Tag: M.W=200-350

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

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

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

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

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

Kiehl, Isis G. A. published the artcileBoosting bladder cancer treatment by intravesical nitazoxanide and bacillus calmette-guerin association, Application In Synthesis of 55981-09-4, the main research area is bladder cancer intravesical nitazoxanide BCG; Bacillus calmette-guérin; Nitazoxanide; Repurposed drug; Treatment; Urinary bladder cancer.

Abstract: Purpose: Nitazoxanide (NTZ) has shown a promising antitumoral effect, the current study compared the anti-neoplastic effects of intravesical NTZ and BCG plus NTZ in NMIBC animal model. Methods: 30 rats, Fisher 344 were instilled with 4 intravesical doses of 1.5 mg/kg of N-methyl-N-nitrosourea (MNU) every 15 days for BC induction. The animals were divided into 3 groups (Group BCG 106 UFC -1 mg of BCG; Group NTZ -300 mg/kg of NTZ; Group NTZ + BCG -simultaneous treatment of BCG and NTZ) and received weekly intravesical treatment for 6 consecutive weeks. Animals were submitted to ultrasound imaging and euthanasia, their bladders were collected and histopathol., immunohistochem. tests (ki67 e c-Myc) and Western Blotting (PI3K, mTOR, and p-4E-BP) were performed. Results: Histopathol. tests showed 66.67%, 62.5% and 37.5% incidence of BC in animals treated with BCG, NTZ, and NTZ + BCG, resp. Nuclear positivity for ki-67 in BC animals were 12.4%, 13.2% and 8.8% in BCG, NTZ and NTZ + BCG group, resp. Between animals with carcinoma, c-Myc strong pos. was 40.10% in NTZ, 32.2% in BCG and 19.90% in the NTZ + BCG group. Blotting has shown mTOR (p =0.0473) and PI3K inhibition (p = 0.0349) in the presence of BCG, added to 4-EBP inhibition in the presence of NTZ. Conclusions: Results show the possible synergy between the gold standard BC treatment BCG and NTZ, in which multiple targets inhibition such as c-Myc and downstream mTOR, p-4E-BP and PI3K might play a role.

World Journal of Urology published new progress about Antitumor 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 In Synthesis of 55981-09-4.

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

Wang, Shupeng published the artcileTransmucosal Delivery of Self-Assembling Photosensitizer-Nitazoxanide Nanocomplexes with Fluorinated Chitosan for Instillation-Based Photodynamic Therapy of Orthotopic Bladder Tumors, Product Details of C12H9N3O5S, the main research area is photosensitizer nitazoxanide HSA chlorinee6 fluorinated chitosan bladder tumor PDT; bladder cancer; fluorinated chitosan; instillation-based photodynamic therapy; nitazoxanide; transmucosal delivery.

Theor., on account of improved local bioavailability of photosensitizers and attenuated systemic phototoxicity, intravesical instillation-based photodynamic therapy (PDT) for bladder cancer (BCa) would demonstrate significant advantages in comparison with the i.v. route. Actually, the low transmucosal efficiency, hypoxia regulation deficiency, as well as the biosafety risks of intravesical drug agents all have greatly limited the clin. development of instillation-based PDT for BCa. Herein, based on our recent findings on bladder intravesical vectors and photodynamic treatment, we explore and find that the conventional antiparasitic agent nitazoxanide (NTZ) by mixing with chlorine e6 (Ce6) conjugated human serum albumin (HSA), HSA-Ce6, is capable of forming self-assembled HSA-Ce6/NTZ nanoparticles (NPs). Then, the HSA-Ce6/NTZ complexes further fabricate with fluorinated chitosan (FCS), the synthesized transmucosal carrier, to form a biocompatible nanoscale system HSA-Ce6/NTZ/FCS NPs, which exhibit remarkably improved transmucosal delivery and uptake capacities compared with HSA-Ce6/NTZ alone or non-fluorinated HSA-Ce6/NTZ/CS NPs. Meanwhile, due to the metabolic regulation of tumor cells by NTZ, the tumor hypoxia could be efficaciously ameliorated to further favor PDT. This work represents a new photosensitizer nanomedicine formulation for the perfection of PDT performance through the modulation of tumor hypoxia by clin. approved agents. Thus, intravesical instillation of HSA-Ce6/NTZ/FCS NPs with favorable biocompatibility, followed by cystoscope-mediated PDT, could achieve a dramatically improved therapeutic effect to ablate orthotopic bladder tumors.

ACS Biomaterials Science & Engineering published new progress about Antitumor 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, Product Details of C12H9N3O5S.

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

Madbouly, Neveen published the artcileThe immunomodulatory activity of secnidazole-nitazoxanide in a murine cryptosporidiosis model, Formula: C12H9N3O5S, the main research area is nitazoxanide secnidazole immunomodulatory agent Cryptosporidium; C. parvum; immunomodulation; nitazoxanide; secnidazole.

