Category: amides-buliding-blocks

Raffa, Demetrio; Maggio, Benedetta; Plescia, Fabiana; Cascioferro, Stella; Raimondi, Maria Valeria; Cancemi, Gabriella; D’Anneo, Antonella; Lauricella, Marianna; Cusimano, Maria Grazia; Bai, Ruoli; Hamel, Ernest; Daidone, Giuseppe published the artcile< Synthesis, antiproliferative activity and possible mechanism of action of novel 2-acetamidobenzamides bearing the 2-phenoxy functionality>, Formula: C9H12N2O3, the main research area is preparation acetamido benzamide derivative cancer; 2-(2-Phenoxyacetamido)benzamides; Antiproliferative activity; Apoptosis; G0/G1 arrest; Pro-caspase 3.

Several new 2-(2-phenoxyacetamido)benzamides 17a-v, 21 and 22 were synthesized by stirring in pyridine the acid chlorides 16a-e and the appropriate5-R-4-R1-2-aminobenzamide 15a-e and initially evaluated in vitro for antiproliferative activity against the K562 (human chronic myelogenous leukemia) cell line. Some of synthesized compounds were evaluated for their in vitro antiproliferative activity against the full NCI tumor cell line panel derived from nine clin. isolated cancer types (leukemia, non-small cell lung, colon, CNS, melanoma, ovarian, renal, prostate and breast). The most active compounds caused an arrest of K562 cells in the G0-G1 phase of cell cycle and induction of apoptosis, which was mediated by caspase activation.

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

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

Itzhak, Baruch; Home, Philip published the artcile< Heart failure management; a perspective from diabetes care>, HPLC of Formula: 94-20-2, the main research area is human diabetes care heart failure management; Diabetes care; Diabetes mellitus; Glucose-lowering therapy; Heart failure; Prevention and management.

People with type 2 diabetes (T2DM) are recognized as having a 2-4 times increased risk of heart failure (HF). Ambulatory diabetes care has long concentrated on the prevention of microvascular and arterial disease, and surveillance for manageable problems such as with the feet and retinae. Accordingly, management of heart failure has never been a specific focus, although the preventative management of cardiac and kidney disease through glucose-lowering, blood pressure (BP) control, and blood lipid control, have had a pos. impact on its incidence. Indeed, the very complexity of routine diabetes care, and its enormous prevalence, has generally excluded the management of any of the advanced late complications, whether cardiac, arterial, retinal, renal, or neurodegenerative. Furthermore, advances in HF management itself, in diagnostics, medications, and technol., has carried it deeper into the remit of specialist cardiol. care. More recently and in addition to medications already routinely used in diabetes care such as renin-angiotensin system (RAS) blockers, some glucose-lowering therapies such as sodium glucose transporter inhibitors 2 (SGLT-2 inhibitors), have been found to have very pos. effects on hospitalization for HF, indeed even in people who do not have T2DM. Here, from the perspective of the diabetologist, we review the clin. scenario of ambulatory diabetes care, in regard of how HF prevention and management should fit in to clin. practice.

Diabetes Research and Clinical Practice published new progress about Antihypertensives. 94-20-2 belongs to class amides-buliding-blocks, and the molecular formula is C10H13ClN2O3S, HPLC of Formula: 94-20-2.

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

Jin, Pengfei; Xu, Shuo; Xu, Wenfeng; He, Xiaorong; Kuang, Yongmei; Hu, Xin published the artcile< Screening and quantification of fourteen synthetic antidiabetic adulterants in herbal pharmaceuticals and health foods by HPLC and confirmation by LC-Q-TOF-MS/MS>, Formula: C10H13ClN2O3S, the main research area is antidiabetic adulterant herbal pharmaceutical; HPLC; Q-TOF; adulterant; antidiabetic; health food; herbal pharmaceutical.

A procedure was established and fully validated for the screening and quantification of fourteen synthetic antidiabetic adulterants in herbal pharmaceuticals and health foods, including metformin (MF), buformin (BF), phenformin (PHF), rosiglitazone (RGZ), pioglitazone (PGZ), chlorpropamide (CPM), glipizide (GPZ), tolbutamide (TBM), gliclazide (GCZ), glibenclamide (GBM), glimepiride (GMR), repaglinide (RGN), gliquidone (GQD) and nateglinide (NGN). The samples were extracted by methanol and separated by HPLC. Retention times and UV spectra were used for the preliminary screening, and the suspected adulterants were then confirmed by liquid chromatog.-quadrupole-time of flight mass spectrometry (LC-Q-TOF-MS/MS) and quantified by HPLC. The developed procedure was successfully applied to assess twenty-four herbal samples, and PHF, GCZ, GBM, MF, GPZ and BF were found in many. To the best of our knowledge, this is the first report of simultaneous screening and quantification of these fourteen synthetic antidiabetic adulterants from any matrix.

