Month: December 2022

Mashal, Mohammad Shafiq published the artcileSimultaneous quantification of 19 nonsteroidal anti-inflammatory drugs in oral fluid by liquid chromatography-high resolution mass spectrometry: Application on ultratrail runners oral fluid, Application of 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, the publication is Drug Testing and Analysis (2022), 14(4), 701-712, database is CAplus and MEDLINE.

Nonsteroidal anti-inflammatory drugs (NSAIDs) are a therapeutic class suspected to be used by ultratrail runners. The use of NSAIDs during ultratrails is known to be associated with various adverse effects. To study the prevalence of NSAIDs intake in ultratrail runners, oral fluid (OF) is a relevant matrix as it is noninvasive and easy to collect. The aim of our work was to develop and validate a liquid-liquid extraction followed by a liquid chromatog. (LC)-mass spectrometry (MS)/high resolution mass spectrometry (HRMS) method for the simultaneous quantification of 19 NSAIDs in OF. After a comparison of different liquid-liquid extraction methods, a double step liquid-liquid extraction with chloroform was performed on OF collected with Quantisal, with extraction recoveries higher than 90%. An Accucore AQ column was selected for the chromatog. separation of NSAIDs. The Q Exactive Plus mass spectrometer operated in full scan and ddms2 mode after pos. and neg. electrospray ionization. Selectivity, carry-over, matrix effect, and linearity were validated for all NSAIDs. Within-day and between-day accuracy and precision were validated for all NSAIDs (<15% for quality control [QC] samples and <20% for lower limit of quantitation [LLOQ]), except within-day accuracy for the LLOQ of mefenamic acid. A stability study was also performed on OF at room temperature and +4°C. The method was applied on OF from runners who participate to Ultra Trail du Mont Blanc.

Drug Testing and Analysis 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 C17H14F3N3O2S, Application of 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide.

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

Matsumoto, Katsuhiko published the artcileA peptide nucleic acid (PNA) heteroduplex probe containing an inosine-cytosine base pair discriminates a single-nucleotide difference in RNA, HPLC of Formula: 186046-83-3, the publication is Chemistry – A European Journal (2013), 19(16), 5034-5040, database is CAplus and MEDLINE.

Selective discrimination of a single-nucleotide difference in single-stranded DNA or RNA remains a challenge with conventional DNA or RNA probes. A peptide nucleic acid (PNA)-derived probe, in which PNA forms a pseudocomplementary heteroduplex with inosine-containing DNA or RNA, effectively discriminates a single-nucleotide difference in a closely related group of sequences of single-stranded DNA and/or RNA. The pseudocomplementary PNA heteroduplex is easily converted to a fluorescent probe that distinctively detects a member of highly homologous let-7 microRNAs.

Chemistry – A European Journal 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, HPLC of Formula: 186046-83-3.

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

Miyoshi, Toru published the artcileLCZ696 ameliorates doxorubicin-induced cardiomyocyte toxicity in rats, Synthetic Route of 137862-53-4, the publication is Scientific Reports (2022), 12(1), 4930, database is CAplus and MEDLINE.

Doxorubicin (DOX)-based chemotherapy induces cardiotoxicity, which is considered the main bottleneck for its clin. application. In this study, we investigated the potential benefit of LCZ696, an angiotensin receptor-neprilysin inhibitor against DOX-induced cardiotoxicity in rats and H9c2 cells and determined whether the mechanism underlying any such effects involves its antioxidant activity. Male Sprague-Dawley rats were randomly separated into four groups, each consisting of 15 rats (DOX (1.5 mg/kg/day i.p. for 10 days followed by non-treatment for 8 days); DOX + valsartan (31 mg/kg/day by gavage from day 1 to day 18); DOX + LCZ696 (68 mg/kg/day by gavage from day 1 to day 18); and control (saline i.p. for 10 days)). DOX-induced elevation of cardiac troponin T levels on day 18 was significantly reduced by LCZ696, but not valsartan. The DOX-induced increase in myocardial reactive oxygen species (ROS) levels determined using dihydroethidium was significantly ameliorated by LCZ696, but not valsartan, and was accompanied by the suppression of DOX-induced increase in p47phox. LCZ696 recovered the DOX-induced decrease in phosphorylation of adenosine monophosphate-activated protein kinase and increased the ratio of Bax and Bcl-2. In H9c2 cardiomyocytes, LCZ696 reduced DOX-induced mitochondrial ROS generation and improved cell viability more than valsartan. Our findings indicated that LCZ696 ameliorated DOX-induced cardiotoxicity in rat hearts in vivo and in vitro, possibly by mediating a decrease in oxidative stress.

Scientific Reports 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, Synthetic Route of 137862-53-4.

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

Badalanloo, Kimia published the artcileCytotoxic and Apoptotic Effects of Celecoxib and Topotecan on AGS and HEK 293 Cell Lines, Category: amides-buliding-blocks, the publication is Journal of Gastrointestinal Cancer (2022), 53(1), 99-104, database is CAplus and MEDLINE.

