Tag: M.W=200-350

Maccesi, Martina published the artcileMulti-center screening of the Pathogen Box collection for schistosomiasis drug discovery, Application In Synthesis of 55981-09-4, the main research area is schistosomiasis drug discovery pathogen Box; Drug discovery; MMV; Pathogen Box; Phenotypic screen; Schistosoma; Schistosomiasis.

Over the past five years, as a public service to encourage and accelerate drug discovery for diseases of poverty, the Medicines for Malaria Venture (MMV) has released box sets of 400 compounds named the Malaria, Pathogen and Stasis Boxes. Here, we screened the Pathogen Box against the post-infective larvae (schistosomula) of Schistosoma mansoni using assays particular to the three contributing institutions, namely, the University of California San Diego (UCSD) in the USA, the Swiss Tropical and Public Health Institute (Swiss TPH) in Switzerland, and the Fundaça Oswaldo Cruz (FIOCRUZ) in Brazil. With the same set of compounds, the goal was to determine the degree of inter-assay variability and identify a core set of active compounds common to all three assays. New drugs for schistosomiasis would be welcome given that current treatment and control strategies rely on chemotherapy with just one drug, praziquantel. Both the UCSD and Swiss TPH assays utilize daily observational scoring methodologies over 72 h, whereas the FIOCRUZ assay employs XTT (2,3-bis(2-methoxy-4-nitro-5-sulfophenyl)-5-[(phenylamino)carbonyl]-2H-tetrazolium hydroxide) at 72 h to measure viability as a function of NAD+/NADH redox state. Raw and transformed data arising from each assay were assembled for comparative anal. For the UCSD and Swiss TPH assays, there was strong concordance of at least 87% in identifying active and inactive compounds on one or more of the three days. When all three assays were compared at 72 h, concordance remained a robust 74%. Further, robust Pearsos correlations (0.48-0.68) were measured between the assays. Of those actives at 72 h, the UCSD, Swiss TPH and FIOCRUZ assays identified 86, 103 and 66 compounds, resp., of which 35 were common. Assay idiosyncrasies included the identification of unique compounds, the differential ability to identify known antischistosomal compounds and the concept that compounds of interest might include those that increase metabolic activity above baseline. The inter-assay data generated were in good agreement, including with previously reported data. A common set of antischistosomal mols. for further exploration has been identified[Figure not available: see fulltext.].

Parasites & Vectors published new progress about Chemotherapy. 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

Rajoli, Rajith K. R. published the artcileDose prediction for repurposing nitazoxanide in SARS-CoV-2 treatment or chemoprophylaxis, Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is nitazoxanide dose prediction SARS CoV treatment chemoprophylaxis; COVID-19; SARS-CoV-2; coronavirus; lung; pharmacokinetics.

Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has been declared a global pandemic and urgent treatment and prevention strategies are needed. Nitazoxanide, an anthelmintic drug, has been shown to exhibit in vitro activity against SARS-CoV-2. The present study used physiol. based pharmacokinetic (PBPK) modeling to inform optimal doses of nitazoxanide capable of maintaining plasma and lung tizoxanide exposures above the reported SARS-CoV-2 EC90. A whole-body PBPK model was validated against available pharmacokinetic data for healthy individuals receiving single and multiple doses between 500 and 4000 mg with and without food. The validated model was used to predict doses expected to maintain tizoxanide plasma and lung concentrations above the EC90 in >90% of the simulated population. PopDes was used to estimate an optimal sparse sampling strategy for future clin. trials. The PBPK model was successfully validated against the reported human pharmacokinetics. The model predicted optimal doses of 1200 mg QID, 1600 mg TID and 2900 mg BID in the fasted state and 700 mg QID, 900 mg TID and 1400 mg BID when given with food. For BID regimens an optimal sparse sampling strategy of 0.25, 1, 3 and 12 h post dose was estimated The PBPK model predicted tizoxanide concentrations within doses of nitazoxanide already given to humans previously. The reported dosing strategies provide a rational basis for design of clin. trials with nitazoxanide for the treatment or prevention of SARS-CoV-2 infection. A concordant higher dose of nitazoxanide is now planned for investigation in the seamless phase I/IIa AGILE trial.

