Category: 55981-09-4

Xu, Siyu published the artcileAnti-infective nitazoxanide disrupts transcription of ribosome biogenesis-related genes in yeast, Related Products of esters-buliding-blocks, the main research area is Saccharomyces nitazoxanide transcriptome ribosome; Gene ontology; Over-representation analysis; RNA-seq; Ribosome; SSU processome; Thiazolides.

Abstract: Background: Nitazoxanide is a broad-spectrum, anti-parasitic, anti-protozoal, anti-viral drug, whose mechanisms of action have remained elusive. Objective: In this study, we aimed to provide insight into the mechanisms of action of nitazoxanide and the related eukaryotic host responses by characterizing transcriptome profiles of Saccharomyces cerevisiae exposed to nitazoxanide. Methods: RNA-Seq was used to investigate the transcriptome profiles of three strains of S. cerevisiae with dsRNA virus-like elements, including a strain that hosts M28 encoding the toxic protein K28. From the strain with M28, an addnl. sub-strain was prepared by excluding M28 using a nitazoxanide treatment. Results: Our transcriptome anal. revealed the effects of nitazoxanide on ribosome biogenesis. Many genes related to the UTP A, UTP B, Mpp10-Imp3-Imp4, and Box C/D snoRNP complexes were differentially regulated by nitazoxanide exposure in all of the four tested strains/sub-strains. Examples of the differentially regulated genes included UTP14, UTP4, NOP4, UTP21, UTP6, and IMP3. The comparison between the M28-laden and non-M28-laden sub-strains showed that the mitotic cell cycle was more significantly affected by nitazoxanide exposure in the non-M28-laden sub-strain. Conclusions: Overall, our study reveals that nitazoxanide disrupts regulation of ribosome biogenesis-related genes in yeast.

Genes & Genomics published new progress about Cell cycle. 55981-09-4 belongs to class esters-buliding-blocks, name is 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, and the molecular formula is C12H9N3O5S, Related Products of esters-buliding-blocks.

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

Moghadam, S. Arbabi published the artcileCell death and survival due to cytotoxic exposure modelled as a two-state Ising system, Quality Control of 55981-09-4, the main research area is Ising system cell death survival cytotoxic exposure; Ising model; bystander effect; cancer cell response; cytotoxicity; phase transition.

Cancer chemotherapy agents are assessed for their therapeutic utility primarily by their ability to cause apoptosis of cancer cells and their potency is given by an IC50 value. Chemotherapy uses both target-specific and systemic-action drugs and drug combinations to treat cancer. It is important to judiciously choose a drug type, its dosage and schedule for optimized drug selection and administration. Consequently, the precise math. formulation of cancer cells’ response to chemotherapy may assist in the selection process. In this paper, we propose a math. description of the cancer cell response to chemotherapeutic agent exposure based on a time-tested phys. model of two-state multiple-component systems near criticality. We describe the Ising model methodol. and apply it to a diverse panel of cytotoxic drugs administered against numerous cancer cell lines in a dose- response manner. The analyzed dataset was generated by the Netherlands Translational Research Center B.V. (Oncolines). This approach allows for an accurate and consistent anal. of cytotoxic agents’ effects on cancer cell lines and reveals the presence or absence of the bystander effect through the interaction constant By calculating the susceptibility function, we see the value of IC50 coinciding with the peak of this measure of the system’s sensitivity to external perturbations.

Royal Society Open Science published new progress about Cell death. 55981-09-4 belongs to class esters-buliding-blocks, name is 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, and the molecular formula is C12H9N3O5S, Quality Control of 55981-09-4.

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

Lin, Yi-Sian published the artcileGWAS Meta-Analysis Reveals Shared Genes and Biological Pathways between Major Depressive Disorder and Insomnia, Product Details of C12H9N3O5S, the main research area is major depressive disorder insomnia gene biol pathway metaanalysis; GWAS; MDD; STRING; comorbidity; eQTL; gene network; insomnia; meta-analysis.

