Tag: 300-400

Xu, Jing;Gao, Liangqin;Liang, Huiqing;Chen, Shao-dong published 《In silico screening of potential anti-COVID-19 bioactive natural constituents from food sources by molecular docking》 in 2021. The article was appeared in 《Nutrition (New York, NY, United States)》. They have made some progress in their research.Application of 55981-09-4 The article mentions the following:

The aim of this study was to seek potential natural compounds that can resist COVID-19 using computer virtual screening technol. through mol. docking of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) 3CL hydrolytic enzyme (3CL^pro) and angiotensin-converting enzyme 2 (ACE2). Mol. docking was achieved by using the Autodock Vina software. The natural phytocompounds acting on 3CL^pro and ACE2 were then selected from the Traditional Chinese Medicine Systems Pharmacol. Database and Anal. Platform. This was followed by speculation on the mechanism of action of phytocompounds. Six potential natural anti-COVID-19 phytocompounds were selected and were evaluated for absorption, distribution, metabolism and excretion (ADME) and Lipinski rules. The content of the six phytocompounds in various fruits and vegetables was determined via a literature search. Red wine, Chinese hawthorn, and blackberry were recommended as supplements because they contained antiviral phytocompounds. Red wine, Chinese hawthorn, and blackberry show promise for resisting COVID-19 and are thus recommended as supplements to prevent the infection of COVID-19 during its outbreak period. To complete the study, the researchers used 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate (cas: 55981-09-4) .

2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate(cas: 55981-09-4) has been approved as an orphan drug for the treatment of diarrhea in children (age, 1–11 years) and is associated with giardiasis, but it also is approved for diarrhea caused by crytosporidiosis in patients with AIDS.Application of 55981-09-4

Reference:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Rahman, Sajid Ur;Mi, Rongsheng;Zhou, Shasha;Gong, Haiyan;Ullah, Munib;Huang, Yan;Han, Xiangan;Chen, Zhaoguo published 《Advances in therapeutic and vaccine targets for Cryptosporidium: Challenges and possible mitigation strategies》 in 2022. The article was appeared in 《Acta Tropica》. They have made some progress in their research.Name: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate The article mentions the following:

A review. Cryptosporidium is known to be the second most common diarrheal pathogen in children, causing potentially fatal diarrhea and associated with long-term growth stunting and cognitive deficits. The only Food and Drug Administration-approved treatment for cryptosporidiosis is nitazoxanide, but this drug has not shown potentially effective results in susceptible hosts. Therefore, a safe and effective drug for cryptosporidiosis is urgently needed. Cryptosporidium genome sequencing anal. may help develop an effective drug, but both in vitro and in vivo approaches to drug evaluation are not fully standardized. On the other hand, the development of partial immunity after exposure suggests the possibility of a successful and effective vaccine, but protective surrogates are not precise. In this review, we present our current perspectives on novel cryptosporidiosis therapies, vaccine targets and efficacies, as well as potential mitigation plans, recommendations and perceived challenges.2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate (cas: 55981-09-4) were involved in the experimental procedure.

2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate(cas: 55981-09-4), a thiazolide compound, is a antiparasitic drug with structure similar to niclosamide.Name: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate

Reference:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Safety of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetateIn 2021, Wipperman, Matthew F.;Bhattarai, Shakti K.;Vorkas, Charles Kyriakos;Maringati, Venkata Suhas;Taur, Ying;Mathurin, Laurent;McAulay, Katherine;Vilbrun, Stalz Charles;Francois, Daphie;Bean, James;Walsh, Kathleen F.;Nathan, Carl;Fitzgerald, Daniel W.;Glickman, Michael S.;Bucci, Vanni published 《Gastrointestinal microbiota composition predicts peripheral inflammatory state during treatment of human tuberculosis》. 《Nature Communications》published the findings. The article contains the following contents:

