Category: thiazole

Behera, Ahalya;Rakshit, Amitava;Sahoo, Ashish K.;Patel, Bhisma K. published 《One Pot Sequential Synthesis of N-[2-(Phenylsulfinyl)phenyl]acetamides: A Ring Opening Rearrangement Functionalization (RORF)》 in 2019. The article was appeared in 《European Journal of Organic Chemistry》. They have made some progress in their research.Safety of 6-Nitrobenzo[d]thiazol-2-amine The article mentions the following:

A Cu^II catalyzed one-pot sequential synthesis of N-[2-(phenylthio)phenyl]acetamides from benzo[d]thiazol-2-amines, iodoarenes and carboxylic acids (RCOOH) has been accomplished via ring opening rearrangement functionalization (RORF). Here, the ring opening is associated with the loss of carbon and nitrogen atoms with concurrent S-arylation and N-acylation leading to ortho-bifunctionalized products. A further sequential addition of tert-Bu hydroperoxide (TBHP) results in the formation of a sulfur oxidized product, N-[2-(phenylsulfinyl)phenyl]acetamide. A plausible mechanism has been proposed for this unprecedented ring opening rearrangement functionalization (RORF).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 Safety of 6-Nitrobenzo[d]thiazol-2-amine) inhibits the activity of amines, which are small molecules found in many pharmaceuticals. The chemical structure of this drug contains one or more methylene groups that can be activated by diazonium salt to form an intermediate molecule with a reactive amine group.

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

Quality Control of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate《Review on nitazoxanide: a broad spectrum antiparasitic agent》 was published in 2021. The authors were Kothari, Ruchita M.;Patil, Javesh K.;Jain, Akash S.;Chaudhari, Hitendra S.;Dhankani, Amitkumar R.;Rokade, Yogesh B., and the article was included in《European Journal of Biomedical and Pharmaceutical Sciences》. The author mentioned the following in the article:

A review. Nitazoxanide is a thiazolide antiparasitic agent that shows excellent in vitro activity against a wide variety of parasites as well as some bacteria. It has been used as a single agent to treat mixed infections with intestinal parasites i.e. protozoas and helminths. It was originally discovered in 1975 by Jean Francois Rossignol & It was initially developed as a veterinary antihelminthic with activity against intestinal nematodes, cestodes, and liver trematodes & In humans, nitazoxanide has been reported to be effective against a broad range of parasites, including Giardia lamblia, Entamoeba histolytica, Cryptosporidium parvum, Cyclospora cayetanens, etc. The main objective of this review is to study detailed profile of nitazoxanide like physicochem. properties, pharmacokinetics, clin. uses, and adverse effects of Nitazoxanide. 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 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.Quality Control of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate

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

Cindric, Maja;Peric, Mihaela;Kralj, Marijeta;Martin-Kleiner, Irena;David-Cordonnier, Marie-Helene;Paljetak, Hana Cipcic;Matijasic, Mario;Verbanac, Donatella;Karminski-Zamola, Grace;Hranjec, Marijana published 《Antibacterial and antiproliferative activity of novel 2-benzimidazolyl- and 2-benzothiazolyl-substituted benzo[b]thieno-2-carboxamides》. The research results were published in《Molecular Diversity》 in 2018.Application In Synthesis of 6-Nitrobenzo[d]thiazol-2-amine The article conveys some information:

Novel (nitro/amino)substituted 2-benzimidazolyl and 2-benzothiazolyl benzo[b]thieno-2-carboxamides I and I • HCl [R¹ = R² = H, NH₂, NO₂; X = NH, S] were designed and synthesized as potential antibacterial agents. The antibacterial activity of these compounds I were evaluated against Gram-pos. (Staphylococcus aureus and Enterococcus faecalis) and Gram-neg. bacteria (Escherichia coli and Moraxella catarrhalis). The most promising antibacterial activity was observed for the nitro- and amino-substituted benzimidazole derivatives I [R¹ = H; R² = NH₂, NO₂; X = NH] and I •Hcl [R¹ = H, R² = NH₂, X = NH; R¹ = NH₂, R² = H, X = NH] with MICs 2-8 μg/mL. Addnl., compounds with inferior antibacterial activity were further tested for their antiproliferative activity in-vitro against three human cancer cell lines. Amino-substituted benzothiazole hydrochloride salt I [R¹ = H, R² = NH₂, X = S] displayed the most pronounced and selective activity against the MCF-7 cell line with an IC₅₀ of 40 nM. Furthermore, DNA binding experiments of selected derivatives indicated that DNA cannot be considered as a primary biol. target for this type of compounds6-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 Application In Synthesis of 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

Tomczak, Ewa;McDougal, April N.;White, A. Clinton Jr. published 《Resolution of cryptosporidiosis in transplant recipients: review of the literature and presentation of a renal transplant patient treated with nitazoxanide, azithromycin, and rifaximin》 in 2022. The article was appeared in 《Open Forum Infectious Diseases》. They have made some progress in their research.Category: thiazole The article mentions the following:

Background.Cryptosporidium is a major cause of diarrheal disease worldwide, including chronic disease in malnourished children and patients with acquired immune deficiency syndrome. There are increasing reports of cryptosporidiosis in transplant patients, especially from middle-income countries. Methods. The literature on treatment of cryptosporidiosis in transplant patients was reviewed and included no controlled trials but only small case series. Nitazoxanide, azithromycin, spiramycin, and combination therapies have been used, but none are consistently efficacious. Results. We present a case of chronic diarrhea from cryptosporidiosis in a renal transplant patient. His illness resolved with decreasing immunosuppression and treatment with the 3-drug combination of nitazoxanide, azithromycin, and rifaximin. Conclusions. Although current therapies are not reliably effective in the absence of an effective cellular immune response, combination therapies hold promise for improved responses.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.Category: thiazole

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

Name: 6-Nitrobenzo[d]thiazol-2-amine《Synthesis, Characterization and Biological Evaluation of 2-(p-Nitrophenyl)quinazolin-4(3H)-one Derivatives》 was published in 2020. The authors were Giradkar, V. N.;Kabra, U. D.;Diwakar, R. S.;Lohiya, R. T.;Umekar, M. J., and the article was included in《Russian Journal of Organic Chemistry》. The author mentioned the following in the article:

A series of novel 2-(4-nitrophenyl)-3-(R-benzothiazol-2-yl)quinazolin-4(3H)-ones I [R = H, 5-Br, 6-NO₂, etc.] was synthesized from the 2-aminobenzothiazoles and 2-(4-nitrophenyl)-4H-3,1-benzoxazin-4-one via a nucleophilic addition reaction. The synthesized compounds I were tested for anticonvulsant, antimicrobial, and antioxidant activities. All the compounds I increased the seizure latency compared to control. Compound I [R = 6-NO₂] exhibited significant anticonvulsant activity, comparable to that of the standard drug Phenytoin. Antimicrobial activity testing revealed moderate to good activity in all the test compounds, I and I [R = H, 6-NO₂] compared in activity with the standard drug Chloramphenicol. The antioxidant activity of compounds I [R = H], I [R = 5-Br] and I [ R = 4,6-Me₂] IC₅₀ 39.30, 15.55, and 42.95μg/mL, resp. was found to be higher compared to the standard drug ascorbic acid (IC50 48.30μg/mL). To complete the study, the researchers used 6-Nitrobenzo[d]thiazol-2-amine (cas: 6285-57-0) .

6-Nitrobenzo[d]thiazol-2-amine(cas:6285-57-0Name: 6-Nitrobenzo[d]thiazol-2-amine) has been shown to lower blood pressure in mice by inhibiting angiotensin converting enzyme and potassium channels. This drug also has a protective effect on the heart and brain from ischemia reperfusion injury.

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

Ahmed, Tasmia;Rahman, S. M. Abdur;Asaduzzaman, Muhammad;Islam, Abul Bashar Mir Khademul Md.;Chowdhury, A. K. Azad published 《Synthesis, in vitro bioassays, and computational study of heteroaryl nitazoxanide analogs》 in 2021. The article was appeared in 《Pharmacology Research & Perspectives》. They have made some progress in their research.COA of Formula: C12H9N3O5S The article mentions the following:

Antiprotozoal drug nitazoxanide (NTZ) has shown diverse pharmacol. properties and has appeared in several clin. trials. Herein we present the synthesis, characterization, in vitro biol. investigation, and in silico study of four hetero aryl amide analogs of NTZ. Among the synthesized mols., compound 2 and compound 4 exhibited promising antibacterial activity against Escherichia coli (E. coli), superior to that displayed by the parent drug nitazoxanide as revealed from the in vitro antibacterial assay. Compound 2 displayed zone of inhibition of 20 mm, twice as large as the parent drug NTZ (10 mm) in their least concentration (12.5 Μg/mL). Compound 1 also showed antibacterial effect similar to that of nitazoxanide. The analogs were also tested for in vitro cytotoxic activity by employing cell counting kit-8 (CCK-8) assay technique in HeLa cell line, and compound 2 was identified as a potential anticancer agent having IC₅₀ value of 172 Μg which proves it to be more potent than nitazoxanide (IC₅₀ = 428 Μg). Furthermore, the compounds were subjected to mol. docking study against various bacterial and cancer signaling proteins. The in vitro test results corroborated with the in silico docking study as compound 2 and compound 4 had comparatively stronger binding affinity against the proteins and showed a higher docking score than nitazoxanide toward human mitogen-activated protein kinase (MAPK9) and fatty acid biosynthesis enzyme (FabH) of E. coli. Moreover, the docking study demonstrated dihydrofolate reductase (DHFR) and thymidylate synthase (TS) as probable new targets for nitazoxanide and its synthetic analogs. Overall, the study suggests that nitazoxanide and its analogs can be a potential lead compound in the drug development. 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.COA of Formula: C12H9N3O5S

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

Related Products of 55981-09-4《Interferon-inducer antivirals: Potential candidates to combat COVID-19》 was published in 2021. The authors were Bagheri, Ashkan;Moezzi, Seyed Mohammad Iman;Mosaddeghi, Pouria;Nadimi Parashkouhi, Sadra;Fazel Hoseini, Seyed Mostafa;Badakhshan, Fatemeh;Negahdaripour, Manica, and the article was included in《International Immunopharmacology》. The author mentioned the following in the article:

A review. Coronavirus disease 2019 (COVID-19) is an infective disease generated by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). Given the pandemic urgency and lack of an effective cure for this disease, drug repurposing could open the way for finding a solution Lots of investigations are ongoing to test the compounds already identified as antivirals. On the other hand, induction of type I interferons are found to play an important role in the generation of immune responses against SARS-CoV-2. Therefore, it was opined that the antivirals capable of triggering the interferons and their signaling pathway, could rationally be beneficial for treating COVID-19. On this basis, using a database of antivirals, called drugvirus, some antiviral agents were derived, followed by searches on their relevance to interferon induction. The examined list included drugs from different categories such as antibiotics, immunosuppressants, anti-cancers, non-steroidal anti-inflammatory drugs (NSAID), calcium channel blocker compounds, and some others. The results as briefed here, could help in finding potential drug candidates for COVID-19 treatment. However, their advantages and risks should be taken into account through precise studies, considering a systemic approach. Even though the adverse effects of some of these drugs may overweight their benefits, considering their mechanisms and structures may give a clue for designing novel drugs in the future. Furthermore, the antiviral effect and IFN-modifying mechanisms possessed by some of these drugs might lead to a synergistic effect against SARS-CoV-2, which deserve to be evaluated in further investigations. 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 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 cellsRelated Products of 55981-09-4

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

Computed Properties of C12H9N3O5SIn 2021, Rajoli, Rajith K. R.;Pertinez, Henry;Arshad, Usman;Box, Helen;Tatham, Lee;Curley, Paul;Neary, Megan;Sharp, Joanne;Liptrott, Neill J.;Valentijn, Anthony;David, Christopher;Rannard, Steven P.;Aljayyoussi, Ghaith;Pennington, Shaun H.;Hill, Andrew;Boffito, Marta;Ward, Steve A.;Khoo, Saye H.;Bray, Patrick G.;O’Neill, Paul M.;Hong, W. David;Biagini, Giancarlo A.;Owen, Andrew published 《Dose prediction for repurposing nitazoxanide in SARS-CoV-2 treatment or chemoprophylaxis》. 《British Journal of Clinical Pharmacology》published the findings. The article contains the following contents:

Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has been declared a global pandemic and urgent treatment and prevention strategies are needed. Nitazoxanide, an anthelmintic drug, has been shown to exhibit in vitro activity against SARS-CoV-2. The present study used physiol. based pharmacokinetic (PBPK) modeling to inform optimal doses of nitazoxanide capable of maintaining plasma and lung tizoxanide exposures above the reported SARS-CoV-2 EC₉₀. A whole-body PBPK model was validated against available pharmacokinetic data for healthy individuals receiving single and multiple doses between 500 and 4000 mg with and without food. The validated model was used to predict doses expected to maintain tizoxanide plasma and lung concentrations above the EC90 in >90% of the simulated population. PopDes was used to estimate an optimal sparse sampling strategy for future clin. trials. The PBPK model was successfully validated against the reported human pharmacokinetics. The model predicted optimal doses of 1200 mg QID, 1600 mg TID and 2900 mg BID in the fasted state and 700 mg QID, 900 mg TID and 1400 mg BID when given with food. For BID regimens an optimal sparse sampling strategy of 0.25, 1, 3 and 12 h post dose was estimated The PBPK model predicted tizoxanide concentrations within doses of nitazoxanide already given to humans previously. The reported dosing strategies provide a rational basis for design of clin. trials with nitazoxanide for the treatment or prevention of SARS-CoV-2 infection. A concordant higher dose of nitazoxanide is now planned for investigation in the seamless phase I/IIa AGILE trial.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.Computed Properties of C12H9N3O5S

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

Category: thiazole《Drug design and repurposing with DockThor-VS web server focusing on SARS-CoV-2 therapeutic targets and their non-synonym variants》 was published in 2021. The authors were Guedes, Isabella A.;Costa, Leon S. C.;dos Santos, Karina B.;Karl, Ana L. M.;Rocha, Gregorio K.;Teixeira, Iury M.;Galheigo, Marcelo M.;Medeiros, Vivian;Krempser, Eduardo;Custodio, Fabio L.;Barbosa, Helio J. C.;Nicolas, Marisa F.;Dardenne, Laurent E., and the article was included in《Scientific Reports》. The author mentioned the following in the article:

The COVID-19 caused by the SARS-CoV-2 virus was declared a pandemic disease in March 2020 by the World Health Organization (WHO). Structure-Based Drug Design strategies based on docking methodologies have been widely used for both new drug development and drug repurposing to find effective treatments against this disease. In this work, we present the developments implemented in the DockThor-VS web server to provide a virtual screening (VS) platform with curated structures of potential therapeutic targets from SARS-CoV-2 incorporating genetic information regarding relevant non-synonymous variations. The web server facilitates repurposing VS experiments providing curated libraries of currently available drugs on the market. At present, DockThor-V S provides ready-for-docking 3D structures for wild type and selected mutations for Nsp3 (papain-like, PLpro domain), Nsp5 (Mpro, 3CLpro), Nsp12 (RdRp), Nsp15 (NendoU), N protein, and Spike. We performed VS experiments of FDA-approved drugs considering the therapeutic targets available at the web server to assess the impact of considering different structures and mutations to identify possible new treatments of SARS-CoV-2 infections. The DockThor-VS is freely available at www.dockthor.lncc.br. 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.Category: thiazole

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

Ahmadi, Fereshteh;Imani, Kaveh;Mozafari, Hadi;Bazgir, Ayoob published 《Metal-free isocyanide insertion reaction to benzothiazolyl urea derivatives》. The research results were published in《Journal of Molecular Structure》 in 2022.Name: 6-Nitrobenzo[d]thiazol-2-amine The article conveys some information:

An efficient iodine-catalyzed reaction of 2-aminobenzothiazole and isocyanides for the synthesis of benzothiazolyl urea derivatives via a metal-free isocyanide insertion reaction is reported. Introducing a simple method for the synthesis of desired benzothiazolyl urea skeletons and use of more acceptable iodine mol. instead of expensive transition metal catalysts are the most important advantages of this strategy. To complete the study, the researchers used 6-Nitrobenzo[d]thiazol-2-amine (cas: 6285-57-0) .

6-Nitrobenzo[d]thiazol-2-amine(cas:6285-57-0Name: 6-Nitrobenzo[d]thiazol-2-amine) has been shown to lower blood pressure in mice by inhibiting angiotensin converting enzyme and potassium channels. This drug also has a protective effect on the heart and brain from ischemia reperfusion injury.

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