Major depressive disorder (MDD) is one of the most prevalent and disabling mental disorders worldwide. Among the symptoms of MDD, sleep disturbance such as insomnia is prominent, and the first reason patients may seek professional help. However, the underlying pathophysiol. of this comorbidity is still elusive. Recently, genome-wide association studies (GWAS) have begun to unveil the genetic background of several psychiatric disorders, including MDD and insomnia. Identifying the shared genomic risk loci between comorbid psychiatric disorders could be a valuable strategy to understanding their comorbidity. This study seeks to identify the shared genes and biol. pathways between MDD and insomnia based on their shared genetic variants. First, we performed a meta-anal. based on the GWAS summary statistics of MDD and insomnia obtained from Psychiatric Genomics Consortium and UK Biobank, resp. Next, we associated shared genetic variants to genes using two gene mapping strategies: (a) positional mapping based on genomic proximity and (b) expression quant. trait loci (eQTL) mapping based on gene expression linkage across multiple tissues. As a result, a total of 719 shared genes were identified. Over half (51%) of them are protein-coding genes. Functional enrichment anal. shows that the most enriched biol. pathways are related to epigenetic modification, sensory perception, and immunol. signatures. We also identified druggable targets using a network approach. Together, these results may provide insights into understanding the genetic predisposition and underlying biol. pathways of comorbid MDD and insomnia symptoms.

Genes published new progress about Cerebellum. 55981-09-4 belongs to class esters-buliding-blocks, name is 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, and the molecular formula is C12H9N3O5S, Product Details of C12H9N3O5S.

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

Mostafa, Ahmed published the artcileFDA-approved drugs with potent in vitro antiviral activity against severe acute respiratory syndrome coronavirus 2, Application of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is FDA drug potent antiviral agent SARSCoV2; COVID-19; SARS-CoV-2; antiviral; drug repurposing; virtual screening.

(1) Background: Drug repositioning is an unconventional drug discovery approach to explore new therapeutic benefits of existing drugs. Currently, it emerges as a rapid avenue to alleviate the COVID-19 pandemic disease. (2) Methods: Herein, we tested the antiviral activity of anti-microbial and anti-inflammatory Food and Drug Administration (FDA)-approved drugs, commonly prescribed to relieve respiratory symptoms, against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2), the viral causative agent of the COVID-19 pandemic. (3) Results: Of these FDA-approved antimicrobial drugs, Azithromycin, Niclosamide, and Nitazoxanide showed a promising ability to hinder the replication of a SARS-CoV-2 isolate, with IC50 of 0.32, 0.16, and 1.29 μM, resp. We provided evidence that several antihistamine and anti-inflammatory drugs could partially reduce SARS-CoV-2 replication in vitro. Furthermore, this study showed that Azithromycin can selectively impair SARS-CoV-2 replication, but not the Middle East Respiratory Syndrome Coronavirus (MERS-CoV). A virtual screening study illustrated that Azithromycin, Niclosamide, and Nitazoxanide bind to the main protease of SARS-CoV-2 (Protein data bank (PDB) ID: 6lu7) in binding mode similar to the reported co-crystalized ligand. Also, Niclosamide displayed hydrogen bond (HB) interaction with the key peptide moiety GLN: 493A of the spike glycoprotein active site. (4) Conclusions: The results suggest that Piroxicam should be prescribed in combination with Azithromycin for COVID-19 patients.

Pharmaceuticals published new progress about Analgesics. 55981-09-4 belongs to class esters-buliding-blocks, name is 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, and the molecular formula is C12H9N3O5S, Application of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate.

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

Guanabens, Nuria published the artcileTartrate-resistant acid phosphatase 5b, but not periostin, is useful for assessing Paget’s disease of bone, Synthetic Route of 55981-09-4, the main research area is Pagets disease bone osteoarthritis TRAPb periostin; Bone turnover markers; Paget’s disease of bone; Periostin; TRAP5b.

