Tag: M.W=250-300

Baruah, Prayasee; Das, Abhinandan; Paul, Debojit; Chakrabarty, Suman; Aguan, Kripamoy; Mitra, Sivaprasad published the artcile< Sulfonylurea Class of Antidiabetic Drugs Inhibit Acetylcholinesterase Activity: Unexplored Auxiliary Pharmacological Benefit toward Alzheimer's Disease>, SDS of cas: 94-20-2, the main research area is antidiabetic sulfonylurea drugrepurposing AChE inhibitor Alzheimer’s.

Contemporary literature documents extensive research on common causative mechanisms, pathogenic pathways and dual effective remedies for Alzheimer’s disease (AD) and Type 2 diabetes mellitus (T2DM). Tolbutamide (TBM), chlorpropamide (CPM), and glyburide (GLY) are three sulfonylurea antidiabetic drugs of different generations. All these drugs were found to exhibit moderate to strong inhibitory efficiency on the neurotransmitter degrading enzyme acetylcholinesterase (AChE) with GLY (IC50 = 0.74 ± 0.02μM) being the most potent, followed by CPM (IC50 = 5.72 ± 0.24μM) and TBM (IC50 = 28.9 ± 1.60μM). Notably, the inhibition efficiency of GLY is even comparable with the FDA approved AD drug, donepezil (DON). The larger size of GLY spans almost the full gorge of AChE ranging from catalytic active site (CAS) to the peripheral active site (PAS) with relatively strong binding affinity (6.0 x 105 M-1) and acts as a competitive inhibitor for AChE. On the other hand, while they show relatively weak binding ((2-6) x 104 M-1), both CPM and TBM act as noncompetitive binders. While these two drugs can bind to PAS, MD simulation results predict an alternative noncompetitive inhibition mechanism for CPM. These results open the possibility of repurposing the antidiabetic drugs, particularly GLY, in the treatment of AD. The consequential side effect of excess acetylcholine production, due to the administration of these drugs to AD-unaffected patients, can be rectified by using colloidal gold and silver nanofluids as potential AChE activity boosters.

ACS Pharmacology & Translational Science published new progress about Alzheimer disease. 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

Zhuang, Xiaohui; Ling, Lan; Wang, Yingying; Li, Bingqian; Sun, Bin; Su, Weike; Jin, Can published the artcile< Photoinduced Cascade C-N/C=O Bond Formation from Bromodifluoroalkyl Reagents, Amines, and H2O via a Triple-Cleavage Process>, SDS of cas: 6280-57-5, the main research area is unsym oxalamide derivative green preparation; bromodifluoroalkyl reagent amine water cascade bond formation photocatalyst.

A green, sustainable, and straightforward method for synthesis of unsym. oxalamides RC(O)NR1R2 [R = C(O)NHPh, C(O)NH-4-BrC6H4, C(O)Ph, etc.; R1 = Me, Et, nPr, etc.; R2 = Me, Et, nPr, etc.; R1R2 = pyrrolidin-1-yl, morpholin-4-yl, cyclohex-1-yl] via photoinduced C-N/C=O bonds formation of bromodifluoroacetamide, amine and H2O through proceeding triple cleavage process was developed. In addition, this approach also gave an access to build the known bioactive compounds, and a feasible reaction mechanism was proposed. Moreover, the advantages of this transformation, including mild reaction conditions, broad substrate scope and operational simplicity, made this protocol attractive for further applications.

Organic Letters published new progress about Acetamides Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation) (bromodifluoro-). 6280-57-5 belongs to class amides-buliding-blocks, and the molecular formula is C17H35NO, SDS of cas: 6280-57-5.

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

Liu, Huimin; Wang, Shui; Qu, Chao; Li, Manman; Qu, Yixin published the artcile< Solid-Liquid Equilibrium of Chlorpropamide in 14 Pure Solvents at Temperature of 283.15 to 323.15 K>, Formula: C10H13ClN2O3S, the main research area is solid liquid equilibrium chlorpropamide alkanol acetate ester solubility thermodn.

The solubility of chlorpropamide (CPA) in 14 solvents including 8 alcs. (ethanol, n-propanol, isopropanol, n-butanol, 2-butanol, iso-butanol, n-pentanol, and isopentanol) and 6 acetate esters (Et acetate, Pr acetate, iso-Pr acetate, Bu acetate, amyl acetate, and Me propionate) at temperatures of 283.15 to 323.15 K and atm. pressure was determined using a laser method. The solubility as a function of temperature was regressed using modified Apelblat, Van’t Hoff, λh, Wilson, and nonrandom two-liquid (NRTL) models. On the basis of the exptl. and the simulation results, the mixing properties of the solutions, i.e., mixing Gibbs energy, enthalpy, and entropy, were estimated

