Category: 94-20-2

Tigori, Mougo Andre; Kouyate, Amadou; Kouakou, Victorien; Niamien, Paulin Marius; Trokourey, Albert published the artcile< Inhibition performance of some sulfonylurea on copper corrosion in nitric acid solution evaluated theoretically by DFT calculations>, Category: amides-buliding-blocks, the main research area is sulfonylurea copper corrosion nitric acid density functional theory calculation.

The theor. study of chlorpropamide, tolazamide and glipizide was carried out by the D. Functional Theory (DFT) at B3LYP/6-31G(d) level. This study made it possible to determine the global reactivity parameters in order to better understand the interactions between the mols. studied and the copper surface. Then, the determination of local reactivity indexes (Fukui functions and dual descriptor) on these mols. resulted in the precision on the most probable centers of nucleophilic and electrophilic attacks within each mol. The results obtained, show that chloropropamide, tolazamide and glipizide can be good inhibitors against copper corrosion. Thus, the mechanism of copper corrosion inhibition of these compounds in nitric acid solution has been explained by means of theor. calculations

Open Journal of Physical Chemistry published new progress about Band gap. 94-20-2 belongs to class amides-buliding-blocks, and the molecular formula is C10H13ClN2O3S, Category: amides-buliding-blocks.

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

Yen, Fu-Shun; Lai, Jung-Nien; Wei, James Cheng-Chung; Chiu, Lu-Ting; Hwu, Chii-Min; Hou, Ming-Chih; Hsu, Chih-Cheng published the artcile< Sulfonylureas may be useful for glycemic management in patients with diabetes and liver cirrhosis>, Electric Literature of 94-20-2, the main research area is sulfonylurea antidiabetic agent hyperglycemia diabetes liver cirrhosis.

This study aimed to investigate the long-term outcomes of sulfonylurea (SU) use in patients with T2DM and compensated liver cirrhosis. From Jan. 1, 2000, to Dec. 31, 2012, we selected the data of 3781 propensity-score-matched SU users and nonusers from Taiwan’s National Health Insurance Research Database. The mean follow-up time for this study was 5.74 years. Cox proportional hazards models with robust sandwich standard error estimates were used to compare the risks of main outcomes between SU users and nonusers. The incidence of mortality during follow-up was 3.24 and 4.09 per 100 person-years for SU users and nonusers, resp. The adjusted hazard ratios and 95% confidence intervals for all-cause mortality, major cardiovascular events, and decompensated cirrhosis in SU users relative to SU nonusers were 0.79 (0.71-0.88), 0.69 (0.61-0.80), and 0.82 (0.66-1.03), resp. The SU-associated lower risks of death and cardiovascular events seemed to have a dose-response trend. This population-based cohort study demonstrated that SU use was associated with lower risks of death and major cardiovascular events compared with SU non-use in patients with T2DM and compensated liver cirrhosis. SUs may be useful for glycemic management for patients with liver cirrhosis.

PLoS One published new progress about Angiotensin-converting enzyme inhibitors. 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

Abdel-Salam, Omar M. E.; Sleem, Amany A.; Youness, Eman R.; Morsy, Fatma A. published the artcile< Exacerbation of toluene's neuro- and hepato-toxicity by amiodarone or chlorpropamide: involvement of oxidative stress>, Name: 4-Chloro-N-(propylcarbamoyl)benzenesulfonamide, the main research area is amiodarone chlorpropamide neuroprotectant neurotoxicity hepatotoxicity.