To analyze if circulating periostin is a biomarker for PDB, and if it is associated with disease activity and involvement of long bones that represent major cortical contribution. Also, to analyze whether TRAP5b, a scarcely explored bone resorption marker, is useful in the assessment of PDB. No significant differences were observed between patients with and without active disease (964.5 ± 168.8 vs.1051.6 ± 175.6 pMol/L, p = 0.143), involvement or not of long bones (1022.2 ± 145.8 vs 949.7 ± 198.2 pMol/L, p = 0.181) and monostotic or polyostotic disease (963.8 ± 198.7 vs 1002.2 ± 161.4 pMol/L, p = 0.505). There were significant correlations between serum periostin and all bone turnover markers (bone ALP, PINP, uNTX, sCTX and TRAP5b) in PDB patients with active disease, but not in the inactive PDB group. Serum TRAP5b was significantly higher in PDB patients than in controls (4.43 ± 1.76 vs. 3.21 ± 1.02 U/L, p < 0.001), in those with active disease (4.98 ± 1.76 vs. 3.07 ± 0.72 U/L, p < 0.001) and in patients with polyostotic disease than in those with monostotic disease (4.81 ± 1.79 vs 3.68 ± 1.5 U/L, p = 0.005). TRAP5b levels were not influenced by previous bisphosphonate treatment (4.14 ± 1.42 vs. 4.84 ± 2.02 U/L, p = 0.206). Periostin is not useful for assessing PDB, while TRAP5b, which has been a scarcely explored bone turnover marker until now, may be useful in the anal. of this disease, providing new information on the resorption process. States. Bone (New York, NY, United States) published new progress about Biomarkers. 55981-09-4 belongs to class esters-buliding-blocks, name is 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, and the molecular formula is C12H9N3O5S, Synthetic Route of 55981-09-4.

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

AbdelGhaffar, Muhammad M. published the artcilePrediction of mortality in hospitalized Egyptian patients with Coronavirus disease-2019: A multicenter retrospective study, Safety of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is prediction mortality human coronavirus disease.

A aimed to assess the epidemiol., clin., and laboratory characteristics associated with mortality among hospitalized Egyptian patients with COVID-19. A multicenter, retrospective study was conducted on all polymerase chain reaction (PCR)-confirmed COVID-19 cases admitted through the period from Apr. to July 2020. A generalized linear model was reconstructed with covariates based on predictor’s statistical significance and clin. relevance. The odds ratio (OR) was calculated by using stepwise logistic regression modeling. A total of 3712 hospitalized patients were included; of them, 900 deaths were recorded (24.2%). Compared to survived patients, non-survived patients were more likely to be older than 60 years (65.7%), males (53.6%) diabetic (37.6%), hypertensive (37.2%), and had chronic renal insufficiency (9%). Non-survived patients were less likely to receive azithromycin (p <0.001), anticoagulants (p <0.001), and steroids (p <0.001). In this found that age ≥ 60 years old (OR = 2.82, 95% CI 2.05-3.86; p <0.0001), diabetes mellitus (OR = 1.58, 95% CI 1.14-2.19; p = 0.006), hypertension (OR = 1.69, 95% CI 1.22-2.36; p = 0.002), chronic renal insufficiency (OR = 3.15, 95% CI 1.84-5.38; p <0.0001), tachycardia (OR = 1.65, 95% CI 1.22-2.23; p <0.001), hypoxemia (OR = 5.69, 95% CI 4.05-7.98; p <0.0001), GCS <13 (OR 515.2, 95% CI 148.5-1786.9; p <0.0001), the use of therapeutic dose of anticoagulation (OR = 0.4, 95% CI 0.22-0.74, p = 0.003) and azithromycin (OR = 0.16, 95% CI 0.09-0.26; p <0.0001) were independent neg. predictors of mortality. In conclusion, age >60 years, comorbidities, tachycardia, hypoxemia, and altered consciousness level are independent predictors of mortality among Egyptian hospitalized patients with COVID-19. On the other hand, the use of anticoagulants and azithromycin is associated with reduced mortality.

