Category: 55981-09-4

Auer, Michael published the artcileSoluble Vascular Cell Adhesion Molecule-1 (sVCAM-1) and Natalizumab Serum Concentration as Potential Biomarkers for Pharmacodynamics and Treatment Response of Patients with Multiple Sclerosis Receiving Natalizumab., Category: esters-buliding-blocks, the main research area is .

BACKGROUND: Natalizumab (NTZ) is an established treatment for highly active, relapsing-remitting multiple sclerosis. In the context of rare progressive multifocal leukoencephalopathy and extended interval dosing as a treatment option, biomarkers for treatment monitoring are required. Natalizumab serum concentration (NTZ SC) and soluble vascular cell adhesion molecule 1 (sVCAM-1) concentration were shown to change on treatment with NTZ. We aimed to investigate whether NTZ SC and sVCAM-1 could be suitable pharmacodynamic markers and whether they could predict disease activity on NTZ, improving the concept of personalized multiple sclerosis treatment. METHODS: In a retrospective study at the Medical University of Innsbruck, Austria, we identified patients treated with NTZ and chose samples longitudinally collected during routine follow-ups for the measurement of NTZ SC and sVCAM-1 by an enzyme-linked immunosorbent assay. We correlated these with clinical and demographic variables and clinical outcomes. Furthermore, we analyzed the stability of NTZ SC and sVCAM-1 during treatment. RESULTS: One hundred and thirty-seven patients were included. We found a strong negative correlation between NTZ SC and sVCAM-1. Both showed significant associations with body mass index, infusion interval, sample age, and anti-drug-antibodies. Natalizumab serum concentration was reduced in extended interval dosing, but not sVCAM-1. Only sVCAM-1 showed a weak association with relapses during treatment, while there was no association with disease progression. Both NTZ SC and sVCAM-1 showed a wide inter-individual distribution while levels in single patients were stable on treatment. CONCLUSIONS: Soluble vascular cell adhesion molecule 1 is a suitable pharmacodynamic marker during treatment with NTZ, which is significantly reduced already after the first dose, remains stable in individual patients even on extended interval dosing, and strongly correlates with NTZ SC. Because of the high inter-individual range, absolute levels of sVCAM-1 and NTZ SC are difficult to introduce as treatment monitoring biomarkers in order to predict disease activity in single patients.

CNS drugs published new progress in MEDLINE about 55981-09-4, 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, Category: esters-buliding-blocks.

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

DeBoer, Mark D. published the artcileEffect of scheduled antimicrobial and nicotinamide treatment on linear growth in children in rural Tanzania: A factorial randomized, double-blind, placebo-controlled trial, Name: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is .

Background: Stunting among children in low-resource settings is associated with enteric pathogen carriage and micronutrient deficiencies. Our goal was to test whether administration of scheduled antimicrobials and daily nicotinamide improved linear growth in a region with a high prevalence of stunting and enteric pathogen carriage. Methods and findings: We performed a randomized, 2 x 2 factorial, double-blind, placebo-controlled trial in the area around Haydom, Tanzania. Mother-child dyads were enrolled by age 14 days and followed with monthly home visits and every 3-mo anthropometry assessments through 18 mo. Those randomized to the antimicrobial arm received 2 medications (vs. corresponding placebos): azithromycin (single dose of 20 mg/kg) at months 6, 9, 12, and 15 and nitazoxanide (3-day course of 100 mg twice daily) at months 12 and 15. Those randomized to nicotinamide arm received daily nicotinamide to the mother (250 mg pills months 0 to 6) and to the child (100 mg sachets months 6 to 18). Primary outcome was length-for-age z-score (LAZ) at 18 mo in the modified intention-to-treat group. Between Sept. 5, 2017 and August 31, 2018, 1,188 children were randomized, of whom 1,084 (n = 277 placebo/placebo, 273 antimicrobial/placebo, 274 placebo/nicotinamide, and 260 antimicrobial/nicotinamide) were included in the modified intention-to-treat anal. The study was suspended for a 3-mo period by the Tanzanian National Institute for Medical Research (NIMR) because of concerns related to the timing of laboratory testing and the total number of serious adverse events (SAEs); this resulted in some participants receiving their final study assessment late. There was a high prevalence of stunting overall (533/1,084, 49.2%). Mean 18-mo LAZ did not differ between groups for either intervention (mean LAZ with 95% confidence interval [CI]: antimicrobial: -2.05 CI -2.13, -1.96, placebo: -2.05 CI -2.14, -1.97; mean difference: 0.01 CI -0.13, 0.11, p = 0.91; nicotinamide: -2.06 CI -2.13, -1.95, placebo: -2.04 CI -2.14, -1.98, mean difference 0.03 CI -0.15, 0.09, p = 0.66). There was no difference in LAZ for either intervention after adjusting for possible confounders (baseline LAZ, age in days at 18-mo measurement, ward, hospital birth, birth month, years of maternal education, socioeconomic status (SES) quartile category, sex, whether the mother was a member of the Datoga tribe, and mother’s height). Adverse events (AEs) and SAEs were overall similar between treatment groups for both the nicotinamide and antimicrobial interventions. Key limitations include the absence of laboratory measures of pathogen carriage and nicotinamide metabolism to provide context for the neg. findings. Conclusions: In this study, we observed that neither scheduled administration of azithromycin and nitazoxanide nor daily provision of nicotinamide was associated with improved growth in this resource-poor setting with a high force of enteric infections. Further research remains critical to identify interventions toward improved early childhood growth in challenging conditions. Trial registration: ClinicalTrials.gov NCT03268902.