Volatile solvent abuse is an important health problem and results in serious injury to the central nervous system. Neuroprotective effects were reported for the sulfonylurea group of drugs and for the anti-arrhythmic agent amiodarone, and these drugs have a K+ channel-blocking effect. The K+ channels are of interest for their ability to modulate brain damage. The aim of this study was to investigate the effect of amiodarone and chlorpropamide on the development of oxidative stress and brain and liver damage induced by toluene injection in rats. Toluene (900 mg/kg) was i.p. (i.p.) administered alone or in combination with amiodarone or chlorpropamide (18 or 36 mg/kg, orally) once a day for 2 consecutive days. The brain and liver content of malondialdehyde (MDA), reduced glutathione (GSH), and nitric oxide (NO), and the activity of paraoxonase-1 (PON-1) were determined In addition, butyrylcholinesterase (BChE) and the concentration of the anti-apoptotic protein (Bcl-2) were determined in brain homogenates. Histopathol. examination of brain and liver sections was also performed. Results showed that compared to controls, toluene resulted in increased oxidative stress in the brain and liver tissues. MDA and NO concentrations were markedly raised along with decreased levels of GSH and PON-1 activity. Toluene also inhibited BChE activity and decreased Bcl-2 level in the brain tissue. The biochem. changes induced by toluene were aggravated by the administration of either amiodarone or chlorpropamide. Rats treated with toluene exhibited dead neurons, perineuronal vacuolations, infiltrative cells, glial cells, and degeneration of some Purkinje cells. In the liver, massive hepatic inflammatory infiltrate, hemorrhage, vacuolar degeneration, apoptosis, and degeneration of hepatocytes were observed The co-administration of either amiodarone or chlorpropamide caused dose-dependent exacerbation of the toluene-induced pathol. changes. These findings suggest the involvement of oxidative stress in the neuro- and hepato-toxicity by toluene and imply a greater toxicity in toluene abusers treated with either amiodarone or chlorpropamide.

Reactive Oxygen Species published new progress about Bcl-2 proteins Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 94-20-2 belongs to class amides-buliding-blocks, and the molecular formula is C10H13ClN2O3S, Name: 4-Chloro-N-(propylcarbamoyl)benzenesulfonamide.

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

Nevidalova, Hana; Michalcova, Lenka; Glatz, Zdenek published the artcile< Applicability of capillary electrophoresis-frontal analysis for displacement studies: Effect of several drugs on L-tryptophan and lidocaine binding to human serum albumin>, Synthetic Route of 94-20-2, the main research area is tryptophan lidocaine human serum albumin binding constant capillary electrophoresis; drug protein binding screening; binding constant; binding sites; capillary electrophoresis-frontal analysis; drug competition; human serum albumin.

The effective concentration of a drug in the blood, i.e. the concentration of a free drug in the blood, is influenced by the strength of drug binding onto plasma proteins. Besides its efficacy, these interactions subsequently influence the liberation, absorption, distribution, metabolism, excretion, and toxicol. properties of the drug. It is important to not only determine the binding strength and stoichiometry, but also the binding site of a drug on the plasma protein mol., because the co-administration of drugs with the same binding site can affect the above-mentioned concentration and as a result the pharmacol. behavior of the drugs and lead to side effects caused by the change in free drug concentration, its toxicity. In this study, the binding characteristics of six drugs with human serum albumin, the most abundant protein in human plasma, were determined by capillary electrophoresis-frontal anal., and the obtained values of binding parameters were compared with the literature data. The effect of several drugs and site markers on the binding of L-tryptophan and lidocaine to human serum albumin was investigated in subsequent displacement studies which thus demonstrated the usability of capillary electrophoresis as an automated high-throughput screening method for drug-protein binding studies.

Journal of Separation Science published new progress about Capillary electrophoresis. 94-20-2 belongs to class amides-buliding-blocks, and the molecular formula is C10H13ClN2O3S, Synthetic Route of 94-20-2.

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

Barry, Jeremy A.; Groseclose, Mark Reid; Castellino, Stephen published the artcile< Quantification and assessment of detection capability in imaging mass spectrometry using a revised mimetic tissue model>, Related Products of 94-20-2, the main research area is liver kidney brain tissue distribution clozapine; LC–MS validation; detection capability; imaging MS; mimetic tissue model; quantification.