The composition of the gastrointestinal microbiota influences systemic immune responses, but how this affects infectious disease pathogenesis and antibiotic therapy outcome is poorly understood. This question is rarely examined in humans due to the difficulty in dissociating the immunol. effects of antibiotic-induced pathogen clearance and microbiome alteration. Here, we analyze data from two longitudinal studies of tuberculosis (TB) therapy (35 and 20 individuals) and a cross sectional study from 55 healthy controls, in which we collected fecal samples (for microbiome anal.), sputum (for determination of Mycobacterium tuberculosis (Mtb) bacterial load), and peripheral blood (for transcriptomic anal.). We decouple microbiome effects from pathogen sterilization by comparing standard TB therapy with an exptl. TB treatment that did not reduce Mtb bacterial load. Random forest regression to the microbiome-transcriptome-sputum data from the two longitudinal datasets reveals that renormalization of the TB inflammatory state is associated with Mtb pathogen clearance, increased abundance of Clusters IV and XIVa Clostridia, and decreased abundance of Bacilli and Proteobacteria. We find similar associations when applying machine learning to peripheral gene expression and microbiota profiling in the independent cohort of healthy individuals. Our findings indicate that antibiotic-induced reduction in pathogen burden and changes in the microbiome are independently associated with treatment-induced changes of the inflammatory response of active TB, and the response to antibiotic therapy may be a combined effect of pathogen killing and microbiome driven immunomodulation. The experimental procedure involved many compounds, such as 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate (cas: 55981-09-4) .

2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate(cas: 55981-09-4), an anthelmintic agent, exhibits a broad spectrum of activities against a wide variety of helminths, protozoa, and enteric bacteria infecting animals and humans.Safety of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate

Reference:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Angeles-Arvizu, Adriana;Enriquez-Flores, Sergio;Jimenez-Gutierrez, Alma;Perez-Rangel, Armando;Luna-Arias, Juan Pedro;Castillo-Romero, Araceli;Hernandez, Jose Manuel;Leon-Avila, Gloria published 《MDR1 protein (ABC-C1) Over Expression in Giardia Intestinalis Incubated with Albendazole and Nitazoxanide》. The research results were published in《Acta Parasitologica》 in 2021.Quality Control of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate The article conveys some information:

Giardia intestinalis is a worldwide parasite. Drugs used for the treatment of giardiasis are metronidazole, albendazole and nitazoxanide. The development of drug resistance is an obstacle to the effective treatment. Resistance mechanisms in some parasites involve the participation of ATP-binding cassette (ABC) transporter superfamily. To find if the ATP-binding cassette genes are overexpressed in trophozoites treated with albendazole or nitazoxanide. A search for ATP-binding cassette genes in Giardia sequence database (GiardiaDB) was done and six genes were selected. Trophozoites treated with albendazole or nitazoxanide and the expression of these six ABC genes was quantitated by real-time RT-PCR. The ABC-C1 gene was selected, and a fragment cloned. The ABC-C1 protein was expressed, and polyclonal antibodies were elicited in mice to detect the protein in treated trophozoites, finally a docking anal. was performed for ABC-C1 and tizoxanide interaction. Bioinformatics anal. showed that the ATP-binding cassette (ABC) topol. is present in the six proteins. The qRT-PCR revealed that the ABC-C1 gene was overexpressed in cells incubated with nitazoxanide or albendazole. Confocal anal. showed that ABC-C1 protein levels increased in trophozoites with both treatments but was higher with nitazoxanide. The mark was detected heavily in the periphery of the cells. Using a docking anal., it was found that the nitazoxanide metabolite, tizoxanide was docked close to the ATP-binding region as well as in the exit tunnel, located in the transmembrane region. These findings in Giardia intestinalis, support the possible role of ABC-C1 in drug efflux. To complete the study, the researchers used 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate (cas: 55981-09-4) .

2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate(cas: 55981-09-4), an anthelmintic agent, exhibits a broad spectrum of activities against a wide variety of helminths, protozoa, and enteric bacteria infecting animals and humans.Quality Control of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate

Reference:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Bhandari, Ranjana;Khanna, Garima;Kuhad, Anurag published 《Pharmacological insight into potential therapeutic agents for the deadly Covid-19 pandemic》. The research results were published in《European Journal of Pharmacology》 in 2021.Electric Literature of C12H9N3O5S The article conveys some information:

