Category: 55981-09-4

Dumond, Clement published the artcileEpidemiological and clinical study of microsporidiosis in French kidney transplant recipients from 2005 to 2019: TRANS-SPORE registry, SDS of cas: 55981-09-4, the main research area is microsporidiosis kidney transplant recipients Enterocytozoon bieneusi fumagillin; fumagillin; immunosuppressive regimen; kidney transplantation; microsporidiosis.

Introduction : Microsporidiosis is an emerging opportunistic infection in renal transplantation (RT) recipients. We aimed to describe its clin. presentation and treatment. Materials and methods : We collected microsporidiosis cases identified in RT recipients between 2005 and 2019 in six French centers from the Crystal, Divat and Astre prospective databases. Results : We report 68 RT recipients with intestinal microsporidiosis; the patients were predominantly male (61.8%), with a median age of 58 (46-69) years. Infection occurred at a median time of 3 (0.8-6.8) years posttransplant. Only Enterocytozoon bieneusi was found. Microsporidiosis manifested as diarrhea (98.5% of patients) with weight loss (72.1%) and acute renal injury (57.4%) without inflammatory biol. parameters. The therapeutic approaches were no treatment (N = 9), reduction of the immunosuppressive regimen (ΔIS) (N = 22), fumagillin alone (N = 9), fumagillin and ΔIS (N = 19), and albendazole or nitazoxanide and ΔIS (N = 9). Overall clin. remission was observed in 60 patients (88.2%). We observed no acute kidney rejection, renal transplant failure, or death within 6 mo after microsporidiosis. Conclusion : E. bieneusi is an underestimated opportunistic pathogen in RT recipients, and infection with E. bieneusi leads to diarrhea with important dehydration and acute renal injury. The treatment is based on the reduction of the immunosuppressive regimen and the administration of fumagillin if available.

Transplant Infectious Disease published new progress about Acute kidney injury. 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

Omolabi, Kehinde F. published the artcileA probable means to an end: exploring P131 pharmacophoric scaffold to identify potential inhibitors of Cryptosporidium parvum inosine monophosphate dehydrogenase, Name: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is P131 anticryptosporidial antimicrobial IMPDH inhibitor pharmacokinetic cryptosporidiosis Cryptosporidium; ADMET; Cryptosporidium parvum IMPDH; MM/PBSA; P131; Per-residue energy decomposition; Virtual screening.

Compound P131 has been established to inhibit Cryptosporidium parvum′s inosine monophosphate dehydrogenase (CpIMPDH). Its inhibitory activity supersedes that of paromomycin, which is extensively used in treating cryptosporidiosis. Through the per-residue energy decomposition approach, crucial moieties of P131 were identified and subsequently adopted to create a pharmacophore model for virtual screening in the ZINC database. This search generated eight ADMET-compliant hits that were examined thoroughly to fit into the active site of CpIMPDH via mol. docking. Three compounds ZINC46542062, ZINC58646829, and ZINC89780094, with favorable docking scores of – 8.3 kcal/mol, – 8.2 kcal/mol, and – 7.5 kcal/mol, were selected. The potential inhibitory mechanism of these compounds was probed using mol. dynamics simulation and Mol. Mechanics Generalized Poisson Boltzmann Surface Area (MM/PBSA) analyses. Results revealed that one of the hits (ZINC46542062) exhibited a lower binding free energy of – 39.52 kcal/mol than P131, which had – 34.6 kcal/mol. Conformational perturbation induced by the binding of the identified hits to CpIMPDH was similar to P131, suggesting a similarity in inhibitory mechanisms. Also, in silico investigation of the properties of the hit compounds implied superior physicochem. properties with regards to their synthetic accessibility, lipophilicity, and number of hydrogen bond donors and acceptors in comparison with P131. ZINC46542062 was identified as a promising hit compound with the highest binding affinity to the target protein and favorable physicochem. and pharmacokinetic properties relative to P131. The identified compounds can serve as a basis for conducting further exptl. investigations toward the development of anticryptosporidials, which can overcome the challenges of existing therapeutic options. Graphical abstractP131 and the identified compounds docked in the NAD+ binding site of Cryptosporidium parvum IMPDH .

Journal of Molecular Modeling published new progress about Antimicrobial agents. 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

Lima, William Gustavo published the artcileThe potential of drug repositioning as a short-term strategy for the control and treatment of COVID-19 (SARS-CoV-2): a systematic review, Related Products of esters-buliding-blocks, the main research area is potential drug repositioning short term strategy control treatment COVID.

