Tag: M.W=250-300

Mannucci, Edoardo; Monami, Matteo; Candido, Riccardo; Pintaudi, Basilio; Targher, Giovanni published the artcile< Effect of insulin secretagogues A meta-analysis of randomized controlled trials>, Application In Synthesis of 94-20-2, the main research area is meta analysis cardiovascular disease mortality insulin secretagogues; Insulin secretagogues; Major cardiovascular events; Metanalysis; Mortality; Type 2 diabetes.

Meta-anal. of insulin secretagogues (sulfonylureas and glinides) on major cardiovascular events and all-cause mortality. A MEDLINE database search was performed to identify all RCTs, up to Jan. 1st, 2020, with duration≥52 wk, in which insulin secretagogues (glibenclamide, gliclazide, glimepiride, glipizide, chlorpropamide, repaglinide, nateglinide) were compared with either placebo or active comparators. The principal endpoints were MACE (restricted for RCT reporting MACEs within their outcomes) and all-cause mortality (irresp. of the inclusion of MACEs among the pre-specified outcomes). Mantel-Haenszel odds ratio (MH-OR) with 95% Confidence Interval (95% CI) was calculated for all the endpoints considered. Fourteen RCTs were included in the anal. for MACEs (919 in insulin secretagogues and 1,087 in control group). Insulin secretagogues were not significantly associated with an increased risk of MACEs in comparison with controls (MH-OR 1.08 [95% CI 0.96, 1.22], p = 0.20). When considering the 48 RCTs fulfilling criteria for inclusion in the anal. on all-cause mortality, insulin secretagogues were associated with a significantly increased risk of all-cause mortality (MH-OR 1.11 [1.00, 1.23], p = 0.04).This meta-anal. suggests that insulin secretagogues are associated with an increased risk of all-cause mortality when compared with placebo or other anti-hyperglycemic drugs.

Nutrition, Metabolism & Cardiovascular Diseases published new progress about Cardiovascular disease. 94-20-2 belongs to class amides-buliding-blocks, and the molecular formula is C10H13ClN2O3S, Application In Synthesis of 94-20-2.

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

Lin, Kai-Huang; Luo, Ci-Wen; Chen, Shih-Pin; Tu, Dom-Gene; Lin, Ming-Shian; Kuan, Yu-Hsiang published the artcile< Inhibitor of α-glucosidase can effectively inhibit therisk of tuberculosis in patients with diabetes: a nestedcase-control study>, Computed Properties of 94-20-2, the main research area is alpha glucosidase inhibitor antituberculosis antidiabetic agent tuberculosis diabetes.

Diabetes mellitus (DM) and tuberculosis (TB) are major public health and economic burdens. DM increases Mycobacterium tuberculosis infection rates and treatment durations. This study evaluated the relationship between five classes of oral DM medications and TB infection risk in DM patients. We used longitudinal records from the Taiwan Longitudinal Health Insurance Research Database. DM patients were identified using the International Classification of Diseases. TB patients were identified. Oral DM medications were divided into five classes: sulfonylureas, biguanides, meglitinides, α-glucosidase inhibitors (AGIs), and thiazolidinediones. Users were classified as nonusers, low-concentration users, and high-concentration users. The incidence rate ratio (IRR) was derived using multivariate Poisson regression to calculate the relative risk of TB infection. DM patients using low- and high-concentration AGIs had significantly lower TB infection risks compared with nonusers. The IRRs of the sulfonylureas and AGI users were (CI 0.693-0.948) and (95% CI 0.651-0.995), resp. The other four classes of medications exhibited no significant effect on TB infection risk in DM patients. Furthermore, DM patients using highconcn. AGIs had a significantly lower TB infection risk compared with those using low-concentration AGIs (IRR 0.918, 95% CI: 0.854-0.987). We noted a dose-response relationship in the effects of DM medications on TB risk. Accordingly, we suggest that DM patients use AGIs to benefit from their protective effect on TB infection risk.

BioMed Research International published new progress about Antidiabetic agents. 94-20-2 belongs to class amides-buliding-blocks, and the molecular formula is C10H13ClN2O3S, Computed Properties of 94-20-2.

