Tag: M.W=200-350

Stachulski, Andrew V. published the artcileSynthesis, antiviral activity, preliminary pharmacokinetics and structural parameters of thiazolide amine salts, Name: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is thiazolide amine salt xray crystal structure antiviral activity pharmacokinetics; amine salts; antiviral; pharmacokinetics; thiazolides; x-ray structure.

The thiazolides, typified by nitazoxanide, are an important class of anti-infective agents. A significant problem with nitazoxanide and its active circulating metabolite tizoxanide is their poor solubility We report the preparation and evaluation of a series of amine salts of tizoxanide and the corresponding 5-Cl thiazolide. These salts demonstrated improved aqueous solubility and absorption, as shown by physicochem. and in vivo measurements. They combine antiviral activity against influenza A virus with excellent cell safety indexes. We also report the x-ray crystal structural data of the ethanolamine salt. The ethanol salt of thiazolide retains the activity of the parent together with an improved cell safety index, making it a good candidate for further evaluation.

Future Medicinal Chemistry published new progress about Absorption. 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

Baunwall, Simon Mark Dahl published the artcileDanish national guideline for the treatment of Clostridioides difficile infection and use of faecal microbiota transplantation (FMT), Quality Control of 55981-09-4, the main research area is review antibiotics Clostridioides difficile fecal microbiota transplantation; Clostridioides difficile; fecal microbiota transplantation.

This Danish national guideline describes the treatment of adult patients with Clostridioides (formerly Clostridium) difficile (CD) infection and the use of fecal microbiota transplantation (FMT). It suggests min. standard for implementing an FMT service. Four scientific societies appointed members for a working group which conducted a systematic literature review and agreed on the text and recommendations. All clin. recommendations were evalluated for evidence level and grade of recommendation. In CD infection, the use of marketed and exptl. antibiotics as well as microbiota-based therapies including FMT are described. An algorithm for evaluating treatment effect is suggested. The organization of FMT, donor recruitment and screening, laboratory preparation, clin. application and follow-up are described. Updated evidence for the treatment of CD infection and the use of FMT is provided.

Scandinavian Journal of Gastroenterology published new progress about Antibiotics. 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

Maricuto, Andrea L. published the artcileAmoebic liver abscess in a COVID-19 patient: a case report, Related Products of esters-buliding-blocks, the main research area is amoebic liver abscess COVID19; Amoebic liver abscess; COVID-19; Case report; Entamoeba histolytica; SARS-CoV-2; Venezuela.

Amoebiasis is a parasitic disease caused by Entamoeba histolytica, which affects people living in low- and middle-income countries and has intestinal and extraintestinal manifestations. To date, knowledge on coronavirus disease 2019 (COVID-19) coinfection with enteric parasites is limited, and E. histolytica coinfection has not been previously described. Here we present the case of a patient with COVID-19 who, during hospitalisation, presented a clin. picture consistent with an amoebic liver abscess (ALA). Case presentation: A 54-yr-old man, admitted as a suspected case of COVID-19, presented to our hospital with dyspnoea, malaise, fever and hypoxemia. A nasopharyngeal swab was pos. for severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) by reverse-transcription polymerase chain reaction. After 7 days, he developed diarrhoea, choluria and dysentery. An abdominal ultrasound showed a lesion compatible with a liver abscess; stool examination revealed E. histolytica trophozoites, and addnl. serol. for E. histolytica was pos. After 12 days of treatment with metronidazole, ceftazidime and nitazoxanide, the patient reported acute abdominal pain, and an ultrasound examination revealed free liquid in the abdominal cavity. An emergency exploratory laparotomy was performed, finding 3000 mL of a thick fluid described as “”anchovy paste””. Computed tomog. scan revealed a second abscess. He ended up receiving 21 days of antibiotic treatment and was discharged with satisfactory improvement. Conclusion: Here we present, to the best of our knowledge, the first report of ALA and COVID-19 co-presenting. Based on their pathophysiol. similarities, coinfection with SARS-CoV-2 and E. histolytica could change the patient’s clin. course; however, larger studies are needed to fully understand the interaction between these pathogens.

BMC Infectious Diseases published new progress about Antibiotics. 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, Related Products of esters-buliding-blocks.