Abstract: The novel human coronavirus (SARS-CoV-2), the causative agent of COVID-19, has quickly become a threat to the public health and economy worldwide. Despite the severity of some cases, there are no current pathogen-specific antivirals available to treat the disease. Therefore, many studies have focused on the evaluation of the anti-SARS-CoV-2 activity of clin. available drugs. Here, we conducted a systematic review to describe the drug repositioning strategy against SARS-CoV-2 and to discuss the clin. impact of this approach in the current pandemic context. The systematic review was performed on March 23, 2020, using PubMed/MEDLINE, Scopus, Cochrane Library, and Biblioteca Virtual de Saud́e (BVS). The data were summarized in tables and critically analyzed. After the database search, 12 relevant studies were identified as eligible for the review. Among the drugs reported in these studies, 57 showed some evidence of antiviral activity. Antivirals, especially antiretrovirals, are the main class of therapeutic agents evaluated against COVID-19. Moreover, studies have reported the anti-SARS-CoV-2 activity of antitumor (16%; 9/57), antimalarial (7%, 4/57), and antibacterial (5%; 3/57) agents. Addnl., seven pharmacol. agents (chloroquine, tetrandrine, umifenovir (arbidol), carrimycin, damageprevir, lopinavir/ritonavir) are in phase IV of clin. trials. Due to the evidence of the anti-SARS-CoV-2 activity of various clin. available agents, drug repositioning stands out as a promising strategy for a short-term response in the fight against the novel coronavirus.

Archives of Virology published new progress about Antibacterial agents. 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

Hooshmand, Seyed Aghil published the artcileA multimodal deep learning-based drug repurposing approach for treatment of COVID-19, Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is drug repurposing deep learning multimodal data fusion SARSCoV2 COVID19; COVID-19; Deep learning; Drug repurposing; Multimodal data fusion; Restricted Boltzmann machine.

Abstract: Recently, various computational methods have been proposed to find new therapeutic applications of the existing drugs. The Multimodal Restricted Boltzmann Machine approach (MM-RBM), which has the capability to connect the information about the multiple modalities, can be applied to the problem of drug repurposing. The present study utilized MM-RBM to combine two types of data, including the chem. structures data of small mols. and differentially expressed genes as well as small mols. perturbations. In the proposed method, two sep. RBMs were applied to find out the features and the specific probability distribution of each datum (modality). Besides, RBM was used to integrate the discovered features, resulting in the identification of the probability distribution of the combined data. The results demonstrated the significance of the clusters acquired by our model. These clusters were used to discover the medicines which were remarkably similar to the proposed medications to treat COVID-19. Moreover, the chem. structures of some small mols. as well as dysregulated genes’ effect led us to suggest using these mols. to treat COVID-19. The results also showed that the proposed method might prove useful in detecting the highly promising remedies for COVID-19 with min. side effects. All the source codes are accessible using https://github.com/LBBSoft/Multimodal-Drug-Repurposing.git Graphic abstract: [graphic not available: see fulltext].

Molecular Diversity published new progress about Algorithm (contrastive divergence, data reconstruction iterations). 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

Fahmy, Mennat-Elrahman Ahmed published the artcileAntiparasitic and immunomodulating effects of nitazoxanide, ivermectin and selenium on Cryptosporidium infection in diabetic mice., COA of Formula: C12H9N3O5S, the main research area is .

The present work aims to investigate the antiparasitic and the immunomodulating effects of nitazoxanide (NTZ) and ivermectin (IVC) alone or combined together or combined with selenium (Se), on Cryptosporidium infection in diabetic mice. The results revealed that the combined NTZ and IVC therapy achieved the highest reduction of fecal oocysts (92%), whereas single NTZ showed the lowest reduction (63%). Also, adding Se to either NTZ or IVC resulted in elevation of oocyst reduction from 63% to 71% and from 82% to 84% respectively. All treatment regimens, with the exception of NTZ monotherapy, showed a significant improvement in the intestinal histopathology, the highest score was in combined NTZ and IVC therapy. The unique results of immunohistochemistry in this study showed reversal of the normal CD4/CD8 T cell ratio in the infected untreated mice, however, following therapy it reverts back to a normal balanced ratio. The combined (NTZ+ IVC) treatment demonstrated the highest level of CD4 T cell expression. Taken together, NTZ and IVC combined therapy showed remarkable anti-parasitic and immunostimulatory effects, specifically towards the CD4 population that seem to be promising in controlling cryptosporidiosis in diabetic individuals. Further research is required to explore other effective treatment strategies for those comorbid patients.