Aim: A revised method of preparing the mimetic tissue model for quant. imaging mass spectrometry (IMS) is evaluated. Concepts of assessing detection capability are adapted from other imaging or mass spectrometry (MS)-based technologies to improve upon the reliability of IMS quantification. Materials & methods: The mimetic tissue model is prepared by serially freezing spiked-tissue homogenates into a cylindrical mold to create a plug of tissue with a stepped concentration gradient of matrix-matched standards Weighted least squares (WLS) linear regression is applied due to the heteroscedastisity (change in variance with intensity) of most MS data. Results & conclusions: Imaging poses several caveats for quantification which are unique compared with other MS-based methods. Aspects of the design, construction, application, and evaluation of the matrix-matched standard curve for the mimetic tissue model are discussed. In addition, the criticality of the ion distribution in the design of a purposeful liquid chromatog. coupled to mass spectrometry (LC-MS) validation is reviewed.

Bioanalysis published new progress about Biopsy. 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

Tao, Pingyang; Li, Zhao; Woolfork, Ashley G.; Hage, David S. published the artcile< Characterization of tolazamide binding with glycated and normal human serum albumin by using high-performance affinity chromatography>, Safety of 4-Chloro-N-(propylcarbamoyl)benzenesulfonamide, the main research area is tolazamide human serum albumin binding glycation affinity microcolumn; Affinity microcolumn; Drug-protein binding; Glycation; Human serum albumin; Tolazamide.

Sulfonylurea drugs are antidiabetic drugs that are utilized in the treatment of type II diabetes and often have significant binding with human serum albumin (HSA). Immobilized samples of normal or glycated HSA in affinity microcolumns were used to investigate interactions of these proteins with the sulfonylurea drug tolazamide. HPLC and frontal anal. were used to first examine the overall binding of this drug with these samples of HSA. It was found that tolazamide had two general classes of binding sites (i.e., high and low affinity) for normal and glycated HSA. The higher affinity sites had binding constants of around 4.3-6.0 × 104 M-1 for these interactions at pH 7.4 and 37 °C, while the lower affinity sites had binding strengths of 4.9-9.1 × 103 M-1. Zonal competition studies between tolazamide and probes for Sudlow sites I and II on HSA were also performed and used to provide site-specific affinities for tolazamide at these sites. A decrease of 22% in affinity was observed for tolazamide at Sudlow site I and an increase up to 58% was seen at Sudlow site II when comparing glycated HSA with normal HSA. These observed changes were compared to those of other first-generation sulfonylurea drugs, providing information on how glycation can alter the total and local binding strength of tolazamide and related compounds with HSA under levels of glycation seen in patients with diabetes.

Journal of Pharmaceutical and Biomedical Analysis published new progress about Affinity HPLC. 94-20-2 belongs to class amides-buliding-blocks, and the molecular formula is C10H13ClN2O3S, Safety of 4-Chloro-N-(propylcarbamoyl)benzenesulfonamide.

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

Drebushchak, T. N.; Drebushchak, V. A. published the artcile< Structural similarity and similarity in thermal properties of the polymorphs: melting and crystallization from the melt of tolbutamide and chlorpropamide>, Application of C10H13ClN2O3S, the main research area is tolbutamide chlorpropamide polymorphism melting crystallization thermal property.

Abstract: The polymorphism of tolbutamide and chlorpropamide under melting/crystallization was investigated with using DSC and in situ X-ray powder diffraction. The asymmetry in thermal transformations was revealed for both substances. Under heating, all tolbutamide/chlorpropamide polymorphs transform into high-temperature IH/ε polymorph, which melts at 128°C. The crystal structures of the high-temperature polymorphs, IH and ε, are very similar to each other in the unit cell parameters and in the arrangement of z-shaped infinite hydrogen-bonded ribbons. Under cooling, other polymorph crystallizes from the melt, V for tolbutamide and β for chlorpropamide, thus making easy the obtaining of these metastable polymorphs. The polymorphs of tolbutamide and chlorpropamide crystallized from their melts turned out to be also very similar to each other in their structures (space group, unit cell parameters, arrangement of π-shaped infinite hydrogen-bonded ribbons). Solid-solid transformation V → II in tolbutamide was detected both in samples stored under room conditions and those melted in capillaries, thus providing new easy way for II tolbutamide crystallization In generalizing our results, one can expect that if evident similarity is found among the polymorphs of similar mols. in their crystal structure, the similarity in their thermal properties can be also found, and vice versa.