Food Additives & Contaminants, Part A published new progress about Drug stability. 94-20-2 belongs to class amides-buliding-blocks, and the molecular formula is C10H13ClN2O3S, Formula: C10H13ClN2O3S.

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

Harapko, Tetiana V; Mateshuk-Vatseba, Lesia R published the artcile< MORPHOMETRIC AND ELECTRON MICROSCOPIC CHANGES OF STRUCTURAL COMPONENTS OF LYMPH NODES DURING CORRECTION OF THE ACTION OF SODIUM GLUTAMATE WITH ORLISTAT.>, HPLC of Formula: 96829-58-2, the main research area is correction; endotheliocyte; lymphocyte ; orlistat ; sodium glutamate.

OBJECTIVE: The aim: To study morphometric and electron microscopic changes in the parenchyma of rat lymph nodes under the action of sodium glutamate and its correction by orlistat. PATIENTS AND METHODS: Materials and methods: The article presents and analyzes the data of an experimental study conducted on 66 white male rats and females of reproductive age. Experimental animals are divided into 4 groups. RESULTS: Results: After six weeks of exposure to monosodium glutamate, there was a significant decrease in the relative area of the cortical substance in the lymph nodes of white male and female rats by 11.95% and 9.31% and, respectively, an increase in the relative area of the medullary substance by 18.76% and 14.7% in compared with an intact group of animals. After six weeks of sodium glutamate and the next six weeks of the standard diet of vivarium and orlistat, the relative area of the cortical substance in the lymph node parenchyma was 2.55% and 0.38% more than the parameters of the intact group of animals, respectively. Accordingly, the relative area of the medullary substance decreased and was 4.01% and 0.59% less compared to the intact group of animals. CONCLUSION: Conclusions: Electron microscopic examination showed that monosodium glutamate causes changes in the parenchyma of the lymph nodes as in a high-calorie diet. The introduction of orlistat (xenical) leads to a partial restoration of the structural organization, and hence the function of this organ.

Wiadomosci lekarskie (Warsaw, Poland : 1960) published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, HPLC of Formula: 96829-58-2.

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

Son, Jang Won; Kim, Sungrae published the artcile< Comprehensive Review of Current and Upcoming Anti-Obesity Drugs.>, Product Details of C29H53NO5, the main research area is Bupropion; Drug therapy; Liraglutide; Naltrexone; Obesity; Orlistat; Phentermine.

Obesity is among the leading causes of morbidity and mortality worldwide and its prevalence continues to increase globally. Because obesity is a chronic, complex, and heterogeneous disease influenced by genetic, developmental, biological, and environmental factors, it is necessary to approach obesity with an integrated and comprehensive treatment strategy. As it is difficult to achieve and sustain successful long-term weight loss in most patients with obesity through lifestyle modifications (e.g., diet, exercise, and behavioral therapy), pharmacological approaches to the treatment of obesity should be considered as an adjunct therapy. Currently, four drugs (orlistat, naltrexone extended-release [ER]/bupropion ER, phentermine/topiramate controlled-release, and liraglutide) can be used long-term (>12 weeks) to promote weight loss by suppressing appetite or decreasing fat absorption. Pharmacotherapy for obesity should be conducted according to a proper assessment of the clinical evidence and customized to individual patients considering the characteristics of each drug and comorbidities associated with obesity. In this review, we discuss the mechanisms of action, efficacy, and safety of these available long-term anti-obesity drugs and introduce other potential agents under investigation. Furthermore, we discuss the need for research on personalized obesity medicine.

Diabetes & metabolism journal published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Product Details of C29H53NO5.

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

Gadzekpo, V. P. Y.; Hungerford, J. M.; Kadry, A. M.; Ibrahim, Y. A.; Xie, R. Y.; Christian, Gary D. published the artcile< Comparative study of neutral carriers in polymeric lithium ion selective electrodes>, Product Details of C10H20ClNO, the main research area is ionophore lithium selective electrode; lipophilic diamide ionophore lithium selective electrode; pyridine diamide ionophore lithium selective electrode; furan diamide ionophore lithium selective electrode; dioxanonane diamide ionophore lithium selective electrode; polyether diamide ionophore lithium selective electrode; ether diamide ionophore lithium selective electrode.

