Category: amides-buliding-blocks

Nakanishi, Yoshimitsu published the artcileStepwise phosphorylation of leukotriene B₄ receptor 1 defines cellular responses to leukotriene B₄, Formula: C12H23N3S, the publication is Science Signaling (2018), 11(544), eaao5390/1-eaao5390/15, database is CAplus and MEDLINE.

Leukotriene B₄ (LTB₄) receptor type 1 (BLT1) is abundant in phagocytic and immune cells and plays crucial roles in various inflammatory diseases. BLT1 is phosphorylated at several serine and threonine residues upon stimulation with the inflammatory lipid LTB₄. Using Phos-tag gel electrophoresis to sep. differentially phosphorylated forms of BLT1, we identified two distinct types of phosphorylation, basal and ligand-induced, in the carboxyl terminus of human BLT1. In the absence of LTB₄, the basal phosphorylation sites were modified to various degrees, giving rise to many different phosphorylated forms of BLT1. Different concentrations of LTB₄ induced distinct phosphorylation events, and these ligand-induced modifications facilitated addnl. phosphorylation events at the basal phosphorylation sites. Because neutrophils migrate toward inflammatory sites along a gradient of LTB₄, the degree of BLT1 phosphorylation likely increases in parallel with the increase in LTB₄ concentration as the cells migrate. At high concentrations of LTB₄, deficiencies in these two types of phosphorylation events impaired chemotaxis and β-hexosaminidase release, a proxy for degranulation, in Chinese hamster ovary (CHO-K1) and rat basophilic leukemia (RBL-2H3) cells, resp. These results suggest that an LTB₄ gradient around inflammatory sites enhances BLT1 phosphorylation in a stepwise manner to facilitate the precise migration of phagocytic and immune cells and the initiation of local responses, including degranulation.

Science Signaling published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C12H23N3S, Formula: C12H23N3S.

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

Greene, Stephen J. published the artcileFactors associated with non-use and sub-target dosing of medical therapy for heart failure with reduced ejection fraction, Product Details of C24H29N5O3, the publication is Heart Failure Reviews (2022), 27(3), 741-753, database is CAplus and MEDLINE.

A review. In clin. practice, many patients with heart failure with reduced ejection fraction (HFrEF) are either not prescribed guideline-directed medical therapies for which they are eligible or are prescribed therapies at sub-target doses. The objective of this study was to examine the factors associated with not receiving guideline-directed medical therapies or receiving sub-target doses. We conducted a systematic review of articles published between Jan. 2014 and May 2019 that described dosing patterns and factors associated with non-use and sub-target dosing of HFrEF therapies in clin. practice. Thirty-seven studies were included. The percentages of patients reaching target doses for angiotensin-converting enzyme inhibitors/angiotensin receptor blockers, sacubitril/valsartan, beta-blockers, and mineralocorticoid receptor antagonists ranged from 4 to 55%, 11 to 87%, 4 to 60%, and 22 to 80%, resp. Older age and worsening renal function were associated with non-use and sub-target dosing, lower body mass index was commonly associated with non-use, and hyperkalemia and hypotension were commonly associated with sub-target dosing. In conclusion, several common patient characteristics are associated with non-use and sub-target dosing of medical therapy for HFrEF. These high-risk groups are in particular need of further studies to improve implementation of available medications and to define the role of novel therapies.

Heart Failure Reviews 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

Liu, Wenbo published the artcileCu₂O-Catalyzed Conversion of Benzyl Alcohols Into Aromatic Nitriles via the Complete Cleavage of the C≡N Triple Bond in the Cyanide Anion, Product Details of C6H6N2O, the publication is Chemistry – An Asian Journal (2021), 16(21), 3509-3513, database is CAplus and MEDLINE.

Nitrogen transfer from cyanide anion to an aldehyde is emerging as a promising method for the synthesis of aromatic nitriles. However, this method still suffers from a disadvantage that a use of stoichiometric Cu(II) or Cu(I) salts is required to enable the reaction. As authors report herein, overcame this drawback and developed a catalytic method for nitrogen transfer from cyanide anion to an alc. via the complete cleavage of the C≡N triple bond using phen/Cu₂O as the catalyst. The present condition allowed a series of benzyl alcs. to be smoothly converted into aromatic nitriles in moderate to high yields. In addition, the present method could be extended to the conversion of cinnamic alc. to 3-phenylacrylonitrile.

Chemistry – An Asian 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, Product Details of C6H6N2O.

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

Barman, Hasan Ali published the artcileImpact of Sacubitril/Valsartan on Lipid Parameters in Patients with Heart Failure with Reduced Ejection Fraction, Product Details of C24H29N5O3, the publication is Clinical Drug Investigation (2022), 42(6), 533-540, database is CAplus and MEDLINE.