A review. Coronaviruses are pleomorphic, enveloped, or spherical viruses, which have a size ranging from 80 to 120 nm. These viruses act on receptors that cause the triggering of fusion. Coronaviruses were first described after cultivation from patients with common colds by Tyrell and Bynoe in 1966. There are various subtypes of coronavirus, 7 out of these can cause infection in human beings. The Alpha subtype is responsible for mild infection showing symptoms or infection without any prevailing symptoms. On the other hand, the beta subtype is responsible for very serious diseases leading to fatality. The lineage of this novel SARS-CoV-2 falls under the beta lineage of the beta coronavirus which has been observed to have a relation to the MERS and SARS coronavirus. In the Huanan market selling seafood, the transition of this novel virus in humans from animals has occurred. It has the potential to be the cause of widespread fatality amongst the people of the globe. On August 16, 2020, the World Health Organization had reported 2,1294,845 cases which are confirmed to date out of which 413,372 deaths have occurred. Currently, no targeted antiviral vaccines or drugs to fight against COVID-19 infection have been approved for use in humans. This pandemic is fast emerging and drug repurposing is the only ray of hope which can ensure quick availability. Vaccine development is progressing each day with various platforms such as DNA, Live Attenuated Virus, Non-Replicating Viral Vector, Protein Subunit, and RNA, being utilized for the development. COVID-19 attacks the immune system of the host & this can result in a cytokine storm. As a result, various herbal agents both acting as antivirals and immunomodulatory can also be used. Convalescent Plasma Therapy and Mesenchymal Stem Cell therapy are also being explored as a plausible therapeutic. There remains a considerable unmet need for therapeutics to be addressed. The development and availability of accessible and efficient therapy are essential for the treatment of patients. This review discusses the epidemiol., pathogenesis, the tale of origin, and transmission of COVID-19 or Sars-Cov2 virus and gives evidence of potential therapeutic agents that can be explored to cast away this pandemic. To complete the study, the researchers used 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate (cas: 55981-09-4) .

2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate(cas: 55981-09-4) has been used: to test its anti-viral activity against chikungunya virus as an antiprotozoal agent to test its effect on cell viability in various cancer cell lines; to test its effect on human cytomegalovirus (HCMV) infected human fibroblast HFF cellsElectric Literature of C12H9N3O5S

Reference:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

SDS of cas: 55981-09-4《Nitazoxanide and related thiazolides induce cell death in cancer cells by targeting the 20S proteasome with novel binding modes》 was published in 2022. The authors were Lu, Zirui;Li, Xiaona;Li, Kebin;Ripani, Paola;Shi, Xiaomeng;Xu, Fengrong;Wang, Mopei;Zhang, Liangren;Brunner, Thomas;Xu, Ping;Niu, Yan, and the article was included in《Biochemical Pharmacology (Amsterdam, Netherlands)》. The author mentioned the following in the article:

Nitazoxanide and related thiazolides are a novel class of anti-infectious agents against protozoan parasites, bacteria and viruses. In recent years, it is demonstrated that thiazolides can also induce cell cycle arrest and apoptotic cell death in cancer cells. Due to their fast proliferating nature, cancer cells highly depend on the proteasome system to remove aberrant proteins. Many of these aberrant proteins are regulators of cell cycle progression and apoptosis, such as the cyclins, BCL2 family members and nuclear factor of κB (NF-κB). Here, we demonstrate at both mol. and cellular levels that the 20S proteasome is a direct target of NTZ and related thiazolides. By concurrently inhibiting the multiple catalytic subunits of 20S proteasome, NTZ promotes cell cycle arrest and triggers cell death in colon cancer cells, either directly or as a sensitizer to other anti-tumor agents, especially doxorubicin. We further show that the binding mode of NTZ in the β5 subunit of the 20S proteasome is different from that of bortezomib and other existing proteasome inhibitors. These findings provide new insights in the design of novel small mol. proteasome inhibitors as anti-tumor agents suitable for solid tumor treatment in an oral dosing form.2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate (cas: 55981-09-4) were involved in the experimental procedure.

2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate(cas: 55981-09-4), an anthelmintic agent, exhibits a broad spectrum of activities against a wide variety of helminths, protozoa, and enteric bacteria infecting animals and humans.SDS of cas: 55981-09-4

Reference:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Jaladanki, Chaitanya K.;Khatun, Samima;Gohlke, Holger;Bharatam, Prasad V. published 《Reactive Metabolites from Thiazole-Containing Drugs: Quantum Chemical Insights into Biotransformation and Toxicity》 in 2021. The article was appeared in 《Chemical Research in Toxicology》. They have made some progress in their research.Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate The article mentions the following:

Drugs containing thiazole and aminothiazole groups are known to generate reactive metabolites (RMs) catalyzed by cytochrome P450s (CYPs). These RMs can covalently modify essential cellular macromols. and lead to toxicity and induce idiosyncratic adverse drug reactions. Mol. docking and quantum chem. hybrid DFT study were carried out to explore the mol. mechanisms involved in the biotransformation of thiazole (TZ) and aminothiazole (ATZ) groups leading to RM epoxide, S-oxide, N-oxide, and oxaziridine. The energy barrier required for the epoxidation is 13.63 kcal/mol, that is lower than that of S-oxidation, N-oxidation, and oxaziridine formation (14.56, 17.90, and 20.20, kcal/mol resp.). The presence of the amino group in ATZ further facilitates all the metabolic pathways, for example, the barrier for the epoxidation reaction is reduced by ~2.5 kcal/mol. Some of the RMs/their isomers are highly electrophilic and tend to form covalent bonds with nucleophilic amino acids, finally leading to the formation of metabolic intermediate complexes (MICs). The energy profiles of these competitive pathways have also been explored. And 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate (cas: 55981-09-4) was used in the research process.

2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate(cas: 55981-09-4) has been approved as an orphan drug for the treatment of diarrhea in children (age, 1–11 years) and is associated with giardiasis, but it also is approved for diarrhea caused by crytosporidiosis in patients with AIDS.Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate

Reference:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Goel, Vasudha;Jain, Anubhav;Sharma, Garima;Jhajharia, Ashok;Agarwal, Vishnu Kumar;Ashdhir, Prachis;Pokharna, Rupesh;Chauhan, Virender published 《Evaluating the efficacy of nitazoxanide in uncomplicated amebic liver abscess.》. The research results were published in《Indian journal of gastroenterology : official journal of the Indian Society of Gastroenterology》 in 2021.HPLC of Formula: 55981-09-4 The article conveys some information:

BACKGROUND: Amebic liver abscess is treated successfully with metronidazole or another nitroimidazole drug followed by a luminal amebicide. Metronidazole has long been preferred, but has been associated with several adverse effects including intolerance in certain clinical situations. Mechanisms of metronidazole resistance and mutagenic potential have been described. Effects of the use of drug in pregnant women and infants of lactating women are unknown. Nitazoxanide was proven to be efficacious in treating invasive intestinal amebiasis. Therefore, the present study was undertaken to assess the efficacy and safety of nitazoxanide as compared to metronidazole in patients with uncomplicated amebic liver abscess. METHODS: Patients with clinical and ultrasonography features suggestive of liver abscess, positive amebic serology, and/or anchovy sauce appearance on aspiration of the pus were included in the study and randomized into two parallel treatment groups. Group M received metronidazole, 2-2.5 g/day intravenous (IV), for inpatients, or 2-2.4 g/day oral, for outpatients in three divided doses for 14 days. Group N received nitazoxanide 500 mg BD per oral for 10 days. RESULTS: A total of sixty subjects fulfilling the inclusion criteria were randomized equally into two groups, group M and group N. Number of patients achieving symptomatic clinical response (SCR) was similar in the two groups (80% vs. 76.7%, p = 1.00), though time to achieve symptomatic clinical response was significantly lower in metronidazole group as compared to that in nitazoxanide group. Greater proportion of patients achieved early clinical response (ECR) in metronidazole group as compared to nitazoxanide group. Complete resolution of abscess, at 6 months, was noted in 18 (60%) patients in the M group and 22 (73.3%) patients in the N group (p = 0.273). Metronidazole was associated with significantly greater frequency of adverse effects than nitazoxanide. CONCLUSIONS: This study shows equivalent efficacy of nitazoxanide in uncomplicated amebic liver abscess as compared to metronidazole, with better tolerability and advantage of simultaneous luminal clearance, thus reducing chances of recurrence. TRIAL REGISTRATION: CTRI/2019/01/017249. To complete the study, the researchers used 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate (cas: 55981-09-4) .

2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate(cas: 55981-09-4), a thiazolide compound, is a antiparasitic drug with structure similar to niclosamide.HPLC of Formula: 55981-09-4

Reference:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Application In Synthesis of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate《Current pharmacotherapy of cryptosporidiosis: an update of the state-of-the-art》 was published in 2021. The authors were Schneider, Anne;Wendt, Sebastian;Luebbert, Christoph;Trawinski, Henning, and the article was included in《Expert Opinion on Pharmacotherapy》. The author mentioned the following in the article:

Cryptosporidiosis has emerged as a major cause of diarrheal disease worldwide. It has especially serious health consequences for young, malnourished children living in endemic areas and for individuals with highly impaired T-cell function, such as HIV-pos. individuals with low CD4 counts or immunosuppressed solid-organ transplant recipients. A selective literature search using PubMed was performed to review the available therapeutics to treat cryptosporidiosis, as well as related advances in drug development. The only FDA-approved antiparasitic treatment in immunocompetent patients is nitazoxanide; however, it has failed to demonstrate convincing effectiveness among HIV-pos. patients, immunosuppressed individuals and malnourished children. Thus, restoring HIV-pos. patients’ cellular immune response through effective antiretroviral therapy (ART), or reducing or changing immunosuppressive drugs, is important. Several new targets have been identified for chemotherapy, and the development of drugs for these targets has progressed, including parasite kinases, nucleic acid synthesis and processing, proteases and lipid metabolism Candidate drugs that have been shown to be effective and safe in a neonatal calf model will most likely constitute the next advance for clin. trials in humans. However, developing an effective and inexpensive vaccination, as well as complementing structural preventive measures, would most decisively reduce the global cryptosporidiosis burden. And 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate (cas: 55981-09-4) was used in the research process.

2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate(cas: 55981-09-4) has been approved as an orphan drug for the treatment of diarrhea in children (age, 1–11 years) and is associated with giardiasis, but it also is approved for diarrhea caused by crytosporidiosis in patients with AIDS.Application In Synthesis of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate

Reference:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Reference of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate《Therapeutic Potential of Nitazoxanide: An Appropriate Choice for Repurposing versus SARS-CoV-2?》 was published in 2021. The authors were Stachulski, Andrew V.;Taujanskas, Joshua;Pate, Sophie L.;Rajoli, Rajith K. R.;Aljayyoussi, Ghaith;Pennington, Shaun H.;Ward, Stephen A.;Hong, Weiqian David;Biagini, Giancarlo A.;Owen, Andrew;Nixon, Gemma L.;Leung, Suet C.;O’Neill, Paul M., and the article was included in《ACS Infectious Diseases》. The author mentioned the following in the article:

A review. The rapidly growing COVID-19 pandemic is the most serious global health crisis since the Spanish flu of 1918. There is currently no proven effective drug treatment or prophylaxis for this coronavirus infection. While developing safe and effective vaccines is 1 of the key focuses, a number of existing antiviral drugs are being evaluated for their potency and efficiency against SARS-CoV-2 in vitro and in the clinic. We review the significant potential of nitazoxanide (NTZ) as an antiviral agent that can be repurposed as a treatment for COVID-19. Originally, NTZ was developed as an antiparasitic agent especially against Cryptosporidium spp.; it was later shown to possess potent activity against a broad range of both RNA and DNA viruses, including influenza A, hepatitis B and C, and coronaviruses. Recent in vitro assessment of NTZ has confirmed its promising activity against SARS-CoV-2 with an EC₅₀ of 2.12μM. We examine its drug properties, antiviral activity against different viruses, clin. trials outcomes, and mechanisms of antiviral action from the literature to highlight the therapeutic potential for the treatment of COVID-19. Furthermore, in preliminary PK/PD analyses using clin. data reported in the literature, comparison of simulated TIZ (active metabolite of NTZ) exposures at 2 doses with the in vitro potency of NTZ against SARS-CoV-2 gives further support for drug repurposing with potential in combination chemotherapy approaches. The review concludes with details of 2nd generation thiazolides under development that could lead to improved antiviral therapies for future indications.2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate (cas: 55981-09-4) were involved in the experimental procedure.

2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate(cas: 55981-09-4) has been approved as an orphan drug for the treatment of diarrhea in children (age, 1–11 years) and is associated with giardiasis, but it also is approved for diarrhea caused by crytosporidiosis in patients with AIDS.Reference of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate

Reference:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica