Month: October 2022

Asano, Toru; Yoshikawa, Tomohiro; Nakamura, Hiroyuki; Uehara, Yoshimasa; Yamamoto, Yoshinori published the artcile< Synthesis and biological evaluation of benzamides and benzamidines: structural requirement of a pyrimidine ring for inhibition of EGFR tyrosine kinase>, HPLC of Formula: 5004-88-6, the main research area is benzamide benzamidine preparation epidermal growth factor receptor tyrosine kinase.

The benzamides I (R = cyclohexyl, 3-BrC6H4, 2-pyridyl, etc.) benzamidines II (R1 = 3-BrC6H4, 3-ClC6H4, 3-MeOC6H4, 3-chloro-4-fluorophenyl), and protected benzamidines (III, same R1) were synthesized as the mimics of 4-anilinoquinazolines, which possess inhibition of epidermal growth factor receptor (EGFR) tyrosine kinase, and were tested for cytotoxicity toward A431 and inhibitory activity toward autophosphorylation by the enzyme assay. High cell growth inhibition was observed in a series of the cyclic benzamides III: the IC50 values are 0.09-0.32 mM. The benzamidines III (R1 = 3-BrC6H4, 3-ClC6H4) exhibited high inhibition of EGFR tyrosine kinase at a 1.0 μM concentration, although the benzamides I and the benzamidines II did not show significant kinase inhibition at a 10 μM concentration

Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, HPLC of Formula: 5004-88-6.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Pant, Amar D.; Ruhela, R.; Limje, C.; Anil Kumar, S.; Singh, A. K.; Kumar, Suja A.; Sugandhi, S.; Kain, V.; Tomar, B. S. published the artcile< Evaluation of BenzoDODA grafted polymeric resin for rapid and reliable assaying of plutonium in sediment samples>, Category: amides-buliding-blocks, the main research area is plutonium BenzoDODA grafted polymeric resin sediment pollution; Alpha spectrometry; BenzoDODA grafted resin; Extraction chromatography; Plutonium; SPEC; Sediments.

The paper reports a new rapid radioanal. procedure for the determination of plutonium (Pu) in sediments by solid phase extraction chromatog. (SPEC) using Bis-(2-ethylhexyl) carbamoyl methoxy phenoxy-bis-(2-ethylhexyl) grafted resin, abbreviated as Benzodioxodiamide (BenzoDODA) grafted resin. The resin was synthesized and evaluated for its sorption behavior towards Pu in batch and column mode to determine its efficacy for selective recovery of Pu from sediment samples. The anal. procedure was based on the radiochem. separation of samples by acid digestion, followed by preconcentration of actinides by co-precipitation with Fe(OH)3 and finally selective recovery of Pu by SPEC using a column filled with BenzoDODA grafted resin. Pu was then radiometrically assayed by preparing alpha disk sources with electro-deposition followed by alpha spectrometry. The method was further validated with IAEA reference materials. This method gives reliable and reproducible results for the activity concentration of Pu in sediment samples within 24 h.

Journal of Environmental Radioactivity published new progress about Acid digestion. 5326-82-9 belongs to class amides-buliding-blocks, and the molecular formula is C10H20ClNO, Category: amides-buliding-blocks.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Zhao, Yichao; Bruce, Lachlan David; Jin, Jianwen; Xia, Bo; Chan, Philip Wai Hong published the artcile< Copper catalyzed N-formylation of α-silyl-substituted tertiary N-alkylamines by air>, HPLC of Formula: 6280-57-5, the main research area is dialkylaminomethyl trimethylsilane copper catalyst formylation; dialkyl formylamine preparation.

A site-selective method to prepare N-formyl amines efficiently that relies on the copper(I)-catalyzed oxidation of α-silyl-substituted tertiary N-alkylamines by air at room temperature was described. The oxidative protocol was shown to exhibited excellent functional group tolerance as it was applicable to a wide variety of amine substrates and a number of bioactive mols. and natural products. Moreover, it delinates a ligand- and additive-free amine oxidation process mediated by a low-cost metal salt with oxygen from air taking on the role of both the terminal oxidant and as part of the formylation reagent, which was unprecedented in copper catalysis. It also offered the first synthetic method that can selectively generate α-amino radical species as reactive intermediates from α-silylamines under non-photochem. reaction conditions.