PLoS Medicine published new progress in CAplus and MEDLINE about 55981-09-4, 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, Name: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate.

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

de Jesus, Joao Paulo Almirao published the artcileEffect of drug metabolism in the treatment of SARS-CoV-2 from an entirely computational perspective, SDS of cas: 55981-09-4, the main research area is .

Abstract: Understanding the effects of metabolism on the rational design of novel and more effective drugs is still a considerable challenge. To the best of our knowledge, there are no entirely computational strategies that make it possible to predict these effects. From this perspective, the development of such methodologies could contribute to significantly reduce the side effects of medicines, leading to the emergence of more effective and safer drugs. Thereby, in this study, our strategy is based on simulating the electron ionization mass spectrometry (EI-MS) fragmentation of the drug mols. and combined with mol. docking and ADMET models in two different situations. In the first model, the drug is docked without considering the possible metabolic effects. In the second model, each of the intermediates from the EI-MS results is docked, and metabolism occurs before the drug accesses the biol. target. As a proof of concept, in this work, we investigate the main antiviral drugs used in clin. research to treat COVID-19. As a result, our strategy made it possible to assess the biol. activity and toxicity of all potential byproducts. We believed that our findings provide new chem. insights that can benefit the rational development of novel drugs in the future.

Scientific Reports published new progress in CAplus and MEDLINE about 55981-09-4, 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, SDS of cas: 55981-09-4.

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

Escobedo, Angel A published the artcileEfficacy of 5-nitroimidazole compounds for giardiasis in Cuban children: systematic review and meta-analysis., Category: esters-buliding-blocks, the main research area is .

Five-nitroimidazole (5-NI) compounds are among the most commonly used medications in the treatment of giardiasis. However, after more than five decades of their initial indication for such treatment, there are some concerns about the efficacy of 5-NIs in giardiasis. This study sought to compare the efficacy of any 5-NI with any other antigiardial drug for the treatment of Cuban children with giardiasis. We conducted a systematic review and meta-analysis of randomized controlled trials (RCTs). We searched CUMED, EBSCOhost and PubMed databases. Two reviewers independently assessed trial eligibility, trial quality and extracted appropriate data. The primary outcome was the parasitological cure. The effect estimate was the pooled relative risk (RR) with 95% confidence intervals (CI). We included seven RCTs in the systematic review, involving a total of 1046 children. When the effect of 5-NIs was compared with that of benzimidazole compounds, the pooled effect was significant and favored 5-NIs [the relative risk (RR) is 1.35, 95% CI =1.05 to 1.75], with high heterogeneity (4 studies, I2 =79%). Compared with chloroquine, the pooled effects of the 5-NIs were not significant [RR is 0.96, 95% CI=0.79 to 1.18, (2 studies, I2=68%)]. Our results support the use of 5-NIs (mainly tinidazole) as first-line therapy for Cuban pediatric patients infected with Giardia and may continue being used as reference drugs in future RCTs of giardiasis. These data could help inform policy decisions in Cuba. Caution is needed in extrapolating such data in other settings.

Le infezioni in medicina published new progress in MEDLINE about 55981-09-4, 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, Category: esters-buliding-blocks.

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

Iza, José A published the artcileGiardiasis: report of a case refractory to treatment., Formula: C12H9N3O5S, the main research area is .

Caused by the protozoan Giardia lamblia, giardiasis is one of the most common parasitic diarrheal infections affecting humans. Although a variety of antigiardial drugs are available to treat infections in humans, failure of conventional treatment with nitroimidazoles for giardiasis has been increasingly reported. We describe the follow-up of a patient with recurrent giardiasis refractory to nitroimidazoles. Despite the different therapies received, the symptomatology and parasitic forms of G. lamblia persisted in the patient. There is no standard treatment regimen for giardiasis refractory to nitroimidazoles. When treatment failure is confirmed, it is necessary to switch to second-line regimens.