Abstract: Background and Objective: Sacubitril/valsartan, an angiotensin receptor-neprilysin inhibitor, has been shown to significantly reduce cardiovascular mortality, heart failure hospitalizations, and all-cause mortality in patients with heart failure with reduced ejection fraction. This study aims to investigate the long-term impact of the sacubitril/valsartan combination on lipid parameters in patients with heart failure with reduced ejection fraction. Methods: For this single-center retrospective cross-sectional study, data of patients using sacubitril/valsartan because of heart failure with reduced ejection fraction were collected. In addition to routine controls, the patients′ lipid levels were measured at 3-mo intervals. The parameters that were obtained over 3 years included total cholesterol, high-d. lipoprotein cholesterol, triglyceride, and N-terminal pro-B-type natriuretic peptide levels. Results: A total of 192 patients with a functional capacity New York Heart Association II-V, and who were using sacubitril/valsartan because of heart failure with reduced ejection fraction, were included in this study. Independent of statin use, there was a decrease in total cholesterol levels (196.1 ± 44.8 mg/dL vs 161.5 ± 41.7 mg/dL, p < 0.001) and triglyceride levels (159.1 ± 10.4 mg/dL vs 121.4 ± 6.9 mg/dL, p < 0.001), and there was an improvement in high-d. lipoprotein cholesterol levels (44.9 ± 1.9 mg/dL vs 48.2 ± 2.4 mg/dL, p < 0.001) when comparing baseline levels with third-year levels. Conclusions: Sacubitril/valsartan in patients with heart failure with reduced ejection fraction, independent of statin use, may cause a decrease in total cholesterol and triglyceride levels and an improvement in high-d. lipoprotein cholesterol levels.

Clinical Drug Investigation 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

Rotili, Dante published the artcileBenzodeazaoxaflavins as Sirtuin Inhibitors with Antiproliferative Properties in Cancer Stem Cells, Recommanded Product: 4-(tert-Butyl)-N-((4-(5-(dimethylamino)pentanamido)phenyl)carbamothioyl)benzamide, the publication is Journal of Medicinal Chemistry (2012), 55(18), 8193-8197, database is CAplus and MEDLINE.

Inhibition of sirtuins has recently been proposed as a promising anticancer strategy. Some of the new benzodeazaoxaflavins (2a, 2b, and 2d) here reported as SIRT1/2 inhibitors were endowed with pro-apoptotic properties in human U937 leukemia cells and, most importantly, together with the prototype MC2141 (1) displayed antiproliferative effects in cancer stem cells from patients with colorectal carcinoma and glioblastoma multiforme, known to be highly tumorigenic, resistant to conventional cancer chemotherapy, and responsible, at least in part, for cancer relapse or recurrence.

Journal of Medicinal Chemistry 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, Recommanded Product: 4-(tert-Butyl)-N-((4-(5-(dimethylamino)pentanamido)phenyl)carbamothioyl)benzamide.

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

Lundrigan, Travis published the artcileNickel-Catalyzed N-Arylation of Amides with (Hetero)aryl Electrophiles by Using a DBU/NaTFA Dual-Base System, SDS of cas: 1453-82-3, the publication is Synlett (2021), 32(16), 1665-1669, database is CAplus.

The first nickel-catalyzed N-arylation of amides with (hetero)aryl (pseudo)halides employing an organic amine base is described. By using a bis(cyclooctadienyl)nickel/8-[2-(dicyclohexylphosphinyl)phenyl]-1,3,5,7-tetramethyl-2,4,6-trioxa-8-phosphaadamantane catalyst mixture in combination with DBU/NaTFA as a dual-base system, a diversity of (hetero)aryl chloride, bromide, tosylate, and mesylate electrophiles were successfully cross-coupled with structurally diverse primary amides, as well as a selection of secondary amide, lactam, and oxazolidone nucleophiles.

Synlett 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, SDS of cas: 1453-82-3.

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

Forbus, T. R. Jr. published the artcileReactions of the readily accessible electrophile, trifluoroacetyl triflate: a very reactive agent for trifluoroacetylations at oxygen, nitrogen, carbon, or halogen centers, Recommanded Product: N,N-Diethyl-2,2,2-trifluoroacetamide, the publication is Journal of Organic Chemistry (1987), 52(19), 4156-9, database is CAplus.

Trifluoroacetyl triflate (I) is readily prepared in 82% yield by the dehydration (P₂O₅) of a 2:1 mixture of CF₃CO₂H and CF₃SO₃H. Reactions of this highly electrophilic trifluoroacetylating reagent with alcs., ketones, ethers, amines, and pyridines give esters, enol esters, ether cleavage, amides, and acylpyridinium ions, resp. Reactions with ionic or easily ionizable alkyl halides give the very volatile trifluoroacetyl halides and the ionic triflate. Triphenylmethyl chloride, for example, is quant. converted to triphenylcarbenium triflate in a very convenient synthetic procedure. I is used in the synthesis of the first member of a new class of pyrylium salts, 2,6-dimethoxypyrylium triflate.

