Month: October 2022

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

Wang, Chao-Jie; Guo, Xinxin; Zhai, Rui-Qin; Sun, Changning; Xiao, Guokai; Chen, Jin; Wei, Mei-Yan; Shao, Chang-Lun; Gu, Yuchao published the artcile< Discovery of penipanoid C-inspired 2-(3,4,5-trimethoxybenzoyl)quinazolin-4(3H)-one derivatives as potential anticancer agents by inhibiting cell proliferation and inducing apoptosis in hepatocellular carcinoma cells>, Recommanded Product: 2-Amino-4,5-dimethoxybenzamide, the main research area is trimethoxybenzoyl quinazolinone anticancer discovery preparation human apoptosis; Apoptosis; Cell cycle; Hepatocellular carcinoma; Penipanoid C; Quinazoline.

Hepatocellular carcinoma (HCC) is the most common form of liver cancer and the fourth leading cause of cancer-related death worldwide. First-line drugs such as sorafenib provide only a modest benefit to HCC patients. In this study, the gram-scale synthesis of 2-benzoylquinazolin-4(3H)-one skeleton was achieved successfully via the I2/DMSO catalytic system. A series of penipanoid C-inspired 2-(3,4,5-trimethoxybenzoyl)quinazolin-4(3H)-one derivatives was synthesized and evaluated for their cytotoxic activities against four cancer cell lines, HepG2, Bel-7402, A549, and U251. Among these compounds, I was the most effective one with IC50 values of 1.22μM and 1.71μM against HepG2 and Bel-7402 cells, resp. Mechanistic studies showed that I inhibited hepatocellular carcinoma cell proliferation via arresting cell cycle. Addnl., I induced HepG2 cells apoptosis by inducing reactive oxygen species production and elevating the expression of apoptosis-related proteins. More importantly, I displayed significant in vivo anticancer effects in the HepG2 xenograft models. This suggests that I is a promising lead compound with the potential to be developed as a chemotherapy agent for hepatocellular carcinoma.

European Journal of Medicinal Chemistry published new progress about Acetophenones Role: RCT (Reactant), RACT (Reactant or Reagent). 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, Recommanded Product: 2-Amino-4,5-dimethoxybenzamide.

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

Bhargava, P. N.; Singh, H. D. published the artcile< Synthesis of 3-aryl-6-bromo-2-(substituted)-thio-4(3H)-quinazolones as CNS depressants>, Application of C10H20ClNO, the main research area is quinazolone preparation central depressant.

Fourteen new 3-aryl-6-bromo-2-(N,N-dialkylcarboxamidomethylthio)-4(3H)quinazolones were prepared Pharmacol. screening indicates that 6-bromo-2-(N,N-diisobutylcarboxamidomethylthio)-3-phenyl-, 6-bromo-2-(N,N-dibenzylcarboxamidomethylthio)-3-p-chlorophenyl- and 6-bromo-2-(N,N-dibenzylcarboxamidomethylthio)-3-p-methoxyphenyl-4(3H)quinazolones possess CNS depressant activity.

Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry published new progress about Nervous system depressants. 5326-82-9 belongs to class amides-buliding-blocks, and the molecular formula is C10H20ClNO, Application of C10H20ClNO.

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

McAtee, Rory C.; Noten, Efrey A.; Stephenson, Corey R. J. published the artcile< Arene dearomatization through a catalytic N-centered radical cascade reaction>, Name: 3-Fluorobenzenesulfonamide, the main research area is cyclohexadiene fused sultam diastereoselective preparation; arylsulfonamide arene dearomatization iridium catalyzed centered radical cascade.

Herein, a catalytic protocol was reported to initiate a carboamination/dearomatization cascade that proceeded through transient sulfonamidyl radical intermediates formed from native sulfonamide N-H bonds leading to 1,4-cyclohexadiene-fused sultams such as I [R1 = F, CN, CF3, etc.; R2 = H, F; R3 = R4 = Me; R3R4 = (CH2)3; R5 = H, Me; X = CH2, O]. Importantly, this work demonstrated a facile approach to employ two-dimensional aromatic compounds as modular building blocks to generate richly substituted, three-dimensional compounds These reactions occurred at room temperature under visible light irradiation and were catalyzed by the combination of an iridium(III) photocatalyst and a dialkyl phosphate base. Reaction optimization, substrate scope, mechanistic features and synthetic applications of this transformation were presented.