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

Gunaratne, Anoja W. published the artcileCombinations of antibiotics and vonoprazan for the treatment of Helicobacter pylori infections-Exploratory study, Computed Properties of 55981-09-4, the main research area is Helicobacter infection vonoprazan amoxicillin rifabutin levofloxacin drug safety; Helicobacter pylori ; antibiotics; potassium-competitive acid blockers; proton pump inhibitors; urea breath test.

Vonoprazan fumarate is a novel potassium-competitive acid blocker more effective in suppressing acid production than proton pump inhibitors (PPIs) and when combined with antibiotics has been used to eradicate Helicobacter pylori (H. pylori) infection. However, it has not yet been examined in an Australian setting. This study aimed to report on the efficacy and safety of vonoprazan-containing antibiotic combination therapies in the eradication of H. pylori. A single-center, exploratory, clin. review of patients 18 years or over, pos. for H. pylori on Urea Breath Test (UBT), and/or histopathol. who underwent a 10-day treatment of combination antibiotics plus vonoprazan between Jan. 2017 and Sept. 2019 was conducted. Eleven different combinations of antibiotics that included 2-5 different antibiotics predominantly amoxicillin, rifabutin, levofloxacin, furazolidone, nitazoxanide, and tetracycline were included. The eradication success was based on neg. UBT results and/or histopathol. results after the treatment. Descriptive statistics were summarized. One hundred and fifty-three patients (Female n = 74, 48%) with a pos. for H. pylori were treated with vonoprazan-containing antibiotic combination therapy during the study period. Of the 153 patients, 48 (31%) had previously failed a PPI-based H. pylori treatment. Follow-up was available for 66/153 (43%) patients. In those who completed follow-up, overall eradication was achieved in 97% (64/66) of patients. In the subgroup of patients treated for the first time, eradication was achieved in 100% (44/44). In those who had failed prior, non-vonoprazan-containing treatment, eradication was achieved in 91% (20/22) of patients. Vonoprazan-containing antibiotic therapy is an effective H. pylori eradication treatment. It is capable of achieving 100% efficacy in patients treated for the first time and even 91% efficacy in patients with previous eradication failure. Subsequent studies utilizing a factorial design will be needed to optimize each regimen as most regimens contained more than two antibiotics.

Helicobacter published new progress about Antibiotics. 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

Radzki, Radoslaw Piotr published the artcileLipoic acid (LA) dose-dependently protects bone losses in the mandible of rats during the development of osteopenia by inhibiting oxidative stress and promoting bone formation, Safety of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is osteopenia bone loss oxidative stress lipoic acid; DXA; Lipoic acid; Osteoporosis; Oxidative stress; Peripheral quantitative tomography; Rats.

Our study was carried out to evaluate the effect of lipoic acid (LA) on the densitometric properties, structure and mech. strength of the mandible of Wistar rats with developing osteopenia. The study used 42 sham-operated (SHO) and ovariectomized (OVX) rats. The OVX rats were randomly divided (n = 6) onto two controls treated s.c. with physiol. saline (OVX-PhS) and 17β-estradiol (OVX-E2), resp., and onto four exptl. OVX groups that received LA in the doses of 12.5, 25, 50 and 100 mg/kg/day for 28 days. The results demonstrated that the lack of estrogen brought about osteopenic bone changes, especially in the trabecular compartment. In addition, while the usage of LA in the doses of 12.5 and 25 LA had no effect in OVX rats, the dose of 100 effectively inhibited osteopenic changes of the mandible. This dose maintained structural, densitometric and mech. parameters at levels like that in the SHO and OVX-E2 groups by inhibiting the destructive influence of oxidative stress. Dose 50, however, was revealed to be the most effective. It not only inhibited atrophic changes and the influence of oxidative stress, but also stimulated the formation of mandibular bone tissue. Our results suggest that the administration of LA is effective in preventing atrophic changes in the mandibular bone tissue in conditions of ovarian hormone deficiency and suggest its potential in the therapy of osteoporosis.

Biomedicine & Pharmacotherapy published new progress about Blood serum. 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

Shaikh, Jaweriah Ali published the artcileEfficacy of nitazoxanide and probiotics in children presenting with acute watery diarrhea presenting at Tertiary Care Hospital, Karachi, Category: esters-buliding-blocks, the main research area is acute watery diarrhea nitazoxanide probiotics.

Objective: To compare the efficacy of nitazoxanide and probiotics in children presenting with acute watery diarrhea presenting at Tertiary Care Hospital, Karachi. Material andMethods: The study design was randomized control trial. Study was conducted at Department of Pediatrics, Ziauddin University Hospital, Karachi. The duration of this study was Six months after approval from 02 Dec. 2019 to 02 June 2020. Data was prospectively collected from patients after taking a verbal consent. 160 patients who met the diagnostic criteria were included. Brief history was taken and demog. information was entered in the Performa. Quant. data was presented as simple descriptive statistics giving mean and standard deviation and qual. variables was presented as frequency and percentages. Results: Out of 80 patients in the nitazoxanide group mean age, duration of diarrhea, length of hospital stay, height, weight and Vesikari score in our study was 24.21±4.24 mo, 5.87±1.78 days, 8±2.54 days, 130.6±10.21 cm, 27.7±2.25 kg and 4.7±0.89 resp. Whereas, out of 80 patients in the probiotics group min. age, duration of diarrhea, length of hospital stay, height, weight and Vesikari score in our study was 26.48±4.24 mo, 6.41±1.14 days, 8±1.89 days, 121.9±7.47 cm, 29.2±3.41 kg and 5.1±0.58 resp. Efficacy in the nitazoxanide group was 67 (83.8%) compared with 58 (72.5%) in the probiotic group. Conclusion: Treatment with nitazoxanide and probiotics is effective in the management of children with acute watery diarrhea. Small differences in favor of nitazoxanide were found in comparison with probiotics. Nitazoxanide is an important treatment option for acute watery diarrhea.

Indo American Journal of Pharmaceutical Sciences published new progress about Body height. 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

Mueller, Joachim published the artcileNitroreductases of bacterial origin in Giardia lamblia: Potential role in detoxification of xenobiotics, Application In Synthesis of 55981-09-4, the main research area is Giardia nitroreductase bacterial origin detoxification xenobiotics; anaerobic metabolism; detoxification; electron transfer; pathogenicity; resistance; susceptibility.

The anaerobic parasite Giardia lamblia, causative agent of persistent diarrhea, contains a family of nitroreductase genes most likely acquired by lateral transfer from anaerobic bacteria or archaebacteria. Two of these nitroreductases, containing a ferredoxin domain at their N-terminus, NR1, and NR2, have been characterized previously. Here, we present the characterization of a third member of this family, NR3. In functional assays, recombinant NR1 and NR3 reduced quinones like menadione and the antibiotic tetracycline, and-to much lesser extents-the nitro compound dinitrotoluene. Conversely, recombinant NR2 had no activity on tetracycline. Escherichia coli expressing NR3 were less susceptible to tetracycline, but more susceptible to the nitro compound metronidazole under semi-aerobic growth conditions. G. lamblia overexpressing NR1 and NR3, but not lines overexpressing NR2, are more susceptible to the nitro drug nitazoxanide. These findings suggest that NR3 is an active quinone reductase with a mode of action similar to NR1, but different from NR2. The biol. function of this family of enzymes may reside in the use of xenobiotics as final electron acceptors. Thereby, these enzymes may provide at least two evolutionary advantages namely a higher potential to recycle NAD(P) as electron acceptors for the (fermentative) energy and intermediary metabolism, and the possibility to inactivate toxic xenobiotics produced by microorganisms living in concurrence inside the intestinal habitat.

MicrobiologyOpen published new progress about Amino group. 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

Kushnirov Melnitzer, Vladislav published the artcileHybrid Titanium Oxide/Polymer Amphiphilic Nanomaterials with Controlled Size for Drug Encapsulation and Delivery, Application of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is nanoparticle titanium oxide polymer pharmaceutical.

This work describes for the first time the synthesis of hybrid drug-loaded TiO2/polymer amphiphilic nanoparticles of finely controlled size utilizing a simple and reproducible sol-gel process that comprises the formation of a titanium(IV)/acetone oxo-organo complex followed by its blending with an amphiphilic poly(ethylene oxide)-b-poly(propylene oxide) block copolymer in acetone and its aqueous-phase nanopptn. The size of the hybrid nanoparticles is governed by the complex aging, e.g., hybrid nanoparticles display diameter between 228 and 53 nm for aging of 1 and 36 days, resp. (dynamic light scattering). In addition, they show excellent phys. stability in water owing to the coating of the surface with poly(ethylene oxide) blocks of the copolymer. Conversely, polymer-free TiO2 particles are large and precipitate fast. Incorporation of a model hydrophobic drug, nitazoxanide, to the precursor solution results in hybrid nanoparticles containing 12.9% weight/weight cargo that is released following a bimodal profile. High-resolution transmission electron microscopy (Titan Cubed Themis G2 300) anal. reveals the porous amorphous nanostructure of these novel hybrids and colocalization of drug and copolymer in the nanoparticle bulk. Finally, upon ultrasonication, our hybrid nanoparticles produce reactive oxygen species in vitro which paves the way for their use in sonodynamic and drug release therapies.

Advanced Functional Materials published new progress about Amphiphiles. 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

Kufel, Wesley D. published the artcileSuccessful treatment with secnidazole for trichomoniasis in the setting of metronidazole hypersensitivity, Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is secnidazole metronidazole trichomoniasis nitazoxanide Trichomonas vaginalis; Secnidazole; Trichomonas vaginalis; metronidazole; nitazoxanide; trichomoniasis.

Limited effective treatment options currently exist for trichomoniasis management among patients with metronidazole hypersensitivity. We report a patient with a documented history of metronidazole hypersensitivity who initially was treated with nitazoxanide but demonstrated clin. and microbiol. failure. Secnidazole was subsequently used for treatment, which resulted in clin. and microbiol. cure without observation of cross-reactivity. Secnidazole may represent a potential treatment option for trichomoniasis in patients with metronidazole hypersensitivity after consultation with an infectious disease specialist.

International Journal of STD & AIDS published new progress about Homo sapiens. 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

Sayed, Ahmed M. published the artcileRepurposing of some anti-infective drugs for COVID-19 treatment: A surveillance study supported by an in silico investigation, SDS of cas: 55981-09-4, the main research area is human nitazoxanide doxycycline azithromycin silico investigation coronavirus.

The repurposing of nitazoxanide, doxycycline and azithromycin may be effective to improve the symptoms in mild and moderate COVID-19 subjects. This study aimed to detect and explain the efficacy of reusing of these drugs in treating COVID-19. The study was divided into two parts: clin. and computational parts. In the clin. part, 80 (30 females) subjects with reverse transcription-polymerase chain reaction-confirmed COVID-19 with mild and moderate symptoms were enrolled in the study. Subjects were treated with azithromycin or doxycycline, and nitazoxanide was added to the treatment if the subject had diarrhoea. Subjects were divided into four groups: Group 1: subjects treated with azithromycin (20 subjects); Group 2: subjects treated with doxycycline (20 subjects); Group 3: subjects treated with a combination of nitazoxanide and doxycycline (20 subjects); and Group 4: subjects treated with a combination of nitazoxanide and azithromycin (20 subjects). In the computational part, we docked the three drugs against all currently available COVID-19-related protein targets (viral and non-viral). Subsequently, top hits were subjected to mol. dynamic simulations (MDSs) (50 ns) and binding free energy calculations to further validate the docking experiments and to investigate the binding modes of the potential inhibitors. The symptomatic improvement of mild to moderate subjects was seen on the fifth day after starting treatment in Group 3 and Group 4 and on the seventh day in Group 2. However, for Group 1, the symptomatic improvement of mild to moderate subjects was not seen on the fifth day and required replacement by doxycycline to get the symptomatic improvement. None of the subjects needed intensive care admission and no deaths were reported. In silico, results were in good accordance with the clin. outcomes, where both nitazoxanide and doxycycline achieved the best docking scores against the viral ADP-ribose phosphatase (ADPRP) and the human Adaptor-Associated Kinase 1 (AAK1). MDSs revealed that both drugs were stable in their bindings indicating that they can be considered as lead mols. for targeting ADPRP and AAK1. The clin. and computational studies applied on three FDA-approved antimicrobials together with their recent clin. findings revealed that both nitazoxanide and doxycycline have great therapeutic potential against COVID-19. The future in vitro mechanistic investigation may confirm our primary computational outcomes, and in turn, these classes of compounds provide a promising starting point for further anti-COVID-19 therapeutics.

International Journal of Clinical Practice 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, SDS of cas: 55981-09-4.

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