Category: 55981-09-4

Sgarlata, Eleonora published the artcileChanges in John Cunningham Virus Index in Multiple Sclerosis Patients Treated with Different Disease-Modifying Therapies., Computed Properties of 55981-09-4, the main research area is B cells depleting drugs; JCV index; Multiple sclerosis; PML risk; T cells depleting drugs; disease-modifying therapies; treatment strategy.

BACKGROUND: Progressive Multifocal Leukoencephalopathy (PML) is an opportunistic infection caused by John Cunningham virus (JCV) reactivation, potentially associated with natalizumab (NTZ) treatment for Multiple Sclerosis (MS). The anti-JCV antibodies titre (JCV index) increases during NTZ treatment; however, the effects of other disease-modifying therapies (DMTs) on the JCV index have not been fully explored. OBJECTIVE: The aim of the study was to evaluate changes in the JCV index during treatment with several DMTs. METHODS: This longitudinal study evaluated the JCV index before starting DMT (T0) and during treatment with DMT (T1). RESULTS: A total of 260 participants (65.4 % females, mean age 43 ± 11.3 ) were enrolled: 68 (26.2 %) treated with fingolimod (FTY), 65 (25 %) rituximab or ocrelizumab (RTX/OCR), 37 (14.2 %) dimethyl-fumarate (DMF), 29 (11.2 %) cladribine (CLD), 23 (8.8 %) teriflunomide (TFM), 20 (7.7 %) interferon or glatiramer acetate (IFN/GA), and 18 (6.9 %) alemtuzumab (ALM). At T1, the percentage of patients with JCV index <0.90 was found to be significantly increased in the ALM group (16.7 % versus 66.7 %, p = 0.05), while the percentage of patients with JCV index >1.51 was found to be significantly reduced in the RTX/OCR group (51.6 % versus 37.5 %, p = 0.04). In the FTY group, a significant reduction in the percentage of patients with JCV index <0.90 was also found (23.5 % versus 1.4 %, p = 0.0006). The mean JCV index was reduced in the RTX/OCR and ALM groups, while a significant increase was observed in the FTY group. CONCLUSION: DMTs with a T and/or B depleting mechanism of action induced a significant reduction in the JCV index. These results may suggest new possible sequencing strategies potentially maximizing disease control while reducing the PML risk. Current neuropharmacology published new progress about B cells depleting drugs; JCV index; Multiple sclerosis; PML risk; T cells depleting drugs; disease-modifying therapies; treatment strategy. 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

Walsh, K. F. published the artcileEarly bactericidal activity trial of nitazoxanide for pulmonary tuberculosis, Product Details of C12H9N3O5S, the main research area is bactericidal activity; nitazoxanide; tuberculosis.

This study was conducted in treatment-naive adults with drug-susceptible pulmonary tuberculosis in Port-au-Prince, Haiti, to assess the safety, bactericidal activity, and pharmacokinetics of nitazoxanide (NTZ). This was a prospective phase II clin. trial in 30 adults with pulmonary tuberculosis. Twenty participants received 1 g of NTZ orally twice daily for 14 days. A control group of 10 participants received standard therapy over 14 days. The primary outcome was the change in time to culture positivity (TTP) in an automated liquid culture system. The most common adverse events seen in the NTZ group were gastrointestinal complaints and headache. The mean change in TTP in sputum over 14 days in the NTZ group was 3.2 h 22.6 h and was not statistically significant (P = 0.56). The mean change in TTP in the standard therapy group was significantly increased, at 134 h 45.2 h (P = 0.0001). The mean NTZ MIC for Mycobacterium tuberculosis isolates was 12.3 g/mL; the mean NTZ maximum concentration (Cmax) in plasma was 10.2g/mL. Negligible NTZ levels were measured in sputum. At the doses used, NTZ did not show bactericidal activity against M. tuberculosis. Plasma concentrations of NTZ were below the MIC, and its negligible accumulation in pulmonary sites may explain the lack of bactericidal activity. (This study has been registered at ClinicalTrials.gov under identifier NCT02684240.)

Antimicrobial Agents and Chemotherapy published new progress about bactericidal activity; nitazoxanide; tuberculosis. 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

Glal, Khadija A M published the artcileNitazoxanide versus rifaximin in preventing the recurrence of hepatic encephalopathy: A randomized double-blind controlled trial., Formula: C12H9N3O5S, the main research area is CHESS; hepatic encephalopathy; nitazoxanide; octopamine; quality of life.