Brazilian journal of veterinary parasitology 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, COA of Formula: C12H9N3O5S.

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

Parpia, Tarina C published the artcileBaseline Characteristics of Study Participants in the Early Life Interventions for Childhood Growth and Development in Tanzania (ELICIT) Trial., Application of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is .

Recurrent enteric infections and micronutrient deficiencies, including deficiencies in the tryptophan-kynurenine-niacin pathway, have been associated with environmental enteric dysfunction, potentially contributing to poor child growth and development. We are conducting a randomized, placebo-controlled, 2 × 2 factorial interventional trial in a rural population in Haydom, Tanzania, to determine the effect of 1) antimicrobials (azithromycin and nitazoxanide) and/or 2) nicotinamide, a niacin vitamer, on attained length at 18 months. Mother/infant dyads were enrolled within 14 days of the infant’s birth from September 2017 to September 2018, with the follow-up to be completed in February 2020. Here, we describe the baseline characteristics of the study cohort, risk factors for low enrollment weight, and neonatal adverse events (AEs). Risk factors for a low enrollment weight included being a firstborn child (-0.54 difference in weight-for-age z-score [WAZ] versus other children, 95% CI: -0.71, -0.37), lower socioeconomic status (-0.28, 95% CI: -0.43, -0.12 difference in WAZ), and birth during the preharvest season (November to March) (-0.22, 95% CI: -0.33, -0.11 difference in WAZ). The most common neonatal serious AEs were respiratory tract infections and neonatal sepsis (2.2 and 1.4 events per 100 child-months, respectively). The study cohort represents a high-risk population for whom interventions to improve child growth and development are urgently needed. Further analyses are needed to understand the persistent impacts of seasonal malnutrition and the interactions between seasonality, socioeconomic status, and the study interventions.

The American journal of tropical medicine and hygiene 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 of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate.

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

Shawky, D published the artcileNitazoxanide-based therapeutic regimen as a novel treatment for Helicobacter pylori infection in children and adolescents: a randomized trial., SDS of cas: 55981-09-4, the main research area is .

OBJECTIVE: Antibiotic resistance and poor patient compliance with treatment cause Helicobacter pylori to show increased resistance to typical first-line therapeutic regimens. This study aimed to evaluate the efficacy of the new nitazoxanide-based treatment regimens for Helicobacter pylori infection vs. the current metronidazole-based regimens to address the problem of increasing metronidazole resistance. PATIENTS AND METHODS: This randomized clinical trial enrolled 100 patients with Helicobacter pylori infection. The patients were randomly assigned to one of two groups: group I received nitazoxanide-based triple therapy (nitazoxanide, proton pump inhibitor, and clarithromycin) for 14 days, whereas group II received standard treatment (metronidazole, omeprazole, and clarithromycin) for 14 days. On enrollment and after six weeks of treatment, all patients underwent careful history taking, full clinical examination, laboratory investigations (complete blood count, liver and renal function tests), and Helicobacter pylori stool antigen testing. RESULTS: Of the patients, 92% in the nitazoxanide group and 84% in the metronidazole group recovered from infection, with no statistically significant difference between the two groups. Patients in the nitazoxanide group showed a 54% lower risk of resistant infection (odds ratio, 0.5; 95% confidence interval, 0.161-1.555) than those in the metronidazole group. CONCLUSIONS: The nitazoxanide-based therapeutic regimen produced higher eradication rates than the standard treatment. However, the difference was not substantial in this particular group of patients.

European review for medical and pharmacological sciences 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, SDS of cas: 55981-09-4.

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

Trivedi, N published the artcilePossible treatment and strategies for COVID-19: review and assessment., HPLC of Formula: 55981-09-4, the main research area is .

The coronavirus disease 2019 (COVID-19) is declared as an international emergency in 2020. Its prevalence and fatality rate are rapidly increasing but the medication options are still limited for this perilous disease. The emergent outbreak of COVID-19 triggered by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) keeps propagating globally. The present scenario has emphasized the requirement for therapeutic opportunities to relive and overcome this latest pandemic. Despite the fact, the deteriorating developments of COVID-19, there is no drug certified to have considerable effects in the medical treatment for COVID-19 patients. The COVID-19 pandemic requests for the rapid testing of new treatment approaches. Based on the evidence, hydroxychloroquine is the first medicine opted for the treatment of disease. Umifenovir, remdesivir, and fevipiravir are deemed the most hopeful antiviral agent by improving the health of infected patients. The dexamethasone is a first known steroid medicine that can save the lives of seriously ill patients, and it is shown in a randomized clinical trial by the United Kingdom that it reduced the death rate in COVID-19 patients. The current review recapitulates the existing evidence of possible therapeutic drugs, peptides, humanized antibodies, convulsant plasma, and vaccination that has revealed potential in fighting COVID-19 infections. Many randomized and controlled clinical trials are taking place to further validate these agent’s safety and effectiveness in curing COVID-19.