Journal of Chemical & Engineering Data published new progress about Free energy of transfer (mixing free energy). 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

Yuan, Zhong; DeFalco, Frank; Wang, Lu; Hester, Laura; Weaver, James; Swerdel, Joel N.; Freedman, Amy; Ryan, Patrick; Schuemie, Martijn; Qiu, Rose; Yee, Jacqueline; Meininger, Gary; Berlin, Jesse A.; Rosenthal, Norman published the artcile< Acute pancreatitis risk in type 2 diabetes patients treated with canagliflozin versus other antihyperglycemic agents: an observational claims database study>, Related Products of 94-20-2, the main research area is canagliflozin antihyperglycemic SGLT2 inhibitor acute pancreatitis type 2 diabetes; Acute pancreatitis; canagliflozin; observational study; type 2 diabetes.

Observational evidence suggests that patients with type 2 diabetes mellitus (T2DM) are at increased risk for acute pancreatitis (AP) vs. those without T2DM. A small number of AP events were reported in clin. trials of the sodium glucose co-transporter 2 inhibitor canagliflozin, though no imbalances were observed between treatment groups. This observational study evaluated risk of AP among new users of canagliflozin compared with new users of six classes of other antihyperglycemic agents (AHAs). Three US claims databases were analyzed based on a prespecified protocol approved by the European Medicines Agency. Propensity score adjustment controlled for imbalances in baseline covariates. Cox regression models estimated the hazard ratio of AP with canagliflozin compared with other AHAs using on-treatment (primary) and intent-to-treat approaches. Sensitivity analyses assessed robustness of findings. Across the three databases, there were between 12,023-80,986 new users of canagliflozin; the unadjusted incidence rates of AP (per 1000 person-years) were between 1.5-2.2 for canagliflozin and 1.1-6.6 for other AHAs. The risk of AP was generally similar for new users of canagliflozin compared with new users of glucagon-like peptide-1 receptor agonists, dipeptidyl peptidase-4 inhibitors, sulfonylureas, thiazolidinediones, insulin, and other AHAs, with no consistent between-treatment differences observed across databases. Intent-to-treat and sensitivity anal. findings were qual. consistent with on-treatment findings. In this large observational study, incidence rates of AP in patients with T2DM treated with canagliflozin or other AHAs were generally similar, with no evidence suggesting that canagliflozin is associated with increased risk of AP compared with other AHAs.

Current Medical Research and Opinion published new progress about Acute pancreatitis. 94-20-2 belongs to class amides-buliding-blocks, and the molecular formula is C10H13ClN2O3S, Related Products of 94-20-2.

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

Singh, Imocha Rajkumar; Mitra, Sivaprasad published the artcile< Interaction of chlorpropamide with serum albumin: Effect on advanced glycated end (AGE) product fluorescence>, HPLC of Formula: 94-20-2, the main research area is chlorpropamide blood albumin interaction advanced glycated end product fluorescence; AGE product; Chlorpropamide; Diabetes; Fluorescence quenching; Serum albumin.

Carrier proteins like bovine or human serum albumin (BSA and HSA, resp.) are prone to glycation as compared to the other available proteins. Reducing sugars such as L-arabinose (ara), D-(-) galactose (gal) and D-(-) fructose (fru) were used to create model glycated serum albumins and binding ability of these with known antidiabetic drug chlorpropamide (CPM) was monitored. Fluorescence quenching experiment revealed that interaction of CPM with native as well as glycated albumins undergoes through a ground state complex formation. CPM binds strongly to glycated HSA with arabinose (gHSAara) as compared to other glycated systems and to the native proteins. CPM interacts through Van der Waals and hydrogen bonding interaction to glycated BSA by D-(-) fructose (gBSAfru) and also with native HSA; whereas, it’s interaction with BSA and others glycated systems like gBSAara, gBSAgal and gHSAara occurs primarily through hydrophobic interaction. CPM showed an enhancement in the production of the advanced glycated end products (AGE) in all the glycated proteins. The difference in the binding capability of CPM to differently glycated albumins could be a major model to understand the drug carrying capacity of the glycated serum albumins.

Spectrochimica Acta, Part A: Molecular and Biomolecular Spectroscopy published new progress about Advanced glycosylation end products Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 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

Mishra, Rashmi; Sehring, Ivonne; Cederlund, Maria; Mulaw, Medhanie; Weidinger, Gilbert published the artcile< NF-κB Signaling Negatively Regulates Osteoblast Dedifferentiation during Zebrafish Bone Regeneration>, COA of Formula: C10H13ClN2O3S, the main research area is Danio osteoblast dedifferentiation bone regeneration; NF-kappaB; bglap; bone; dedifferentiation; fin; osteoblast; osteocalcin; plasticity; regeneration; zebrafish.

