Category: 94-20-2

Ahmad, Tanveer; Mehmood, Tariq; Shahid, Muhammad; Ahmad, Adnan; Basra, Muhammad Asim Raza; Zia-ur-Rehman, Muhammad; Munawar, Munawar Ali published the artcile< In vivo anti-diabetic studies of sulfonylurea-sulfonamide hybrids>, HPLC of Formula: 94-20-2, the main research area is antidiabetic sulfonylurea sulfonamide hybrid.

Owing to alarming increase of diabetes mellitus around the world, there is a need to discover new mols. to tackle with the problem. In this work, sulfonamides and sulfonylurea-sulfonamide hybrids were synthesized from simple mol. of 4-aminobenzenesulfonamide by its reaction with aryl sulfonyl chlorides. Anti-diabetic activities of these pharmacophores were studied by oral glucose tolerance test (OGTT) percentage anal. on Sprague Dawley (SD) rats at the dose of 20mg/kg using glibenclamide (GC). Among these synthesized pharmacophores, six compounds exhibited percentage reduction (20.47 ± 2.54 to 44.97 ± 2.16%) and (20.79 ± 1.55 to 37 ± 2.94%) in blood glucose level at 20mg/kg dose compared to glibenclamide (74 ± 3.10% reduction) 50mg/kg dose of glibenclamide after 2 and 5 h of oral administration resp. Present results showed that these compounds might be excellent addition in the drugs used to suppress the higher level of blood glucose level in diabetes mellitus.

Pakistan Journal of Zoology published new progress about Antidiabetic agents. 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

Mao, Zhifan; Liu, Wenwen; Huang, Yunyuan; Sun, Tianyue; Bao, Keting; Feng, Jiali; Moskalev, Alexey; Hu, Zelan; Li, Jian published the artcile< Anti-aging effects of chlorpropamide depend on mitochondrial complex-II and the production of mitochondrial reactive oxygen species>, SDS of cas: 94-20-2, the main research area is chlorpropamide antiaging agent mitochondrial complex2 aging; ATP sensitive potassium channels; Anti-aging; Chlorpropamide; Mitochondrial complex II; Mitochondrial reactive oxygen species; Senescence; Succinate dehydrogenase; Sulfonylureas.

Sulfonylureas are widely used oral anti-diabetic drugs. However, its long-term usage effects on patients lifespan remain controversial, with no reports of influence on animal longevity. Hence, the anti-aging effects of chlorpropamide along with glimepiride, glibenclamide, and tolbutamide were studied with special emphasis on the interaction of chlorpropamide with mitochondrial ATP-sensitive K+ (mitoK-ATP) channels and mitochondrial complex II. Chlorpropamide delayed aging in Caenorhabditis elegans, human lung fibroblast MRC-5 cells and reduced doxorubicin-induced senescence in both MRC-5 cells and mice. In addition, the mitochondrial membrane potential and ATP levels were significantly increased in chlorpropamide-treated worms, which is consistent with the function of its reported targets, mitoK-ATP channels. Increased levels of mitochondrial reactive oxygen species (mtROS) were observed in chlorpropamide-treated worms. Moreover, the lifespan extension by chlorpropamide required complex II and increased mtROS levels, indicating that chlorpropamide acts on complex II directly or indirectly via mitoK-ATP to increase the production of mtROS as a pro-longevity signal. This study provides mechanistic insight into the anti-aging effects of sulfonylureas in C. elegans.

Acta Pharmaceutica Sinica B published new progress about Aging, animal. 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

Vasconcelos, Ingrid; da Silva, Pedro Henrique Reis; Dias, Derick Rodrigues Davila; de Freitas Marques, Maria Betania; da Nova Mussel, Wagner; Pedrosa, Tercio Assuncao; Ribeiro e Silva, Maria Elisa Scarpelli; de Souza Freitas, Roberto Fernando; de Sousa, Ricardo Geraldo; Fernandes, Christian published the artcile< Synthesis and characterization of a molecularly imprinted polymer (MIP) for solid-phase extraction of the antidiabetic gliclazide from human plasma>, Computed Properties of 94-20-2, the main research area is gliclazide molecularly imprinted polymer solid phase extraction; Diabetes mellitus; Molecularly imprinted solid-phase extraction; Sample preparation; Sulfonylureas.

