Category: 94-20-2

Suvada, Kara; Plantinga, Laura; Vaughan, Camille P.; Markland, Alayne D.; Mirk, Anna; Burgio, Kathryn L.; Erni, Susanne M.; Ali, Mohammed K.; Okosun, Ike; Young, Henry; Goode, Patricia S.; Johnson, Theodore M. published the artcile< Comorbidities, Age, and Polypharmacy Limit the Use by US Older Adults with Nocturia of the Only FDA-approved Drugs for the Symptom>, Related Products of 94-20-2, the main research area is nocturia desmopressin acetate comorbidity polypharmacy aging United States; aged or elderly; comorbidity; medications; polypharmacy; risk factors; safety.

The goal of this study was to determine if the US adult population with nocturia (waking from sleep at night to void) can easily take medications (desmopressin acetate) approved by the US Food and Drug Administration for nocturia. Using a cross-sectional anal. of four US National Health and Nutrition Examination Survey (NHANES) waves (2005-2012), a total of 4111 participants aged ≥50 years who reported ≥2 nightly episodes of nocturia were identified. The main outcome was frequency of contraindications and drug interactions as described in US Food and Drug Administration-approved prescribing information. Desmopressin prescribing concerns were present in 80.5% (95% CI, 78.0-82.9) of those ≥50 years of age with nocturia; 50.0% (95% CI, 47.0-53.0) had contraindications, and 41.6% (95% CI, 39.3-44.0) took a concomitant drug that could increase risk of low serum sodium. Desmopressin contraindications were higher with older age (P < 0.001) and present in 73.2% (95% CI, 69.3-77.1) of those ≥80 years of age. This study showed that older US adults with nocturia have a high prevalence of medical conditions, concomitant medications, and baseline laboratory abnormalities that likely increase the risk of potentially severe adverse side effects from desmopressin use. A medication designed and approved for a clin. symptom that is most common in older adults could not be taken by most of the older adults with the symptom. Clinical Therapeutics published new progress about 5-HT reuptake inhibitors. 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

Mazhar, Faizan; Pozzi, Marco; Gentili, Marta; Scatigna, Marco; Clementi, Emilio; Radice, Sonia; Carnovale, Carla published the artcile< Association of Hyponatraemia and Antidepressant Drugs: A Pharmacovigilance-Pharmacodynamic Assessment Through an Analysis of the US Food and Drug Administration Adverse Event Reporting System (FAERS) Database>, Product Details of C10H13ClN2O3S, the main research area is mirtazapine vortioxetine antidepressant pharmacodynamics pharmacovigilance hyponatremia.

Background: Hyponatremia induced by antidepressant drugs is a rare but potentially life-threatening adverse reaction. Whether it is associated with all or only some antidepressant drugs is still unclear. This needs to be clarified to guide antidepressant therapies, especially in patients with electrolytic imbalances. Objectives: The primary objective of this study was to quantify the strength of association between the use of different antidepressant drugs and hyponatremia by using information reported to the US Food and Drug Administration (FDA) Adverse Event Reporting System (FAERS). The secondary objective was to investigate the putative relationship between different antidepressant pharmacol. targets and the risks of hyponatremia induced by antidepressant drugs using the ′pharmacovigilance-pharmacodynamic′ method. Methods: We used the FAERS database to conduct a case/non-case anal. on spontaneous reports, focusing on events of hyponatremia/syndrome of inappropriate antidiuretic hormone secretion (SIADH) reported in connection with the use of antidepressant drugs. Risk was expressed as a measure of disproportionality using the reporting odds ratio while adjusting for sex, age and concomitant medications associated with hyponatremia/SIADH. We assessed to what extent the receptor-binding properties of antidepressant drugs could associate with the reporting odds ratios of hyponatremia/SIADH of antidepressant drugs, building a linear regression model that included as independent variables the binding affinities (pKi) to the serotonin transporter, dopamine transporter, norepinephrine transporter, and serotonin 5-HT2C, 5-HT2A and 5-HT1A, and α1- and α2-adrenergic receptors. Results: There were 2233 reports identified. The adjusted reporting odds ratio for the association between antidepressant drug use and hyponatremia was 1.91 (95% confidence interval 1.83-2.00). The association was strongest for mirtazapine, followed by selective serotonin reuptake inhibitors, and lowest with serotonin-modulating antidepressant drugs. A significant linear correlation was found between the adjusted reporting odds ratios for hyponatremia and pKi for the adrenergic receptors α1 and α2. Conclusions: Hyponatremia is reported at a disproportionately higher level with classes of antidepressant drugs (noradrenergic and specific serotonergic antidepressant [mirtazapine] and serotonin modulators [vortioxetine]) that are in general considered to have a better profile of tolerability in terms of hyponatremia. With regard to the presented results, the risk of hyponatremia with mirtazapine appears to be greater than what was reported in the literature; however, confounding by indication cannot be ruled out. Our pharmacovigilance-pharmacodynamic anal. also indicates that inhibition of the serotonin transporter may not be involved in the hyponatremia linked to the use of antidepressant drugs.

