Day: September 21, 2022

Nishad, Ravi K.;Shukla, Karuna S.;Chawla, Pooja A. published 《Design and Synthesis of 2-Substituted Benzothiazole Derivatives as Antioxidant and Antimicrobial Agents》 in 2020. The article was appeared in 《Current Bioactive Compounds》. They have made some progress in their research.Recommanded Product: 6-Nitrobenzo[d]thiazol-2-amine The article mentions the following:

An upsurge in the number of antibiotic-resistant microbial infections has warranted the discovery and development of new antibiotics. This is a matter of great concern for effective therapy for a search of novel antimicrobial agents. Literature has a number of reports of involvement of oxidative stress due to an imbalance between the generation and neutralization of free radicals in many diseases. Heterocyclic compounds have been involved in the treatment of various disorders. Benzothiazole is one such heterocyclic nucleus having benzene ring merged with the thiazole ring. Among the various substitutions possible in this nucleus, substitutions at position-2 have already been reported with potential bioactivities. Thus, different substituted compounds have been synthesized which could serve as antimicrobials and antioxidants. Benzothiazole derivatives (B₁-B₇) were synthesized by two-step reactions and the structures were confirmed through IR, mass and NMR spectroscopy. The compounds were evaluated for in vitro antioxidant and antimicrobial activities using standard methods. The results of antibacterial and antifungal activity showed that compound B₄ exhibited maximum activity against all the tested strains of microorganisms with the zone of inhibition 17.1-18.5 mm and MIC value 1.1-1.5μg/mL. Compound B₅ exhibited potent antioxidant activity. The compounds substituted with halogen on the aryl ring showed increased antimicrobial activity as seen in the case of compound B₄ (6-fluoro). The compounds substituted with a hydroxyl group (B₅) exhibited good antioxidant activity.6-Nitrobenzo[d]thiazol-2-amine (cas: 6285-57-0) were involved in the experimental procedure.

6-Nitrobenzo[d]thiazol-2-amine(cas:6285-57-0 Recommanded Product: 6-Nitrobenzo[d]thiazol-2-amine) is an antimicrobial agent that inhibits bacterial growth by cleaving the peptide bonds of proteins. It has been shown to be active against a number of microorganisms, including Gram-positive and Gram-negative bacteria, as well as fungi.

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

de Andrade Picanco, Guaraciara;Ferreira de Lima, Nayana;Cristina Gomes, Taynara;de Sousa Mendes Moreira Alves, Daniella;Luisa da Costa, Tatiane;Vinaud, Marina Clare published 《Intraperitoneal and intracranial experimental cysticercosis present different metabolic preferences after treatment with isolated or combined albendazole and nitazoxanide》 in 2022. The article was appeared in 《Acta Tropica》. They have made some progress in their research.Safety of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate The article mentions the following:

Cysticercosis is a zoonotic public health issue especially severe when the parasite is in the central nervous system although it may be found all over the human organism. Taenia crassiceps cysticerci inoculated in mice is the exptl. model used to study cysticercosis. The most used cysticercosis treatment is with albendazole (ABZ). Nitazoxanide (NTZ) has been exptl. tested against this parasite. Metabolic anal. has been used to determine drugs impact on the parasite. The aim of this study was to determine the in vivo metabolic impact of the ABZ-NTZ combination in T. crassiceps cysticerci inoculated in mice peritoneal and intracranial cavities. Mice were exptl. inoculated with T. crassiceps cysticerci in the i.p. cavity or in the intracranial one. Thirty days after the infection they were treated with NaCl 0.9% (control group), 50 mg/kg of ABZ, 50 mg/kg of NTZ or 50 mg/kg of NTZ and ABZ (ABZ/NTZ combination). 24 h after treatment the animals were euthanized and the cysticerci analyzed through high performance chromatog. and spectrophotometry in order to detect the glycolytic, mitochondrial and protein catabolism pathways. The intracranial parasites used more intensely the homolactic fermentation while the i.p. ones presented a greater use of the mitochondrial pathways and protein catabolism. Regarding the glycolytic pathways, it was possible to observe a significant impact induced by the drugs used, both isolated or in combination. It was possible to detect an increase in the fumarate reductase pathway after the drugs exposure and no impact in the protein’s catabolism. Therefore, the cysticerci showed different uses of metabolic pathways regarding the site of inoculation due to the availability of nutrients inherent of each environment. This study showed the parasite metabolic resilience and capability of use of different biochem. pathways in order to ensure survival in spite of a hostile environment. 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), 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

Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate《Nitazoxanide versus rifaximin in preventing the recurrence of hepatic encephalopathy: A randomized double-blind controlled trial.》 was published in 2021. The authors were Glal, Khadija A M;Abd-Elsalam, Sherief M;Mostafa, Tarek M, and the article was included in《Journal of hepato-biliary-pancreatic sciences》. The author mentioned the following in the article:

