Month: November 2022

Burger, Klaus published the artcileHexafluoroacetone as protective group and activating reagent in amino acid and peptide chemistry. 10. Synthesis of 3-(thiazol-4-yl)alanine and 3-(selenazol-4-yl)alanine derivatives from aspartic acid, Product Details of C5H10N2OS, the publication is Synthesis (1992), 1145-50, database is CAplus.

3-(Thiazol-4-yl)alanines I (R = Ph, 4-MeC₆H₄, 4-MeOC₆H₄, 2-furyl, NMe₂, 4-FC₆H₄, 2-thienyl, H, Me; R¹ = H, Me) and the 3-(selenazol-4-yl)alanine II were obtained from aspartic acid via 2,2-bis(trifluoromethyl)-4-(3-bromo-2-oxopropyl)-1,3-oxazolidin-5-one in a Hantzsch synthesis, using hexafluoroacetone as protective group.

Synthesis 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, Product Details of C5H10N2OS.

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

Lajin, Bassam published the artcileFluorinated carboxylic acids as “ion repelling agents” in reversed-phase chromatography, Application of 2-Chloroacetamide, the publication is Journal of Chromatography A (2020), 461575, database is CAplus and MEDLINE.

Fluorinated carboxylic acids have been in use as ion-pairing reagents for over three decades. It has been observed that ion-pairing reagents not only increase the retention of oppositely charged analytes on reversed-phase HPLC columns but also decrease the retention of similarly charged analytes; these latter effects, however, have not been thoroughly investigated for the fluorinated carboxylic acids, and the application of these reagents has been rather restricted to their ion-pairing capacity to sep. basic analytes. In the present study, we report a systematic investigation about the effects of three fluorinated carboxylic acids (trifluoroacetic acid (TFA), pentafluoropropionic acid (PFPA), and heptafluorobutyric acid (HFBA)) on the retention and selectivity of the separation of halogenated carboxylic acids and sulfonic acids by reversed-phase chromatog. with an inductively coupled plasma mass spectrometry detector (ICPMS). Several eluents were tested and compared at different concentrations (0-100 mM) and pH values, including sulfate, nitrate, phosphate, oxalate, TFA, PFPA, and HFBA. The fluorinated carboxylic acids resulted in a consistent decrease in the retention factors (up to ca. 9-fold with HFBA) in a concentration dependent manner, which plateaued at around 50 mM. Significant improvement of the peak symmetry of the chromatographed acids was also observed We highlight the advantages of incorporating the fluorinated carboxylic acids in modifying the selectivity and retention of organic acids in reversed phase chromatog. in general, and particularly when employing chromatog. detectors with limited compatibility with organic mobile phases such as the ICPMS.

Journal of Chromatography A 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, Application of 2-Chloroacetamide.

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

Marin, Sela published the artcileValsartan and sacubitril combination treatment enhances collagen production in older adult human skin cells, Safety of (S)-2-(N-((2′-(1H-Tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid, the publication is Experimental Gerontology (2022), 111835, database is CAplus and MEDLINE.

Collagen is a major component of the skin′s support system, allowing for its firmness, elasticity, and mech. strength. Skin collagen production decreases as we age and is associated with increased sagging, wrinkling, and thinning. The Renin-Angiotensin System (RAS) is a key hormonal system that changes with age and affects multiple organ systems. The primary health benefits of Angiotensin (Ang) receptor type1 (AT₁R) blockers are believed to arise from systemic effects on blood pressure. However, there is also a skin-specific RAS, though this system has been less well characterized. There are eight FDA-approved angiotensin receptor blockers (ARBs) on the market, although the impact of topical ARBs on aging skin is unknown. Here, we evaluated the topical penetration of gel formulations of eight ARBs using human cadaver skin. Our results show that valsartan achieved the highest skin penetration compared to other ARBs. We then treated human skin fibroblasts from 2-yr-old and 57-yr-old individuals with valsartan alone or in combination with the neprilysin inhibitor sacubitril. Sacubitril works synergistically with valsartan by inhibiting the degradation of angiotensin II, thereby increasing its bioavailability. Treatment of young and older adult human skin cells with valsartan and sacubitril led to a five-fold increase in collagen type-1 production in the young cells and a four-fold increase in collagen type-1 in older adult cells. This study demonstrates a potential novel application for the widely prescribed drug combination sacubitril-valsartan as a topical agent in aged skin.

Experimental Gerontology 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, Safety of (S)-2-(N-((2′-(1H-Tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid.