Green Chemistry published new progress about Formamides Role: SPN (Synthetic Preparation), PREP (Preparation) (N,N-dialkyl). 6280-57-5 belongs to class amides-buliding-blocks, and the molecular formula is C17H35NO, HPLC of Formula: 6280-57-5.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Singh, Shashi Kala; Yende, Ashutosh S.; Ponnusamy, Kalaiarasan; Tyagi, Rakesh K. published the artcile< A comprehensive evaluation of anti-diabetic drugs on nuclear receptor PXR platform>, Electric Literature of 94-20-2, the main research area is antidiabetic drug screening PXR; Anti-diabetic drugs; Drug screening; Promoter-reporter; Small molecules; Stable cell line.

Pregnane & Xenobiotic Receptor (PXR), one of the members of nuclear receptor superfamily, acts as a ‘master-regulator’ of drug metabolism and disposition machinery (DMD). Activation of PXR enables detoxification and elimination of toxic xenobiotics/endobiotics, and defends the authors’ body against chem. insults. On the contrary, PXR activation also imposes a serious concern for drug-drug interactions (DDIs). Such DDIs could either decrease the efficacy or lead to accumulation of co-administered drugs at toxic level. Therefore, it is desirable that during drug development process the small drug mols. are screened on PXR-platform prior to their clin. trial and prevent late stage failures. In view of this, the authors have selected a group of anti-diabetic drug mols. to examine if the success and potential failure of small mol. modulators can be pre-assessed and judiciously correlated on PXR platform. For this purpose, the authors have examined the PXR activation potential of the selected anti-diabetic drugs. Subsequent to screening of these anti-diabetic drugs, the authors elaborated the study further with rosiglitazone and pioglitazone (thiazolidinediones, TZDs) which are oral anti-diabetic formulations and have been in controversy owing to their association with cardiotoxicity and bladder cancer resp. The authors’ study revealed that some of the selected anti-diabetic drugs possess PXR activation potential, implying that these can up-regulate the expression of CYP3A4, UGT1A1, MDR1 and thereby can be predicted to inflict undesirable consequences.

Toxicology In Vitro published new progress about Animal cell line (HepXREM). 94-20-2 belongs to class amides-buliding-blocks, and the molecular formula is C10H13ClN2O3S, Electric Literature of 94-20-2.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Jolley, Katherine E.; Zanotti-Gerosa, Antonio; Hancock, Fred; Dyke, Alan; Grainger, Damian M.; Medlock, Jonathan A.; Nedden, Hans G.; Le Paih, Jacques J. M.; Roseblade, Stephen J.; Seger, Andreas; Sivakumar, Vilvanathan; Prokes, Ivan; Morris, David J.; Wills, Martin published the artcile< Application of Tethered Ruthenium Catalysts to Asymmetric Hydrogenation of Ketones, and the Selective Hydrogenation of Aldehydes>, Quality Control of 1192620-83-9, the main research area is tethered ruthenium catalyst preparation asym hydrogenation ketone aldehyde; sulfonyldiaminoalkyl ruthenium tethered preparation catalyst asym hydrogenation aldehyde ketone.

An improved method for the synthesis of tethered ruthenium(II) complexes of monosulfonylated diamines is described, together with their application to the hydrogenation of ketones and aldehydes. The complexes were applied directly, in their chloride form, to asym. ketone hydrogenation, to give products in excess of 99% ee in the best cases, using 30 bar of hydrogen at 60°, and to the selective reduction of aldehydes over other functional groups.

Advanced Synthesis & Catalysis published new progress about Aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 1192620-83-9 belongs to class amides-buliding-blocks, and the molecular formula is C30H31ClN2O2RuS, Quality Control of 1192620-83-9.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Singh, Y; Gupta, G; Anand, K; Kumar Jha, N; Thangavelu, L; Kumar Chellappan, D; Dua, K published the artcile< Molecular exploration of combinational therapy of orlistat with metformin prevents the COVID-19 consequences in obese diabetic patients.>, Safety of (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate, the main research area is .

There is no abstract available for this document.

