Day: September 21, 2022

Lu, Chunxia;Liu, Xianyong;Liu, Jie;Tang, Xinming;Zhu, Guan;Striepen, Boris;Suo, Xun published 《Immunocompetent rabbits infected with Cryptosporidium cuniculus as an animal model for anti-cryptosporidial drug testing》 in 2022. The article was appeared in 《International Journal for Parasitology》. They have made some progress in their research.Recommanded Product: 55981-09-4 The article mentions the following:

Cryptosporidium is one of the leading causes of diarrheal disease in humans and animals, which can be severe and deadly in neonates and immunocompromised hosts. Studies on the biol. of Cryptosporidium and drug discovery efforts have been hindered by a number of factors including the limited availability of animal models. Here, we report the establishment and characterization of an immunocompetent rabbit model for infection with Cryptosporidium cuniculus. By testing four known anti-cryptosporidial compounds (nitazoxanide, baicalein, curcumin and matrine), we showed that the rabbit could be used as an alternative animal model for evaluating anti-cryptosporidial drug efficacy in vivo.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

Jakopec, Silvio;Pantalon Juraj, Natalija;Brozovic, Anamaria;Jadresko, Dijana;Peric, Berislav;Kirin, Srecko I.;Raic-Malic, Silvana published 《Ferrocene conjugates linked by 1,2,3-triazole and their Zn(II) and Cu(II) complexes: Synthesis, characterization and biological activity》. The research results were published in《Applied Organometallic Chemistry》 in 2022.Synthetic Route of C7H5N3O2S The article conveys some information:

Ferrocene derivatives with mono- Py₂NCH₂Trz-1-R (8a–c; Py = 2-pyridyl, Trz = 1,2,3-triazol-5-yl; R = Fc, FcCH₂, FcCHMe) and bis-1,2,3-triazolyl fc(CH₂-1-TrzCH₂NPy₂)₂(9, fc = 1,1′-ferrocenediyl) and ArN(CH₂Trz-1-R)₂ (10a–13c; R = Fc, FcCH₂, FcCHMe; Ar = Ph, 2-benzothiazolyl, 6-chloro-2-benzothiazolyl, 6-nitro-2-benzothiazolyl) chelating groups were synthesized by regioselective copper(I)-catalyzed 1,3-dipolar cycloaddition of terminal alkynes with ferrocene azides. Metal complexes of the ligands were prepared with Cu(II) and Zn(II) salts. Crystal structures of ligands 9 and 11a were determined, as well as the structures of complexes [Cu(8a)₂](CF₃SO₃)₂ (8a-Cu) and [Cu(8c)₂(MeOH)₂](BF₄)₂ (8c-Cu). In addition to NMR and UV-Vis spectroscopy, the metal complexes were characterized by cyclic voltammetry. The cytotoxic effect of ferrocene conjugates and their Zn(II) and Cu(II) complexes was explored, and cell cycle anal. was performed. The complex [Cu(8c)₂](CF₃SO₃)₂ showed the most prominent and selective cytotoxicity on cervical carcinoma (HeLa), ovarian cancer (MES-OV), non-small cell lung cancer (A549) and breast carcinoma (MDA-MB-231) cells. This complex increased cell population in the S and G₂/M phase of the cell cycle, which was accompanied by an increase of the cells present in the sub-G₀/G₁ fraction. 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) 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

Pawde, A. V.;Kadam, D. B.;Vartale, S. P. published 《Synthesis and evaluation of antimicrobial, antioxidant activities of pyrido[3,2-d]pyrazolo[3,2-b]-4H-pyrimido[5,6-e]-4H-pyrimido[2,3-b]benzothiazole derivatives》. The research results were published in《Journal of Applicable Chemistry (Lumami, India)》 in 2019.Category: thiazole The article conveys some information:

The objective of the present investigation was to synthesize 3-cyano-4-oxo-2-(methylthio)-6-N-Ph pyrido[3,2-d]pyrazolo[3,2-b]pyrimidine by condensation of 1-phenyl-1H-pyrazolo[3,4-b]pyridine-3-amine with Et cyano bis(methylthio)acrylate which on further condensation with various 2-amino 1/2/3/4-substituted benzothiazoles gives 15-imino-14-oxo-12-N-Ph pyrido[3,2-d]pyrazolo[3,2-b]-4H-pyrimido[5,6-e]-4H-pyrimido[2,3-b]benzothiazole and their 1/3 substituted derivatives I (R¹ = H, CH₃, OCH₃, Cl, NO₂; R² = H, CH₃). These newly synthesized compounds were further screened for antimicrobial and antioxidant properties. The experimental procedure involved many compounds, such as 6-Nitrobenzo[d]thiazol-2-amine (cas: 6285-57-0) .