European review for medical and pharmacological sciences 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, HPLC of Formula: 55981-09-4.

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

Walker, Lauren E. published the artcileAn Open Label, Adaptive, Phase 1 Trial of High-Dose Oral Nitazoxanide in Healthy Volunteers: An Antiviral Candidate for SARS-CoV-2, Safety of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is .

Repurposing approved drugs may rapidly establish effective interventions during a public health crisis. This has yielded immunomodulatory treatments for severe coronavirus disease 2019 (COVID-19), but repurposed antivirals have not been successful to date because of redundancy of the target in vivo or suboptimal exposures at studied doses. Nitazoxanide is a US Food and Drug Administration (FDA) approved antiparasitic medicine, that physiol.-based pharmacokinetic (PBPK) modeling has indicated may provide antiviral concentrations across the dosing interval, when repurposed at higher than approved doses. Within the AGILE trial platform (NCT04746183) an open label, adaptive, phase I trial in healthy adult participants was undertaken with high-dose nitazoxanide. Participants received 1500 mg nitazoxanide orally twice-daily with food for 7 days. Primary outcomes were safety, tolerability, optimum dose, and schedule. Intensive pharmacokinetic (PK) sampling was undertaken day 1 and 5 with min. concentration (Cmin) sampling on days 3 and 7. Fourteen healthy participants were enrolled between Feb. 18 and May 11, 2021. All 14 doses were completed by 10 of 14 participants. Nitazoxanide was safe and with no significant adverse events. Moderate gastrointestinal disturbance (loose stools or diarrhea) occurred in 8 participants (57.1%), with urine and sclera discoloration in 12 (85.7%) and 9 (64.3%) participants, resp., without clin. significant bilirubin elevation. This was self-limiting and resolved upon drug discontinuation. PBPK predictions were confirmed on day 1 but with underprediction at day 5. Median Cmin was above the in vitro target concentration on the first dose and maintained throughout. Nitazoxanide administered at 1,500 mg b.i.d. with food was safe with acceptable tolerability a phase Ib/IIa study is now being initiated in patients with COVID-19.

Clinical Pharmacology & Therapeutics (Hoboken, NJ, United States) 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, Safety of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate.

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

Castillo-Salazar, Mauricio published the artcileNitazoxanide Exerts Immunomodulatory Effects on Peripheral Blood Mononuclear Cells from Type 2 Diabetes Patients, Application of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is T2D; immunomodulation; inflammation; miRNAs; nitazoxanide.

Background: Type 2 diabetes (T2D) is a low-grade inflammatory condition with abnormalities in the immune response mediated by T lymphocytes and macrophages. Drug repositioning for immunomodulatory mols. is an attractive proposal for treating T2D. Nitazoxanide (NTZ) is a broad-spectrum drug with promising immunomodulatory effects. Thus, we investigated the immunomodulatory effect of NTZ on peripheral blood mononuclear cells (PBMCs) from patients with T2D. Methods: Fifty patients with T2D were selected, and the proliferative response of T lymphocytes and the M1/M2 ratio of macrophages post cell culture were evaluated by flow cytometry, as well as measuring the concentration of cytokines by ELISA and the relative expression of microRNAs (miRNAs) related to the immune response by real-time PCR. Results: NTZ exerts an inhibitory effect on the cell proliferation of T lymphocytes stimulated with anti-CD3 and anti-CD28 antibodies without modifying cell viability, and significant decreases in the supernatant concentrations of interleukin (IL)-1β, IL-2, IL-6, IL-10, and IL-12. Furthermore, NTZ neg. regulates the relative expression of miR-155-5p without changes in miR-146a-5p. The M1/M2 ratio of monocytes/macrophages decreased the M1 and increased the M2 subpopulation by NTZ. Conclusions: Our results suggest that NTZ exerts immunomodulatory effects on PBMCs from T2D patients, and shows potential alternative therapeutic benefits.

Biomolecules published new progress about T2D; immunomodulation; inflammation; miRNAs; 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