Tag: M.W=200-350

Pinto, Erika Gracielle published the artcileTargeting intracellular Leishmania (L.) infantum with nitazoxanide entrapped into phosphatidylserine-nanoliposomes: An experimental study, Formula: C12H9N3O5S, the main research area is nitazoxanide nanolipossome delivery system phosphatidylserine leishmaniasis Leishmania; Leishmania; Liposomes; Macrophage interaction; Nitazoxanide; Therapy.

Leishmaniasis is a parasitic neglected tropical disease and result in a broad spectrum of clin. manifestations, ranging from a single ulceration to a progressive and fatal visceral disease. Comprising a limited and highly toxic therapeutic arsenal, new treatments are urgently needed. Targeting delivery of drugs has been a promising approach for visceral leishmaniasis (VL). Phosphatidylserine-liposomes have demonstrated superior efficacy in VL, targeting intracellular parasites in host cells through macrophage scavenger receptors. In this work, we investigated the in vitro and in vivo efficacy of the antihelminthic drug nitazoxanide in a nanoliposomal formulation against Leishmania (L.) infantum. Physicochem. parameters of liposomes containing nitazoxanide (NTZ-LP) were determined by dynamic light scattering and small angle X-ray scattering. The efficacy of the formulation was verified in an intracellular amastigote model and in an exptl. hamster model. Our findings showed that NTZ-LP was able to eliminate the amastigotes inside the host cell with an IC50 value of 16μM. NTZ-LP was labeled a fluorescent probe and by spectrofluorimetry, we observed that the infected macrophages internalized similar levels of the drug to the uninfected cells. The confocal microscopy images confirmed the uptake and demonstrated a diffuse distribution of the NTZ-LP in the cytoplasm of Leishmania-infected macrophages, with the vesicles in a closer proximity to the parasites. For the in vivo efficacy, the liposomal NTZ-LP was administrated i.p. to Leishmania-infected hamsters for 10 consecutive days at 2 mg/kg/day. By qPCR we demonstrated a reduction of the parasite burden by 82% and 50% in the liver (p < 0.05) and spleen (p < 0.05), resp. NTZ (non-liposomal) was administered at 100 mg/kg/day per oral (p.o.) for the same period, but demonstrated no efficacy. This liposomal formulation ensured a targeting delivery of NTZ to the intracellular parasites, resulting in an good efficacy at a low dose in animals, and it may represent a new candidate therapy for VL. Chemico-Biological Interactions 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, Formula: C12H9N3O5S.

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

Srikala, S. Vinaya published the artcileFormulation, characterization and antihelminthic activity testing of nitazoxanide superporous hydrogel tablets, Application of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is antihelminthic activity nitazoxanide superporous hydrogel tablets.

In the pharmaceutical field controlled release products have the ability to maintain desired medicament concentration or a longer period of time. Certain drugs are relatively insoluble in water and have high dose requirements that render unsuitable formulation difficulties in sustained release formulations. Nitazoxanide which is a high dose water insoluble antiprotozoal drug was formulated with the aim. To modulate gastro-retentive dosage form based on the superporous hydrogel composites. Foaming technique was used in the preparation of SPH composites. The superporous hydrogels were extremely sensitive to pH of swelling media and good porosity. Superporous hydrogels tablets of nitazoxanide showed good pre-compressional and post-compressional properties. Formulation X is the best formulation containing chitosan, polyvinyl alc., formaldehyde, exhibited good swelling ratio. The compatibility studies were performed by Fourier Transform IR (FT-IR) Spectroscopic Studies, Differential Scanning Calorimetry Studies (DSC). All formulations were evaluated for stability, drug content, and kinetic drug release & in-vitro drug release profile. It was concluded that the proposed gastro-retention drug delivery provides a different supply of nitazoxanide directly to the stomach.

Journal of Drug Delivery and Therapeutics 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, Application of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate.

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

Talaam, Keith Kiplangat published the artcileMitochondria as a potential target for the development of prophylactic and therapeutic drugs against Schistosoma mansoni infection, Product Details of C12H9N3O5S, the main research area is Schistosoma mansoni infection mitochondria prophylactic therapeutic drug; drug development; electron transport chain; fumarate respiration; in vivo model; mitochondria; schistosomiasis.

