Tag: M.W=200-350

Ajima, Ukpe published the artcileA review of the structure-activity relationships (SAR) of selected drugs with potential to be repurposed against SARS-COV-2, Formula: C12H9N3O5S, the main research area is review SARSCoV2 antiviral drug repurposing structure activity relationship.

Background: The pandemic caused by the novel SARS-CoV-2 virus has escalated rapidly and impacted human health worldwide, in addition to causing severe disruptions to socioeconomic life. There is presently no effective treatment for the disease and this underscores the urgent need for new therapeutic options against this life threatening disease. The traditional strategy for the development of new drugs is a slow and expensive process. Drug repurposing is a valuable alternative strategy that can be used to bypass some of the limitations of traditional drug discovery in order to rapidly develop new therapeutic agents for the management of Covid-19. Objectives: The present review x-rays recent efforts to re-purpose some antiviral drugs for the treatment of SARS-Cov-2 with an emphasis on the structure activity relationships (SAR) of the compounds Methods: A systematic internet search of three academic databases of published literature was undertaken using relevant keywords and search terms which focused on drug re-purposing against SARS-CoV-2. Results: A total of 853 results were generated and evaluated. The results of the search were screened and relevant articles identified, yielding a total of 83 articles. Some of the drugs identified with potential for re-purposing against SARS-CoV-2 include: Arbidol, Favipiravir, Ribavirin, Nitazoxanide etc. Conclusion: It is hoped that the information generated in this review will help deepen understanding of the potential mechanism of anti-SARS-CoV-2 action of the compounds and also draw attention to opportunities that exist for structural modification of these mols. with the aim of improving and enhancing their selectivity and efficacy against SARS-CoV-2.

Asian Journal of Pharmacy and Pharmacology published new progress about Antiviral 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, Formula: C12H9N3O5S.

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

Guedes, Isabella A. published the artcileDrug design and repurposing with DockThor-VS web server focusing on SARS-CoV-2 therapeutic targets and their non-synonym variants, Name: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is SARSCOV2 therapeutic target drug design repurposing.

The COVID-19 caused by the SARS-CoV-2 virus was declared a pandemic disease in March 2020 by the World Health Organization (WHO). Structure-Based Drug Design strategies based on docking methodologies have been widely used for both new drug development and drug repurposing to find effective treatments against this disease. In this work, we present the developments implemented in the DockThor-VS web server to provide a virtual screening (VS) platform with curated structures of potential therapeutic targets from SARS-CoV-2 incorporating genetic information regarding relevant non-synonymous variations. The web server facilitates repurposing VS experiments providing curated libraries of currently available drugs on the market. At present, DockThor-V S provides ready-for-docking 3D structures for wild type and selected mutations for Nsp3 (papain-like, PLpro domain), Nsp5 (Mpro, 3CLpro), Nsp12 (RdRp), Nsp15 (NendoU), N protein, and Spike. We performed VS experiments of FDA-approved drugs considering the therapeutic targets available at the web server to assess the impact of considering different structures and mutations to identify possible new treatments of SARS-CoV-2 infections. The DockThor-VS is freely available at www.dockthor.lncc.br.

Scientific Reports published new progress about Antiviral 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

Zhao, Mengmeng published the artcileRecent progress of antiviral therapy for coronavirus disease 2019, Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is review COVID19 antiviral therapy; Antiviral therapy; COVID-19; SARS-CoV-2.

The coronavirus disease 2019 (COVID-19) pandemic has become a global public health crisis, for which antiviral treatments are considered mainstream therapeutic approaches. With the development of this pandemic, the number of clin. studies on antiviral therapy, including remdesivir, chloroquine and hydroxychloroquine, lopinavir/ritonavir, ribavirin, arbidol, interferon, favipiravir, oseltamivir, nitazoxanide, nelfinavir, and camostat mesylate, has been increasing. However, the efficacy of these antiviral drugs for COVID-19 remains controversial. In this review, we summarize the recent progress and findings on antiviral therapies, aiming to provide clin. support for the management of COVID-19. In addition, we analyze the causes of controversy in antiviral drug research and discuss the quality of current studies on antiviral treatments. High-quality randomized clin. trials are required to demonstrate the efficacy and safety of antiviral drugs for the treatment of COVID-19.

