Tag: M.W=250-300

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

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

Zhao, Yichao; Bruce, Lachlan David; Jin, Jianwen; Xia, Bo; Chan, Philip Wai Hong published the artcile< Copper catalyzed N-formylation of α-silyl-substituted tertiary N-alkylamines by air>, HPLC of Formula: 6280-57-5, the main research area is dialkylaminomethyl trimethylsilane copper catalyst formylation; dialkyl formylamine preparation.

A site-selective method to prepare N-formyl amines efficiently that relies on the copper(I)-catalyzed oxidation of α-silyl-substituted tertiary N-alkylamines by air at room temperature was described. The oxidative protocol was shown to exhibited excellent functional group tolerance as it was applicable to a wide variety of amine substrates and a number of bioactive mols. and natural products. Moreover, it delinates a ligand- and additive-free amine oxidation process mediated by a low-cost metal salt with oxygen from air taking on the role of both the terminal oxidant and as part of the formylation reagent, which was unprecedented in copper catalysis. It also offered the first synthetic method that can selectively generate α-amino radical species as reactive intermediates from α-silylamines under non-photochem. reaction conditions.

Green Chemistry published new progress about Formamides Role: SPN (Synthetic Preparation), PREP (Preparation) (N,N-dialkyl). 6280-57-5 belongs to class amides-buliding-blocks, and the molecular formula is C17H35NO, HPLC of Formula: 6280-57-5.

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

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

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

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

Toigawa, Tomohiro; Peterman, Dean R.; Meeker, David S.; Grimes, Travis S.; Zalupski, Peter R.; Mezyk, Stephen P.; Cook, Andrew R.; Yamashita, Shinichi; Kumagai, Yuta; Matsumura, Tatsuro; Horne, Gregory P. published the artcile< Radiation-induced effects on the extraction properties of hexa-n-octylnitrilo-triacetamide (HONTA) complexes of americium and europium>, Category: amides-buliding-blocks, the main research area is radiation induced extraction hexa octylnitrilo triacetamide complex americium europium.

The candidate An(III)/Ln(III) separation ligand hexa-n-octylnitrilo-triacetamide (HONTA) was irradiated under envisioned SELECT (Solvent Extraction from Liquid waste using Extractants of CHON-type for Transmutation) process conditions (n-dodecane/0.1 M HNO3) using a solvent test loop in conjunction with cobalt-60 gamma irradiation The extent of HONTA radiolysis and complementary degradation product formation was quantified by HPLC-ESI-MS/MS. Further, the impact of HONTA radiolysis on process performance was evaluated by measuring the change in 243Am and 154Eu distribution ratios as a function of absorbed gamma dose. HONTA was found to decay exponentially with increasing dose, affording a dose coefficient of d = (4.48 ± 0.19) x 10-3 kGy-1. Multiple degradation products were detected by HPLC-ESI-MS/MS with dioctylamine being the dominant quantifiable species. Both 243Am and 154Eu distribution ratios exhibited an induction period of ~70 kGy for extraction (0.1 M HNO3) and back-extraction (4.0 M HNO3) conditions, after which both values decreased with absorbed dose. The decrease in distribution ratios was attributed to a combination of the destruction of HONTA and ingrowth of dioctylamine, which is capable of interfering in metal ion complexation. The loss of HONTA with absorbed gamma dose was predominantly attributed to its reaction with the n-dodecane radical cation (R ̇+). These R ̇+ reaction kinetics were measured for HONTA and its 241Am and 154Eu complexes using picosecond pulsed electron radiolysis techniques. All three second-order rate coefficients (k) were essentially diffusion limited in n-dodecane indicating a significant reaction pathway: k(HONTA + R ̇+) = (7.6 ± 0.8) x 109 M-1 s-1, k(Am(HONTA)2 + R ̇+) = (7.1 ± 0.7) x 1010 M-1 s-1, and k(Eu(HONTA)2 + R ̇+) = (9.5 ± 0.5) x 1010 M-1 s-1. HONTA-metal ion complexation afforded an order-of-magnitude increase in rate coefficient Nanosecond time-resolved measurements showed that both direct and indirect HONTA radiolysis yielded the short-lived (<100 ns) HONTA radical cation and a second long-lived (μs) species identified as the HONTA triplet excited state. The latter was confirmed by a series of oxygen quenching picosecond pulsed electron measurements, affording a quenching rate coefficient of k(3[HONTA]* + O2) = 2.2 x 108 M-1 s-1. Overall, both the HONTA radical cation and triplet excited state are important precursors to the suite of measured HONTA degradation products. Physical Chemistry Chemical Physics published new progress about Complexation (metal complexation). 6280-57-5 belongs to class amides-buliding-blocks, and the molecular formula is C17H35NO, Category: amides-buliding-blocks.

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