Category: amides-buliding-blocks

Peikert, Alexander published the artcileEffects of sacubitril/valsartan versus valsartan on renal function in patients with and without diabetes and heart failure with preserved ejection fraction: insights from PARAGON-HF, Quality Control of 137862-53-4, the publication is European Journal of Heart Failure (2022), 24(5), 794-803, database is CAplus and MEDLINE.

Diabetes is associated with a faster rate of renal function decline in patients with heart failure (HF). Sacubitril/valsartan attenuates the deterioration of renal function to a greater extent in patients with diabetes and HF with reduced ejection fraction compared with renin-angiotensin system inhibitors alone. We assessed whether the same may be true in HF with preserved ejection fraction (HFpEF). In the PARAGON-HF trial in patients with HF and left ventricular ejection fraction of ≥45% (n = 4796), we characterized the effects of sacubitril/valsartan on changes in estimated glomerular filtration rate (eGFR) over a period of 192 wk, and on the pre-specified renal composite outcome (eGFR reduction of ≥50%, end-stage renal disease, or death attributable to renal causes) in patients with (n = 2388) and without diabetes (n = 2408). The decline in eGFR was greater in patients with diabetes than in those without (-2.6 vs. -1.7 mL/min/1.73 m2 per yr, p < 0.001), regardless of treatment assignment. Sacubitril/valsartan attenuated decline in eGFR similarly in patients with (-2.2 vs. -2.9 mL/min/1.73 m2 per yr, p = 0.001) and without diabetes (-1.5 vs. -2.0 mL/min/1.73 m2 per yr, p = 0.006) (pinteraction for difference in eGFR slopes = 0.40). Compared with valsartan, sacubitril/valsartan reduced the renal composite outcome similarly in patients without diabetes (hazard ratio [HR] 0.42, 95% confidence interval [CI] 0.19-0.91) and those with diabetes (HR 0.54, 95% CI 0.33-0.89; pinteraction = 0.59), as well as across a range of baseline glycated Hb (pinteraction = 0.71). Sacubitril/valsartan, compared with valsartan, attenuates the decline of eGFR and reduces clin. relevant kidney events similarly among patients with HFpEF with and without diabetes.

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, Quality Control of 137862-53-4.

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

Mastrangelo, M. M. published the artcileOccurrence and accumulation of pharmaceutical products in water and biota of urban lowland rivers, Application In Synthesis of 137862-53-4, the publication is Science of the Total Environment (2022), 154303, database is CAplus and MEDLINE.

We evaluated the distribution of eleven groups of pharmaceutically active compounds (PhACs) in surface waters and biota of different trophic levels, in five sites of two lowland urban rivers in Argentine. Twenty-nine out of 39 PhACs and two metabolites were detected in at least one water sample (2-9622 ng/L), eleven detected in biofilms (1-179 ng/g d.w.) and eight in the macrophyte Lemna gibba (4-112 ng/g d.w). The two more polluted sites had a similar distribution of the main groups of compounds In surface waters, the largest concentrations were for the analgesic acetaminophen (9622 ng/L), the antibiotic sulfamethoxazole (326 ng/L), the antihypertensive valsartan (963 ng/L), the β-blocking agent atenolol (427 ng/L), the diuretic hydrochlorothiazide (445 ng/L) and the psychiatric drug carbamazepine (99 ng/L). The antibiotic ciprofloxacin exhibited the highest concentration in the biofilm (179 ng/g d.w.) and in the macrophyte L. gibba (112 ng/g d.w.) Several compounds were detected in the water but not in the biota (e.g., codeine and bezafibrate), and others (e.g., azithromycin and citalopram) were found in the biota but not in the surface water. Significant bioaccumulation factors (>1000 L/kg d.w.) were obtained for venlafaxine and ciprofloxacin in biofilm. Our results show that PhACs may accumulate in several biol. compartments. Within an environmental compartment, similar PhACs profile and concentrations were found in different sites receiving urban pollution. Among different compartments, biofilms may be the most suitable biota matrix to monitor the immediate reception of PhACs in the biota. Our results indicate that the presence of PhACs in urban rivers and their accumulation in the biota could be incorporated as symptoms of the urban stream syndrome.

