Day: September 21, 2022

Computed Properties of C12H9N3O5S《Impairment of SARS-CoV-2 spike glycoprotein maturation and fusion activity by nitazoxanide: an effect independent of spike variants emergence》 was published in 2022. The authors were Riccio, Anna;Santopolo, Silvia;Rossi, Antonio;Piacentini, Sara;Rossignol, Jean-Francois;Santoro, M. Gabriella, and the article was included in《Cellular and Molecular Life Sciences》. The author mentioned the following in the article:

SARS-CoV-2, the causative agent of COVID-19, has caused an unprecedented global health crisis. The SARS-CoV-2 spike, a surface-anchored trimeric class-I fusion glycoprotein essential for viral entry, represents a key target for developing vaccines and therapeutics capable of blocking virus invasion. The emergence of SARS-CoV-2 spike variants that facilitate virus spread and may affect vaccine efficacy highlights the need to identify novel antiviral strategies for COVID-19 therapy. Here, we demonstrate that nitazoxanide, an antiprotozoal agent with recognized broad-spectrum antiviral activity, interferes with SARS-CoV-2 spike maturation, hampering its terminal glycosylation at an endoglycosidase H-sensitive stage. Engineering multiple SARS-CoV-2 variant-pseudoviruses and utilizing quant. cell-cell fusion assays, we show that nitazoxanide-induced spike modifications hinder progeny virion infectivity as well as spike-driven pulmonary cell-cell fusion, a critical feature of COVID-19 pathol. Nitazoxanide, being equally effective against the ancestral SARS-CoV-2 Wuhan-spike and different emerging variants, including the Delta variant of concern, may represent a useful tool in the fight against COVID-19 infections. 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.Computed Properties of C12H9N3O5S

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

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

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

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

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

Chan, Christina;Foster, Sean T.;Chan, Kayla G.;Cacace, Matthew J.;Ladd, Shay L.;Sandum, Caleb T.;Wright, Paul T.;Volmert, Brett;Yang, Weiyang;Aguirre, Aitor;Li, Wen;Wright, Neil T. published 《Repositioned Drugs for COVID-19-the Impact on Multiple Organs》 in 2021. The article was appeared in 《SN Comprehensive Clinical Medicine》. They have made some progress in their research.HPLC of Formula: 55981-09-4 The article mentions the following:

Abstract: This review summarizes published findings of the beneficial and harmful effects on the heart, lungs, immune system, kidney, liver, and central nervous system of 47 drugs that have been proposed to treat COVID-19. Many of the repurposed drugs were chosen for their benefits to the pulmonary system, as well as immunosuppressive and anti-inflammatory effects. However, these drugs have mixed effects on the heart, liver, kidney, and central nervous system. Drug treatments are critical in the fight against COVID-19, along with vaccines and public health protocols. Drug treatments are particularly needed as variants of the SARS-Cov-2 virus emerge with some mutations that could diminish the efficacy of the vaccines. Patients with comorbidities are more likely to require hospitalization and greater interventions. The combination of treating severe COVID-19 symptoms in the presence of comorbidities underscores the importance of understanding the effects of potential COVID-19 treatments on other organs. 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.HPLC of Formula: 55981-09-4

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

Mule, Shubham;Singh, Ajit;Greish, Khaled;Sahebkar, Amirhossein;Kesharwani, Prashant;Shukla, Rahul published 《Drug repurposing strategies and key challenges for COVID-19 management》. The research results were published in《Journal of Drug Targeting》 in 2022.Quality Control of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate The article conveys some information:

A review. COVID-19 is a clin. outcome of viral infection emerged due to strain of beta coronavirus which attacks the type-2 pneumocytes in alveoli via angiotensin-converting enzyme 2 (ACE2) receptors. There is no satisfactory drug developed against ‘SARS-CoV2’, highlighting an immediate necessity chemotherapeutic repurposing plan COVID-19. Drug repurposing is a method of selection of approved therapeutics for new use and is considered to be the most effective drug finding strategy since it includes less time and cost to obtain treatment compared to the de novo drug acquisition process. Several drugs such as hydroxychloroquine, remdesivir, teicoplanin, darunavir, ritonavir, nitazoxanide, chloroquine, tocilizumab and favipiravir (FPV) showed their activity against ‘SARS-CoV2’; in vitro. This review has emphasized on repurposing of drugs, and biologics used in clin. set up for targeting COVID-19 and to evaluate their pharmacokinetics, pharmacodynamics and safety with their future aspect. The key benefit of drug repurposing is the wealth of information related to its safety, and easy accessibility. Altogether repurposing approach allows access to regulatory approval as well as reducing sophisticated safety studies. 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 cellsQuality Control of 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 acetate《1,3-Thiazolbenzamide Derivatives as Chikungunya Virus nsP2 Protease Inhibitors》 was published in 2021. The authors were Ivanova, Larisa;Rausalu, Kai;Zusinaite, Eva;Tammiku-Taul, Jaana;Merits, Andres;Karelson, Mati, and the article was included in《ACS Omega》. The author mentioned the following in the article:

Chikungunya fever results from an infection with Chikungunya virus (CHIKV, genus Alphavirus) that is prevalent in tropical regions and is spreading fast to temperate climates with documented outbreaks in Europe and the Americas. Currently, there are no available vaccines or antiviral drugs for prevention or treatment of Chikungunya fever. The nonstructural proteins (nsPs) of CHIKV responsible for virus replication are promising targets for the development of new antivirals. This study was attempted to find out new potential inhibitors of CHIKV nsP2 protease using the ligand-based drug design. Two compounds 10 and 10c, identified by mol. docking, showed antiviral activity against CHIKV with IC₅₀ of 13.1 and 8.3μM, resp. Both compounds demonstrated the ability to inhibit the activity of nsP2 in a cell-free assay, and the impact of compound 10 on virus replication was confirmed by western blot. The mol. dynamics study of the interactions of compounds 10 and 10c with CHIKV nsP2 showed that a possible mechanism of action of these compounds is the blocking of the active site and the catalytic dyad of nsP2. 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 cellsSafety of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate

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

Quality Control of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetateIn 2021, Talaam, Keith Kiplangat;Inaoka, Daniel Ken;Hatta, Takeshi;Tsubokawa, Daigo;Tsuji, Naotoshi;Wada, Minoru;Saimoto, Hiroyuki;Kita, Kiyoshi;Hamano, Shinjiro published 《Mitochondria as a potential target for the development of prophylactic and therapeutic drugs against Schistosoma mansoni infection》. 《Antimicrobial Agents and Chemotherapy》published the findings. The article contains the following contents:

The emergence of parasites resistant to praziquantel, the only therapeutic agent, and its ineffectiveness as a prophylactic agent (inactive against the migratory/juvenile Schistosoma mansoni), make the development of new antischistosomal drugs urgent. The parasite’s mitochondrion is an attractive target for drug development, because this organelle is essential for survival throughout the parasite’s life cycle. We investigated the effects of 116 compounds against Schistosoma mansoni cercaria motility that have been reported to affect mitochondrion-related processes in other organisms. Next, eight compounds plus two controls (mefloquine and praziquantel) were selected and assayed against the motility of schistosomula (in vitro) and adults (ex vivo). Prophylactic and therapeutic assays were performed using infected mouse models. Inhibition of oxygen consumption rate (OCR) was assayed using Seahorse XFe24 analyzer. All selected compounds showed excellent prophylactic activity, reducing the worm burden in the lungs to less than 15% of that obtained in the vehicle control. Notably, ascofuranone showed the highest activity, with a 98% reduction of the worm burden, suggesting the potential for the development of ascofuranone as a prophylactic agent. The worm burden of infected mice with S. mansoni at the adult stage was reduced by more than 50% in mice treated with mefloquine, nitazoxanide, amiodarone, ascofuranone, pyrvinium pamoate, or plumbagin. Moreover, adult mitochondrial OCR was severely inhibited by ascofuranone, atovaquone, and nitazoxanide, while pyrvinium pamoate inhibited both mitochondrial and nonmitochondrial OCRs. These results demonstrate that the mitochondria of S. mansoni are a feasible target for drug development. 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.Quality Control of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate

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