PLoS One published new progress about Age groups. 55981-09-4 belongs to class esters-buliding-blocks, name is 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, and the molecular formula is C12H9N3O5S, Safety of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate.

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

Cadegiani, F. A. published the artcileEarly COVID-19 therapy with azithromycin plus nitazoxanide, ivermectin or hydroxychloroquine in outpatient settings significantly improved COVID-19 outcomes compared to known outcomes in untreated patients, Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is azithromycin nitazoxanide ivermectin hydroxychloroquine COVID therapy human; Antiandrogen; COVID-19; SARS-CoV-2; clinical equipoise; dutasteride; hydroxychloroquine; ivermectin; nitazoxanide; proxalutamide; spironolactone.

In a prospective observational study (pre-AndroCoV Trial), the use of nitazoxanide, ivermectin and hydroxychloroquine demonstrated unexpected improvements in COVID-19 outcomes when compared to untreated patients. The apparent yet likely pos. results raised ethical concerns on the employment of further full placebo controlled studies in early-stage COVID-19. The present anal. aimed to elucidate, through a comparative anal. with two control groups, whether full placebo-control randomized clin. trials (RCTs) on early-stage COVID-19 are still ethically acceptable. The Active group (AG) consisted of patients enrolled in the Pre-AndroCoV-Trial (n = 585). Control Group 1 (CG1) consisted of a retrospectively obtained group of untreated patients of the same population (n = 137), and Control Group 2 (CG2) resulted from a precise prediction of clin. outcomes based on a thorough and structured review of indexed articles and official statements. Patients were matched for sex, age, comorbidities and disease severity at baseline. Compared to CG1 and CG2, AG showed reduction of 31.5-36.5% in viral shedding (p < 0.0001), 70-85% in disease duration (p < 0.0001), and 100% in respiratory complications, hospitalization, mech. ventilation, deaths and post-COVID manifestations (p < 0.0001 for all). For every 1000 confirmed cases for COVID-19, at least 70 hospitalizations, 50 mech. ventilations and five deaths were prevented. Benefits from the combination of early COVID-19 detection and early pharmacol. approaches were consistent and overwhelming when compared to untreated groups, which, together with the well-established safety profile of the drug combinations tested in the Pre-AndroCoV Trial, precluded our study from continuing employing full placebo in early COVID-19. New Microbes and New Infections published new progress about Age groups. 55981-09-4 belongs to class esters-buliding-blocks, name is 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, and the molecular formula is C12H9N3O5S, Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate.

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

Jaladanki, Chaitanya K. published the artcileReactive Metabolites from Thiazole-Containing Drugs: Quantum Chemical Insights into Biotransformation and Toxicity, Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is thiazole containing drug metabolite biotransformation toxicity.

Drugs containing thiazole and aminothiazole groups are known to generate reactive metabolites (RMs) catalyzed by cytochrome P450s (CYPs). These RMs can covalently modify essential cellular macromols. and lead to toxicity and induce idiosyncratic adverse drug reactions. Mol. docking and quantum chem. hybrid DFT study were carried out to explore the mol. mechanisms involved in the biotransformation of thiazole (TZ) and aminothiazole (ATZ) groups leading to RM epoxide, S-oxide, N-oxide, and oxaziridine. The energy barrier required for the epoxidation is 13.63 kcal/mol, that is lower than that of S-oxidation, N-oxidation, and oxaziridine formation (14.56, 17.90, and 20.20, kcal/mol resp.). The presence of the amino group in ATZ further facilitates all the metabolic pathways, for example, the barrier for the epoxidation reaction is reduced by ~2.5 kcal/mol. Some of the RMs/their isomers are highly electrophilic and tend to form covalent bonds with nucleophilic amino acids, finally leading to the formation of metabolic intermediate complexes (MICs). The energy profiles of these competitive pathways have also been explored.