Science of the Total Environment 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, Application In Synthesis of 137862-53-4.

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

Uzal-Varela, Rocio published the artcileUnderstanding the Effect of the Electron Spin Relaxation on the Relaxivities of Mn(II) Complexes with Triazacyclononane Derivatives, Application of 2-Chloroacetamide, the publication is Inorganic Chemistry (2021), 60(20), 15055-15068, database is CAplus and MEDLINE.

Investigating the relaxation of water ¹H nuclei induced by paramagnetic Mn(II) complexes is important to understand the mechanisms that control the efficiency of contrast agents used in diagnostic magnetic resonance imaging (MRI). Herein, a series of potentially hexadentate triazacyclononane (TACN) derivatives containing different pendant arms were designed to explore the relaxation of the electron spin in the corresponding Mn(II) complexes using a combination of ¹H NMR relaxometry and theor. calculations These ligands include 1,4,7-triazacyclononane-1,4,7-triacetic acid (H₃NOTA) and three derivatives in which an acetate group is replaced by sulfonamide (H₃NO2ASAm), amide (H₂NO2AM) or pyridyl (H₂NO2APy) pendants, resp. The analog of H₃NOTA containing three propionate pendant arms (H₃NOTPrA) was also investigated. The x-ray structure of the derivative containing two acetate groups and a sulfonamide pendant arm [Mn(NO2ASAm)]^– evidenced six-coordination of the ligand to the metal ion, with the coordination polyhedron being close to a trigonal prism. The relaxivities of all complexes at 20 MHz and 25° (1.1-1.3 mM^-1 s^-1) are typical of systems that lack water mols. coordinated to the metal ion. The nuclear magnetic relaxation profiles evidence significant differences in the relaxivities of the complexes at low fields (<1 MHz), which are associated with different spin relaxation rates. The zero field splitting (ZFS) parameters calculated using DFT and CASSCF methods show that electronic relaxation is relatively insensitive to the nature of the donor atoms. However, the twist angle of the two tripodal faces that delineate the coordination polyhedron, defined by the N atoms of the TACN unit (lower face) and the donor atoms of the pendant arms (upper face), has an important effect in the ZFS parameters. A twist angle close to the ideal value for an octahedral coordination (60°), such as that in [Mn(NOTPrA)]^–, leads to a small ZFS energy, whereas this value increases as the coordination polyhedron approaches to a trigonal prism.

Inorganic Chemistry 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 C9H7NO4, Application of 2-Chloroacetamide.

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

Batenko, N. G. published the artcileSynthesis of 2,5-bis(2-aminothiazol-5-yl)-3,6-dichloro-1,4-benzoquinones, Application In Synthesis of 14294-10-1, the publication is Chemistry of Heterocyclic Compounds (New York)(Translation of Khimiya Geterotsiklicheskikh Soedinenii) (2000), 36(6), 733-737, database is CAplus.

A series of 2-(2-aminothiazol-5-yl)-3,6-dichloro-5-diethylaminoethenyl-1,4-benzoquinones was synthesized from 2-(2-aminothiazol-5-yl)-3,5,6-trichloro-1,4-benzoquinones using acetaldehyde and diethylamine in toluene solution Refluxing these compounds with substituted thioureas in acetonitrile in the presence of hydrochloric acid gives the corresponding 2,5-bis(2-aminothiazol-5-yl)-3,6-dichlorohydroquinones which can be oxidized to the target products with ferric chloride in aqueous DMF.

Chemistry of Heterocyclic Compounds (New York)(Translation of Khimiya Geterotsiklicheskikh Soedinenii) published new progress about 14294-10-1. 14294-10-1 belongs to amides-buliding-blocks, auxiliary class Morpholine,Thiourea,Amine,Amide, name is Morpholine-4-carbothioamide, and the molecular formula is C5H10N2OS, Application In Synthesis of 14294-10-1.

