval. The proposed facile fabrication protocol and the better-performance of optimized PVDF-HFP -based AEM demonstrate the potential ED application.

Polymer published new progress about 79-07-2. 79-07-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Aliphatic hydrocarbon chain,Amide,Inhibitor, name is 2-Chloroacetamide, and the molecular formula is C2H4ClNO, Related Products of amides-buliding-blocks.

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

Mu, Ruixu published the artcileDiscovery of novel triazole compounds as selective IL-1β releasement inhibitors, HPLC of Formula: 15029-36-4, the publication is Bioorganic & Medicinal Chemistry Letters (2021), 128415, database is CAplus and MEDLINE.

Inflammation and immunity are closely related to the occurrence and development of a variety of immune diseases. Although IL-1β has been identified as a key cytokine in many immune diseases, safe and specific small mol. IL-1β releasement inhibitors are still scarce and urgently required in clinic. The investigation prospect of triazoleis limited by its complicated pharmacol. effect which exhibited inferior effects on IL-1β and TNF-α. Herein, 36 novel derivatives were designed and synthesized, and nearly half of the derivatives exhibited much better selectivity on IL-1β releasement inhibition as well as keep similar inhibitory activities to lead compound In 20 μM, compound 19 exhibited IL-1β releasement inhibitory activity (IC50 = 5.489 μM) which closed to the original compound, and 4.5-fold superior selectivity (SI = 4.71) to the lead compound (SI = 0.82). A probable SAR model of triazole derivatives for IL-1β releasement inhibition and selectivity was also proposed, which might promote the discovery of more effective and specific IL-1β releasement inhibitors in the future.

Bioorganic & Medicinal Chemistry Letters published new progress about 15029-36-4. 15029-36-4 belongs to amides-buliding-blocks, auxiliary class Nitrile,Amine,Aliphatic hydrocarbon chain,Amide, name is 2-Cyano-N-ethylacetamide, and the molecular formula is C5H8N2O, HPLC of Formula: 15029-36-4.

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

Wu, Huaiguo published the artcilemiR-34a in extracellular vesicles from bone marrow mesenchymal stem cells reduces rheumatoid arthritis inflammation via the cyclin I/ATM/ATR/p53 axis, Name: 4-(tert-Butyl)-N-((4-(5-(dimethylamino)pentanamido)phenyl)carbamothioyl)benzamide, the publication is Journal of Cellular and Molecular Medicine (2021), 25(4), 1896-1910, database is CAplus and MEDLINE.

Extracellular vesicles (Evs) participate in the development of rheumatoid arthritis (RA), but the mechanisms remain unclear. This study aimed to determine the mechanism by which microRNA-34a (miR-34a) contained in bone marrow mesenchymal stem cell (BM-MSC)-derived Evs functions in RA fibroblast-like synoviocytes (RA-FLSs). BM-MSC-derived Evs and an Evs inhibitor were extracted A rat model of RA was established. miR-34a gain- and loss-of-function experiments were performed, and the inflammation in rat synovial fluid and tissues was detected. The role of miR-34a in RA-FLSs was also measured in vitro. The target gene of miR-34a was predicted using the online software TargetScan and identified using a dual-luciferase reporter gene assay, and the activation of the ATM/ATR/p53 signalling pathway was assessed. BM-MSC-derived Evs mainly elevated miR-34a expression, which reduced RA inflammation in vivo and inhibited RA-FLS proliferation and resistance to apoptosis in vitro, while inhibited miR-34a expression enhanced RA development. In addition, miR-34a could target cyclin I to activate the ATM/ATR/p53 signalling pathway, thus inhibiting abnormal RA-FLS growth and RA inflammation. Our study showed that miR-34a contained in BM-MSC-derived Evs could reduce RA inflammation by inhibiting the cyclin I/ATM/ATR/p53 signalling pathway.

Journal of Cellular and Molecular Medicine published new progress about 1011557-82-6. 1011557-82-6 belongs to amides-buliding-blocks, auxiliary class Epigenetics,Sirtuin, name is 4-(tert-Butyl)-N-((4-(5-(dimethylamino)pentanamido)phenyl)carbamothioyl)benzamide, and the molecular formula is C19H24BNO2, Name: 4-(tert-Butyl)-N-((4-(5-(dimethylamino)pentanamido)phenyl)carbamothioyl)benzamide.