BACKGROUND/PURPOSE: Hepatic encephalopathy (HE) is a neuropsychiatric complication of liver cirrhosis. HE is associated with poor survival and detrimental effects on quality of life (QOL). The drawbacks of the long-term use of rifaximin in HE necessitates searching for alternative therapies. In this context, our study aimed at evaluating the safety and efficacy of nitazoxanide (NTZ) as compared to rifaximin (RFX) in preventing the recurrence of HE and assessing its impact on QOL. PATIENTS AND METHODS: This prospective, randomized, double-blind controlled study included 60 patients who were randomly assigned to receive either rifaximin 550 mg twice daily (group 1; n = 30) or nitazoxanide 500 mg twice daily (group 2; n = 30) for 24 weeks. During the study period, the patients’ neurological symptoms, mental status, and performance were monitored. The serum levels of HE triggers (ammonia, TNF-α, and octopamine) were assessed. The patients’ health-related quality of life was also evaluated. RESULTS: Six months after treatment, patients on NTZ therapy showed a statistically significant improvement in CHESS score and mental status. NTZ provided 136 days of remission vs 67 days of remission for patients on RFX (P₁  = .0001) and significant reduction in Child score (P₁  = .018). Additionally, NTZ showed a statistically significant decrease in serum ammonia, TNF-α, and octopamine levels as compared to rifaximin. Regarding QOL, NTZ group showed an improvement in total Chronic Liver Disease Questionnaire (CLDQ) score. Both groups experienced minor controllable side effects. CONCLUSION: Nitazoxanide may represent a suitable and safe alternative therapy to rifaximin in preventing the recurrence of hepatic encephalopathy. 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 cellsRecommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate

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

Application of 55981-09-4In 2022, Gibson, Alexis R.;Sateriale, Adam;Dumaine, Jennifer E.;Engiles, Julie B.;Pardy, Ryan D.;Gullicksrud, Jodi A.;O’Dea, Keenan M.;Doench, John G.;Beiting, Daniel P.;Hunter, Christopher A.;Striepen, Boris published 《A genetic screen identifies a protective type III interferon response to Cryptosporidium that requires TLR3 dependent recognition》. 《PLoS Pathogens》published the findings. The article contains the following contents:

Cryptosporidium is a leading cause of severe diarrhea and diarrheal-related death in children worldwide. As an obligate intracellular parasite, Cryptosporidium relies on intestinal epithelial cells to provide a niche for its growth and survival, but little is known about the contributions that the infected cell makes to this relationship. Here we conducted a genome wide CRISPR/Cas9 knockout screen to discover host genes that influence Cryptosporidium parvum infection and/or host cell survival. Gene enrichment anal. indicated that the host interferon response, glycosaminoglycan (GAG) and glycosylphosphatidylinositol (GPI) anchor biosynthesis are important determinants of susceptibility to C. parvum infection and impact on the viability of host cells in the context of parasite infection. Several of these pathways are linked to parasite attachment and invasion and C-type lectins on the surface of the parasite. Evaluation of transcript and protein induction of innate interferons revealed a pronounced type III interferon response to Cryptosporidium in human cells as well as in mice. Treatment of mice with IFNλ reduced infection burden and protected immunocompromised mice from severe outcomes including death, with effects that required STAT1 signaling in the enterocyte. Initiation of this type III interferon response was dependent on sustained intracellular growth and mediated by the pattern recognition receptor TLR3. We conclude that host cell intrinsic recognition of Cryptosporidium results in IFNλ production critical to early protection against this infection. 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

SDS of cas: 6285-57-0《Development of β-carboline-benzothiazole hybrids via carboxamide formation as cytotoxic agents: DNA intercalative topoisomerase IIα inhibition and apoptosis induction》 was published in 2021. The authors were Tokala, Ramya;Mahajan, Surbhi;Kiranmai, Gaddam;Sigalapalli, Dilep Kumar;Sana, Sravani;John, Stephy Elza;Nagesh, Narayana;Shankaraiah, Nagula, and the article was included in《Bioorganic Chemistry》. The author mentioned the following in the article:

In quest of promising anticancer agents, the pharmacophores of natural (β-carboline) and synthetic origin (benzothiazole) were adjoined by a carboxamide bridge and three-point diversification was accomplished. The in vitro cytotoxic ability of the compounds was established on adherent and suspension human cancer cell lines and compounds I and II advanced as pre-eminent mols. with IC₅₀ values of 1.46 and 1.81μM resp. in A549 cell line. The cytospecificity was entrenched for potent compounds I and II by evaluating against normal human lung epithelial cells and selectivity index was calculated Furthermore, EtBr displacement, relative viscosity and gel-based topoisomerase II target assays unveiled the intercalative topo-II inhibitory capability and DNA binding studies (absorbance) revealed the dissociation constant (K_d) for compounds I and II as 98 and 103μM resp. Addnl., cell-based flow cytometric assays like Annexin-V/PI dual staining aids in the quantification of apoptosis induced and JC-1 staining disclosed the depolarization of mitochondrial membrane potential by compound I in A549 cells in a dose-dependent manner. Moreover, wound healing assay established the inhibition of in vitro cell migration by compound I on A549 cells. In addition, mol. docking studies proved the binding of compounds I and II in the active site of DNA complexed with topo IIα and stabilized by interactions with DNA base pairs and amino acid residues. Remarkably, the compounds I and II follow Lipinski’s rule of five and are in the recommended range for Jorgensen’s rule of three with a minimal violation and other pharmacokinetic parameters revealing druggability of the synthesized hybrids. To complete the study, the researchers used 6-Nitrobenzo[d]thiazol-2-amine (cas: 6285-57-0) .

6-Nitrobenzo[d]thiazol-2-amine(cas:6285-57-0) has been used:
as model analyte for voltammetric determination of electrochemically reducible organic substances;
in the synthesis of 2-methyl-4-nitro-2H-pyrazole-3-carboxylic acid[2-(cyclohexanecarbonylamino)benzothiazol-6-yl]amide derivatives;
in the preparation of push-pull nonlinear optical chromophores containing thiazole and benzothiazole acceptors;
as a base in dye production by diazotation reaction.

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

Synthetic Route of C7H5N3O2S《Cyclic (Alkyl)(amino)carbene Ligand-Promoted Nitro Deoxygenative Hydroboration with Chromium Catalysis: Scope, Mechanism, and Applications》 was published in 2021. The authors were Zhao, Lixing;Hu, Chenyang;Cong, Xuefeng;Deng, Gongda;Liu, Liu Leo;Luo, Meiming;Zeng, Xiaoming, and the article was included in《Journal of the American Chemical Society》. The author mentioned the following in the article:

Transition metal catalysis that utilizes N-heterocyclic carbenes as noninnocent ligands in promoting transformations has not been well studied. We report here a cyclic (alkyl)(amino)carbene (CAAC) ligand-promoted nitro deoxygenative hydroboration with cost-effective chromium catalysis. Using 1 mol % of CAAC-Cr precatalyst, the addition of HBpin to nitro scaffolds leads to deoxygenation, allowing for the retention of various reducible functionalities and the compatibility of sensitive groups toward hydroboration, thereby providing a mild, chemoselective, and facile strategy to form anilines, as well as heteroaryl and aliphatic amine derivatives, with broad scope and particularly high turnover numbers (up to 1.8 x 10⁶). Mechanistic studies, based on theor. calculations, indicate that the CAAC ligand plays an important role in promoting polarity reversal of hydride of HBpin; it serves as an H-shuttle to facilitate deoxygenative hydroboration. The preparation of several com. available pharmaceuticals by means of this strategy highlights its potential application in medicinal chem. And 6-Nitrobenzo[d]thiazol-2-amine (cas: 6285-57-0) was used in the research process.

6-Nitrobenzo[d]thiazol-2-amine(cas:6285-57-0 Synthetic Route of C7H5N3O2S) is an antimicrobial agent that inhibits bacterial growth by cleaving the peptide bonds of proteins. It has been shown to be active against a number of microorganisms, including Gram-positive and Gram-negative bacteria, as well as fungi.

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

Xu, Junlin;Meng, Yajie;Peng, Lihong;Cai, Lijun;Tang, Xianfang;Liang, Yuebin;Tian, Geng;Yang, Jialiang published 《Computational drug repositioning using similarity constrained weight regularization matrix factorization: A case of COVID -19》. The research results were published in《Journal of Cellular and Molecular Medicine》 in 2022.SDS of cas: 55981-09-4 The article conveys some information:

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. 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) 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 cellsSDS of cas: 55981-09-4

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

Lima, Nayana F.;Picanco, Guaraciara A.;Costa, Tatiane L.;Lino, Ruy de Souza Jr.;Vinaud, Marina C. published 《In Vivo Treatment with the Combination of Nitazoxanide and Flubendazole Induces Gluconeogenesis and Protein Catabolism in Taenia crassiceps cysticerci》. The research results were published in《Acta Parasitologica》 in 2021.Recommanded Product: 55981-09-4 The article conveys some information:

Abstract: Purpose: Cysticercosis is the presence of Taenia solium larva in humans or swines tissues. It is a public health problem related to bad hygienic habits and consumption of infected pork. T. crassiceps is a widely used cysticercosis exptl. model. The combination of two effective drugs such as nitazoxanide (NTZ) and flubendazole (FBZ) may potentialize their effect. The aim of this study was to use biochem. anal. to determine the metabolic impact of the combination of NTZ and FBZ on cysticerci inoculated i.p. in mice. Methods: Balb/c mice i.p. infected with T. crassiceps cysticerci received a single oral dose NTZ/FBZ (50 mg/kg). 24 h after the treatment the cysticerci were removed, frozen and analyzed by high performance liquid chromatog. regarding the detection of the following metabolic pathways: glycolysis, gluconeogenesis, homolactic fermentation, tricarboxylic acid cycle, proteins catabolism and fatty acids oxidation Results: The treatment with the drugs combination induced a statistically significant increase in gluconeogenesis and in protein catabolism when compared to the control groups. Conclusion: The drugs combination is potentialized and capable of causing greater metabolic stress than the sep. treatment with NTZ or FBZ, showing its potential for an alternative cysticercosis treatment.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 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 cellsRecommanded Product: 55981-09-4

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

Safety of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetateIn 2022, Shawky, D;Salamah, A M;Abd-Elsalam, S M;Habba, E;Elnaggar, M H;Elsawy, A A;Baiomy, N;Bahaa, M M;Gamal, R M published 《Nitazoxanide-based therapeutic regimen as a novel treatment for Helicobacter pylori infection in children and adolescents: a randomized trial.》. 《European review for medical and pharmacological sciences》published the findings. The article contains the following contents:

OBJECTIVE: Antibiotic resistance and poor patient compliance with treatment cause Helicobacter pylori to show increased resistance to typical first-line therapeutic regimens. This study aimed to evaluate the efficacy of the new nitazoxanide-based treatment regimens for Helicobacter pylori infection vs. the current metronidazole-based regimens to address the problem of increasing metronidazole resistance. PATIENTS AND METHODS: This randomized clinical trial enrolled 100 patients with Helicobacter pylori infection. The patients were randomly assigned to one of two groups: group I received nitazoxanide-based triple therapy (nitazoxanide, proton pump inhibitor, and clarithromycin) for 14 days, whereas group II received standard treatment (metronidazole, omeprazole, and clarithromycin) for 14 days. On enrollment and after six weeks of treatment, all patients underwent careful history taking, full clinical examination, laboratory investigations (complete blood count, liver and renal function tests), and Helicobacter pylori stool antigen testing. RESULTS: Of the patients, 92% in the nitazoxanide group and 84% in the metronidazole group recovered from infection, with no statistically significant difference between the two groups. Patients in the nitazoxanide group showed a 54% lower risk of resistant infection (odds ratio, 0.5; 95% confidence interval, 0.161-1.555) than those in the metronidazole group. CONCLUSIONS: The nitazoxanide-based therapeutic regimen produced higher eradication rates than the standard treatment. However, the difference was not substantial in this particular group of patients.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.Safety of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate

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

Parpia, Tarina;Svensen, Erling;Elwood, Sarah;Wanjuhi, Anne;Blacy, Ladislaus;Bayo, Eliwaza;Houpt, Eric;McQuade, Elizabeth Rogawski;DeBoer, Mark;Platts-Mills, James;Mduma, Estomih;Scharf, Rebecca published 《Cognitive outcomes at 18 months: findings from the early life interventions for childhood growth and development in Tanzania (ELICIT) trial》 in 2022. The article was appeared in 《American Journal of Tropical Medicine and Hygiene》. They have made some progress in their research.SDS of cas: 55981-09-4 The article mentions the following:

Micronutrient deficiencies and enteric infections neg. impact child growth and development. We enrolled children shortly after birth in a randomized, placebo-controlled, 2 x 2 factorial interventional trial in Haydom, Tanzania, to assess nicotinamide and/or antimicrobials (azithromycin and nitazoxanide) effect on length at 18 mo of age. Cognitive score at 18 mo using the Malawi Developmental Assessment Tool (MDAT), which includes gross motor, fine motor, language, and social assessments, was a secondary outcome. Here, we present the MDAT results of 1,032 children. There was no effect of nicotinamide (change in development-for-age Z score [DAZ] -0.08; 95% CI: -0.16, 0) or antimicrobials (change in DAZ 0.04; 95% CI: -0.06, 0.13) on overall MDAT score. The interventions had no effect on cognitive outcomes in subgroups defined by gender, socioeconomic status, birthweight, and birth season or on MDAT subscores. Further analyses are needed to identify targetable risk factors for impaired cognitive development in these settings. 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), a thiazolide compound, is a antiparasitic drug with structure similar to niclosamide.SDS of cas: 55981-09-4

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