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

Grigoreva, Yu S published the artcile[The role of p53 in the regulation of proliferation and differentiation of the neural progenitors in mouse hippocampal organotypic culture]., Product Details of C20H23N3O2S, the publication is Rossiiskii fiziologicheskii zhurnal imeni I.M. Sechenova (2013), 99(10), 1160-74, database is MEDLINE.

In the present work we have studied the effects of p53 on the proliferation and differentiation of neural progenitor cells (NPC) in mouse hippocampal organotypic culture. To study the role of p53 the selective p53 inhibitor pifithrin-alpha (PFT) and activator tenovin 1 (TEN) were used in the experiments. Obtained data demonstrated that the injections of PFT did not affect on the amount of phospho-H3 positive cells in the subgranular zone of hippocampus. This data revealed that p53 inhibition does not change the proliferation level of the NPC. In opposite, at the TEN treatments we observed increased of the proliferation activity. Analysis of Pim-1 and Phb 1, which regulate cell cycle progression, demonstrated that p53 activation led to increased level of Pim-1 as well as the proliferation. Thus, our data correlate with published ones and proposed that Pim-1 positively regulates NPC cell cycle progression. In opposite to Pim-1, Phb 1 has anti-proliferative action. Our obtained data demonstrated that TEN diminished Phb 1 expression. Primarily PFT injections led to the increasing Phbl level, but then dramatically decreased it that accompanied with unchanged proliferation level. In other words, increased proliferation level after TEN treatments, which we observed, can be partly depend from the inhibition of anti-proliferative activity of Phb. In our study we demonstrated that both TEN and in a greater degree PFT stimulates neuronal differentiation by activation of CRMP-2 expression, but do not affect on gliogenesis. Thus, obtained data revealed that p53 is an important factor of neuronal differentiation and, probably, p53 action is mediated by cell cycle regulator protein such as Pim-1 and Phbl.

Rossiiskii fiziologicheskii zhurnal imeni I.M. Sechenova 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, Product Details of C20H23N3O2S.

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

Sleevi, P. published the artcileTrifluoroacetyl chloride for characterization of organic functional groups by fluorine-19 nuclear magnetic resonance spectrometry, Formula: C6H10F3NO, the publication is Analytical Chemistry (1979), 51(12), 1931-4, database is CAplus.

The potential utility of trifluoroacetyl chloride as an anal. ¹⁹F NMR reagent to characterize alcs., phenols, thiols, and primary and secondary amines is discussed. The ¹⁹F chem. shift and yield data for trifluoroacetyl derivatives of approx. 50 model compounds are presented. The importance of an added organic base (2,6-lutidine) in derivative preparation for phenols, and primary and secondary amines is also discussed.

Analytical 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 C18H34N4O5S, Formula: C6H10F3NO.

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

Bryantsev, Vyacheslav S. published the artcileInvestigation of Fluorinated Amides for Solid-Electrolyte Interphase Stabilization in Li-O₂ Batteries Using Amide-Based Electrolytes, Computed Properties of 360-92-9, the publication is Journal of Physical Chemistry C (2013), 117(23), 11977-11988, database is CAplus.

Solvent and electrode stability is critical for the successful development of the rechargeable, organic electrolyte Li-O₂ (air) battery. Straight-chain alkyl amides, such as N,N-dimethylacetamide (DMA), show superior stability at the O₂ cathode compared to organic carbonates and glymes, but these solvents do not form a stable solid-electrolyte interphase (SEI) to prevent a sustained reaction with Li metal. In this work, we use electrochem. impedance spectroscopy and cycling tests on a sym. Li/electrolyte/Li cell to determine the ability of several fluorinated amide solvents to stabilize the lithium/electrolyte interface. The LiTFSI/N,N-dimethyltrifluoroacetamide (DMTFA) system shows the smallest interfacial impedance and the lowest polarization for Li dissolution and deposition. We present quantum chem. calculations indicating that α-fluorinated alkyl amides are reduced on Li to form insoluble LiF with no or little activation energy. XPS anal. confirms the presence of LiF in the SEI on Li metal exposed to DMTFA, which is likely to play an important role in stabilizing the lithium/electrolyte interface. The improved stability of a metallic Li anode in a rechargeable Li-O₂ battery with LiTFSI/DMA electrolyte is demonstrated using 2% DMTFA as the SEI-stabilizing additive.

Journal of Physical Chemistry C 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, Computed Properties of 360-92-9.

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

Verdugo, Edgard M. published the artcileControlling disinfection byproducts from treated wastewater using adsorption with granular activated carbon: Impact of pre-ozonation and pre-chlorination, Category: amides-buliding-blocks, the publication is Water Research: X (2020), 100068, database is CAplus and MEDLINE.

This study measured chlorine- and chloramine-reactive precursors using formation potential (FP) tests of nine U. S. Environmental Protection Agency (EPA) regulated and 57 unregulated disinfection byproducts (DBPs) in tertiary-filtered wastewater before and after pilot-scale granular activated carbon (GAC) adsorption. Using breakthrough of precursor concentration and of concentration associated calculated cytotoxicity and genotoxicity (by correlating known lethal concentrations reported elsewhere), the performance of three parallel GAC treatment trains were compared against tertiary-filtered wastewater: ozone/GAC, chlorine/GAC, and GAC alone. Results show GAC alone was the primary process, vs. ozone or chlorine alone, to remove the largest fraction of total chlorine- and chloramine-reactive DBP precursors and calculated cytotoxicity and genotoxicity potencies. GAC with pre-ozonation removed the most chlorine- and chloramine-reactive DBP precursors followed by GAC with pre-chlorination and lastly GAC without pre-treatment. GAC with pre-ozonation produced an effluent with cytotoxicity and genotoxicity of DBPs from FP that generally matched that of GAC without pre-oxidation; meanwhile removal of toxicity was greater by GAC with pre-chlorination. The cytotoxicity and genotoxicity of DBPs from FP tests did not scale with DBP concentration; for example, more than 90% of the calculated cytotoxicity resulted from 20% of the DBPs, principally from haloacetaldehydes, haloacetamides, and haloacetonitriles. The calculated cytotoxicity and genotoxicity from DBPs associated with FP-chloramination were at times higher than with FP-chlorination though the concentration of DBPs was five times higher with FP-chlorination. The removal of DBP precursors using GAC based treatment was at least as effective as removal of DOC (except for halonitromethanes for GAC without pre-oxidation and with pre-chlorination), indicating DOC can be used as an indicator for DBP precursor adsorption efficacy. However, the DOC was not a good surrogate for total cytotoxicity and genotoxicity breakthrough behavior, therefore, unregulated DBPs could have neg. health implications that are disconnected from general water quality parameters, such as DOC, and regulated classes of DBPs. Instead, cytotoxicity and genotoxicity correlate with the concentration of specific classes of unregulated DBPs.

Water Research: X 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 C22H18Cl2N2, Category: amides-buliding-blocks.

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

Rouleau, Cecile published the artcileAnti-Endosialin Antibody-Drug Conjugate: Potential in Sarcoma and Other Malignancies, HPLC of Formula: 916746-27-5, the publication is Molecular Cancer Therapeutics (2015), 14(9), 2081-2089, database is CAplus and MEDLINE.

Endosialin/TEM1/CD248 is a cell surface protein expressed at high levels by the malignant cells of about 50% of sarcomas and neuroblastomas. The antibody-drug conjugate (ADC) anti-endosialin-MC-VC-PABC-MMAE was selectively cytotoxic to endosialin-pos. cells in vitro and achieved profound and durable antitumor efficacy in preclin. human tumor xenograft models of endosialin-pos. disease. MC-VC-PABC-MMAE was conjugated with anti-endosialin with 3-4 MMAE mols. per ADC. The anti-endosialin-MC-VC-PABC-MMAE conjugate was tested for activity in four human cell lines with varied endosialin levels. The HT-1080 fibrosarcoma cells do not express endosialin, A-673 Ewing sarcoma cells and SK-N-AS neuroblastoma cells are moderate expressers of endosialin, and SJSA-1 osteosarcoma cells express very high levels of endosialin. To determine whether endosialin expression was maintained in vivo, A-673 Ewing sarcoma, SK-N-AS neuroblastoma, and SJSA-1 osteosarcoma cells were grown as xenograft tumors in nude mice. The SK-N-AS neuroblastoma and the A-673 Ewing sarcoma lines were selected for in vivo efficacy testing of the anti-endosialin-MC-VC-PABC-MMAE conjugate. The treatment groups included a vehicle control, unconjugated anti-endosialin, an admix control consisting of anti-endosialin and a dose of free MMAE equivalent to the dose administered as the ADC, and the anti-endosialin-MC-VC-PABC-MMAE conjugate. The unconjugated anti-endosialin had no antitumor activity and resulted in similar tumor growth as the vehicle control. The admix control produced a modest tumor growth delay. Administration of the anti-endosialin-MC-VC-PABC-MMAE conjugate resulted in a marked prolonged tumor response of both xenograts. These proof-of-concept results break new ground and open a promising drug discovery approach to these rare and neglected tumors. Mol Cancer Ther; 14(9); 2081-9. ©2015 AACR.