British Journal of Clinical Pharmacology published new progress about Blood plasma. 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

de Lima, Nayana Ferreira published the artcileAlterations in Taenia crassiceps cysticerci cytoskeleton induced by nitazoxanide and flubendazole, HPLC of Formula: 55981-09-4, the main research area is Taenia cytoskeleton nitazoxanide flubendazole; Cysticercosis; Cytoskeleton; Drugs combination; Morphology.

Cysticercosis is the presence of Taenia solium larval stage in tissues such as central nervous system, skin, muscles and eye globe. The current treatment is based on albendazole and praziquantel which already present resistance reports. Therefore, the search for alternative treatments is paramount. The aim of this study was to determine the effect of flubendazole and nitazoxanide on cytoskeleton proteins from Taenia crassiceps cysticerci, an exptl. model for cysticercosis. Cysticerci were cultured in RPMI supplemented medium containing nitazoxanide and/or flubendazole. 24 h after the exposure the cysticerci were processed for scanning and transmission electron microscopy and for protein anal. of the cytoskeleton. The proteins were detected through 1D electrophoresis and identified through Western Blot. Nitazoxanide exposure increased tubulin and actin quantifications in T. crassiceps cysticerci. While flubendazole alone and the drugs combinations induced an increase in α-tubulin and actin and decreased β-tubulin quantifications in the parasite. Morphol. changes such as swelling and rupture of vesicle, stiff membrane, decrease in movements were observed when the cysticerci were incubated with the different compounds In conclusion the drugs induced significative impact in the parasites cytoskeleton and may be considered as alternative treatments for cysticercosis.

Acta Tropica published new progress about Cysticercosis. 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

Ferreira de Lima, Nayana published the artcileIn vitro metabolic stress induced by nitazoxanide and flubendazole combination in Taenia crassiceps cysticerci, Computed Properties of 55981-09-4, the main research area is Taenia crassiceps nitazoxanide flubendazole antiparasitic cysticercosis; Experimental cysticercosis; Flubendazole; Metabolism; Nitazoxanide.

Taenia crassiceps is often used as exptl. model for T. solium cysticercosis studies. Currently cysticercosis antiparasitic treatment is based on albendazole and praziquantel which may present side effects and parasitic resistance. The search for other antiparasitic drugs is necessary. Nitazoxanide (NTZ) and flubendazole (FLB) are broad spectrum antiparasitic drugs that present anti-cysticercosis effect. Metabolic analyses help to determine the impact of these drugs on parasites. The aim of this study was to determine the impact on the production and excretion of organic metabolites in T. crassiceps cysticerci after in vitro exposure to NTZ and FLB, isolated or in combination. T. crassiceps cysticerci were culture in RPMI medium and exposed to 10μg/mL of NTZ, 10μg/mL of FLB or 10μg/mL of NTZ +10μg/mL of FLB. 24 h after exposure, the parasites were chromatog. analyzed to determine the impact of these drugs on glycolysis, homolactic fermentation, tricarboxylic acid cycle, fatty acids oxidation and proteins catabolism. It was possible to determine that the drugs combination induced greater metabolic impact on cysticerci in comparison to the isolated drugs exposure. The drugs combination induced gluconeogenesis, metabolic acidosis, increase in tricarboxylic acid cycle and in proteins catabolism. While the NTZ isolated exposure induced metabolic acidosis and protein catabolism and the FLB isolate exposure induced gluconeogenesis and protein catabolism. These results show that the combination of drugs with different modes of action increase the antiparasitic effect and may be indicated as alternative cysticercosis treatments.