Abstract: Purpose: This study is aimed to assess the anti-cancer effects of Celecoxib and topotecan against Human Gastric cancer cell line (AGS) in comparison to the control in an in-vitro study. Methods: In this exptl. study, Celecoxib and topotecan was prepared at concentrations of 500, 250, 125, 62.5, 31.2, 15.6 and 7.8 mg/mL. The effect of celecoxib and topotecan sep. and in mixed form were investigated on AGS and normal HEK cells. To investigate the cell survival, MTT method was used to study the pathway of apoptosis using flowcytometry and Caspase kits based on colorimetric. Finally, one-way ANOVA and t-test were used to analyze the data. Results: The results of this study indicated that Celecoxib was cytotoxic against AGS and HEK cell lines. The topotecan indicated a significant cytotoxicity against AGS cells and was not toxic against HEK cell line. Our results indicated that Celecoxib and topotecan have synergist effects against AGS and HEK cell lines and were more effective than sep. celecoxib or topotecan. Conclusion: The mixture of clecoxib and topotecan was more effective than celecoxib and topotecan in sep. form. Our results indicated that use mixed forms of treatments can cause excellent therapeutic effects and can cause less side effects.

Journal of Gastrointestinal Cancer 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 C17H14F3N3O2S, Category: amides-buliding-blocks.

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

Gilani, Saeedeh published the artcileEvaluation of the extraction process parameters on bioactive compounds of cinnamon bark: A comparative study, Related Products of amides-buliding-blocks, the publication is Process Biochemistry (Oxford, United Kingdom) (2022), 93-101, database is CAplus.

In recent times, there has been special attention to the antidiabetic properties of herbal medicine like cinnamon, because of its major compounds such as cinnamic acid and cinnamaldehyde. This study optimizes an effective technique for the extraction of cinnamic acid and cinnamaldehyde from cinnamon bark. The effective parameters of both microwave and ultrasound methods were considered and then compared with the soxhlet extraction method. The impact of different solvent types, temperature and process time, solid: solvent portion, particle size, on the yield of cinnamic acid and cinnamaldehyde extraction were investigated. In addition, all the obtained extraction samples were analyzed by the newly developed HPLC method via UV detector. Finally, the optimized extraction factors were obtained 85 % aqueous ethanol; solid: solvent portion, 1:40 g/mL; particle size of 0.18 mm; for both microwave and ultrasound extraction methods. The maximum yield of cinnamic acid and cinnamaldehyde in microwave extraction were gained 3.9 and 49.4 mg/g, resp. Both advanced extraction techniques with our obtained optimized conditions are suggested for cinnamon bark.

Process Biochemistry (Oxford, United Kingdom) 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

Cherian, Joseph published the artcileStructure-Activity Relationship Studies of Mitogen Activated Protein Kinase Interacting Kinase (MNK) 1 and 2 and BCR-ABL1 Inhibitors Targeting Chronic Myeloid Leukemic Cells, Synthetic Route of 947533-21-3, the publication is Journal of Medicinal Chemistry (2016), 59(7), 3063-3078, database is CAplus and MEDLINE.

Clin. used BCR-ABL1 inhibitors for the treatment of chronic myeloid leukemia do not eliminate leukemic stem cells (LSC). It has been shown that MNK1 and 2 inhibitors prevent phosphorylation of eIF4E and eliminate the self-renewal capacity of LSCs. Herein, the authors describe the identification of novel dual MNK1 and 2 and BCR-ABL1 inhibitors, starting from the known kinase inhibitor. Initial structure-activity relationship studies resulted in a compound with loss of BCR-ABL1 inhibition. Further modification led to orally bioavailable dual MNK1 and 2 and BCR-ABL1 inhibitors I and II, which are efficacious in a mouse xenograft model and also reduce the level of phosphorylated eukaryotic translation initiation factor 4E in the tumor tissues. Kinase selectivity of these compounds is also presented.

Journal of Medicinal Chemistry published new progress about 947533-21-3. 947533-21-3 belongs to amides-buliding-blocks, auxiliary class Pyridine,Boronic acid and ester,Amine,Amide,Boronic Acids,Boronic Acids,Boronic acid and ester,, name is (6-Acetamidopyridin-3-yl)boronic acid, and the molecular formula is C7H9BN2O3, Synthetic Route of 947533-21-3.

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

Kaesnaenen, Heikki published the artcile3-Heterocycle-Phenyl N-Alkylcarbamates as FAAH Inhibitors: Design, Synthesis and 3D-QSAR Studies, Product Details of C8H9NOS, the publication is ChemMedChem (2010), 5(2), 213-231, database is CAplus and MEDLINE.