BACKGROUND/PURPOSE: Hepatic encephalopathy (HE) is a neuropsychiatric complication of liver cirrhosis. HE is associated with poor survival and detrimental effects on quality of life (QOL). The drawbacks of the long-term use of rifaximin in HE necessitates searching for alternative therapies. In this context, our study aimed at evaluating the safety and efficacy of nitazoxanide (NTZ) as compared to rifaximin (RFX) in preventing the recurrence of HE and assessing its impact on QOL. PATIENTS AND METHODS: This prospective, randomized, double-blind controlled study included 60 patients who were randomly assigned to receive either rifaximin 550 mg twice daily (group 1; n = 30) or nitazoxanide 500 mg twice daily (group 2; n = 30) for 24 weeks. During the study period, the patients’ neurological symptoms, mental status, and performance were monitored. The serum levels of HE triggers (ammonia, TNF-α, and octopamine) were assessed. The patients’ health-related quality of life was also evaluated. RESULTS: Six months after treatment, patients on NTZ therapy showed a statistically significant improvement in CHESS score and mental status. NTZ provided 136 days of remission vs 67 days of remission for patients on RFX (P1  = .0001) and significant reduction in Child score (P1  = .018). Additionally, NTZ showed a statistically significant decrease in serum ammonia, TNF-α, and octopamine levels as compared to rifaximin. Regarding QOL, NTZ group showed an improvement in total Chronic Liver Disease Questionnaire (CLDQ) score. Both groups experienced minor controllable side effects. CONCLUSION: Nitazoxanide may represent a suitable and safe alternative therapy to rifaximin in preventing the recurrence of hepatic encephalopathy.

Journal of hepato-biliary-pancreatic sciences published new progress about CHESS; hepatic encephalopathy; nitazoxanide; octopamine; quality of life. 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

Rahman, Sajid Ur published the artcileAdvances in therapeutic and vaccine targets for Cryptosporidium: Challenges and possible mitigation strategies, Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is review cryptosporidiosis Cryptosporidium vaccine nitazoxanide genome immunity; Cryptosporidium; Diarrhea; Mitigation plans; Nitazoxanide; Vaccine targets.

Cryptosporidium is known to be the second most common diarrheal pathogen in children, causing potentially fatal diarrhea and associated with long-term growth stunting and cognitive deficits. The only Food and Drug Administration-approved treatment for cryptosporidiosis is nitazoxanide, but this drug has not shown potentially effective results in susceptible hosts. Therefore, a safe and effective drug for cryptosporidiosis is urgently needed. Cryptosporidium genome sequencing anal. may help develop an effective drug, but both in vitro and in vivo approaches to drug evaluation are not fully standardized. On the other hand, the development of partial immunity after exposure suggests the possibility of a successful and effective vaccine, but protective surrogates are not precise. In this review, we present our current perspectives on novel cryptosporidiosis therapies, vaccine targets and efficacies, as well as potential mitigation plans, recommendations and perceived challenges.

Acta Tropica published new progress about Cognition. 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

Kelleni, Mina T. published the artcileNSAIDs and Kelleni′s protocol as potential early COVID-19 treatment game changer: could it be the final countdown, SDS of cas: 55981-09-4, the main research area is review asprin triggered lipoxin resolvin benefit; Apoptosis; Aspirin; Azithromycin; COVID-19; Caspases; Endoplasmic reticulum stress; Kelleni’s protocol; NSAIDs; Nitazoxanide; SARS-CoV-2.

A review on previously published several papers illustrating numerous immunomodulatory and anti-inflammatory potential benefits when we repurposed safe, generic non-steroidal anti-inflammatory drugs (NSAIDs)/nitazoxanide/azithromycin (Kellenis protocol), to early manage our COVID-19 pediatric, adult, and pregnant patients. In this manuscript, we discuss some recently published meta-anal. and clin. studies supporting our practice and discuss a mol. study that might be interpreted as an academic proof that our protocol might also prevent SARS-CoV-2 replication. Moreover, after aspirin has been suggested to be independently associated with reduced risk of mech. ventilation, ICU admission and in-hospital mortality of COVID-19, we claim that the mol. interpretation of the results that led to this suggestion was not scientifically accurate, and we provide our academic interpretation confirming that low-dose aspirin is least likely to improve COVID-19 mortality through anticoagulation as was suggested. Furthermore, we describe other potential benefits related to aspirin-triggered lipoxins and resolvins while illustrating how NSAIDs interfere with COX-1, COX-2, SARS-CoV-2/ SARS-CoV-2 ORF protein-dependent activation of caspases and their subsequent mitochondrial dysfunction, endoplasmic reticulum stress, apoptosis and necroptosis which were associated with COVID-19 complications. Similarly, NSAIDs are known caspase inhibitors and thus they might independently inhibit other caspase-related COVID-19-associated downstream pathol. signaling mechanisms. Finally, we postulated that CARD-14, a caspase recruitment domain-containing protein, polymorphisms might play a role in the development of severe and critical COVID-19 and confirmed our old call to early adopt NSAIDs, as an integral part of Kellenis protocol, as of choice in its management aiming to end this pandemic.

Inflammopharmacology published new progress about Apoptosis. 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

Verma, Akalesh Kumar published the artcileRepurposing potential of FDA-approved and investigational drugs for COVID-19 targeting SARS-CoV-2 spike and main protease and validation by machine learning algorithm, Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is drug repurposing COVID 19 coronavirus spike glycoprotein protease inhibitor; 2019nCov; antiviral drugs; cordycepin; coronavirus; drug repurposing.

The present study aimed to assess the repurposing potential of existing antiviral drug candidates (FDA-approved and investigational) against SARS-CoV-2 target proteins that facilitates viral entry and replication into the host body. To evaluate mol. affinities between antiviral drug candidates and SARS-CoV-2 associated target proteins such as spike protein (S) and main protease (Mpro), a mol. interaction simulation was performed by docking software (MVD) and subsequently the applicability score was calculated by machine learning algorithm. Furthermore, the STITCH algorithm was used to predict the pharmacol. network involving multiple pathways of active drug candidate(s). Pharmacophore features of active drug(s) mol. was also determined to predict structure-activity relationship (SAR). The mol. interaction anal. showed that cordycepin has strong binding affinities with S protein (-180) and Mpro proteins (-205) which were relatively highest among other drug candidates used. Interestingly, compounds with low IC50 showed high binding energy. Furthermore, machine learning algorithm also revealed high applicability scores (0.42-0.47) of cordycepin. It is worth mentioning that the pharmacol. network depicted the involvement of cordycepin in different pathways associated with bacterial and viral diseases including tuberculosis, hepatitis B, influenza A, viral myocarditis, and herpes simplex infection. The embedded pharmacophore features with cordycepin also suggested strong SAR. Cordycepin’s anti-SARS-CoV-2 activity indicated 65% (E-gene) and 42% (N-gene) viral replication inhibition after 48 h of treatment. Since, cordycepin has both preclin. and clin. evidences on antiviral activity, in addition the present findings further validate and suggest repurposing potential of cordycepin against COVID-19.

Chemical Biology & Drug Design published new progress about Algorithm. 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

Naik, Vankudavath Raju published the artcileRemdesivir (GS-5734) as a therapeutic option of 2019-nCOV main protease – in silico approach, Quality Control of 55981-09-4, the main research area is human covid19 virus mol docking remdesivir genome; 2019-nCOV; COVID-19; Remdesivir; dynamics simulations; molecular docking; phylogeny; sequence analysis.

2019 – Novel Coronavirus (2019-nCOV), enclosed large genome pos.-sense RNA virus characterized by crown-like spikes that protrude from their surface, and have a distinctive replication strategy. The 2019-nCOV belongs to the Coronaviridae family, principally consists of virulent pathogens showing zoonotic property, has emerged as a pandemic outbreak with high mortality and high morbidity rate around the globe and no therapeutic vaccine or drugs against 2019-nCoV are discovered till now. In this study, in silico methods and algorithms were used for sequence, structure anal. and mol. docking on Mpro of 2019-nCOV. The co-crystal structure of 2019-nCOV protease, 6LU7 have ∼99% identity with SARS-CoV protease. The 6LU7 residues, Cys145 and His164 are playing a significant role in replication and are essential for the survival of 2019-nCOV. Alongside, 2019-nCOV Mpro sequence is non-homologous to human host-pathogen. Complete genome sequence anal., structural and mol. docking results revealed that Remdesivir is having a better binding affinity with -8.2kcal/mol than the rest of protease inhibitors, and peptide. Remdesivir is strongly forming h-bonds with crucial Mpro residues, Cys145, and His164. Further, MD simulation anal. also confirmed, that these residues are forming H-bond with Remdesivir during 100ns simulations run and found stable (∼99%) by RMSD and RMSF. Thus, present in silico study at mol. approaches suggest that, Remdesivir is a potent therapeutic inhibitor against 2019-nCoV.

Journal of Biomolecular Structure and Dynamics published new progress about Algorithm. 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

Tang, Xianfang published the artcileIndicator regularized non-negative matrix factorization method-based drug repurposing for COVID-19, Synthetic Route of 55981-09-4, the main research area is human COVID19 nonneg matrix factorization method drug repurposing; COVID-19; biological networks; drug repurposing; non-negative matrix factorization; semi-supervised learning.

A novel coronavirus, named COVID-19, has become one of the most prevalent and severe infectious diseases in human history. Currently, there are only very few vaccines and therapeutic drugs against COVID-19, and their effi cacies are yet to be tested. Drug repurposing aims to explore new applications of approved drugs, which can signifi cantly reduce time and cost compared with de novo drug discovery. In this study, we built a virus-drug dataset, which included 34 viruses, 210 drugs, and 437 confirmed related virus-drug pairs from existing literature. Besides, we developed an Indicator Regularized non-neg. Matrix Factorization (IRNMF) method, which introduced the indicator matrix and Karush-Kuhn-Tucker condition into the non-neg. matrix factorization algorithm. According to the 5-fold cross-validation on the virus-drug dataset, the performance of IRNMF was better than other methods, and its Area Under receiver operating characteristic Curve (AUC) value was 0.8127. Addnl., we analyzed the case on COVID-19 infection, and our results suggested that the IRNMF algorithm could prioritize unknown virus-drug associations

Frontiers in Immunology published new progress about Algorithm. 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

Seghezzo, Sara P. published the artcileExtended Follow-up After Hematopoietic Cell Transplantation for IκBα Deficiency with Disseminated Mycobacterium avium Infection, SDS of cas: 55981-09-4, the main research area is Mycobacterium hematopoietic cell transplantation IkB alpha; IκBα; Mycobacterium avium; NFKBIA; hematopoietic cell transplantation; immunodeficiency; recurrent infection.

This article relates to extended follow-up after hematopoietic cell transplantation for IκBα deficiency with disseminated Mycobacterium avium infection. Pre-transplant imaging revealed enlarged retroperitoneal lymph nodes that were pos. for MAC on biopsy. This infection was controlled but not resolved after 5 mo of a 5-drug regimen that included clofazimine, azithromycin, amikacin, ethambutol, and rifampin. The patient developed grade 2 skin graft vs. host disease (GVHD) starting day + 90, which responded to steroids and sirolimus. Addnl. post-transplant complications included a Pseudomonas putida central line infection and disseminated reactivation of vaccine-strain varicella following discontinuation of acyclovir 6 mo post-transplant. Reconstitution of the adaptive immune system was lifesaving for our patient and allowed for resolution of his MAC infection; however, he remains vulnerable to recurrent. Sinopulmonary infections.

Journal of Clinical Immunology published new progress about Apoptosis. 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

Lima, Nayana F. published the artcileIn Vivo Treatment with the Combination of Nitazoxanide and Flubendazole Induces Gluconeogenesis and Protein Catabolism in Taenia crassiceps cysticerci, Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is Taenia gluconeogenesis nitazoxanide flubendazole; Drugs combination; Experimental cysticercosis; Flubendazole; Metabolism; Nitazoxanide.

Abstract: Purpose: Cysticercosis is the presence of Taenia solium larva in humans or swines tissues. It is a public health problem related to bad hygienic habits and consumption of infected pork. T. crassiceps is a widely used cysticercosis exptl. model. The combination of two effective drugs such as nitazoxanide (NTZ) and flubendazole (FBZ) may potentialize their effect. The aim of this study was to use biochem. anal. to determine the metabolic impact of the combination of NTZ and FBZ on cysticerci inoculated i.p. in mice. Methods: Balb/c mice i.p. infected with T. crassiceps cysticerci received a single oral dose NTZ/FBZ (50 mg/kg). 24 h after the treatment the cysticerci were removed, frozen and analyzed by high performance liquid chromatog. regarding the detection of the following metabolic pathways: glycolysis, gluconeogenesis, homolactic fermentation, tricarboxylic acid cycle, proteins catabolism and fatty acids oxidation Results: The treatment with the drugs combination induced a statistically significant increase in gluconeogenesis and in protein catabolism when compared to the control groups. Conclusion: The drugs combination is potentialized and capable of causing greater metabolic stress than the sep. treatment with NTZ or FBZ, showing its potential for an alternative cysticercosis treatment.

Acta Parasitologica published new progress about Catabolism. 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