Chemical Research in Toxicology published new progress about Alkylation. 55981-09-4 belongs to class esters-buliding-blocks, name is 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, and the molecular formula is C12H9N3O5S, Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate.

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

Xu, Jing published the artcileIn silico screening of potential anti-COVID-19 bioactive natural constituents from food sources by molecular docking, Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is human covid19 virus anticoronaviral agent mol docking; Angiotensin-converting enzyme 2; COVID-19; Chinese hawthorn and blackberry; Molecular docking; Red wine; SARS-CoV-2 3CL hydrolytic enzyme.

The aim of this study was to seek potential natural compounds that can resist COVID-19 using computer virtual screening technol. through mol. docking of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) 3CL hydrolytic enzyme (3CLpro) and angiotensin-converting enzyme 2 (ACE2). Mol. docking was achieved by using the Autodock Vina software. The natural phytocompounds acting on 3CLpro and ACE2 were then selected from the Traditional Chinese Medicine Systems Pharmacol. Database and Anal. Platform. This was followed by speculation on the mechanism of action of phytocompounds. Six potential natural anti-COVID-19 phytocompounds were selected and were evaluated for absorption, distribution, metabolism and excretion (ADME) and Lipinski rules. The content of the six phytocompounds in various fruits and vegetables was determined via a literature search. Red wine, Chinese hawthorn, and blackberry were recommended as supplements because they contained antiviral phytocompounds. Red wine, Chinese hawthorn, and blackberry show promise for resisting COVID-19 and are thus recommended as supplements to prevent the infection of COVID-19 during its outbreak period.

Nutrition (New York, NY, United States) published new progress about Adsorption. 55981-09-4 belongs to class esters-buliding-blocks, name is 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, and the molecular formula is C12H9N3O5S, Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate.

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

Marsaulina, Hutagaol Debora published the artcileApplication of ultraviolet spectrophotometry with dual wavelength method for the simultaneous determination of ecstasy tablet content, Computed Properties of 55981-09-4, the main research area is methylene dioxymetamphetamine methamphetamine aracetamol caffeine ephedrine dual wavelength method.

Ecstasy is a type of narcotic tablet and is very popularly used as a stimulant. The main content is Methylene dioxymetamphetamine (MDMA) and Methamphetamine (MA), but because a large amount of demand is not balanced with sufficient supply, ecstasy tablets are often adulterated with various contents, such as Paracetamol (PCT), Caffeine (KFN) and Ephedrine (EFD). Ecstasy tablets are often combined with other active compounds so that they can cause problems in determining the levels of tablets carried out in the Police Forensic Lab, so a cheaper, effective, and fast method is needed in determining the levels of these tablets. The research was conducted exptl. with the spectrophotometric method, namely the dual-wavelength method, then the validation was tested based on the validation parameters, namely linearity, accuracy, precision, LOD and LOQ. Then, this method was applied to determine levels of MA, EFD, KFN and PCT in tablet preparations The results showed that the application of the dual-wavelength method for the assay was carried out at λ 250.6 nm and 263 nm for KFN, at λ 263 nm and 281.8 nm for MA, at λ 259.4 nm and 255 nm for PCT at λ 255 nm and 236 nm for EFD, resp. with a level result of 40.05; 1.63; 38.11; 20.21 for MA, EFD, KFN and PCT resp., and with good precision and accuracy. The dual-wavelength UV spectrophotometric method was successfully applied to determine the levels of MA, EFD, KFN and PCT mixtures in tablets.

Asian Journal of Pharmaceutical Research and Development published new progress about Absorption. 55981-09-4 belongs to class esters-buliding-blocks, name is 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, and the molecular formula is C12H9N3O5S, Computed Properties of 55981-09-4.

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