CNS Drugs published new progress about 5-HT reuptake inhibitors Role: THU (Therapeutic Use), BIOL (Biological Study), USES (Uses). 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

Chhajed, Priyanka N.; Garud, Aniket A.; Kakde, A. P.; Chaudhari, S. R.; Patil, Ravindra B. published the artcile< Anatomization of diabetes and its current marketed pharmacophores for its better indulgent>, Quality Control of 94-20-2, the main research area is diabetes antidiabetic.

Diabetes mellitus is a chronic disease that requires life-long pharmacol. and non-pharmacol. management to prevent complications such as cardiovascular disease, retinopathy, nephropathy, and neuropathy. While type 2 diabetes mellitus is the most common form of diabetes comprising of 90% to 95% of all diabetes cases. Its prevalence is constantly increasing and has already reached epidemic proportions, particularly in urban India. Currently available sulfonylurea’s (SU), the most commonly used pharmacol. agents in treatment of type 2 diabetes; have gradually increasing secondary failure rates reaching 50% at the end of 5 years of disease, though the initial response is good in 70-75% of patients. The biguanides are mainly used as adjuvant to sulfonylureas. The gastrointestinal intolerance limits their use in many patients. Thus, large number of patients with type 2 diabetes fails to achieve persistent good metabolic control. The limitations of currently available pharmacol. agents for control of blood glucose have stimulated research on novel anti-diabetic agents with different mechanism of action. The newer drugs already developed or in the process of development for management of type 2 diabetes are GLP-1 Receptor Agonists, DPP-4 Inhibitors, SGLT-2 Inhibitors, and Glucokinase activators.

Pharma Science Monitor published new progress about Autonomic neuropathy. 94-20-2 belongs to class amides-buliding-blocks, and the molecular formula is C10H13ClN2O3S, Quality Control of 94-20-2.

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

Gonnet, Lori; Lennox, Cameron B.; Do, Jean-Louis; Malvestiti, Ivani; Koenig, Stefan G.; Nagapudi, Karthik; Friscic, Tomislav published the artcile< Metal-Catalyzed Organic Reactions by Resonant Acoustic Mixing>, Application of C10H13ClN2O3S, the main research area is tolbutamide preparation antidiabetic; Acoustic Mixing; Catalysis; Green Chemistry; Mechanochemistry; Pharmaceuticals.

Catalytic organic synthesis by resonant acoustic mixing (RAM), a mechanochem. methodol. that does not require bulk solvent or milling media. Using as model reactions ruthenium-catalyzed ring-closing metathesis and copper-catalyzed sulfonamide-isocyanate coupling, RAM mechanosynthesis was shown to be faster, operationally simpler than conventional ball-milling, while also provided the first example of a mechanochem. strategy for ruthenium-catalyzed ene-yne metathesis. Reactions by RAM were readily and directly scaled-up without any significant changes in reaction conditions, as shown by the straightforward 200-fold scaling-up of the synthesis of the antidiabetic drug Tolbutamide, from hundreds of milligrams directly to 30 g.

Angewandte Chemie, International Edition published new progress about Antidiabetic agents. 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

Iyer, Malliga R.; Bhattacharjee, Pinaki; Kundu, Biswajit; Rutland, Nicholas; Wood, Casey M. published the artcile< One-Pot Synthesis of Thio-Augmented Sulfonylureas via a Modified Bunte's Reaction>, Category: amides-buliding-blocks, the main research area is thio sulfonylurea preparation; sulfonylurea one pot Bunte reaction.

Authors report the development of a one-pot Bunte’s reaction-enabled expeditious platform under aqueous conditions for the scalable conversion of sulfonylureas to synthetically versatile thio-sulfonylureas. The reaction was further propagated in the same pot to yield diverse chiral and achiral isothiosulfonyl analogs. The protocol enabled the synthesis of various drug-like mols. and was applied to an enantiomeric synthesis of a cannabinoid receptor antagonist SLV326.

ACS Omega published new progress about One-pot synthesis. 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

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

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

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

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

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