Gliclazide is a sulfonylurea frequently prescribed for the management of type 2 diabetes mellitus in elderly patients and for patients with chronic renal or hepatic diseases. Even though it is considered a safer alternative, the drug can provoke side effects in some patients, especially hypoglycemia, due to the high interindividual variability. Therefore, the quantification of gliclazide in biol. samples is usually recommended in order to assure efficacy and safety of the pharmacotherapy. However, due to the complexity of biol. matrixes, therapeutic monitoring can be very challenging, especially in the sample preparation step. Synthesis conditions were optimized (monomer, crosslinker and porogen) and the polymer was characterized for its morphol., physicochem. and stability properties. The influence of drug concentration, solvent composition and pH on the coefficient of distribution (Kd) and imprinting factor (IF) were studied, as well as repeatability between batches and selectivity. The best reaction yield, extraction capacity, and selectivity was obtained using 2-hydroxyethyl methacrylate (2-HEMA), ethyleneglycol dimethacrylate (EGDMA) and acetonitrile. The developed method by MISPE-HPLC-UV showed to be appropriate to determine gliclazide in human plasma samples.

Materials Science & Engineering, C: Materials for Biological Applications published new progress about Blood plasma. 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

Sagandira, Cloudius R.; Watts, Paul published the artcile< Rapid Multigram-Scale End-to-End Continuous-Flow Synthesis of Sulfonylurea Antidiabetes Drugs: Gliclazide, Chlorpropamide, and Tolbutamide>, Related Products of 94-20-2, the main research area is chlorpropamide gliclazide tolbutamide continuous flow preparation antidiabetic agent.

A multigram-scale robust, efficient, and safe end-to-end continuous-flow process for the diabetes sulfonylurea drugs gliclazide, chlorpropamide, and tolbutamide is reported. The drugs were prepared by the treatment of an amine with a haloformate affording carbamate, which was subsequently treated with a sulfonamide to afford sulfonylurea. Gliclazide was obtained in 87% yield within 2.5 min total residence time with 26 g/h throughput; 0.2 kg of the drug was produced in 8 h of running the system continuously. Chlorpropamide and tolbutamide were both obtained in 94% yield within 1 min residence time with 184-188 g/h throughput; 1.4-1.5 kg of the drugs was produced in 8 h of running the system continuously. N-Substituted carbamates were used as safe alternatives to the hazardous isocyanates in constructing the sulfonyl urea moiety.

Synthesis published new progress about Antidiabetic agents. 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

Tomaru, Atsuko; Toshimoto, Kota; Lee, Wooin; Ishigame, Keiko; Sugiyama, Yuichi published the artcile< A Simple Decision Tree Suited for Identification of Early Oral Drug Candidates With Likely Pharmacokinetic Nonlinearity by Intestinal CYP3A Saturation>, Product Details of C10H13ClN2O3S, the main research area is CYP3A pharmacokinetic Intestinal absorption type I nonlinearity; Cytochrome P450 (CYP) 3A; First-pass metabolism; Intestinal absorption; Nonlinear pharmacokinetics; Oral absorption.

To identify oral drugs that likely display nonlinear pharmacokinetics due to saturable metabolism by intestinal CYP3A, our previous report using CYP3A substrate drugs proposed an approach using thresholds for the linear index number (LIN3A = dose/Km; Km, Michaelis-Menten constant for CYP3A) and the intestinal availability (FaFg). Here, we aimed to extend the validity of the previous approach using both CYP3A substrate and non-substrate drugs and to devise a decision tree suited for early drug candidates using in vitro metabolic intrinsic clearance (CLint, vitro) instead of FaFg. Out of 152 oral drugs (including 136 drugs approved in Japan, US or both), type I nonlinearity (in which systemic drug exposure increases in a more than dose-proportional manner) was noted with 82 drugs (54%), among which 58 drugs were identified as CYP3A substrates based on public information. Based on practical feasibility, 41 drugs were selected from CYP3A substrates and subjected to inhouse metabolic assessment. The results were used to determine the thresholds for CLint, vitro (0.45μL/min/pmol CYP3A4) and LIN3A (1.0 L). For four drugs incorrectly predicted, potential mechanisms were looked up. Overall, our proposed decision tree may aid in the identification of early drug candidates with intestinal CYP3A-derived type I nonlinearity.

Journal of Pharmaceutical Sciences (Philadelphia, PA, United States) published new progress about Cytochrome P450 CYP3A inhibitors. 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

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

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

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