European Journal of Pharmacology published new progress about Antiviral 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, Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate.

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

Tzou, Philip L. published the artcileCoronavirus antiviral research database (CoV-RDB): an online database designed to facilitate comparisons between candidate anti-coronavirus compounds, Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is coronavirus antiviral database; COVID-19; MERS-CoV; SARS-CoV; SARS-CoV-2; antiviral therapy; coronavirus.

Background: To prioritize the development of antiviral compounds, it is necessary to compare their relative preclin. activity and clin. efficacy. Methods: We reviewed in vitro, animal model, and clin. studies of candidate anti-coronavirus compounds and placed extracted data in an online relational database. Results: As of August 2020, the Coronavirus Antiviral Research Database (CoV-RDB; covdb.stanford.edu) contained over 2800 cell culture, entry assay, and biochem. experiments, 259 animal model studies, and 73 clin. studies from over 400 published papers. SARS-CoV-2, SARS-CoV, and MERS-CoV account for 85% of the data. Approx. 75% of experiments involved compounds with known or likely mechanisms of action, including monoclonal antibodies and receptor binding inhibitors (21%), viral protease inhibitors (17%), miscellaneous host-acting inhibitors (10%), polymerase inhibitors (9%), interferons (7%), fusion inhibitors (5%), and host protease inhibitors (5%). Of 975 compounds with known or likely mechanism, 135 (14%) are licensed in the U.S. for other indications, 197 (20%) are licensed outside the U.S. or are in human trials, and 595 (61%) are pre-clin. investigational compounds Conclusion: CoV-RDB facilitates comparisons between different candidate antiviral compounds, thereby helping scientists, clin. investigators, public health officials, and funding agencies prioritize the most promising compounds and repurposed drugs for further development.

Viruses published new progress about Antiviral 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, Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate.

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

Erturk, Aliye Gediz published the artcileA multidisciplinary approach to coronavirus disease (COVID-19), Application of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is review antiviral COVID19 drug design safety; COVID-19; SARS-CoV-2; cytokine storm; dietary supplements; immunotherapy; in-silico research; natural products; repurposing drugs; small drugs; vaccine development.

Since Dec. 2019, humanity has faced an important global threat. Many studies have been published on the origin, structure, and mechanism of action of the SARS-CoV-2 virus and the treatment of its disease. The priority of scientists all over the world has been to direct their time to research this subject. In this review, we highlight chem. studies and therapeutic approaches to overcome COVID-19 with seven different sections. These sections are the structure and mechanism of action of SARS-CoV-2, immunotherapy and vaccine, computer-aided drug design, repurposing therapeutics for COVID-19, synthesis of new mol. structures against COVID-19, food safety/security and functional food components, and potential natural products against COVID-19. In this work, we aimed to screen all the newly synthesized compounds, repurposing chems. covering antiviral, anti-inflammatory, antibacterial, antiparasitic, anticancer, antipsychotic, and antihistamine compounds against COVID-19. We also highlight computer-aided approaches to develop an anti-COVID-19 mol. We explain that some phytochems. and dietary supplements have been identified as antiviral bioproducts, which have almost been successfully tested against COVID-19. In addition, we present immunotherapy types, targets, immunotherapy and inflammation/mutations of the virus, immune response, and vaccine issues.

Molecules published new progress about Antiviral 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, Application of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate.

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

Olagunju, Adeniyi published the artcileEfficacy and safety of nitazoxanide plus atazanavir/ritonavir for the treatment of moderate to severe COVID-19 (NACOVID): A structured summary of a study protocol for a randomised controlled trial, SDS of cas: 55981-09-4, the main research area is nitazoxanide atazanavir ritonavir efficacy safety human COVID infection; COVID-19; SARS-CoV-2; atazanavir/ritonavir; nitazoxanide; protocol; randomised controlled trial.