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

Sakthi, G. published the artcile< Contradictory opinion of the Terminalia chebula linn. -literature review>, SDS of cas: 94-20-2, the main research area is review Terminalia chebula drug interaction toxicity.

A review. Terminalia chebula is used as common and effective herb in traditional, Siddha & Ayurvedic medicine as Indian Medicine. In siddha medical system know as “”Mother of Herb”” is mentioned in manuscripts texts. In this research paper objected as enumerate the side effect or toxicity effect from Gall Nut or safe drug for all by searching the literatures in books and articles. Finally concluded by collected data results as; continuous drug period of intake for up to 3 mo. And drug interactions reported as; Taking Terminalia along with diabetes medications might cause your blood sugar to go too low. In toxicity studies shows as; In the acute phase of the study, the safe dose was ≤5000 mg/kg for both extracts In sub- acute phase, LD50 (95% CI) of Terminalia chebula extract 2754.436 (2438-3114) mg/kg. The highest dose of T. chebula extract induced few histopathol. changes.

European Journal of Biomedical and Pharmaceutical Sciences published new progress about Diabetes mellitus. 94-20-2 belongs to class amides-buliding-blocks, and the molecular formula is C10H13ClN2O3S, SDS of cas: 94-20-2.

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

Irigoyen, Sonia; Ramasamy, Manikandan; Pant, Shankar; Niraula, Prakash; Bedre, Renesh; Gurung, Meena; Rossi, Denise; Laughlin, Corinne; Gorman, Zachary; Achor, Diann; Levy, Amit; Kolomiets, Michael V.; Setamou, Mamoudou; Badillo-Vargas, Ismael E.; Avila, Carlos A.; Irey, Michael S.; Mandadi, Kranthi K. published the artcile< Plant hairy roots enable high throughput identification of antimicrobials against Candidatus Liberibacter spp.>, Electric Literature of 94-20-2, the main research area is antimicrobial hairy root disease Candidatus.

A major bottleneck in identifying therapies to control citrus greening and other devastating plant diseases caused by fastidious pathogens is our inability to culture the pathogens in defined media or axenic cultures. As such, conventional approaches for antimicrobial evaluation (genetic or chem.) rely on time-consuming, low-throughput and inherently variable whole-plant assays. Here, we report that plant hairy roots support the growth of fastidious pathogens like Candidatus Liberibacter spp., the presumptive causal agents of citrus greening, potato zebra chip and tomato vein greening diseases. Importantly, we leverage the microbial hairy roots for rapid, reproducible efficacy screening of multiple therapies. We identify six antimicrobial peptides, two plant immune regulators and eight chems. which inhibit Candidatus Liberibacter spp. in plant tissues. The antimicrobials, either singly or in combination, can be used as near- and long-term therapies to control citrus greening, potato zebra chip and tomato vein greening diseases.

Nature Communications published new progress about Antimicrobial agents. 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

Abraham, Nathan S.; Shirts, Michael R. published the artcile< Adding Anisotropy to the Standard Quasi-Harmonic Approximation Still Fails in Several Ways to Capture Organic Crystal Thermodynamics>, Electric Literature of 94-20-2, the main research area is organic crystal thermodn quasi harmonic approximation anisotropy.