European review for medical and pharmacological sciences published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Safety of (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Polyzos, Stergios A; Goulis, Dimitrios G; Giouleme, Olga; Germanidis, Georgios S; Goulas, Antonis published the artcile< Anti-obesity Medications for the Management of Nonalcoholic Fatty Liver Disease.>, Safety of (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate, the main research area is Glucagon-like peptide-1 analog; Nonalcoholic fatty liver disease; Nonalcoholic steatohepatitis; Obesity; Orlistat; Sodium-glucose cotransporter-2 inhibitor.

PURPOSE OF REVIEW: Obesity is closely associated with nonalcoholic fatty liver disease (NAFLD), a highly prevalent disease without any approved medication. The aim of this review was to summarize the evidence on the effect of anti-obesity medications on NAFLD, especially focusing on hepatic histology. RECENT FINDINGS: Orlistat and some glucagon-like peptide-1 receptor analogs, including liraglutide and semaglutide, have beneficial effects on hepatic steatosis and inflammation, but not fibrosis. Other anti-obesity medications, including lorcaserin, setmelanotide, phentermine hydrochloric, phentermine/topiramate, and naltrexone/bupropion, have been minimally investigated in NAFLD. Furthermore, medications like sodium-glucose cotransporter-2 inhibitors and farnesoid X receptor have shown beneficial effects in both NAFLD and obesity, but they have not been licensed for either disease. Liraglutide, semaglutide, and orlistat may be currently used in selected patients with obesity and NAFLD. Further research is warranted, since targeting obesity may provide additional benefits on its comorbidities, including NAFLD.

Current obesity reports published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Safety of (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Mazhar, Faizan; Pozzi, Marco; Gentili, Marta; Scatigna, Marco; Clementi, Emilio; Radice, Sonia; Carnovale, Carla published the artcile< Association of Hyponatraemia and Antidepressant Drugs: A Pharmacovigilance-Pharmacodynamic Assessment Through an Analysis of the US Food and Drug Administration Adverse Event Reporting System (FAERS) Database>, Product Details of C10H13ClN2O3S, the main research area is mirtazapine vortioxetine antidepressant pharmacodynamics pharmacovigilance hyponatremia.

Background: Hyponatremia induced by antidepressant drugs is a rare but potentially life-threatening adverse reaction. Whether it is associated with all or only some antidepressant drugs is still unclear. This needs to be clarified to guide antidepressant therapies, especially in patients with electrolytic imbalances. Objectives: The primary objective of this study was to quantify the strength of association between the use of different antidepressant drugs and hyponatremia by using information reported to the US Food and Drug Administration (FDA) Adverse Event Reporting System (FAERS). The secondary objective was to investigate the putative relationship between different antidepressant pharmacol. targets and the risks of hyponatremia induced by antidepressant drugs using the ′pharmacovigilance-pharmacodynamic′ method. Methods: We used the FAERS database to conduct a case/non-case anal. on spontaneous reports, focusing on events of hyponatremia/syndrome of inappropriate antidiuretic hormone secretion (SIADH) reported in connection with the use of antidepressant drugs. Risk was expressed as a measure of disproportionality using the reporting odds ratio while adjusting for sex, age and concomitant medications associated with hyponatremia/SIADH. We assessed to what extent the receptor-binding properties of antidepressant drugs could associate with the reporting odds ratios of hyponatremia/SIADH of antidepressant drugs, building a linear regression model that included as independent variables the binding affinities (pKi) to the serotonin transporter, dopamine transporter, norepinephrine transporter, and serotonin 5-HT2C, 5-HT2A and 5-HT1A, and α1- and α2-adrenergic receptors. Results: There were 2233 reports identified. The adjusted reporting odds ratio for the association between antidepressant drug use and hyponatremia was 1.91 (95% confidence interval 1.83-2.00). The association was strongest for mirtazapine, followed by selective serotonin reuptake inhibitors, and lowest with serotonin-modulating antidepressant drugs. A significant linear correlation was found between the adjusted reporting odds ratios for hyponatremia and pKi for the adrenergic receptors α1 and α2. Conclusions: Hyponatremia is reported at a disproportionately higher level with classes of antidepressant drugs (noradrenergic and specific serotonergic antidepressant [mirtazapine] and serotonin modulators [vortioxetine]) that are in general considered to have a better profile of tolerability in terms of hyponatremia. With regard to the presented results, the risk of hyponatremia with mirtazapine appears to be greater than what was reported in the literature; however, confounding by indication cannot be ruled out. Our pharmacovigilance-pharmacodynamic anal. also indicates that inhibition of the serotonin transporter may not be involved in the hyponatremia linked to the use of antidepressant drugs.