New lipophilic diamide compounds were synthesized and tested as ionophores for Li in poly(vinyl chloride) (PVC) membrane electrodes, including compounds with pyridine, furan, dioxanonane, and polyether backbones with different lipophilic diamide groups. The new ionophores were compared with previously reported ionophores under similar measurement conditions with the same plasticizer, tris(2-ethylhexyl) phosphate, in all membranes. Fixed interference and matched potential methods were used to determine relative selectivity coefficients for all the electrodes. The highest selectivity for Li relative to Na was obtained with N,N-dicyclohexyl-N’,N’-diisobutyl-cis-cyclohexane-1,2-dicarboxamide (140:1) and the 14-crown-4 ether, 3-dodecyl-3-methyl-1,5,8,12-tetraoxacyclotetradecane (125:1) when using NPOE (o-nitrophenyl octyl ether) plasticizer. The latter exhibited faster response at low Li concentrations It exhibited consistently high selectivity using different measurement methods and was stable for 5 mo.

Analytical Chemistry published new progress about Diamides. 5326-82-9 belongs to class amides-buliding-blocks, and the molecular formula is C10H20ClNO, Product Details of C10H20ClNO.

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

Dugad, L. B.; Cooley, C. R.; Gerig, J. T. published the artcile< NMR studies of carbonic anhydrase-fluorinated benzenesulfonamide complexes>, Computed Properties of 1524-40-9, the main research area is carbonic anhydrase fluorobenzenesulfonamide complex NMR.

19F NMR was used to examine complexes formed by 2-fluoro-, 3-fluoro-, and 2,5-difluorobenzenesulfonamide and human carbonic anhydrase (CA) isoenzymes I and II. The results showed that all 3 inhibitors formed complexes with both isoenzymes that had 2:1 inhibitor/enzyme stoichiometry. The 19F spectra observed for all inhibitor-isoenzyme combinations were consistent either with rapid rotation of the aromatic ring of the inhibitor in the complexes or with preferential binding of only 1 of the 2 possible conformations of the inhibitors that were isomeric by virtue of rotation about the C1-C4 bond of the fluoro aromatic ring. Because ring rotation is slow in the case of the pentafluorobenzenesulfonamide-CA I complex, selective binding of rotamers is the explanation of these observations presently favored. A computer graphics study showed that formation of 2:1 complexes of CA I is feasible without the appreciable distortion of the protein tertiary structure found in the crystalline state.

Biochemistry published new progress about NMR (nuclear magnetic resonance). 1524-40-9 belongs to class amides-buliding-blocks, and the molecular formula is C6H6FNO2S, Computed Properties of 1524-40-9.

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

Huang, Yazhong; Knouse, Kyle W.; Qiu, Shenjie; Hao, Wei; Padial, Natalia M.; Vantourout, Julien C.; Zheng, Bin; Mercer, Stephen E.; Lopez-Ogalla, Javier; Narayan, Rohan; Olson, Richard E.; Blackmond, Donna G.; Eastgate, Martin D.; Schmidt, Michael A.; McDonald, Ivar M.; Baran, Phil S. published the artcile< A P(V) platform for oligonucleotide synthesis>, Quality Control of 1192620-83-9, the main research area is DNA LNA preparation phosphodiester phosphorodithioate human; crystal structure DNA preparation phosphodiester phosphorodithioate nucleotide polymer.

The promise of gene-based therapies is being realized at an accelerated pace, with more than 155 active clin. trials and multiple U.S. Food and Drug Administration approvals for therapeutic oligonucleotides, by far most of which contain modified phosphate linkages. These unnatural linkages have desirable biol. and phys. properties but are often accessed with difficulty using phosphoramidite chem. We report a flexible and efficient [P(V)]-based platform that can install a wide variety of phosphate linkages at will into oligonucleotides. This approach uses readily accessible reagents and can install not only stereo-defined or racemic thiophosphates but any combination of (S, R or rac)-PS with native phosphodiester (PO2) and phosphorodithioate (PS2) linkages into DNA and other modified nucleotide polymers. This platform easily accesses this diversity under a standardized coupling protocol with prepared and stable P(V) reagents.