Dedifferentiation of mature cells is an intriguing cellular process associated with regeneration of several organs. During zebrafish fin regeneration, osteoblasts dedifferentiate to osteogenic progenitors that provide source cells for bone restoration. We performed a high-content in vivo chem. screen for regulators of osteoblast dedifferentiation and fin regenerative growth. NF-κB signaling emerged as a specific regulator of dedifferentiation. The pathway is active in mature osteoblasts and downregulated prior to dedifferentiation. Pathway activation blocked osteoblast dedifferentiation, while NF-κB signaling inhibition enhanced dedifferentiation. Conditional Cre-lox-mediated NF-κB signaling manipulation specifically in osteoblasts showed that the pathway acts cell autonomously to interfere with osteoblast dedifferentiation. NF-κB signaling acts upstream of retinoic acid (RA) signaling, which also needs to be downregulated for dedifferentiation to occur, via suppression of the RA-degrading enzyme cyp26b1. Our findings shed light on the mol. regulation of regenerative cellular plasticity.

Developmental Cell published new progress about Biochemistry. 94-20-2 belongs to class amides-buliding-blocks, and the molecular formula is C10H13ClN2O3S, COA of Formula: C10H13ClN2O3S.

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

Tan, Xi; Yang, Lingfeng; Khunti, Kamlesh; Zhang, Ruya; Zhang, Ye; Rajpathak, Swapnil; Yu, Miao published the artcile< Factors associated with switching from sulphonylureas to dipeptidyl peptidase 4 inhibitors among patients with type 2 diabetes in the United States>, Formula: C10H13ClN2O3S, the main research area is sulfonylurea dipeptidyl peptidase diabetes united states; DPP-4 inhibitor; cohort study; database research; observational study; sulphonylureas; type 2 diabetes.

Studies examining the prevalence of and factors associated with switching from sulfonylureas (SUs) to dipeptidyl peptidase 4 (DPP-4) inhibitors in real-world settings are lacking. We assessed the factors associated with switching from SUs to DPP-4 inhibitors in the United States. This retrospective cohort study was conducted using the Optum Clinformatics Data Mart (2009-2018). Adults with type 2 diabetes and newly prescribed at least two SUs were included and were followed for 2 years after the initiation of SU (index date). We compared the characteristics of those who switched from SUs to DPP-4 inhibitors (only; no addnl. antidiabetic drugs) with those who continued with SUs (without adding other antidiabetic drugs) using multivariate logistic regression. Multinomial regression analyses were also conducted to assess the factors associated with switching to different drug classes vs. continuation with SUs. In a sample of 119 107 new SU users, 2.2% (2633) switched to DPP-4 inhibitors, 3.8% (4542) switched to antidiabetic drugs other than DPP-4 inhibitors, 68.3% (81 394) discontinued SUs but did not switch to another antidiabetic drug, 12.9% (15 345) continued with SUs and added other antidiabetic drugs, and 12.8% (15 193) continued with SUs only. Multivariate logistic regression showed that those who had significantly higher likelihood of switching were younger, female [vs. males; adjusted odds ratio (AOR) = 0.70], and living in the south; had previous use of DPP-4 inhibitors (AOR = 1.71); were not using antidiabetic drugs at baseline; had more baseline diabetes-related emergency room visits (AOR = 1.13), depression (AOR = 1.34), post-index hypoglycemia (AOR = 2.20), and an earlier index year; and were glyburide users (vs. glimepiride users; AOR = 1.29). The discontinuation rate for SUs is high. Factors associated with switching from SUs to DPP-4 inhibitors included age, sex, geog. region, baseline antidiabetic drug use, type of SU, baseline diabetes-related emergency room visits, hypoglycemia and depression.

Diabetes, Obesity and Metabolism published new progress about Antidiabetic agents. 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

Ahmed, Mohamed; Baqtiyar, Sheema; Khanum, Ruqiya; Fatima, Kulsum; Fatima, Anees published the artcile< Drug utilization pattern of anti diabetic drugs in type II diabetic patients in a teaching and general hospital>, SDS of cas: 94-20-2, the main research area is antidiabetic drug utilization pattern diabetes type 2.

