Month: December 2022

Apaydin, Cagla Begum published the artcileSmall-molecule Antiviral Agents in Ongoing Clinical Trials for COVID-19, HPLC of Formula: 55981-09-4, the main research area is review coronavirus disease antiviral agent clin trial; COVID-19; SARS-CoV-2; antiviral therapy; clinical trial; mechanism of action.; preclinical study.

The coronavirus disease 2019 (COVID-19) pandemic, due to the novel severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), emerged in Dec. 2019 and has rapidly spread globally. As the confirmed number of cases has reached 83 million worldwide, the potential severity and the deadly complications of the disease requires urgent development of effective drugs for prevention and treatment. No proven effective treatment for this virus currently exists. Most of the antiviral discovery efforts are focused on the repurposing of approved or clin. stage drugs. This review highlights the small-mol. repurposed antiviral agents that are currently under investigation in clin. trials for COVID-19. These include viral polymerase and protease inhibitors remdesivir, galidesivir, favipiravir, ribavirin, sofosbuvir, tenofovir/emtricitabine, baloxavir marboxil, EIDD-2801, lopinavir/ritonavir; virus-/host-directed viral entry and fusion inhibitors arbidol chloroquine/hydroxychloroquine, chlorpromazine, camostat mesylate, nafamostat mesylate, bromhexine and agents with diverse/unclear mechanism of actions as oseltamivir, triazavirin, ivermectin, nitazoxanide, niclosamide and BLD-2660. The published preclin. and clin. data to date on these drugs as well as the mechanisms of action are reviewed.

Current Drug Targets 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, HPLC of Formula: 55981-09-4.

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

Rocco, Patricia R. M. published the artcileEarly use of nitazoxanide in mild COVID-19 disease: randomised, placebo-controlled trial, Synthetic Route of 55981-09-4, the main research area is covid19 pandemic nitazoxanide.

Background: Nitazoxanide is widely available and exerts broad-spectrum antiviral activity in vitro. However, there is no evidence of its impact on severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection. Methods: In a multicentre, randomised, double-blind, placebo-controlled trial, adult patients presenting up to 3 days after onset of coronavirus disease 2019 (COVID-19) symptoms (dry cough, fever and/or fatigue) were enrolled. After confirmation of SARS-CoV-2 infection using reverse transcriptase PCR on a nasopharyngeal swab, patients were randomised 1:1 to receive either nitazoxanide (500 mg) or placebo, three times daily, for 5 days. The primary outcome was complete resolution of symptoms. Secondary outcomes were viral load, laboratory tests, serum biomarkers of inflammation and hospitalisation rate. Adverse events were also assessed. Results: From June 8 to August 20, 2020, 1575 patients were screened. Of these, 392 (198 placebo, 194 nitazoxanide) were analyzed. Median (interquartile range) time from symptom onset to first dose of study drug was 5 (4-5) days. At the 5-day study visit, symptom resolution did not differ between the nitazoxanide and placebo arms. Swabs collected were neg. for SARS-CoV-2 in 29.9% of patients in the nitazoxanide arm vs. 18.2% in the placebo arm (p = 0.009). Viral load was reduced after nitazoxanide compared to placebo (p = 0.006). The percentage viral load reduction from onset to end of therapy was higher with nitazoxanide (55%) than placebo (45%) (p = 0.013). Other secondary outcomes were not significantly different. No serious adverse events were observed Conclusions: In patients with mild COVID-19, symptom resolution did not differ between nitazoxanide and placebo groups after 5 days of therapy. However, early nitazoxanide therapy was safe and reduced viral load significantly.

European Respiratory Journal 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, Synthetic Route of 55981-09-4.

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

Simsek Yavuz, Serap published the artcileAn update of anti-viral treatment of COVID-19, Category: esters-buliding-blocks, the main research area is review COVID19 RNA antiviral remdesivir merimepodib hydroxychloroquine; antiviral; treatment; SARS-CoV-2; COVID-19.