Carbamates are a well-established class of fatty acid amide hydrolase (FAAH) inhibitors. Herein is described the synthesis of meta-substituted phenolic N-alkyl/aryl carbamates and their in vitro FAAH inhibitory activities. The most potent compound, 3-(oxazol-2-yl)phenyl cyclohexylcarbamate (I), inhibited FAAH with a sub-nanomolar IC₅₀ value (IC₅₀=0.74 nM). Addnl., three-dimensional quant. structure-activity relationships (QSAR) models of FAAH inhibition were developed and validated combining the newly disclosed carbamates with previously published inhibitors to give a total set of 99 compounds Prior to 3D-QSAR modeling, the degree of correlation between FAAH inhibition and in silico reactivity was also established. Both 3D-QSAR methods used, CoMSIA and GRID/GOLPE, produced statistically significant models with coefficient of correlation for external prediction (R²_PRED) values of 0.732 and 0.760, resp. These models could be of high value in further FAAH inhibitor design.

ChemMedChem published new progress about 64559-06-4. 64559-06-4 belongs to amides-buliding-blocks, auxiliary class Amine,Benzene,Amide,Ether, name is 3-Methoxybenzothioamide, and the molecular formula is C8H9NOS, Product Details of C8H9NOS.

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

Moccia, Maria published the artcilePreliminary studies on noncovalent hyperbranched polymers based on PNA and DNA building blocks, Computed Properties of 186046-83-3, the publication is Journal of Peptide Science (2009), 15(10), 647-653, database is CAplus and MEDLINE.

In this work, the authors report thermodn., kinetic, and microrheol. studies relative to the formation of PNA- and PNA/DNA-based noncovalent polymeric systems, useful tools for biotechnol. and bioengineering applications. The authors realized two kinds of systems: a PNA-based system formed by a self-assembling PNA tridendron, and a PNA/DNA hybrid system formed by a PNA tridendron and a DNA linker. The formation of a three-dimensional polymeric network, by specific Watson-Crick base pairing, was investigated by a detailed UV and CD spectroscopic study. Preliminary microrheol. experiments were performed on both systems to evaluate their viscoelastic properties which resulted in agreement with the formation of soluble hyperbranched polymers that could be useful for drug/gene delivery, as well as for encapsulating organic pollutants of different shapes and sizes in environmental applications. Copyright © 2009 European Peptide Society and John Wiley & Sons, Ltd.

Journal of Peptide Science 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, Computed Properties of 186046-83-3.

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

Guo, Hui published the artcileHydrogels with Dual Thermoresponsive Mechanical Performance, Category: amides-buliding-blocks, the publication is Macromolecular Rapid Communications (2017), 38(17), n/a, database is CAplus and MEDLINE.

Dual thermoresponsive chem. hydrogels, combining poly(N-isopropylacrylamide) side-chains within a poly(N-acryloylglycinamide) network, are designed following a simple and versatile procedure. These hydrogels exhibit two phase transitions both at low (upper critical solution temperature) and high (lower critical solution temperature) temperatures, thereby modifying their swelling, rheol., and mech. properties. These novel thermo-schizophrenic hydrogels pave the way for the development of thermotoughening wet materials in a broad range of temperatures

Macromolecular Rapid Communications published new progress about 2479-62-1. 2479-62-1 belongs to amides-buliding-blocks, auxiliary class Monomers,Acrylamide Monomers, name is N-(2-Amino-2-oxoethyl)acrylamide, and the molecular formula is C5H8N2O2, Category: amides-buliding-blocks.

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

Muzika, Michael published the artcileChemically-defined lactose-based autoinduction medium for site-specific incorporation of non-canonical amino acids into proteins, HPLC of Formula: 2418-95-3, the publication is RSC Advances (2018), 8(45), 25558-25567, database is CAplus and MEDLINE.

Genetic code expansion technol. enables the site-specific incorporation of dozens of non-canonical amino acids (NCAAs) into proteins expressed in live cells. The NCAAs can introduce various chem. functionalities into proteins, ranging from natural post-translational modifications, to spectroscopic probes and chem. handles for bioorthogonal reactions. These chem. groups provide powerful tools for structural, biochem., and biophys. studies, which may require significant quantities of recombinantly expressed proteins. NCAAs are usually encoded by an in-frame stop codon, such as the TAG (amber) stop codon, which leads to the expression of C-terminally truncated proteins. In addition, the incubation medium should be supplemented with the NCAA at a final concentration of 1-10 mM, which may be challenging when the availability of the NCAA is limited. Hence, bacterial expression of proteins carrying NCAAs can benefit from improvement in protein yield per given amount of added NCAA. Here, we demonstrate the applicability of an optimized chem.-defined lactose-based autoinduction (AI) medium to the expression of proteins carrying a NCAA, using the archaeal pyrrolysyl-tRNA synthetase/tRNA pair from the Methanosarcina genus. Per given amount of added NCAA, the use of AI medium improved protein expression levels by up to 3-fold, compared to IPTG induction, without an increase in misincorporation of canonical amino acids in response to the in-frame stop codon. The suggested medium composition can be used with various Escherichia coli variants transformed with different expression vectors and incubated at different temperatures

RSC Advances 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, HPLC of Formula: 2418-95-3.

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