The emergence of parasites resistant to praziquantel, the only therapeutic agent, and its ineffectiveness as a prophylactic agent (inactive against the migratory/juvenile Schistosoma mansoni), make the development of new antischistosomal drugs urgent. The parasite’s mitochondrion is an attractive target for drug development, because this organelle is essential for survival throughout the parasite’s life cycle. We investigated the effects of 116 compounds against Schistosoma mansoni cercaria motility that have been reported to affect mitochondrion-related processes in other organisms. Next, eight compounds plus two controls (mefloquine and praziquantel) were selected and assayed against the motility of schistosomula (in vitro) and adults (ex vivo). Prophylactic and therapeutic assays were performed using infected mouse models. Inhibition of oxygen consumption rate (OCR) was assayed using Seahorse XFe24 analyzer. All selected compounds showed excellent prophylactic activity, reducing the worm burden in the lungs to less than 15% of that obtained in the vehicle control. Notably, ascofuranone showed the highest activity, with a 98% reduction of the worm burden, suggesting the potential for the development of ascofuranone as a prophylactic agent. The worm burden of infected mice with S. mansoni at the adult stage was reduced by more than 50% in mice treated with mefloquine, nitazoxanide, amiodarone, ascofuranone, pyrvinium pamoate, or plumbagin. Moreover, adult mitochondrial OCR was severely inhibited by ascofuranone, atovaquone, and nitazoxanide, while pyrvinium pamoate inhibited both mitochondrial and nonmitochondrial OCRs. These results demonstrate that the mitochondria of S. mansoni are a feasible target for drug development.

Antimicrobial Agents and Chemotherapy published new progress about Cell migration. 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

Yang, Bo published the artcileHost cells with transient overexpression of MDR1 as a novel in vitro model for evaluating on-target effect for activity against the epicellular Cryptosporidium parasite, Product Details of C12H9N3O5S, the main research area is Cryptosporidium MDR1 anticryptosporidial antiparasitic paclitaxel.

To rapidly generate host cells with resistance to multiple compounds for differentiating drug action on parasite target or the host cell target (i.e. on-target or off-target effect) against the zoonotic enteric parasite Cryptosporidium parvum. Transient overexpression of a multidrug resistance protein 1 (MDR1) gene in host cells (HCT-8 cell line) was explored to increase drug tolerance of the host cells to selected anti-cryptosporidial leads. In vitro cytotoxicity and anti-cryptosporidial efficacy of selected compounds were evaluated on the parasite grown in WT parental and transiently transfected HCT-8 cells. The approach was based on the theory that, for an epicellular parasite receiving consistent exposure to compounds in culture medium, overexpressing MDR1 in HCT-8 cells would increase drug tolerance of host cells to selected compounds but would not affect the anti-cryptosporidial efficacy if the compounds acted solely on the parasite target and the drug action on host cell target played no role on the antiparasitic efficacy. Six known anti-cryptosporidial leads were tested. Transient overexpression of MDR1 increased drug tolerance of HCT-8 cells on paclitaxel, doxorubicin HCl and vincristine sulfate (2.11- to 2.27-fold increase), but not on cyclosporin A, daunorubicin HCl and nitazoxanide. Increased drug tolerance in host cells had no effect on antiparasitic efficacy of paclitaxel, but affected that of doxorubicin HCl. Data confirmed that, at efficacious concentrations, paclitaxel acted mainly on the parasite target, while doxorubicin might act on both parasite and host cell targets. This model can be employed for studying the action of addnl. anti-cryptosporidial leads, and adapted to studying drug action in other epicellular pathogens. The limitation of the model is that the anti-cryptosporidial leads/hits need to be MDR1 substrates.

Journal of Antimicrobial Chemotherapy published new progress about Cell viability. 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

Tachoua, Wafa published the artcileAn in-silico evaluation of COVID-19 main protease with clinically approved drugs, HPLC of Formula: 55981-09-4, the main research area is SARSCoV2 main protease in silico evaluation clin approved drug; ADMET; Approved drugs; COVID-19 main protease; MD simulation; Molecular docking; SwissDock.