Currently there is not an effective antiviral treatment for COVID-19, but a large number of drugs have been evaluated since the beginning of the pandemic, and many of them have been used for the treatment of COVID-19 despite the preliminary or conflicting results of the clin. trials. We aimed to review and summarize all of the current knowledge on the antivirals for COVID-19. There are 2 main drug groups for SARS-CoV-2: agents that target proteins or RNA of the virus or interfere with proteins or biol. processes in the host that support the virus. The main drug groups include inhibitors of viral entry into the human cell (convalescent plasma, monoclonal antibodies, nanobodies, mini proteins, human soluble ACE-2, camostat, dutasteride, proxalutamide, bromhexin, hydroxychloroquine, umifenovir nitazoxanid, niclosamide, lactoferrin), inhibitors of viral proteases (lopinavir/ritonavir, PF-07321332, PF-07304814, GC376), inhibitors of viral RNA (remdesivir, favipiravir, molnupiravir, AT-527, merimepodib, PTC299), inhibitors of host proteins supporting virus (plitidepsin, fluvoxamine, ivermectin), and agents supporting host natural immunity (Interferons). When taking into account the results of all the available laboratory and clin. trials on the subject, monoclonal antibodies seem to be the most effective treatment for COVID-19 at the moment, and high-titer convalescent plasma also could be effective when administered during the early phase of the disease. As lopinavir/ritonavir, hydroxychloroquine, merimepodib, and umifenovir were found to be ineffective in RCTs, they should not be used. Addnl. studies are needed to define the role of remdesivir, favipiravir, interferons, ivermectin, dutasteride, proxulutamide, fluvoxamine, bromhexine, nitazoxanide, and niclosamid in the treatment of COVID-19. Finally, the results of phase trials are waited to learn whether or not the newer agents such as molnupiravir, PF-07321332, PF-07304814, plitidepsin and AT-527 are effective in the treatment of COVID-19.

Turkish Journal of Medical Sciences 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, Category: esters-buliding-blocks.

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

Hossain, Jamal Md. published the artcileRepurposing therapeutic agents against SARS-CoV-2 infection: most promising and neoteric progress, HPLC of Formula: 55981-09-4, the main research area is review public health crisis palliative care repurposing strategy pandemic; SARS covid clin trial review; SARS-CoV-2; clinical trials; covid-19 pandemic; palliative care; public health crisis; repurposing strategy.

The pathogenic and highly transmissible etiol. agent, SARS-CoV-2, has caused a serious threat COVID-19 pandemic. WHO has declared the epidemic a public health emergency of international concern owing to its high contagiosity, mortality rate, and morbidity. Till now, there is no approved vaccine or drug to combat the COVID-19 and avert this global crisis. Areas covered In this narrative review, we summarized the updated results (Jan. to August 2020) of the most promising repurposing therapeutic candidates to treat the SARS-CoV-2 viral infection. The repurposed drugs classified under four headlines like antivirals, anti-parasitic, immune-modulating, and miscellaneous drugs were discussed with their in vitro efficacy to recent clin. advancements against COVID-19. Expert opinion Currently, palliative care, ranging from outpatient management to intensive care, including oxygen administration, ventilator support, i.v. fluids therapy, with some repurposed drugs, are the primary weapons to fight against COVID-19. Until a safe and effective vaccine is developed, an evidence-based drug repurposing strategy might be the wisest option to save people from this catastrophe. Several existing drugs are now under clin. trials, and some of them are approved in different places of the world for emergency use or as adjuvant therapy in COVID-19 with standard of care.

Expert Review of Anti-Infective Therapy 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, HPLC of Formula: 55981-09-4.

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

Rossignol, Jean-Francois published the artcileA Pilot Clinical Trial of Nitazoxanide in the Treatment of Chronic Hepatitis B, COA of Formula: C12H9N3O5S, the main research area is chronic hepatitis B nitazoxanide.