Journal of Organic Chemistry published new progress about 360-92-9. 360-92-9 belongs to amides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Amine,Aliphatic hydrocarbon chain,Amide, name is N,N-Diethyl-2,2,2-trifluoroacetamide, and the molecular formula is C6H10F3NO, Recommanded Product: N,N-Diethyl-2,2,2-trifluoroacetamide.

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

Soley, Jacob published the artcileMild, Rapid, and Chemoselective Procedure for the Introduction of the 9-Phenyl-9-fluorenyl Protecting Group into Amines, Acids, Alcohols, Sulfonamides, Amides, and Thiols, Formula: C11H22N2O4, the publication is Journal of Organic Chemistry (2020), 85(4), 2068-2081, database is CAplus and MEDLINE.

The 9-phenyl-9-fluorenyl (PhF) group has been used as an N^α protecting group of amino acids and their derivatives mainly as a result of its ability to prevent racemization. However, installing this group using the standard protocol, which employs 9-bromo-9-phenylfluorene/K₃PO₄/Pb(NO₃)₂, often takes days and yields can be variable. Here, we demonstrate that the PhF group can be introduced into the amino group of Weinreb’s amides and Me esters of amino acids, as well as into alcs. and carboxylic acids, rapidly and in excellent yields, using 9-chloro-9-phenylfluorene (PhFCl)/N-methylmorpholine (NMM)/AgNO₃. N^α-PhF-protected amino acids can be prepared from unprotected α-amino acids, rapidly and often in near quant. yields, by treatment with N,O-bis(trimethylsilyl)acetamide (BSA) and then PhFCl/NMM/AgNO₃. Primary alcs. can be protected with the PhF group in the presence of secondary alcs. in moderate yield. Using PhFCl/AgNO₃, a primary alc. can be protected in good yield in the presence of a primary ammonium salt or a carboxylic acid. Primary sulfonamides and amides can be protected in moderate to good yields using phenylfluorenyl alc. (PhFOH)/BF₃·OEt₂/K₃PO₄, while thiols can be protected in good to excellent yield using PhFOH/BF₃·OEt₂ even in the presence of a carboxylic acid or primary ammonium group.

Journal of Organic 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 C38H74Cl2N2O4, Formula: C11H22N2O4.

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

Totsingan, Filbert published the artcileHighly selective single nucleotide polymorphism recognition by a chiral (5S) PNA beacon, Computed Properties of 186046-83-3, the publication is Chirality (2008), 21(1), 245-253, database is CAplus and MEDLINE.

A chiral peptide nucleic acid (PNA) beacon containing a C-5 modified monomer based on L-lysine was synthesized. The terminal amino group of the lysine side chain was linked to a spacer for future applications on surfaces. The PNA beacon bears a carboxyfluorescein fluorophore and a dabcyl quencher at opposite ends. The DNA binding properties were compared with those of a homologous PNA beacon containing only achiral monomers. Both beacons underwent a fluorescence increase in the presence of complementary DNA, with higher efficiency and higher selectivity (evaluated using single mismatched DNA sequences) observed for the chiral monomer containing PNA. Ion exchange (IE) HPLC with fluorimetric detection was used in combination with the beacon for the selective detection of complementary DNA. A fluorescent peak corresponding to the PNA beacon:DNA duplex was observed at a very low detection limit (1 nM). The discriminating capacity of the chiral PNA beacon for a single mismatch was found to be superior to those observed with the unmodified one, thus confirming the potency of chirality for increasing the affinity and specificity of DNA recognition.

Chirality 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 C13H18N2, Computed Properties of 186046-83-3.

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

McCall, J. M. published the artcileNew approach to triaminopyrimidine N-oxides, HPLC of Formula: 15029-36-4, the publication is Journal of Organic Chemistry (1975), 40(22), 3304-6, database is CAplus and MEDLINE.

2,4,Diamino-6-(substituted amino)pyrimidine 3-oxides (I, R = H, R2 = Me, Et, Bu, n-C10H21, cyclohexyl; R = R1 = Bu, cyclohexyl; NRR1 = piperidine, 1-pyrrolidinyl) are prepared from amides NCCH2CONRR1 which are O-methylated to NCCH:C(OMe)NRR2, the products reacted with H2NCN to give NCCH2C(NRR1):NCN, and these treated in situ with NH2OH to give I. The sequential generation of the heterocycle from smaller fragments unequivocally establishes the position of the amine and N-oxide functionalities and allows ready variation of the 6-amino substituent. The three-step process proceeds in good yield and is easily performed.

Journal of Organic Chemistry 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