A novel strain of coronavirus, namely, SARS-CoV-2 identified in Wuhan city of China in Dec. 2019, continues to spread at a rapid rate worldwide. There are no specific therapies available and investigations regarding the treatment of this disease are still lacking. In order to identify a novel potent inhibitor, we performed blind docking studies on the main virus protease Mpro with eight approved drugs belonging to four pharmacol. classes such as: anti-malarial, anti-bacterial, anti-infective and anti-histamine. Among the eight studied compounds, Lymecycline and Mizolastine appear as potential inhibitors of this protease. When docked against Mpro crystal structure, these two compounds revealed a min. binding energy of -8.87 and -8.71 kcal/mol with 168 and 256 binding modes detected in the binding substrate pocket, resp. Further, to study the interaction mechanism and conformational dynamics of protein-ligand complexes, Mol. dynamic simulation and MM/PBSA binding free calculations were performed. Our results showed that both Lymecycline and Mizolastine bind in the active site. And exhibited good binding affinities towards target protein. Moreover, the ADMET anal. also indicated drug-likeness properties. Thus it is suggested that the identified compounds can inhibit Chymotrypsin-like protease (3CLpro) of SARS-CoV-2.

Journal of Molecular Graphics & Modelling published new progress about Binding energy. 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

Hashan, Mohammad Rashidul published the artcileEffect of nitazoxanide on diarrhea: A systematic review and network meta-analysis of randomized controlled trials, SDS of cas: 55981-09-4, the main research area is review nitazoxanide antidiarrheals diarrhea; Antibiotic; Diarrhea; Meta-analysis; Nitazoxanide; Systematic review.

We aimed to systematically review evidence pertaining to the safety and efficacy of nitazoxanide in treating infectious diarrhea. On Sept. 21, 2017, we identified relevant studies using 12 databases. The estimates of the included studies were pooled as a risk ratio (RR). We conducted a network and pairwise random-effects meta-anal. for both direct and indirect comparisons of different organisms that are known to cause diarrhea. The primary and secondary anal. outcomes were clin. response until cessation of illness, parasitol. response and adverse events. We included 18 studies in our anal. In cryptosporidiosis, the overall estimate favored nitazoxanide in its clin. response in comparison with placebo RR 1.46 [95% CI 1.22-1.74; P-value <0.0001]. Network meta-anal. among patients with Giardia intestinalis showed an increase in the probability of diarrheal cessation and parasitol. responses in comparison with placebo, RR 1.69 [95% CI 1.08-2.64, P-score 0.27] and RR 2.91 [95% CI 1.72-4.91, P-score 0.55] resp. In Clostridium difficile infection, the network meta-anal. revealed a non-significantly superior clin. response effect of nitazoxanide to metronidazole 31 days after treatment RR 1.21 [95% CI 0.87-1.69, P-score 0.26]. In Entamoeba histolytica, the overall estimate significantly favored nitazoxanide in parasitol. response with placebo RR 1.80 [95% CI 1.35-2.40, P-value < 0.001]. We highlighted the effectiveness of nitazoxanide in the cessation of diarrhea caused by Cryptosporidium, Giardia intestinalis and Entamoeba histolytica infection. We also found significant superiority of NTZ to metronidazole in improving the clin. response to G. intestinalis, thus it may be a suitable candidate for treating infection-induced diarrhea. To prove the superiority of NTZ during a C. difficile infection may warrant a larger-scale clin. trial since its superiority was deemed insignificant. We recommend nitazoxanide as an appropriate option for treating infectious diarrhea. Acta Tropica published new progress about Antidiarrheals. 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

Anastasiou, Ioanna A. published the artcileIn vitro data of current therapies for SARS-CoV-2, Quality Control of 55981-09-4, the main research area is review therapy SARS CoV 2; ACE2 receptor; SARS-CoV-2 (COVID-19); VeroE6 Cells; in vitro studies; therapies; vaccines.

Background: In Dec. 2019, a new coronavirus, named Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2), emerged from China, causing pneumonia outbreaks first in the Wuhan region and then spread worldwide. Due to a lack of efficient and specific treatments and the need to contain the epidemic, drug repurposing appears to be the most efficient tool to find a therapeutic solution Objectives: The aim of this study was to summarize in vitro data of current agents used for the management of SARS-CoV-2 all over the world. Methods: A literature search of articles from Jan. 2000 until Apr. 2020 was performed using MEDLINE, EMBASE and the Cochrane Library to assess in vitro data of current or putative therapies for SARS-CoV-2. Results: Although in vitro studies are scarce, data regarding chloroquine, hydroxychloroquine, remdesivir, nitazoxanide, teicoplanin, ivermectin, lopinavir, homoharringtonine, and emetine seem promising. Conclusion: Scientists all over the world should work together and increase their efforts in order to find feasible and efficient solutions against this new global viral threat.

Current Medicinal Chemistry published new progress about Allium sativum. 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

Xu, Junlin published the artcileComputational drug repositioning using similarity constrained weight regularization matrix factorization: A case of COVID -19, Formula: C12H9N3O5S, the main research area is COVID19 drug repositioning computational modeling; association prediction; drug-target; drug-virus association; matrix factorization; similarity constrained.

Amid the COVID-19 crisis, we put sizeable efforts to collect a high number of exptl. validated drug-virus association entries from literature by text mining and built a human drug-virus association database. To the best of our knowledge, it is the largest publicly available drug-virus database so far. Next, we develop a novel weight regularization matrix factorization approach, termed WRMF, for in silico drug repurposing by integrating three networks: the known drug-virus association network, the drug-drug chem. structure similarity network, and the virus-virus genomic sequencing similarity network. Specifically, WRMF adds a weight to each training sample for reducing the influence of neg. samples (i.e. the drug-virus association is unassocd.). A comparison on the curated drug-virus database shows that WRMF performs better than a few state-of-the-art methods. In addition, we selected the other two different public datasets (i.e. Cdataset and HMDD V2.0) to assess WRMFs performance. The case study also demonstrated the accuracy and reliability of WRMF to infer potential drugs for the novel virus. In summary, we offer a useful tool including a novel drug-virus association database and a powerful method WRMF to repurpose potential drugs for new viruses.

Journal of Cellular and Molecular Medicine published new progress about Clinical trials. 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

Perez-Villanueva, Jaime published the artcileThe giardicidal activity of lobendazole, fabomotizole, tenatoprazole and ipriflavone: A ligand-based virtual screening and in vitro study, Formula: C12H9N3O5S, the main research area is Giardia iobendazole fabomotizole tenatoprazole ipriflavone giardicidal virtual screening; Fabomotizole; Giardia intestinalis; Ipriflavone; Lobendazole; Tenatoprazole; Virtual screening.

A ligand-based virtual screening study to search for giardicidal compounds on a 6551 ChEMBL drugs database was carried out using mol. similarity. Three fingerprints implemented in MayaChemTools with different design and validated by ROC curves, were used. Twelve compounds were retrieved from this screening, from which, four representative compounds were selected to carry out biol. assays. Whereas two compounds were com. available, the addnl. two compounds were synthesized during the development of this work. The biol. assays revealed that the compounds possess in vitro activity against five strains of Giardia intestinalis, each with different susceptibility/resistance rates to metronidazole, albendazole and nitazoxanide. Particularly, tenatoprazole showed the best effect against the WB and IMSS strains. Furthermore, fabomotizole, tenatoprazole and ipriflavone showed a higher activity against resistant strains than the reference drugs: metronidazole, albendazole and nitazoxanide.

European Journal of Medicinal Chemistry published new progress about Drug resistance. 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

Ydsten, Karin A. published the artcileQuinacrine treatment of nitroimidazole-refractory giardiasis, Category: esters-buliding-blocks, the main research area is quinacrine nitroimidazole immunosuppression refractory giardiasis; adverse effects; epidemiology; giardiasis; nitroimidazole refractory; nitroimidazole resistance; quinacrine; tolerability; treatment.

Limited evidence exists on efficacy and tolerability of quinacrine for nitroimidazole-refractory giardiasis. Nitroimidazole-refractory giardiasis cases, defined as microbiol. (microscopy and/or PCR) confirmed treatment failure after 2 courses, during 2008-2020, were retrospectively identified. Of 87 patients, 54 (62%) had visited India. Quinacrine was used in 54 (62%); 51 received monotherapy and 3 combined with metronidazole. Only 3 had pos. stool samples with persisting symptoms after quinacrine treatment (94% parasitol. efficacy) and all were cured after a second treatment. One (1.9%) had mild adverse effects recorded. Quinacrine is an effective treatment for nitroimidazole-refractory giardiasis with good tolerability.

Journal of Infectious Diseases published new progress about Drug resistance. 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