Experimental Parasitology published new progress about Cysticercosis. 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

Nandi, Sisir published the artcileThe Antiviral and Antimalarial Drug Repurposing in Quest of Chemotherapeutics to Combat COVID-19 Utilizing Structure-Based Molecular Docking, Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is COVID antiviral antimalarial drug chemotherapeutic mol docking; COVID-19; drug repurposing; prediction of lead compounds.; structure-based docking.

The novel coronavirus disease (COVID-19) is caused by a new strain (SARS-CoV-2) that erupted in 2019. Nowadays, it is a great threat that claims uncountable lives worldwide. There is no specific chemotherapeutics developed yet to combat COVID-19. Therefore, scientists have been devoted to the quest of the medicine that can cure COVID-19. Existing antivirals, such as ASC09/ritonavir, lopinavir/ritonavir with or without umifenovir in combination with antimalarial chloroquine or hydroxychloroquine, have been repurposed to fight the current coronavirus epidemic. Exact biochem. mechanisms of these drugs towards COVID-19 have not been discovered to date. In-silico mol. docking can predict the mode of binding to sort out the existing chemotherapeutics having a potential affinity towards inhibition of the COVID-19 target. An attempt has been made in the present work to carry out docking analyses of 34 drugs, including antivirals and antimalarials, to explain explicitly the mode of interactions of these ligands towards the COVID-19protease target. 13 Compounds having good binding affinity have been predicted towards protease binding inhibition of COVID-19. Our in silico docking results have been confirmed by current reports from clin. settings through the citation of suitable exptl. in vitro data available in the published literature.

Combinatorial Chemistry & High Throughput Screening published new progress about Antimalarials. 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

Tsanni, Abdullahi published the artcileAfrican scientists race to test COVID drugs – but face major hurdles, Safety of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is remdesivir molnupiravir antiviral agent drug repurposing COVID19; Developing world; Medical research; SARS-CoV-2.

In a bid to stave off looming disaster, scientists are trying to repurpose drugs used for malaria and other diseases, but infrastructure and recruitment challenges stymie progress. The continent desperately needs drug treatments for COVID-19 – not just vaccines – to avert a lingering disaster. But testing them has not been easy. If effective, these treatments may prevent severe disease and hospitalization.

Nature (London, United Kingdom) published new progress about Antimalarials. 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

Carradori, Simone published the artcileAre there any Therapeutic Options Currently Available for Wuhan Coronavirus?, HPLC of Formula: 55981-09-4, the main research area is there any therapeutic options currently available Wuhan coronavirus.

Since its spreading from Wuhan and other cities in China at the end of 2019, The World Health Organization (WHO) established strict and sudden emergency procedures to limit the mortality rate and avoid the development of a global threat. Meanwhile, scientists enlarged their knowledge of 2019-nCoV pathogenicity and transmissibility. Many drugs have been explored in the field of Medicinal Chem. for their anti-viral efficacy. We collected information published on the drug candidates that may be useful to reduce the viral infection.

Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry published new progress about Antimalarials. 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

Mule, Shubham published the artcileDrug repurposing strategies and key challenges for COVID-19 management, Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is review COVID management drug repurposing; SARS-CoV2; clinical trials; drug repurposing; drug targets; pathophysiology.

COVID-19 is a clin. outcome of viral infection emerged due to strain of beta coronavirus which attacks the type-2 pneumocytes in alveoli via angiotensin-converting enzyme 2 (ACE2) receptors. There is no satisfactory drug developed against ‘SARS-CoV2’, highlighting an immediate necessity chemotherapeutic repurposing plan COVID-19. Drug repurposing is a method of selection of approved therapeutics for new use and is considered to be the most effective drug finding strategy since it includes less time and cost to obtain treatment compared to the de novo drug acquisition process. Several drugs such as hydroxychloroquine, remdesivir, teicoplanin, darunavir, ritonavir, nitazoxanide, chloroquine, tocilizumab and favipiravir (FPV) showed their activity against ‘SARS-CoV2’; in vitro. This review has emphasized on repurposing of drugs, and biologics used in clin. set up for targeting COVID-19 and to evaluate their pharmacokinetics, pharmacodynamics and safety with their future aspect. The key benefit of drug repurposing is the wealth of information related to its safety, and easy accessibility. Altogether repurposing approach allows access to regulatory approval as well as reducing sophisticated safety studies.