Journal of Thermal Analysis and Calorimetry published new progress about Cooling. 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

Khaibrakhmanova, Diliara; Nikiforova, Alena; Sedov, Igor published the artcile< Binding constants of drug-albumin complexes from DSC measurements>, Application In Synthesis of 94-20-2, the main research area is tolbutamide albumin differential scanning calorimetry.

The DSC technique is applied for quantification of the thermodn. binding constants in protein-ligand systems. For this purpose, the thermograms of protein denaturation are recorded at different ligand concentrations The observed dependence of the temperature shift of denaturation peak on ligand concentration is fitted to the two-state model of denaturation. First and second sequential binding constants of drugs tolbutamide, chloropropamide, phenylbutazone, meloxicam, and ampicillin with bovine serum albumin (BSA) are determined Ampicillin shows weak binding with BSA, while four other drugs bind quite tightly. Phenylbutazone and meloxicam bind to two different sites of BSA mol. with similar affinity, while tolbutamide and chloropropamide have higher affinities to one of the binding sites. We extensively review the available data on albumin binding of these drugs determined using different exptl. methods, which are in strong disagreement with each other. DSC measurements provide reproducible denaturation curves that can be a source of data on the protein-ligand binding including the second binding constant inaccessible to some other methods.

Thermochimica Acta published new progress about Bovine serum albumin Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 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

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

Liu, Yi-Chun; Nguyen, Phung-Anh; Humayun, Ayesha; Chien, Shuo-Chen; Yang, Hsuan-Chia; Asdary, Rahma Novita; Syed-Abdul, Shabbir; Hsu, Min-Huei; Moldovan, Max; Yen, Yun; Li, Yu-Chuan; Jian, Wen-Shan; Iqbal, Usman published the artcile< Does long-term use of antidiabetic drugs changes cancer risk?>, Synthetic Route of 94-20-2, the main research area is pioglitazone anticancer agent liver lung cancer.

Antidiabetic medications are commonly used around the world, but their safety is still unclear. The aim of this study was to investigate whether long-term use of insulin and oral antidiabetic medications is associated with cancer risk.We conducted a well-designed case-control study using 12 years of data from Taiwans National Health Insurance Research Database and investigated the association between antidiabetic medication use and cancer risk over 20 years. We identified 42,500 patients diagnosed with cancer and calculated each patients exposure to antidiabetic drugs during the study period. We matched cancer and noncancer subjects matched 1:6 by age, gender, and index date, and used Cox proportional hazard regression and conditional logistic regression, adjusted for potential confounding factors, i.e., medications and comorbid diseases that could influence cancer risk during study period.Pioglitazone (adjusted odds ratio [AOR], 1.20; 95% confidence interval [CI], 1.05-1.38); and insulin and its analogs for injection, intermediate or long acting combined with fast acting (AOR, 1.22; 95% CI, 1.05-1.43) were significantly associated with a higher cancer risk. However, metformin (AOR, 1.00; 95% CI, 0.93-1.07), glibenclamide (AOR, 0.98; 95% CI, 0.92-1.05), acarbose (AOR, 1.06; 95% CI, 0.96-1.16), and others do not show evidence of association with cancer risk. Moreover, the risk for specific cancers among antidiabetic users as compared with nonantidiabetic medication users was significantly increased for pancreas cancer (by 45%), liver cancer (by 32%), and lung cancer (by 18%).Antidiabetic drugs do not seem to be associated with an increased cancer risk incidence except for pioglitazone, insulin and its analogs for injection, intermediate or long acting combined with fast acting.

Medicine (Philadelphia, PA, United States) published new progress about Antidiabetic agents. 94-20-2 belongs to class amides-buliding-blocks, and the molecular formula is C10H13ClN2O3S, Synthetic Route of 94-20-2.

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