Nature Communications published new progress about Amination catalysts. 1524-40-9 belongs to class amides-buliding-blocks, and the molecular formula is C6H6FNO2S, Name: 3-Fluorobenzenesulfonamide.

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

Dong, Pei; Li, Zhaojing; Liu, Xiaohua; Dong, Shunxi; Feng, Xiaoming published the artcile< Asymmetric synthesis of polycyclic spiroindolines via the Dy-catalyzed cascade reaction of 3-(2-isocyanoethyl)indoles with aziridines>, Application of C6H6ClNO2S, the main research area is isocyanoethyl indole aziridine dysprosium catalyst enantioselective tandem reaction; phenyltetrahydropyrrolo pyridoindole dicarboxylate preparation.

Herein, a tailored strategy to access such compounds through an asym. ring-opening/Friedel-Crafts/Mannich/desulfonylation cascade reaction was reported. In the presence of the N,N’-dioxide-Dy(III) complex, various 2,2′-diester aziridines and 3-(2-isocyanoethyl)indoles were converted into tetracyclic spiroindolines in a highly diastereo- and enantioselective manner (41 examples, up to 88% yield, 97% ee). On the basis of the absolute configuration of the product and previous works, a possible catalytic cycle was proposed to understand the origin of stereocontrol.

Organic Chemistry Frontiers published new progress about Aziridines Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 6961-82-6 belongs to class amides-buliding-blocks, and the molecular formula is C6H6ClNO2S, Application of C6H6ClNO2S.

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

Ardissino, Maddalena; Vincent, Matthew; Hines, Oliver; Amin, Ravi; Eichhorn, Christian; Tang, Alice R; Collins, Peter; Moussa, Osama; Purkayastha, Sanjay published the artcile< Long-term cardiovascular outcomes after orlistat therapy in patients with obesity: a nationwide, propensity-score matched cohort study.>, SDS of cas: 96829-58-2, the main research area is Cardiovascular; Obesity; Orlistat; Weight loss; outcomes.

AIMS: The rising prevalence of obesity and its associated comorbidities represent a growing public health issue; in particular, obesity is known to be a major risk factor for cardiovascular disease. Despite the evidence behind the efficacy of orlistat in achieving weight loss in patients with obesity, no study thus far has quantified its long-term effect on cardiovascular outcomes. The purpose of this study is to explore long-term cardiovascular outcomes after orlistat therapy. METHODS AND RESULTS: A propensity-score matched cohort study was conducted on the nation-wide electronic primary and integrated secondary healthcare records of the Clinical Practice Research Datalink (CPRD). The 36 876 patients with obesity in the CPRD database who had completed a course of orlistat during follow-up were matched on a 1:1 basis with equal numbers of controls who had not taken orlistat. Patients were followed up for a median of 6 years for the occurrence of the primary composite endpoint of major adverse cardiovascular events (fatal or non-fatal myocardial infarction or ischaemic stroke), and a number of secondary endpoints including primary endpoint components individually, the occurrence of new-onset heart failure, coronary revascularization, new chronic kidney disease stage III+ (CKD3+), and all-cause mortality. During the median study follow-up of 6 years, the occurrence of major adverse cardiovascular events was lower in the orlistat cohort [hazard ratio (HR) 0.74; 95% confidence interval (CI) 0.66-0.83, P < 0.001]. Patients who took orlistat experienced lower rates of myocardial infarction (HR 0.77; 95% CI 0.66-0.88, P < 0.001) and ischaemic stroke (HR 0.68; 95% CI 0.56 to -0.84, P < 0.001) as well as new-onset heart failure (HR 0.79; 95% CI 0.67-0.94, P = 0.007). There was no differences in revascularization rates (HR 1.12; 95% CI 0.91-1.38, P = 0.27), but a lower rate of both CKD3+ development (HR 0.78; 95% CI 0.73-0.83, P < 0.001) and mortality (HR 0.39, 95% CI 0.36 to -0.41, P < 0.001) was observed. CONCLUSION: In this nation-wide, propensity-score matched study, orlistat was associated with lower rates of overall major adverse cardiovascular events, new-onset heart failure, renal failure, and mortality. This study adds to current evidence on the known improvements in cardiovascular risk factor profiles of orlistat treatment by suggesting a potential role in primary prevention. European heart journal. Cardiovascular pharmacotherapy published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, SDS of cas: 96829-58-2.

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