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

Deng, Hongfeng published the artcileDiscovery and Optimization of Potent, Selective, and in Vivo Efficacious 2-Aryl Benzimidazole BCATm Inhibitors, Recommanded Product: 4-Fluoro-N-methyl-3-nitrobenzamide, the publication is ACS Medicinal Chemistry Letters (2016), 7(4), 379-384, database is CAplus and MEDLINE.

To identify BCATm inhibitors suitable for in vivo study, Encoded Library Technol. (ELT) was used to affinity screen a 117 million member benzimidazole based DNA encoded library, which identified an inhibitor series with both biochem. and cellular activities. Subsequent SAR studies led to the discovery of a highly potent and selective compound I with much improved PK properties. X-ray structure revealed that I binds to the active site of BACTm in a unique mode via multiple H-bond and van der Waals interactions. After oral administration, I raised mouse blood levels of all three branched chain amino acids as a consequence of BCATm inhibition.

ACS Medicinal Chemistry Letters published new progress about 475216-25-2. 475216-25-2 belongs to amides-buliding-blocks, auxiliary class Fluoride,Nitro Compound,Amine,Benzene,Amide,Benzene Compounds, name is 4-Fluoro-N-methyl-3-nitrobenzamide, and the molecular formula is C8H7FN2O3, Recommanded Product: 4-Fluoro-N-methyl-3-nitrobenzamide.

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

Dai, Wei published the artcileClass III-specific HDAC inhibitor Tenovin-6 induces apoptosis, suppresses migration and eliminates cancer stem cells in uveal melanoma, Application In Synthesis of 1011557-82-6, the publication is Scientific Reports (2016), 22622, database is CAplus and MEDLINE.

Uveal melanoma (UM) is the most common intraocular malignancy in adults. Despite improvements in surgical, radiation and chemotherapy treatments, the overall survival of UM and prognosis remain poor. In the present study, we hypothesized that Sirtuin 1 and 2 (SIRT1/2), class III histone deacetylases (HDACs), were critical in controlling the destiny of bulk tumor cells and cancer stem cells (CSCs) of UM. We testified this hypothesis in four lines of UM cells (92.1, Mel 270, Omm 1 and Omm 2.3). Our results showed that inhibition of SIRT1/2 by Tenovin-6 induced apoptosis in UM cells by activating the expression of tumor suppressor genes such as p53 and elevating reactive oxygen species (ROS). Tenovin-6 inhibited the growth of UM cells. Tenovin-6 and vinblastine was synergistic in inducing apoptosis of UM cell line 92.1 and Mel 270. Furthermore, Tenovin-6 eliminated cancer stem cells in 92.1 and Mel 270 cells. In conclusion, our findings suggest that Tenovin-6 may be a promising agent to kill UM bulk tumor cells and CSCs.

Scientific Reports published new progress about 1011557-82-6. 1011557-82-6 belongs to amides-buliding-blocks, auxiliary class Epigenetics,Sirtuin, name is 4-(tert-Butyl)-N-((4-(5-(dimethylamino)pentanamido)phenyl)carbamothioyl)benzamide, and the molecular formula is C25H34N4O2S, Application In Synthesis of 1011557-82-6.

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

Zhao, Lulu published the artcileElectrochemical Synthesis of β-Functionalized Ketones via Ring-Opening of Cycloalkanols, SDS of cas: 169590-42-5, the publication is Organic Letters (2022), 24(24), 4421-4426, database is CAplus and MEDLINE.

The electrochem. deconstructive functionalization of cycloalkanols with nucleophiles was studied, which allowed functionalization to occur exclusively at the β-position of ketones. The substrate scope includes a wide range of cycloalkanols as well as diverse N, O, C and P-centered nucleophiles, providing ready access to β-functionalized ketones as products. Mechanistic studies support the generation of α,β-unsaturated ketones as key intermediates followed by Michael addition with nucleophiles.

Organic Letters 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 C13H10F2, SDS of cas: 169590-42-5.

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