We evaluate the accuracy of varying thermal expansion models for the quasi-harmonic approximation (QHA) relative to mol. dynamics (MD) for 10 sets of enantiotropic organic polymorphs. Relative to experiment we find that MD, using an off-the-shelf point charge potential, gets the sign of the enthalpic contributions correct for 6 of the 10 pairs of polymorphs and the sign of the entropic contributions correct for all pairs. We find that anisotropic QHA provides little improvement to the error in free energy differences from MD relative to isotropic QHA, but does a better job capturing the thermal expansion of the crystals. A form of entropy-enthalpy compensation allows the free energy differences of QHA to deviate less than 0.1 kcal/mol from MD for most polymorphic pairs, despite errors up to 0.4 kcal/mol in the entropy and enthalpy. Deviations in the free energy of QHA and MD do not clearly correlate with mol. flexibility, clarifying a previously published finding. Much of the error previously found between QHA and MD for these flexible mols. is reduced when QHA is run from a lattice min. consistent with the same basin as MD, rather than the energy-minimized exptl. crystal structure. Specifically, performing anisotropic QHA on lattice min. quenched from low-temperature replica exchange simulations reduced the error previously found by 0.2 kcal/mol on average However, these conformationally flexible mols. can have many low-temperature conformational min., and the choice of an inconsistent min. causes free energies estimated from QHA to deviate from MD at temperatures as low as 10 K. We also find finite size errors in the polymorph free energy differences using anisotropic QHA, with free energy differences as large as 0.5 kcal/mol between unit and supercells loosely correlated with differences in anisotropic thermal expansion. These larger system sizes are computationally more accessible using our cheaper 1D variant of anisotropic QHA, which gives free energies within 0.02 kcal/mol of the fully anisotropic approach at all temperatures studied. The errors between MD and experiment are 1-2 orders of magnitude larger than those seen between QHA and MD, so the quality of the force field used is still of primary concern, but this study illustrates a number of other important factors that must be considered to obtain quant. organic crystal thermodn. We examine how much of the difference between the quasiharmonic approximation (QHA) and mol. dynamics (MD) is due to anisotropic expansion for 10 enantiotropic sets of polymorphs. Although consistent free energies with QHA are dependent on finding the lattice min. corresponding to the model, differences between methods are relatively small compared the differences from experiment due to choice of model.

Crystal Growth & Design published new progress about Anisotropy. 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

Sarraguca, Mafalda C.; Ribeiro, Paulo R. S.; Nunes, Claudia; Seabra, Catarina Leal published the artcile< Solids Turn into Liquids-Liquid Eutectic Systems of Pharmaceutics to Improve Drug Solubility>, Recommanded Product: 4-Chloro-N-(propylcarbamoyl)benzenesulfonamide, the main research area is chlorpropamide tolbutamide therapeutic liquid eutectic system solubility diabetes; chlorpropamide; diabetes; eutectic systems; green chemistry; solubility; therapeutic liquid eutectic systems; tolbutamide.

The low solubility of active pharmaceutical ingredients (APIs) is a problem in pharmaceutical development. Several methodologies can be used to improve API solubility, including the use of eutectic systems in which one of the constituents is the API. This class of compounds is commonly called Therapeutic Deep Eutectic Systems (THEDES). THEDES has been gaining attention due to their properties such as non-toxicity, biodegradability, and being non-expensive and easy to prepare Since the knowledge of the solid liquid diagram of the mixture and the ideal eutectic point is necessary to ascertain if a mixture is a deep eutectic or just a eutectic mixture that is liquid at ambient temperature, the systems studied in this work are called Therapeutic Liquid Eutectic Systems (THELES). Therefore, the strategy proposed in this work is to improve the solubility of chlorpropamide and tolbutamide by preparing THELES. Both APIs are sulfonylurea compounds used for the treatment of type 2 diabetes mellitus and have low solubility in water. To prepare the THELES, several coformers were tested, namely, tromethamine, L(+)-arginine, L-tryptophan, citric acid, malic acid, ascorbic acid, and p-aminobenzoic acid, in molar ratios of 1:1 and 1:2. To improve viscosity, water was added in different molar ratios to all systems. THELES were characterized by mid-IR spectroscopy (MIR), and differential scanning calorimetry. Their viscosity, solubility, and permeability were also determined Their stability at room temperature and 40°C was accessed by MIR. Cytocompatibility was performed by metabolic activity and cell lysis evaluation, according to ISO10993-5:2009, and compared with the crystalline APIs. THELES with TRIS were successfully synthesized for both APIs. Results showed an increased solubility without a decrease in the permeability of the APIs in the THELES when compared with the pure APIs. The THELES were also considered stable for 8 wk at ambient temperature The cells studied showed that the THELES were not toxic for the cell lines used.

Pharmaceuticals published new progress about Biocompatibility, cytocompatibility. 94-20-2 belongs to class amides-buliding-blocks, and the molecular formula is C10H13ClN2O3S, Recommanded Product: 4-Chloro-N-(propylcarbamoyl)benzenesulfonamide.

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

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