Le infezioni in medicina published new progress in MEDLINE about 55981-09-4, 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, Formula: C12H9N3O5S.

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

Ashigbie, Paul G published the artcileUse-case scenarios for an anti-Cryptosporidium therapeutic., Application In Synthesis of 55981-09-4, the main research area is .

Cryptosporidium is a widely distributed enteric parasite that has an increasingly appreciated pathogenic role, particularly in pediatric diarrhea. While cryptosporidiosis has likely affected humanity for millennia, its recent “”emergence”” is largely the result of discoveries made through major epidemiologic studies in the past decade. There is no vaccine, and the only approved medicine, nitazoxanide, has been shown to have efficacy limitations in several patient groups known to be at elevated risk of disease. In order to help frontline health workers, policymakers, and other stakeholders translate our current understanding of cryptosporidiosis into actionable guidance to address the disease, we sought to assess salient issues relating to clinical management of cryptosporidiosis drawing from a review of the literature and our own field-based practice. This exercise is meant to help inform health system strategies for improving access to current treatments, to highlight recent achievements and outstanding knowledge and clinical practice gaps, and to help guide research activities for new anti-Cryptosporidium therapies.

PLoS neglected tropical diseases published new progress in MEDLINE about 55981-09-4, 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 In Synthesis of 55981-09-4.

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

Kaul, Grace published the artcileNitazoxanide potentiates linezolid against linezolid-resistant Staphylococcus aureus in vitro and in vivo., Computed Properties of 55981-09-4, the main research area is .

BACKGROUND: Antimicrobial resistance is a growing menace, claiming millions of lives all over the world. In this context, drug repurposing is one approach gaining interest as a suitable alternative to conventional drug discovery and development. METHODS: Whole-cell assays were used to screen FDA-approved drugs to identify novel antimicrobial agents active against bacterial pathogens. Following identification of nitazoxanide, its various characteristics, such as antimicrobial activity against MDR isolates, time-kill kinetics, ability to synergize with approved drugs, antibiofilm activity and ability to generate resistance in Staphylococcus aureus, were determined, followed by determination of its in vivo potential against MDR S. aureus. RESULTS: Nitazoxanide demonstrated a potent in vitro antistaphylococcal profile, including equipotent activity against clinical drug-resistant S. aureus and Enterococcus spp. Nitazoxanide exhibited concentration-dependent killing, significantly eradicated preformed S. aureus biofilm and S. aureus did not generate resistance to it. Nitazoxanide strongly synergized with linezolid both in vitro and in vivo against linezolid-susceptible and -resistant S. aureus, displaying superior activity to untreated control and drug-alone treatment groups. CONCLUSIONS: Nitazoxanide can be utilized in combination with linezolid against infections caused by linezolid-resistant S. aureus as it exhibits strong synergism in vitro and in vivo.

The Journal of antimicrobial chemotherapy published new progress in MEDLINE about 55981-09-4, 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

Li, Jinyi published the artcileNitazoxanide in the Treatment of Intestinal Parasitic Infections in Children: A Systematic Review and Meta-Analysis., Application of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is Children; Intestinal parasitic infections; Meta-analysis; Nitazoxanide.

OBJECTIVES: To evaluate the efficacy and safety of nitazoxanide in intestinal parasitic infections in children. METHODS: Four databases, PubMed, EMBASE, Web of Science and Cochrane Library, have been systematically searched from the inception of each database up to March 1st, 2019. The enrolled studies were limited to randomized clinical trials in children, comparing nitazoxanide with placebo or other antiparasitic drugs. The data extraction and quality assessment of pooled studies were conducted by two reviewers independently. For meta-analysis, Stata12.0 was used and a randomized effect model or a fixed effect model was selected according to the outcomes of heterogeneity test. RESULTS: A total of 1645 subjects in 13 randomized controlled trials (RCTs) were enrolled, including 768 cases in the trial group and 877 cases in the control group. The effect of nitazoxanide vs. placebo and other antiparasitic drugs on the excretion rate of pathogens was uncertain (OR = 2.06, 95%CI [1.01,4.20], P = 0.047; I2 = 84.7%; very low quality evidence). Compared with placebo, subgroup analysis suggested that nitazoxanide could significantly improve the excretion rate of pathogens (OR = 7.01, 95%CI [1.82,26.94], P = 0.005; I2 = 79.1%; moderate quality evidence), while it made little or no difference compared with antiparasitic drugs (OR = 0.72, 95%CI [0.47,1.09], P = 0.124; I2 = 33.1%; low quality evidence). Meanwhile, nitazoxanide might increase the remission rate of diarrhea with OR = 5.12, 95%CI [2.00,13.08], P = 0.001; I2 = 72.3%; low quality evidence). However, it might also increase the rate of adverse events (OR = 1.47, 95%CI [1.05,2.07], P = 0.026; I2 = 44.7%; low quality evidence). CONCLUSIONS: The authors are uncertain whether or not nitazoxanide could improve the excretion rate of pathogens. Based on low-certainty evidence, nitazoxanide may improve the remission rate of diarrhea in children with intestinal parasite infections, but it may be associated with an increased risk of adverse reactions. Hence, more RCTs with a low risk of bias are still needed to assess the efficacy and safety of nitazoxanide.