Chronic infection by the hepatitis B virus (HBV) has remained a major public health problem. To achieve an HBV cure, we will likely need to combine antivirals with different viral targets as well as immunotherapy. Here, we report data from a pilot proof-of-concept clin. trial of nitazoxanide in treating chronic hepatitis B. Conclusion: Nitazoxanide offers novel mechanisms of antiviral activity, and it would be interesting to evaluate the potential of combining nitazoxanide with oral nucleos(t)ide analogs.

Hepatology Communications 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, COA of Formula: C12H9N3O5S.

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

Barrett, Jeffrey S. published the artcileRisk assessment of therapeutic agents under consideration to treat COVID-19 in paediatric patients and pregnant women, Computed Properties of 55981-09-4, the main research area is drug repurposing vaccine child pregnancy COVID19 risk assessment; Clinical pharmacology; Infectious diseases; Paediatrics.

Aim : Repurposing strategies to address the COVID-19 pandemic have been accelerated. As both pregnant and paediatric patients are likely to be excluded from most planned investigations, the list of repurposed options and the available data on these drugs and vaccines provide a baseline risk assessment and identify gaps for targeted investigation. Methods : Clin. trials have been searched and reviewed; 23 repurposed drugs and drug combinations and nine candidate vaccines have been assessed regarding the availability of relevant data in paediatrics and pregnant women and to evaluate expected or unanticipated risk. Results : Thirteen of the repurposed drugs or drug combinations are indicated for use in paediatrics in some age category albeit for indications other than COVID-19; 10 of these are indicated for use in pregnant women. Even in cases where these drugs are indicated in the populations, source data from which safety and or dosing could be extrapolated for use in COVID-19 is sparse. Vaccine trials are ongoing and generally exclude pregnant women; only in a few instances have paediatric subgroups been planned for enrolment. Data from individual case studies and RWD may suggest that subpopulations of both paediatric patients and pregnant women may be more at risk, particularly those in an increased inflammatory state. Conclusion : In conjunction with more prospective collaboration, plans are evolving to ensure that we will be better prepared to address similar situations especially in paediatrics and pregnant women where experience is limited and actual practice relies heavily on leveraging data from other populations and indications.

British Journal of Clinical 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, Computed Properties of 55981-09-4.

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

Ivanova, Larisa published the artcile1,3-Thiazolbenzamide Derivatives as Chikungunya Virus nsP2 Protease Inhibitors, COA of Formula: C12H9N3O5S, the main research area is antiviral thiazolbenzamide derivative Chikungunya virus onstructural protein protease inhibitor.

Chikungunya fever results from an infection with Chikungunya virus (CHIKV, genus Alphavirus) that is prevalent in tropical regions and is spreading fast to temperate climates with documented outbreaks in Europe and the Americas. Currently, there are no available vaccines or antiviral drugs for prevention or treatment of Chikungunya fever. The nonstructural proteins (nsPs) of CHIKV responsible for virus replication are promising targets for the development of new antivirals. This study was attempted to find out new potential inhibitors of CHIKV nsP2 protease using the ligand-based drug design. Two compounds 10 and 10c, identified by mol. docking, showed antiviral activity against CHIKV with IC50 of 13.1 and 8.3μM, resp. Both compounds demonstrated the ability to inhibit the activity of nsP2 in a cell-free assay, and the impact of compound 10 on virus replication was confirmed by western blot. The mol. dynamics study of the interactions of compounds 10 and 10c with CHIKV nsP2 showed that a possible mechanism of action of these compounds is the blocking of the active site and the catalytic dyad of nsP2.

ACS Omega 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, COA of Formula: C12H9N3O5S.

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

Danta, Chhanda Charan published the artcileCNS Penetration Ability: A Critical Factor for Drugs in the Treatment of SARS-CoV-2 Brain Infection, Application of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is drug treatment SARS CoV 2; CNS infection; CNS penetration; COVID19; SARS-CoV-2; drug treatment; log P.