Molecular Cancer Therapeutics published new progress about 916746-27-5. 916746-27-5 belongs to amides-buliding-blocks, auxiliary class ADC Linker,Enzymatic Cleavage Linker, name is (S)-2-((S)-2-(6-(2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)hexanamido)-3-methylbutanamido)-5-ureidopentanoic acid, and the molecular formula is C21H33N5O7, HPLC of Formula: 916746-27-5.

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

Xavier, Catarina published the artcileSynthesis, characterization, and evaluation of a novel ^99mTc(CO)₃ pyrazolyl conjugate of a peptide nucleic acid sequence, Quality Control of 186046-83-3, the publication is JBIC, Journal of Biological Inorganic Chemistry (2008), 13(8), 1335-1344, database is CAplus and MEDLINE.

The 16-mer peptide nucleic acid sequence H-A GAT CAT GCC CGG CAT-Lys-NH₂ (1), which is complementary to the translation start region of the N-myc oncogene mRNA, was synthesized and conjugated to a pyrazolyl diamine bifunctional chelator (pz). The novel conjugate pz-A GAT CAT GCC CGG CAT-Lys-NH₂ (2) was labeled with technetium tricarbonyl, yielding quant. the complex fac-[^99mTc(CO)₃(κ³-pz-A GAT CAT GCC CGG CAT-Lys-NH₂)]²⁺ (4). Complex 4 was obtained with high radiochem. purity and high specific activity, revealing high stability in human serum and in cell culture medium. The identity of 4 was confirmed by comparing its reversed-phase high performance liquid chromatog. profile with that of the rhenium analog fac-[Re(CO)₃(κ³-pz-A GAT CAT GCC CGG CAT-Lys-NH₂)]²⁺ (3), prepared by conjugation of fac-[Re(CO)₃(3,5-Me₂pz(CH₂)₂N((CH₂)₃COOH)(CH₂)₂NH₂)]⁺ to 1, using solid-phase techniques. UV melting experiments of 1 and 3 with the complementary DNA sequence led to the formation of stable duplexes, indicating that the conjugation of 1 to the pyrazolyl chelator and to the metal fragment fac-[M(CO)₃]⁺ did not affect the recognition of the complementary sequence as well as the duplex stability. For a first screening, SH-SY5Y human neuroblastoma cells, which express N-myc, were treated with 4. The results show that 4 internalizes (7% of the activity goes into the cells, after 4 h at 37°), presenting also a relatively high cellular retention (only 40% of internalized activity is released from the cells after 5 h).

JBIC, Journal of Biological Inorganic 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 C2H3N3, Quality Control of 186046-83-3.

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

Mohareri, Mohammad Moein published the artcilePreparation and application of Fe₃O₄@Acetamidoxanthate as a unique nanosorbent in heavy metal removing, Synthetic Route of 79-07-2, the publication is Main Group Chemistry (2021), 20(4), 633-643, database is CAplus.

Chelating agents are one of the most important substances in metal extraction, but separation is the main problem in the use of these agents as an adsorbent. After the adsorption of metals by an external magnet, magnetic NPs provide the possibility of easy collecting and isolating the adsorbent nanomaterial for many applications. Given the immense importance of magnetic NPs, there has been widespread interest in accessing the above adsorbent. In the present study, an attempt was made to synthesize acetamido xanthate which was coupled to NPs and has the potential to be used as a nano-adsorbent for the removal of heavy metals. This novel nano sorbent was characterized by SEM (SEM), Fourier transforms IR (FT-IR), and NMR (NMR) spectroscopy. The effect of some parameters such as temperature, time, pH, and the amount of adsorbent on the extraction reaction was investigated. The optimized condition for extraction of cerium was temperature of 30°C, pH=8, reaction time of 45 min using 7.5mg of the prepared nanosorbent, that in such condition the yield of reaction achieved up to 97%. The prepared adsorbent showed high efficiency in the adsorption of heavy metals specifically.

Main Group 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 C2H4ClNO, Synthetic Route of 79-07-2.

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