Science (Washington, DC, United States) published new progress about Coupling reaction. 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

B, Haripriya; Hasija, Avantika; Cruz-Cabeza, Aurora J.; Shruti, Ipsha; Chopra, Deepak published the artcile< Multicomponent Crystals of Chlorpropamide: Multiple Conformers, Multiple Z', and Proton Transfer at Play>, HPLC of Formula: 94-20-2, the main research area is multicomponent crystal chlorpropamide multiple conformer crystallog.

A new organic salt and a cocrystal of the antidiabetic drug chlorpropamide (cpa) were obtained by mechanochem. liquid-assisted grinding (LAG) with several cocrystal formers. An organic salt was formed with 4-(dimethylamino)pyridine (cpa:DMAP) and a cocrystal was obtained with 4,4′-dipyridyl (cpa:BP). After extensive screening for polymorphism/stoichiomorphism, two polymorphs of the cpa:DMAP salt (Forms I and II) and one form of the cocrystal cpa:BP were discovered. cpa:DMAP-I crystallized with eight mols. in the asym. unit (Z’ = 4, Z” = 8), whereas cpa:DMAP-II crystallized with two mols. in the asym. unit (Z’ = 1, Z” = 2). The new forms were characterized via single-crystal X-ray diffraction and powder X-ray diffraction along with thermal methods of characterization. Addnl., the various conformers found in these multicomponent forms are analyzed and compared to the known polymorphs of cpa. Finally, we show that the stable polymorph of the salt cpa:DMAP-I has a drastically enhanced aqueous solubility and dissolution rate relative to the pure cpa, thus giving it an advantage for improved drug delivery.

Crystal Growth & Design published new progress about Cocrystallization. 94-20-2 belongs to class amides-buliding-blocks, and the molecular formula is C10H13ClN2O3S, HPLC of Formula: 94-20-2.

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

Podtelezhnikov, Alexei A.; Monroe, James J.; Aslamkhan, Amy G.; Pearson, Kara; Qin, Chunhua; Tamburino, Alex M.; Loboda, Andrey P.; Glaab, Warren E.; Sistare, Frank D.; Tanis, Keith Q. published the artcile< Quantitative transcriptional biomarkers of xenobiotic receptor activation in rat liver for the early assessment of drug safety liabilities>, Product Details of C10H13ClN2O3S, the main research area is transcriptional biomarker xenobiotic receptor rat liver drug toxicity safety; biomarkers; gene expression/regulation; liver; methods; receptor; safety evaluation; systems; toxicogenomics; toxicology; transcription factors.

The robust transcriptional plasticity of liver mediated through xenobiotic receptors underlies its ability to respond rapidly and effectively to diverse chem. stressors. Thus, drug-induced gene expression changes in liver serve not only as biomarkers of liver injury, but also as mechanistic sentinels of adaptation in metabolism, detoxification, and tissue protection from chems. Modern RNA sequencing methods offer an unmatched opportunity to quant. monitor these processes in parallel and to contextualize the spectrum of dose-dependent stress, adaptation, protection, and injury responses induced in liver by drug treatments. Using this approach, we profiled the transcriptional changes in rat liver following daily oral administration of 120 different compounds, many of which are known to be associated with clin. risk for drug-induced liver injury by diverse mechanisms. Clustering, correlation, and linear modeling analyses were used to identify and optimize coexpressed gene signatures modulated by drug treatment. Here, we specifically focused on prioritizing 9 key signatures for their pragmatic utility for routine monitoring in initial rat tolerability studies just prior to entering drug development. These signatures are associated with 5 canonical xenobiotic nuclear receptors (AHR, CAR, PXR, PPARα, ER), 3 mediators of reactive metabolite-mediated stress responses (NRF2, NRF1, P53), and 1 liver response following activation of the innate immune response. Comparing paradigm chem. inducers of each receptor to the other compounds surveyed enabled us to identify sets of optimized gene expression panels and associated scoring algorithms proposed as quant. mechanistic biomarkers with high sensitivity, specificity, and quant. accuracy. These findings were further qualified using public datasets, Open TG-GATEs and DrugMatrix, and internal development compounds With broader collaboration and addnl. qualification, the quant. toxicogenomic framework described here could inform candidate selection prior to committing to drug development, as well as complement and provide a deeper understanding of the conventional toxicol. study endpoints used later in drug development.

Toxicological Sciences published new progress about Animal gene Role: BSU (Biological Study, Unclassified), BIOL (Biological Study) (CAR). 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