Category: amides-buliding-blocks

Ohishi, Mitsuru published the artcileSacubitril/valsartan-A new weapon for fighting the hypertension paradox, HPLC of Formula: 137862-53-4, the publication is Hypertension Research (2022), 45(5), 915-916, database is CAplus and MEDLINE.

The estimated prevalence of hypertension in Japan is 43 million. However, when good blood pressure (BP) control is defined as <140/90 mmHg, only 12 million patients have achieved the targeted BP. Thus, 27% of individuals with hypertension have achieved satisfactory BP control. The guidelines for the management of hypertension by the Japanese Society of Hypertension (JSH2019) recommended that the antihypertensive target should be <130/80 mmHg, except in older individuals (≥75 years); individuals with cerebrovascular disease, with bilateral carotid artery stenosis or occlusion of the main cerebral artery; or individuals with chronic kidney disease without proteinuria. In the excluded groups, excessive antihypertensive treatments may increase adverse drug effects. Studies have shown that 21.6% of all patients with hypertension have achieved a BP <130/80 mmHg, and the control rate is lower among younger individuals. Sacubitril/valsartan is a new type of antihypertensive drug combination that contains a 1:1 molar ratio of the angiotensin receptor blocker valsartan and the neprilysin inhibitor sacubitril. A recent phase III study assessed the efficacy and safety of sacubitril/valsartan vs. olmesartan in Japanese patients with mild-to-moderate essential hypertension. Strict BP control without giving up will make it possible to extend our healthy life expectancy by preventing stroke and cardiovascular diseases.

Hypertension Research 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

Anstaett, Philipp published the artcileSynthesis of Stable Peptide Nucleic Acid-Modified Gold Nanoparticles and their Assembly onto Gold Surfaces, Related Products of amides-buliding-blocks, the publication is Angewandte Chemie, International Edition (2013), 52(15), 4217-4220, database is CAplus and MEDLINE.

The authors demonstrated the preparation of stable PNA-modified particles through a novel approach involving the use of a thiolated alkyl PEG carboxylate surfactant. Standard, as well as novel, mono- and trithiol linkers were found to be compatible with this approach. The potential of these PNA-nanoparticles as new building blocks for self-assembling systems was confirmed by synthesizing particles that were able to self-assemble under additive-free conditions, an endeavor which has, to the best of the authors’ knowledge, not been directly shown with any other DNA/PNA-based systems.

Angewandte Chemie, International Edition 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, Related Products of amides-buliding-blocks.

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

Musalov, M. V. published the artcileOne-Pot Synthesis of Functionalized 1,1′-(9-Selenabicyclo[3.3.1]nonane-2,6-diyl)dipyridinium Dibromides, Quality Control of 1453-82-3, the publication is Russian Journal of Organic Chemistry (2021), 57(4), 668-670, database is CAplus.

Previously unknown functionally substituted 1,1′-(9-selenabicyclo[3.3.1]nonane-2,6-diyl)dipyridinium dibromides were synthesized in 90-98% yields by one-pot condensation of selenium dibromide, cycloocta-1,5-diene, and substituted pyridines.

Russian 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, Quality Control of 1453-82-3.

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

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

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

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

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

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

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