To investigate the efficacy and safety of repurposed antiprotozoal and antiretroviral drugs, nitazoxanide and atazanavir/ritonavir, in shortening the time to clin. improvement and achievement of SARS-CoV-2 polymerase chain reaction (PCR) negativity in patients diagnosed with moderate to severe COVID-19. This is a pilot phase 2, multicentre 2-arm (1:1 ratio) open-label randomised controlled trial. Patients with confirmed COVID-19 diagnosis (defined as SARS-CoV-2 PCR pos. nasopharyngeal swab) will be recruited from four participating isolation and treatment centers in Nigeria: two secondary care facilities (Infectious Diseases Hospital, Olodo, Ibadan, Oyo State and Specialist State Hospital, Asubiaro, Osogbo, Osun State) and two tertiary care facilities (Obafemi Awolowo University Teaching Hospitals Complex, Ile-Ife, Osun State and Olabisi Onabanjo University Teaching Hospital, Sagamu, Ogun State). These facilities have a combined capacity of 146-bed COVID-19 isolation and treatment ward. Confirmation of SARS-CoV-2 infection by PCR test within two days before randomisation and initiation of treatment, age bracket of 18 and 75 years, symptomatic, able to understand study information and willingness to participate. Exclusion criteria include the inability to take orally administered medication or food, known hypersensitivity to any of the study drugs, pregnant or lactating, current or recent (within 24 h of enrolment) treatment with agents with actual or likely antiviral activity against SARS-CoV-2, concurrent use of agents with known or suspected interaction with study drugs, and requiring mech. ventilation at screening. Participants in the intervention group will receive 1000 mg of nitazoxanide twice daily orally and 300/100 mg of atazanvir/ritonavir once daily orally in addition to standard of care while participants in the control group will receive only standard of care. Standard of care will be determined by the physician at the treatment center in line with the current guidelines for clin. management of COVID-19 in Nigeria. Main outcome measures are: (1) Time to clin. improvement (defined as time from randomisation to either an improvement of two points on a 10-category ordinal scale (developed by the WHO Working Group on the Clin. Characterization and Management of COVID-19 infection) or discharge from the hospital, whichever came first); (2) Proportion of participants with SARS-CoV-2 polymerase chain reaction (PCR) neg. result at days 2, 4, 6, 7, 14 and 28; (3) Temporal patterns of SARS-CoV-2 viral load on days 2, 4, 6, 7, 14 and 28 quantified by RT-PCR from saliva of patients receiving standard of care alone vs. standard of care plus study drugs. Randomisation: Allocation of participants to study arm is randomised within each site with a ratio 1:1 based on randomisation sequences generated centrally at Obafemi Awolowo University. The model was implemented in REDCap and includes stratification by age, gender, viral load at diagnosis and presence of relevant comorbidities. None, this is an open-label trial. 98 Patients (49 per arm). Regulatory approval was issued by the National Agency for Food and Drug Administration and Control on 06 Oct. 2020 (protocol version number is 2.1 dated 06 August 2020). Recruitment started on 9 Oct. 2020 and is anticipated to end before Apr. 2021.

Trials published new progress about Antiviral 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, SDS of cas: 55981-09-4.

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

Martins-Filho, Paulo Ricardo published the artcilePotential role for nitazoxanide in treating SARS-CoV-2 infection, Formula: C12H9N3O5S, the main research area is nitazoxanide SARS CoV 2 COVID 19 disease.

Until specific and effective antiviral therapies against severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) become available, the management of corona-virus disease (COVID-19) is primarily based on supportive care and treatment of complication. Nitazoxanide is an FDA-approved drug for the treatment of parasite-mediated infectious diarrhea and enteritis with a favorable safety profile. High-quality trial evidence on nitazoxanide in the treatment of SARS-CoV-2 infection is urgently needed.

American Journal of Physiology published new progress about Antiviral 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, Formula: C12H9N3O5S.

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

Kadil, Youness published the artcileIn silico study of pharmacological treatments against SARS-CoV2 main protease, Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is in silico pharmacol treatment SARS CoV2 main protease.

The COVID-19 caused by a new type of coronavirus has emerged from China and led to thousands of death globally. Despite the efforts engaged in studying this newly emerged virus and searching for its treatment, the understanding of the COVID-19 drug and target protein interactions still represent a key challenge. Several mols. have demonstrated In-Vitro activity against the SARS-CoV-2 virus and/ or potential clin. benefit in observational and non-randomized studies. Randomized clin. trials of an appropriate size are currently ongoing to establish the efficacy of these therapeutic proposals. Herein, concerning these diverse guidelines and therapeutic suggestions of different approaches to the treatment, this research aims to provide a mol. anal. of the interaction between the principal mols. cited in bibliog. and the active protease site of the virus.