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

Michaelis, Julia published the artcileDNA-Triggered Dye Transfer on a Quantum Dot, Safety of 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, the publication is Bioconjugate Chemistry (2014), 25(1), 18-23, database is CAplus and MEDLINE.

Nucleic acid-templated reactions are frequently explored tools in nucleic acid diagnosis. To enable a separation-free DNA detection, the reactive probe mols. require conjugation with reporter groups that provide measurable changes of an observable parameter upon reaction. A widely used, generic read-out method is based on fluorescence resonance energy transfer (FRET) between two appended dyes. Yet, spectral cross-talk usually limits the achievable enhancements of the FRET signal in DNA-directed chemistries. We describe a DNA-triggered transfer reaction which provides for strong increases of a fluorescent signal caused by FRET. The method may involve DNA- and PNA-based probes and is based upon a proximity-triggered transfer reaction which leads to the covalent fixation of a fluorescence dye on the surface of a quantum dot (QD). The transfer reaction brings the dye closer to the QD than hybridization alone. The resulting FRET signal is a specific monitor of the reaction and allows efficient discrimination of single base mismatched templates. Of note, the 35-fold increase of the FRET signal is measured at 310 nm apparent Stokes shift and turnover in template provides a means for signal amplification.

Bioconjugate Chemistry 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, Safety of 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.

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

Lange, Jos H. M. published the artcileNovel 3,4-diarylpyrazolines as potent cannabinoid CB₁ receptor antagonists with lower lipophilicity, Recommanded Product: N-Methyl-N-isopropylsulfamoyl amide, the publication is Bioorganic & Medicinal Chemistry Letters (2005), 15(21), 4794-4798, database is CAplus and MEDLINE.

3,4-Diarylpyrazolines as potent CB₁ receptor antagonists with lipophilicity lower than that of SLV319 are described. The key change was the replacement of the arylsulfonyl group in the original series by a dialkylaminosulfonyl moiety. The absolute configuration (4S) of enantiomer I was established by X-ray diffraction anal. and I showed a close mol. fit with rimonabant in a CB₁ receptor-based model. II exhibited the highest CB₁ receptor affinity (K_i = 24 nM) in this series, as well as very potent CB₁ antagonistic activity (pA ₂ = 8.8) and a high CB₁/CB₂ subtype selectivity (∼147-fold).

Bioorganic & Medicinal Chemistry Letters published new progress about 372136-76-0. 372136-76-0 belongs to amides-buliding-blocks, auxiliary class Sulfamide,Amine,Aliphatic hydrocarbon chain, name is N-Methyl-N-isopropylsulfamoyl amide, and the molecular formula is C4H12N2O2S, Recommanded Product: N-Methyl-N-isopropylsulfamoyl amide.

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

Tharp, Jeffery M. published the artcileGenetic Encoding of Three Distinct Noncanonical Amino Acids Using Reprogrammed Initiator and Nonsense Codons, Application In Synthesis of 2418-95-3, the publication is ACS Chemical Biology (2021), 16(4), 766-774, database is CAplus and MEDLINE.

We recently described an orthogonal initiator tRNA (itRNA^Ty2) that can initiate protein synthesis with noncanonical amino acids (ncAAs) in response to the UAG nonsense codon. Here, we report that a mutant of itRNA^Ty2 (itRNA^Ty2_AUA) can efficiently initiate translation in response to the UAU tyrosine codon, giving rise to proteins with an ncAA at their N-terminus. We show that, in cells expressing itRNA^Ty2_AUA, UAU can function as a dual-use codon that selectively encodes ncAAs at the initiating position and predominantly tyrosine at elongating positions. Using itRNA^Ty2_AUA, in conjunction with its cognate tyrosyl-tRNA synthetase and two mutually orthogonal pyrrolysyl-tRNA synthetases, we demonstrate that UAU can be reassigned along with UAG or UAA to encode two distinct ncAAs in the same protein. Furthermore, by engineering the substrate specificity of one of the pyrrolysyl-tRNA synthetases, we developed a triply orthogonal system that enables simultaneous reassignment of UAU, UAG, and UAA to produce proteins containing three distinct ncAAs at precisely defined sites. To showcase the utility of this system, we produced proteins containing two or three ncAAs, with unique bioorthogonal functional groups, and demonstrate that these proteins can be sep. modified with multiple fluorescent probes.