Cryptosporidium parvum causes intestinal parasitic infections affcting both immunosuppressed and immuno competent individuals. Given the absence of effctive treatments for cryptosporidiosis, especially in immunodeficient patients, the present study was designed to assess the therapeutic efficy of secnidazole (SEC) and its combination with nitazoxanide (NTZ) in comparison to single NTZ treatment in relation to the immune status of a murine model of C. parvum infection. The infected groups were administered NTZ, SEC or NTZ-SEC for three or five successive doses. At days 10 and 12 post-infection (p.i.), the mice were sacrified, and the efficy of the applied drugs was evaluated by comparing the histo pathol. alterations in ileum and measuring the T helper Th1 (interferon gamma; IFN-γ), Th2 [interleukin (IL)-4 and IL-10] and Th17 (IL-17) cytokine profies in serum. The NTZ-SEC combination recorded the maximal reduction of C. parvum oocyst shedding, endogenous stages count and intestinal histopathol., regardless of the immune status of the infected mice. The efficy of NTZ-SEC was dependent on the period of administration, as the 5 day-based treatment protocol was also more effctive than the 3 day-based one in terms of immunocompetence and immunosuppression. The present treatment schedule induced an immunomodulatory effect from SEC that developed a protective immune response against C. parvum infection with reduced production of serum IL-17, IFN-γ, IL-4 and IL-10. Application of NTZ-SEC combined therapy may be useful in treatment of C. parvum, especially in cases involving immunosuppression.

Journal of Medical Microbiology published new progress about Cryptosporidiosis. 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

Tomczak, Ewa published the artcileResolution of cryptosporidiosis in transplant recipients: review of the literature and presentation of a renal transplant patient treated with nitazoxanide, azithromycin, and rifaximin, Quality Control of 55981-09-4, the main research area is cryptosporidiosis nitazoxanide azithromycin rifaximin renal transplantation; Cryptosporidium; azithromycin; cryptosporidiosis; nitazoxanide; transplant recipient.

Background.Cryptosporidium is a major cause of diarrheal disease worldwide, including chronic disease in malnourished children and patients with acquired immune deficiency syndrome. There are increasing reports of cryptosporidiosis in transplant patients, especially from middle-income countries. Methods. The literature on treatment of cryptosporidiosis in transplant patients was reviewed and included no controlled trials but only small case series. Nitazoxanide, azithromycin, spiramycin, and combination therapies have been used, but none are consistently efficacious. Results. We present a case of chronic diarrhea from cryptosporidiosis in a renal transplant patient. His illness resolved with decreasing immunosuppression and treatment with the 3-drug combination of nitazoxanide, azithromycin, and rifaximin. Conclusions. Although current therapies are not reliably effective in the absence of an effective cellular immune response, combination therapies hold promise for improved responses.

Open Forum Infectious Diseases published new progress about Cryptosporidiosis. 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

Sampaio, Guilherme A. published the artcileHistopathologic evaluation of experimental murine neurocysticercosis after treatment with albendazole/nitazoxanide combination, Category: esters-buliding-blocks, the main research area is neurocysticercosis albendazole nitazoxanide brain; Albendazole; Taenia crassiceps; anthelminthic drugs; experimental neurocysticercosis; nitazoxanide; pathologic evaluation.

Neurocysticercosis (NCC) is most common helminthic brain infection related to epilepsy. Only albendazole (ABZ) and praziquantel are used in its treatment. The development of new therapeutics has been encouraged. Taenia crassiceps cysticerci intracranial infection is the exptl. model used in NCC studies. This study evaluated the histopathol. of the brains of BALB/c mice exptl. infected with T. crassiceps cysticerci after the treatment with the ABZ/nitazoxanide (NTZ) combination. Thirty days after the inoculation the mice received an oral single dose of the ABZ/NTZ combination (40 mg kg-1 each). The control groups were treated with: NaCl 0.9%; ABZ or NTZ. The histopathol. evaluation of the brains was performed 24 h after treatment. The ABZ treatment induced discrete mononuclear inflammatory infiltration, meningitis, gliosis, hyperemia and hippocampus compression; moderate ependimitis and edema. The NTZ treatment induced accentuated inflammatory infiltration, foamy macrophages, ependimitis, choroiditis, gliosis and hyperemia and moderate edema. The ABZ/NTZ combination treatment induced a significant decrease in the polymorphonuclear inflammatory infiltration, ependimitis, choroiditis, gliosis, hyperemia and ventriculomegaly in comparison with the other groups. The cysticerci showed destruction of the tegument not observed in other groups. The ABZ/NTZ combination is efficient as the parasite showed signs of destruction and lower damage to the host’s tissue.

Parasitology published new progress about Brain hippocampus. 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