Journal of Drug Targeting published new progress about Antimalarials. 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

Laudisi, Federica published the artcileRepositioning of anthelmintic drugs for the treatment of cancers of the digestive system, SDS of cas: 55981-09-4, the main research area is review repositioning anthelmintic drug cancer digestive system; STAT3; Wnt/β-catenin; benzimidazole; chemotherapy; colorectal cancer; drug repurposing; hepatocellular carcinoma; niclosamide; rafoxanide; salicylanilide.

Tumors of the digestive system, when combined together, account for more new cases and deaths per yr than tumors arising in any other system of the body and their incidence continues to increase. Despite major efforts aimed at discovering and validating novel and effective drugs against these malignancies, the process of developing such drugs remains lengthy and costly, with high attrition rates. Drug repositioning (also known as drug repurposing), i.e., the process of finding new uses for approved drugs, has been gaining popularity in oncol. drug development as it provides the opportunity to expedite promising anti-cancer agents into clin. trials. Among the drugs considered for repurposing in oncol., compounds belonging to some classes of anthelmintics-a group of agents acting against infections caused by parasitic worms (helminths) that colonize the mammalian intestine-have shown pronounced anti-tumor activities and attracted particular attention due to their ability to target key oncogenic signal transduction pathways. In this review, we summarize and discuss the available exptl. and clin. evidence about the use of anthelmintic drugs for the treatment of cancers of the digestive system.

International Journal of Molecular Sciences published new progress about Anthelmintics. 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

Clarke, Naomi E. published the artcileEfficacy of anthelminthic drugs and drug combinations against soil-transmitted helminths: a systematic review and network meta-analysis, Product Details of C12H9N3O5S, the main research area is meta analysis soil transmitted helminth anthelminthic drug.

Meta-anal. of periodic mass distribution of benzimidazole anthelminthic drugs is the key strategy to control soil-transmitted helminths (STHs) globally. However, benzimidazoles have low efficacy against Trichuris trichiura, and there are concerns about benzimidazole resistance potentially emerging in humans. Therefore, identifying alternative drug regimens is a pressing priority. We present a systematic review and network meta-anal. comparing the efficacy of 21 different anthelminthic drug regimens, including standard, novel, and combination treatments. We searched PubMed, Medline, Embase, Web of Science, and Cochrane databases and identified studies comparing anthelminthic treatments to each other or placebo. The outcomes calculated were relative risk (RR) of cure and difference in egg reduction rates (dERR). We used an automated generalized pairwise modeling framework to generate mixed treatment effects against a common comparator, the current standard treatment (single-dose albendazole). Our search identified 4876 studies, of which 114 were included in the meta-anal. Results identified several drug combinations with higher efficacy than single-dose albendazole for T. trichiura, including albendazole-ivermectin (RR of cure, 3.22 [95% confidence interval {CI}, 1.84-5.63]; dERR, 0.97 [95% CI,.21-1.74]), albendazole-oxantel pamoate (RR, 5.07 [95% CI, 1.65-15.59]; dERR, 0.51 [95% CI,.50-.52]), mebendazole-ivermectin (RR, 3.37 [95% CI, 2.20-5.16]), and tribendimidine-oxantel pamoate (RR, 4.06 [95% CI, 1.30-12.64]). There are several promising drug combinations that may enhance the impact of STH control programs on T. trichiura, without compromising efficacy against Ascaris lumbricoides and hookworm. We suggest further, large-scale trials of these drug combinations and consideration of their use in STH control programs where T. trichiura is present.

Clinical Infectious Diseases published new progress about Anthelmintics. 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