BACKGROUND: Diabetes mellitus is defined as abnormal increase in levels of sugar (glucose) in the blood. Diabetes is a chronic (long-lasting) disease that affects how your body turns food into energy. In people with diabetes, blood sugar levels remain high. This may be because insulin is not being produced at all or is not made at sufficient levels, or is not as effective as it should be. The most common forms of diabetes are type 1diabetes (5%), which is an autoimmune disorder, and type 2 diabetes (95%), which is associated with obesity. Gestational diabetes is a form of diabetes that occurs in pregnancy, and other forms of diabetes are very rare and are caused by a single gene mutation. OBJECTIVE: The present study was undertaken to study the drug utilization pattern of anti-diabetic drugs in diabetic patients. METHOD: A six-month prospective observational study was carried out at Shadan teaching and general hospital, Peerancheru (Hyderabad). The data was collected from the case sheets of in patients and OPD cards of outpatients and critically analyzed using predetermined criteria. RESULTS: Out of 250 patients, 110(44%) patients were males and 140(56%) patients were females. It is observed that diabetes mellitus II is more common in patients of age groups (51-60) years. Pharmacotherapy revealed that 210 (81.6%) patients were treated with monotherapy followed by 34 (14%) patients with 2 drug therapy and 6 (4.4%) patients were prescribed with 3 drug therapy. Metformin was the drug of choice in monotherapy while metformin along with glimepiride was the preferred drug combination used in both 2 drug and 3 drug therapies. The overall drug usages in this study revealed that a total number of 301 drugs were prescribed. Out of which, metformin was most prescribed [128 (42.52%)]. CONCLUSION: Periodic evaluation of drug utilization patterns need to be done to provide suitable medications profile in prescription of drugs to increase the therapeutic benefit and reduce the adverse effects. The study of prescribing patterns require regular monitoring and evaluation and if necessary, suggestion of modification in prescribing pattern of medical practitioners to make medical care rational and cost effective. The current anti diabetic drugs includes insulin preparation and oral hypoglycemic agents (OHA), the preference is given mostly to metformin which is first choice of drug but the other drugs such as human insulin is also prescribed for many patients, also some combinations of (OHA) drugs are also preferred.

Indo American Journal of Pharmaceutical Research published new progress about Antidiabetic agents. 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

Thakral, Naveen K.; Thakral, Seema; Stephenson, Gregory A.; Sedlock, Robert; Suryanarayanan, Raj published the artcile< Compression-Induced Polymorphic Transformation in Tablets: Role of Shear Stress and Development of Mitigation Strategies>, Application of C10H13ClN2O3S, the main research area is Compression polymorphic transformation tablets shear stress; hydrostatic pressure; phase transformation; shear stress; tablet; viscoelastic excipients.

Our goals were to evaluate the effects of (i) hydrostatic pressure alone and (ii) its combined effect with shear stress during compaction, on the polymorphic transformation (form C → A) of a model drug, chlorpropamide. The powder was either subjected to hydrostatic pressure in a pressure vessel or compressed in a tablet press, at pressures ranging from 25 to 150 MPa. The overall extent of phase transformation was determined by powder X-ray diffractometry, whereas 2D-X-ray diffractometry enabled quantification of the spatial distribution of phase composition in tablets. Irresp. of the pressure, the extent of transformation following compaction was higher than that because of hydrostatic pressure alone, the difference attributed to the contribution of shear stress experienced during compaction. At a compression pressure of 25 MPa, there was a pronounced gradient in the extent of phase transformation when monitored from radial tablet surface to core. This gradient decreased with increase in compression pressure. Four approaches were attempted to minimize the effect of compression-induced phase transformation: (a) site-specific lubrication, (b) use of a viscoelastic excipient, (c) ceramic-lined die, and (d) use of cavity tablet. The ceramic-lined die coupled with site-specific lubrication was most effective in minimizing the extent of compression-induced phase transformation.

Journal of Pharmaceutical Sciences (Philadelphia, PA, United States) published new progress about Compression. 94-20-2 belongs to class amides-buliding-blocks, and the molecular formula is C10H13ClN2O3S, Application of C10H13ClN2O3S.

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

Yousef, Farah; Mansour, Oussama; Herbali, Jehad published the artcile< Rigid docking application to investigate sulfonylurea family members' binding site with their receptor KIR6.2SUR1>, Electric Literature of 94-20-2, the main research area is sulfonylurea glibenclamide chlorpropamide antihyperglycemic agent KIR62 SUR1 mol docking.

Sulfonylurea family members have been used as a second preferred line in the treatment of Type II Diabetes Mellitus (TIIDM) for decades. Only one crystal structure for its receptor Kir6.2SUR1 binding with one of sulfonylurea member; Glibenclamide (GBM), is available in Protein Data Bank (PDB) database. The aim of this manuscript is to study in-silico other sulfonylurea family members’ interactions with their receptor Kir6.2SUR1 using a docking software in the default settings. We have checked the validity of the software for the study. Then, rigid docking had been applied on 14 compounds of sulfonylurea group which they have anti-hyperglycemia activity. Next, we have compared their interactions to GBM interactions with Kir6.2SUR1. As a result, many compounds of this family had bound to Kir6.2SUR1 receptor in the same pocket as GBM. These results confirmed a perspective we have discussed about sulfonylurea structure activity relationship.

International Journal of Pharma and Bio Sciences published new progress about Amino acids Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 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