Now, it has been evidenced that Covid19 (SARS-CoV-2) infects the brain tissues. Along with this, a challenge has been raised for research professionals to find effective drugs for its treatment since the recent spread of this virus from Wuhan, China. Targeting the treatment of brain infection, it has also been a challenge that the clin. drug should have good CNS penetration ability to cross the blood-brain barrier.

ACS Chemical Neuroscience 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

Riccio, Anna published the artcileImpairment of SARS-CoV-2 spike glycoprotein maturation and fusion activity by nitazoxanide: an effect independent of spike variants emergence, Name: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is SARS COV2 spike glycoprotein nitazoxanide COVID19; Broad-spectrum antiviral; COVID-19; Nitazoxanide; SARS-CoV-2 spike; SARS-CoV-2 variants; Syncytia formation.

SARS-CoV-2, the causative agent of COVID-19, has caused an unprecedented global health crisis. The SARS-CoV-2 spike, a surface-anchored trimeric class-I fusion glycoprotein essential for viral entry, represents a key target for developing vaccines and therapeutics capable of blocking virus invasion. The emergence of SARS-CoV-2 spike variants that facilitate virus spread and may affect vaccine efficacy highlights the need to identify novel antiviral strategies for COVID-19 therapy. Here, we demonstrate that nitazoxanide, an antiprotozoal agent with recognized broad-spectrum antiviral activity, interferes with SARS-CoV-2 spike maturation, hampering its terminal glycosylation at an endoglycosidase H-sensitive stage. Engineering multiple SARS-CoV-2 variant-pseudoviruses and utilizing quant. cell-cell fusion assays, we show that nitazoxanide-induced spike modifications hinder progeny virion infectivity as well as spike-driven pulmonary cell-cell fusion, a critical feature of COVID-19 pathol. Nitazoxanide, being equally effective against the ancestral SARS-CoV-2 Wuhan-spike and different emerging variants, including the Delta variant of concern, may represent a useful tool in the fight against COVID-19 infections.

Cellular and Molecular Life Sciences 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

Ebenezer, Oluwakemi published the artcileDiscovery of potential inhibitors for RNA-dependent RNA polymerase of Norovirus: virtual screening, and molecular dynamics, Synthetic Route of 55981-09-4, the main research area is CMX521 antiviral agent norwalk virus; CMX521; human norovirus; molecular dynamics; molecular similarity; virtual screening.

Noroviruses are non-enveloped viruses with a pos.-sense single-stranded RNA (ssRNA) genome belonging to the genus Norovirus, from the family Caliciviridae, which are accountable for acute gastroenteritis in humans. The Norovirus genus is subdivided into seven genogroups, i.e., (GI-GVII); among these, the genogroup II and genotype 4 (GII.4) strains caused global outbreaks of human norovirus (HuNov) disease. The viral genome comprises three open reading frames (ORFs). ORF1 encodes the nonstructural polyprotein that is cleaved into six nonstructural proteins, which include 3C-like cysteine protease (3CLpro) and a viral RNA-dependent RNA polymerase. ORF2 and ORF3 encode the proteins VP1 and VP2. The RNA-dependent RNA polymerase (RdRp) from noroviruses is one of the multipurpose enzymes of RNA viruses vital for replicating and transcribing the viral genome, making the virally encoded enzyme one of the critical targets for the development of novel anti-norovirus agents. In the quest for a new antiviral agent that could combat HuNov, high throughput virtual screening (HTVS), combined with e-pharmacophore screening, was applied to screen compounds from the PubChem database. CMX521 mol. was selected as a prototype for a similarity search in the PubChem online database. Mol. dynamics simulations were employed to identify different compounds that may inhibit HuNov. The results predicted that compound CID-57930781 and CID-44396095 formed stable complexes with MNV-RdRp within 50 ns; hence, they may signify as promising human norovirus inhibitors.

International Journal of Molecular Sciences 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, Synthetic Route of 55981-09-4.

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