Indian journal of pediatrics published new progress about Children; Intestinal parasitic infections; Meta-analysis; Nitazoxanide. 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

Abdel-Lateef, Mohamed A. published the artcileA specific turn-on fluorescence probe for determination of nitazoxanide based on feasible oxidation reaction with hypochlorite: Applying cobalt ferrite nanoparticles for pre-concentration and extraction of its metabolite from real urine samples, COA of Formula: C12H9N3O5S, the main research area is Cobalt ferrite NPs; Nitazoxanide; Sodium hypochlorite; Spectrofluorimetry; Tizoxanide; Urine analysis.

Nitazoxanide is an antimicrobial compound that was originally developed as an antiprotozoal drug. Recently nitazoxanide has been identified as broad-spectrum antiviral agent and redirected for the remediation of some respiratory tract viral infections. In this study, the spectrofluorimetric technique has been applied to determine Nitazoxanide (NTX) in tablets or its metabolite, tizoxanide (TZD), in human urine samples. The developed methodol. is based on oxidizing NTX (non-fluorescence) into a highly fluorescent product by sodium hypochlorite. The fluorescence emission intensity was measured at 436.5 nm after fluorescence excitation at 362.5 nm. After optimizing all conditions, the anal. procedures and bio-anal. steps were evaluated and validated using ICH and FDA criteria, resp. The method linearity, LOQ, and LOD values of NTX were 1.0-5.0 μg/mL, 0.434, and 0.143 μg/mL, resp. The other novelty side of the presented work is the application of cobalt ferrite (CoFe2O4) nanoparticles (NPs) as a magnetic solid-phase for the pre-concentration and extraction process. The synthesized magnetic nanoparticles were characterized by scanning electron microscope and zeta sizer techniques. Finally, the utilized magnetic nanoparticles exhibited good recovery results for pre-concentration and extraction of NTX or its metabolite from spiked and real human urine samples, resp.

Journal of Pharmaceutical and Biomedical Analysis published new progress about Cobalt ferrite NPs; Nitazoxanide; Sodium hypochlorite; Spectrofluorimetry; Tizoxanide; Urine analysis. 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, COA of Formula: C12H9N3O5S.

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

Yadav, Ambedkar Kumar published the artcileAntiviral treatment in COVID-19: which is the most promising?-a narrative review., Name: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is Coronavirus disease 2019 (COVID-19); antiviral; coronavirus; severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2); therapeutic agents; treatment.

The whole world is battling through coronavirus disease 2019 (COVID-19) which is a fatal pandemic. In the early 2020, the World Health Organization (WHO) declared it as a global health emergency without definitive treatments and preventive approaches. In the absence of definitive therapeutic agents, this thorough review summarizes and outlines the potency and safety of all molecules and therapeutics which may have potential antiviral effects. A number of molecules and therapeutics licensed or being tested for some other conditions were found effective in different in vitro studies as well as in many small sample-sized clinical trials and independent case studies. However, in those clinical trials, there were some limitations which need to be overcome to find the most promising antiviral against severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). In conclusion, many of above-mentioned antivirals seems to have some therapeutic effects but none of them have been shown to have a strong evidence for their proper recommendation and approval in the treatment of COVID-19. Constantly evolving new evidences, exclusive adult data, language barrier, and type of study (observational, retrospective, small-sized clinical trials, or independent case series) resulted to the several limitations of this review. The need for multicentered, large sample-sized, randomized, placebo-controlled trials on COVID-19 patients to reach a proper conclusion on the most promising antiviral agent is warranted.

Annals of palliative medicine published new progress about Coronavirus disease 2019 (COVID-19); antiviral; coronavirus; severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2); therapeutic agents; treatment. 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, Name: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate.

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