ACS Chemical Biology 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 C4H8Cl2S2, Application In Synthesis of 2418-95-3.

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

Semichenko, E. S. published the artcileZeolites in the synthesis of 1-alkyl-2-oxonicotinonitriles, Product Details of C5H8N2O, the publication is Russian Journal of Organic Chemistry (2005), 41(2), 313-314, database is CAplus.

Cyclocondensation of acetylacetone with cyanoacetamide or N-alkylcyanoacetamides (alkyl = Me, Et) in the presence of NaA zeolite afforded 4,6-dimethyl-2-oxonicotinonitrile or 1-alkyl-4,6-dimethyl-2-oxonicotinonitriles, resp. The condensation of 3-hydroxyiminopenta-2,4-dione with cyanoacetamide in the same manner furnished 4,6-dimethyl-5-nitroso-2-oxonicotinonitrile.

Russian 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 C13H10O2, Product Details of C5H8N2O.

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

Pal, Manojit published the artcileSynthesis and cyclooxygenase-2 (COX-2) inhibiting properties of 1,5-diarylpyrazoles possessing N-substitution on the sulfonamide (-SO₂NH₂) moiety, HPLC of Formula: 489-17-8, the publication is Letters in Drug Design & Discovery (2005), 2(4), 329-340, database is CAplus.

A number of novel 1,5-diarylpyrazoles possessing N-substitution on the sulfonamide (SO₂NH₂) moiety were synthesized and tested for COX-1/COX-2 inhibition in vitro. Many of these 1,1-dioxo-2,3-dihydrobenzo[d]isothiazolyl substituted 1,5-diarylpyrazoles, where the SO₂NH₂ group was a part of the fused ring, showed COX inhibitory activity. Few of them were identified as selective COX-2 inhibitors. A structure-activity relationship study within the series are discussed. Compounds prepared for this study included derivatives of 5-[3-(difluoromethyl)-5-[2-fluoro-4-(methylthio)phenyl]-1H-pyrazol-1-yl]-2,3-dihydro-1,2-benzisothiazole 1,1-dioxide and 5-[5-(4-fluorophenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]-2,3-dihydro-1,2-benzisothiazole dioxide (i.e., cyclic benzenesulfonamide analogs).

Letters in Drug Design & Discovery published new progress about 489-17-8. 489-17-8 belongs to amides-buliding-blocks, auxiliary class Fluoride,Sulfamide,Amine,Benzene, name is 4-Fluoro-2-methylbenzenesulfonamide, and the molecular formula is C7H8FNO2S, HPLC of Formula: 489-17-8.

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

Pal, Manojit published the artcileSynthesis of fused sulfonamide (1,1-dioxoisothiazole)-substituted 1,5-diarylpyrazoles as cyclooxygenase inhibitors, Related Products of amides-buliding-blocks, the publication is Journal of the Indian Chemical Society (2003), 80(12), 1095-1101, database is CAplus.

First synthesis of novel 1,1-dioxo-2,3-dihydrobenzo[d]isothiazolyl substituted arylpyrazoles, e.g., I, has been accomplished via oxidative cyclization of 4-fluoro-2-Me benzenesulfonamide followed by the treatment with hydrazine and then with 1,3-dicarbonyl compounds A number of 1,5-diarylpyrazoles were synthesized in good yields and some of them were of potential biol. interest. In studies evaluating cyclooxygenase inhibiting activity, I was found to be more than 100 fold selective in COX-2 inhibition over COX-1.

Journal of the Indian Chemical Society published new progress about 489-17-8. 489-17-8 belongs to amides-buliding-blocks, auxiliary class Fluoride,Sulfamide,Amine,Benzene, name is 4-Fluoro-2-methylbenzenesulfonamide, and the molecular formula is C7H8FNO2S, Related Products of amides-buliding-blocks.

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