CNS Drugs published new progress about 5-HT reuptake inhibitors Role: THU (Therapeutic Use), BIOL (Biological Study), USES (Uses). 94-20-2 belongs to class amides-buliding-blocks, and the molecular formula is C10H13ClN2O3S, Product Details of C10H13ClN2O3S.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Shueng, Pei-Wei; Chan, Hui-Wen; Lin, Wei-Chan; Kuo, Deng-Yu; Chuang, Hui-Yen published the artcile< Orlistat Resensitizes Sorafenib-Resistance in Hepatocellular Carcinoma Cells through Modulating Metabolism>, Application In Synthesis of 96829-58-2, the main research area is fatty acid synthase; hepatocellular carcinoma; metabolism; sorafenib resistance.

Sorafenib is one of the options for advanced hepatocellular carcinoma treatment and has been shown to extend median overall survival. However, sorafenib resistance often develops a few months after treatment. Hence, developing various strategies to overcome sorafenib resistance and understand the possible mechanisms is urgently needed. We first established sorafenib-resistant hepatocellular carcinoma (HCC) cells. Then, we found that sorafenib-resistant Huh7 cells (Huh7/SR) exhibit higher glucose uptakes and express elevated fatty acid synthesis and glucose metabolism-related proteins than their parental counterparts (Huh7). The current study investigated whether sorafenib resistance could be reversed by suppressing fatty acid synthesis, using a fatty acid synthase (FASN) inhibitor, orlistat, in HCC cells. FASN inhibition-caused changes in protein expressions and cell cycle distribution were analyzed by Western blot and flow cytometry, and changes in glucose uptakes were also evaluated by 18F-FDG uptake. Orlistat remarkably enhanced the cytotoxicity of sorafenib in both Huh7 and Huh7/SR cells, and flow cytometry showed that combination treatment significantly increased the sub-G1 population in both cell lines. Western blot revealed that the combination treatment effectively increased the ratio of Bax/Bcl-2 and decreased expressions of pERK; addnl., the combination treatment also strongly suppressed fatty acid synthesis-related proteins (e.g., FASN and SCD) in both cell lines. Lastly, the 18F-FDG uptake was repressed by the combination treatment in both cell lines. Our results indicated that orlistat-mediated FASN inhibition could overcome sorafenib resistance and enhance cell killing in HCC by changing cell metabolism

International Journal of Molecular Sciences published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Application In Synthesis of 96829-58-2.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Wang, Lei; Riel, Louis P.; Bajrami, Bekim; Deng, Bin; Howell, Amy R.; Yao, Xudong published the artcile< α-Methylene-β-Lactone Scaffold for Developing Chemical Probes at the Two Ends of the Selectivity Spectrum>, Computed Properties of 96829-58-2, the main research area is chemical proteomics; glutathione S-transferase; methylenelactone; orlistat; parthenolide.

The utilities of an α-methylene-β-lactone (MeLac) moiety as a warhead composed of multiple electrophilic sites are reported. We demonstrate that a MeLac-alkyne not only reacts with diverse proteins as a broadly reactive measurement probe, but also recruits reduced endogenous glutathione (GSH) to assemble a selective chemical probe of GSH-β-lactone (GSH-Lac)-alkyne in live cells. Tandem mass spectrometry reveals that MeLac reacts with nucleophilic cysteine, serine, lysine, threonine, and tyrosine residues, through either Michael or acyl addition. A peptide-centric proteomics platform demonstrates that the proteomic selectivity profiles of orlistat and parthenolide, which have distinct reactivities, are measurable by MeLac-alkyne as a high-coverage probe. The GSH-Lac-alkyne selectively probes the glutathione S-transferase P responsible for multidrug resistance. The assembly of the GSH-Lac probe exemplifies a modular and scalable route to develop selective probes with different recognizing moieties.

ChemBioChem published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Computed Properties of 96829-58-2.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics