Category: thiazole

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

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

Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetateIn 2021, Rocco, Patricia R. M.;Silva, Pedro L.;Cruz, Fernanda F.;Melo, Marco Antonio C. Jr.;Tierno, Paulo F. G. M. M.;Moura, Marcos A.;De Oliveira, Luis Frederico G.;Lima, Cristiano C.;Santos, Ezequiel A. Dos;Walter, F. Jr.;Fernandes, Ana Paula S. M.;Franchini, Kleber G.;Magri, Erick;de Moraes, Nara F.;Goncalves, Jose Mario J.;Carbonieri, Melanie N.;Santos, Ivonise S. Dos;Paes, Natalia F.;Maciel, Paula V. M.;Rocha, Raissa P.;de Carvalho, Alex F.;Alves, Pedro Augusto;Proenca-Modena, Jose Luiz;Cordeiro, Artur T.;Trivella, Daniela B. B.;Marques, Rafael E.;Luiz, Ronir R.;Pelosi, Paolo;e Silva, Jose Roberto Lapa published 《Early use of nitazoxanide in mild COVID-19 disease: randomised, placebo-controlled trial》. 《European Respiratory Journal》published the findings. The article contains the following contents:

Background: Nitazoxanide is widely available and exerts broad-spectrum antiviral activity in vitro. However, there is no evidence of its impact on severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection. Methods: In a multicentre, randomised, double-blind, placebo-controlled trial, adult patients presenting up to 3 days after onset of coronavirus disease 2019 (COVID-19) symptoms (dry cough, fever and/or fatigue) were enrolled. After confirmation of SARS-CoV-2 infection using reverse transcriptase PCR on a nasopharyngeal swab, patients were randomised 1:1 to receive either nitazoxanide (500 mg) or placebo, three times daily, for 5 days. The primary outcome was complete resolution of symptoms. Secondary outcomes were viral load, laboratory tests, serum biomarkers of inflammation and hospitalisation rate. Adverse events were also assessed. Results: From June 8 to August 20, 2020, 1575 patients were screened. Of these, 392 (198 placebo, 194 nitazoxanide) were analyzed. Median (interquartile range) time from symptom onset to first dose of study drug was 5 (4-5) days. At the 5-day study visit, symptom resolution did not differ between the nitazoxanide and placebo arms. Swabs collected were neg. for SARS-CoV-2 in 29.9% of patients in the nitazoxanide arm vs. 18.2% in the placebo arm (p = 0.009). Viral load was reduced after nitazoxanide compared to placebo (p = 0.006). The percentage viral load reduction from onset to end of therapy was higher with nitazoxanide (55%) than placebo (45%) (p = 0.013). Other secondary outcomes were not significantly different. No serious adverse events were observed Conclusions: In patients with mild COVID-19, symptom resolution did not differ between nitazoxanide and placebo groups after 5 days of therapy. However, early nitazoxanide therapy was safe and reduced viral load significantly.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.Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate

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

Product Details of 6285-57-0《Synthesis and Evaluation of a Series of 1,3,4-Thiadiazole Derivatives as Potential Anticancer Agents》 was published in 2018. The authors were Altintop, Mehlika D.;Sever, Belgin;Ozdemir, Ahmet;Ilgin, Sinem;Atli, Ozlem;Turan-Zitouni, Gulhan;Kaplancikli, Zafer A., and the article was included in《Anti-Cancer Agents in Medicinal Chemistry》. The author mentioned the following in the article:

In an attempt to develop potent antitumor agents, the synthesis of a series of N-(6-substituted benzothiazol-2-yl)-2-[(5-(arylamino)-1,3,4-thiadiazol-2-yl)thio]acetamides (1-14) was described and their cytotoxic effects on A549 human lung adenocarcinoma, MCF-7 human breast adenocarcinoma, HepG2 human hepatocellular carcinoma and NIH/3T3 mouse embryonic fibroblast cell lines were investigated using MTT assay. Phenyl-substituted compounds (8-14) were found to be more effective than naphthyl-substituted compounds (1-7) on cancer cells. Compounds 8, 9, 10, 12, 13 and 14 were identified as the most potent anticancer agents on MCF-7 and HepG2 cell lines and therefore their effects on DNA synthesis and apoptosis/necrosis in MCF-7 cell line were evaluated. Among these compounds, N-(6-methoxybenzothiazol-2-yl)-2-[(5- (phenylamino)-1,3,4-thiadiazol-2-yl)thio]acetamide (13) was the most selective anticancer agent against MCF-7 and HepG2 cell lines with a SI value of 100. On the other hand, compounds 8, 9, 10, 12, 13 and 14 inhibited DNA synthesis in MCF-7 cell line in a dose-dependent manner. Flow cytometric analyses clearly indicated that the compounds showed significant anticancer activity against MCF-7 cell line via the induction of apoptosis dose dependently. According to in vitro assays, compounds 8, 9, 10, 12, 13 and 14 stand out as promising candidates for further studies. To complete the study, the researchers used 6-Nitrobenzo[d]thiazol-2-amine (cas: 6285-57-0) .

6-Nitrobenzo[d]thiazol-2-amine(cas:6285-57-0Product Details of 6285-57-0) 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

Zheng, Jun;Woerl, Benjamin;Breit, Bernhard published 《Rhodium-Catalyzed Chemo-, Regio-, and Enantioselective Allylation of 2-Aminothiazoles with Terminal Allenes》 in 2019. The article was appeared in 《European Journal of Organic Chemistry》. They have made some progress in their research.Electric Literature of C7H5N3O2S The article mentions the following:

A rhodium-catalyzed chemo-, regio- and enantioselective intermol. coupling reaction of 2-aminobenzothiazoles with terminal allenes is reported. The new reaction displays a wide substrate scope for both reaction partners to deliver the allylation products in good yields, with excellent regio- and enantioselectivity. This novel methodol. was further applied in an efficient synthesis of chiral isothiourea. 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) 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.
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

Electric Literature of C7H5N3O2SIn 2018, Ahlawat, Aarti;Khatkar, Priyanka;Singh, Vikramjeet;Asija, Sonika published 《Diorganotin(IV) complexes of Schiff bases derived from salicylaldehyde and 2-amino-6-substituted benzothiazoles: synthesis, spectral studies, in vitro antimicrobial evaluation and QSAR studies》. 《Research on Chemical Intermediates》published the findings. The article contains the following contents:

In the present work, Schiff base ligands (1–4) were prepared by condensation of 2-amino-6-substituted-benzothiazole and salicylaldehyde in a 1:1 molar ratio and were further treated with diorganotindichloride R’₂SnCl₂ leading to a series of organotin(IV) complexes (5–20) of type R’₂SnL^1-4Cl [R’ = Ph, Bu, Et, Me]. The prepared Schiff base ligands and the organotin(IV) complexes were characterized by various spectroscopic techniques (¹H, ¹³C, ¹¹⁹Sn NMR, FT-IR) and phys. techniques. All the synthesized compounds were evaluated for in vitro antibacterial and antifungal activity against two Gram pos. bacterial strains B. cereus, S. aureus, two Gram neg. bacterial strains E. coli, P. aeruginosa and two fungal strains A. niger and A. flavus by serial dilution method. The spectral data revealed that the complexes were pentacoordinated with bidentate ligands coordinated through oxygen and nitrogen. The results of antimicrobial activity revealed that the synthesized complexes were more toxic towards Gram pos. bacterial strains as compared to Gram neg. bacterial strains. From the results of QSAR anal., it was indicated that the antimicrobial activity of the synthesized compounds were controlled by topol. parameters (mol. connectivity indexes). To complete the study, the researchers used 6-Nitrobenzo[d]thiazol-2-amine (cas: 6285-57-0) .

6-Nitrobenzo[d]thiazol-2-amine(cas:6285-57-0Electric Literature of C7H5N3O2S) 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