Journal of Pure and Applied Microbiology published new progress about Antiviral 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, Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate.

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

Bordicchia, Matteo published the artcileFeline Calicivirus Virulent Systemic Disease: Clinical Epidemiology, Analysis of Viral Isolates and In Vitro Efficacy of Novel Antivirals in Australian Outbreaks, Name: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is sequence antiviral agent feline calicivirus upper respiratory tract disease; 2�C-methylcytidine; Caliciviridae; NITD-008; Vesivirus; nitazoxanide.

Feline calicivirus (FCV) causes upper respiratory tract disease (URTD) and sporadic outbreaks of virulent systemic disease (FCV-VSD). The basis for the increased pathogenicity of FCV-VSD viruses is incompletely understood, and antivirals for FCV-VSD have yet to be developed. We investigated the clinicoepidemiol. and viral features of three FCV-VSD outbreaks in Australia and evaluated the in vitro efficacy of nitazoxanide (NTZ), 2′-C-methylcytidine (2CMC) and NITD-008 against FCV-VSD viruses. Overall mortality among 23 cases of FCV-VSD was 39%. Metagenomic sequencing identified five genetically distinct FCV lineages within the three outbreaks, all seemingly evolving in situ in Australia. Notably, no mutations that clearly distinguished FCV-URTD from FCV-VSD phenotypes were identified. One FCV-URTD strain likely originated from a recombination event. Anal. of seven amino-acid residues from the hypervariable E region of the capsid in the cultured viruses did not support the contention that properties of these residues can reliably differentiate between the two pathotypes. On plaque reduction assays, dose-response inhibition of FCV-VSD was obtained with all antivirals at low micromolar concentrations; NTZ EC50, 0.4-0.6μM, TI = 21; 2CMC EC50, 2.7-5.3μM, TI > 18; NITD-008, 0.5 to 0.9μM, TI > 111. Investigation of these antivirals for the treatment of FCV-VSD is warranted. Feline calicivirus sequence has been deposited in GenBank under accession number MW880757-MW880771.

Viruses published new progress about Antiviral 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

Nunes, Damiana Antonia de Fatima published the artcileNS2B-NS3 protease inhibitors as promising compounds in the development of antivirals against Zika virus: A systematic review, Formula: C12H9N3O5S, the main research area is protease inhibitor antiviral agents zika virus infection enzymic inhibition; NS2B-NS3 protease; Zika virus; antiviral; enzymatic inhibition; noncompetitive inhibitors.

Zika virus (ZIKV) infections are associated with severe neurol. complications and are a global public health concern. There are no approved vaccines or antiviral drugs to inhibit ZIKV replication. NS2B-NS3 protease (NS2B-NS3 pro), which is essential for viral replication, is a promising mol. target for anti-ZIKV drugs. We conducted a systematic review to identify compounds with promising effects against ZIKV; we discussed their pharmacodynamic and pharmacophoric characteristics. The online search, performed using the PubMed/MEDLINE and SCOPUS databases, yielded 56 articles; seven relevant studies that reported nine promising compounds with inhibitory activity against ZIKV NS2B-NS3 pro were selected. Of these, five (niclosamide, nitazoxanide, bromocriptine, temoporfin, and novobiocin) are currently available on the market and have been tested for off-label use against ZIKV. The 50% inhibitory concentration values of these compounds for the inhibition of NS2B-NS3 pro ranged at 0.38-21.6 ΜM; most compounds exhibited noncompetitive inhibition (66%). All compounds that could inhibit the NS2B-NS3 pro complex showed potent in vitro anti-ZIKV activity with a 50% effective concentration ranging 0.024-50 ΜM. The 50% cytotoxic concentration of the compounds assayed using A549, Vero, and WRL-69 cell lines ranged at 0.6-1388.02 ΜM and the selectivity index was 3.07-1698. This review summarizes the most promising antiviral agents against ZIKV that have inhibitory activity against viral proteases.

Journal of Medical Virology published new progress about Antiviral 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, Formula: C12H9N3O5S.

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