6-Nitrobenzo[d]thiazol-2-amine(cas:6285-57-0 Category: thiazole) 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

Zhang, Qing;Zhao, Kuantao;Zhang, Lixun;Jiao, Xiaoyu;Zhang, Yongjie;Tang, Chunlei published 《Synthesis and biological evaluation of diaryl urea derivatives as FLT3 inhibitors》 in 2020. The article was appeared in 《Bioorganic & Medicinal Chemistry Letters》. They have made some progress in their research.Reference of 6-Nitrobenzo[d]thiazol-2-amine The article mentions the following:

As a class III receptor tyrosine kinase (RTK), FMS-like tyrosine kinase 3 (FLT3) is always overexpressed in many cases of acute leukemia. This paper studies the structure-based synthesis and biol. evaluation of diaryl urea derivatives as FLT3 inhibitors. Encouragingly, compounds 1-(3-(tert-butyl)isoxazol-5-yl)-3-(4-(7-methoxybenzo[d]imidazo[2,1-b]thiazol-2-yl)phenyl)urea , 1-(3-(tert-butyl)isoxazol-5-yl)-3-(4-(7-(2-morpholinoethoxy)benzo[d]imidazo[2,1-b]thiazol-2-yl)phenyl)urea , 1-(5-(tert-butyl)isoxazol-3-yl)-3-(2-(4-(2-morpholinoethoxy)phenyl)benzo[d]imidazo[2,1-b]thiazol-7-yl)urea , and 1-(3-(tert-butyl)isoxazol-5-yl)-3-(2-(4-(2-morpholinoethoxy)phenyl)benzo[d]imidazo[2,1-b]thiazol-7-yl)urea showed excellent biol. activities in a low nanomolar range. In particular, compound 1-(3-(tert-butyl)isoxazol-5-yl)-3-(4-(7-(2-morpholinoethoxy)benzo[d]imidazo[2,1-b]thiazol-2-yl)phenyl)urea demonstrated significant inhibitory potency against FLT3-ITD (IC₅₀ = 5.60 nM) and better antiproliferative activity than quizartinib against MV4-11 cell line (IC₅₀ = 0.176 nM). Compound 1-(3-(tert-butyl)isoxazol-5-yl)-3-(4-(7-(2-morpholinoethoxy)benzo[d]imidazo[2,1-b]thiazol-2-yl)phenyl)urea for the treatment of acute myeloid leukemia could be very promising. The experimental procedure involved many compounds, such as 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

Quality Control of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetateIn 2022, Lubinsky, Anthony Steven;Brosnahan, Shari B.;Lehr, Andrew;Elnadoury, Ola;Hagedorn, Jacklyn;Garimella, Bhaskara;Bender, Michael T.;Amoroso, Nancy;Artigas, Antonio;Bos, Lieuwe D. J.;Kaufman, David published 《Inhaled pulmonary vasodilators are not associated with improved gas exchange in mechanically ventilated patients with COVID-19: A retrospective cohort study》. 《Journal of Critical Care》published the findings. The article contains the following contents:

Measure the effect of inhaled pulmonary vasodilators on gas exchange in mech. ventilated patients with COVID-19. A retrospective observational cohort study at three New York University Hospitals was performed including eighty-four mech. ventilated SARS Cov-2 nasopharyngeal PCR pos. patients, sixty nine treated with inhaled nitric oxide (iNO) and fifteen with inhaled epoprostenol (iEPO). The primary outcomes were change in PAO2:FIO2 ratio, oxygenation Index (OI), and ventilatory ratio (VR) after initiation of inhaled pulmonary vasodilators. There was no significant change in PAO2:FIO2ratio after initiation of iNO (mean – 4.1, 95% CI -17.3-9.0, P = 0.54) or iEPO (mean – 3.4, 95% CI -19.7-12.9, P = 0.66), in OI after initiation of iNO (mean 2.1, 95% CI-0.04-4.2, P = 0.054) or iEPO (mean – 3.4, 95% CI -19.7-12.9, P = 0.75), or in VR after initiation of iNO (mean 0.17, 95% CI -0.03-0.36, P = 0.25) or iEPO (mean 0.33, 95% CI -0.0847-0.74, P = 0.11). PAO2:FIO2, OI and VR did not significantly change over a five day period starting the day prior to drug initiation in patients who received either iNO or iEPO assessed with a fixed effects model. Inhaled pulmonary vasodilators were not associated with significant improvement in gas exchange in mech. ventilated patients with COVID-19. 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), a thiazolide compound, is a antiparasitic drug with structure similar to niclosamide.Quality Control of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate

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

Song, Xiyu;Hou, Aiqin;Xie, Kongliang;Hu, Tingli published 《Synthesis and Dyeing Properties of New Bi-heterocyclic Disperse Dyes Containing Pyridone Group for Polyester Fabrics》 in 2020. The article was appeared in 《Fibers and Polymers》. They have made some progress in their research.Product Details of 6285-57-0 The article mentions the following:

A series of novel bi-heterocyclic disperse dyes containing N-ethyl-3-cyano-4-methyl-6-hydroxy-2-pyridine group were synthesized. The structures of the bi-heterocyclic dyes were characterized by Fourier transform IR spectroscopy (FT-IR), NMR spectroscopy (¹H-NMR), UV-vis spectrophotometry, and elemental anal. The distinct spectral behavior and solvatochromic effect of the dyes were discussed. The dyeing properties of the dyes for polyethylene terephthalate (PET) fabric were investigated. Novel bi-heterocyclic disperse dyes had higher molar absorption coefficient, good color strength, and excellent fastness properties, especially light fastness. The bi-heterocyclic disperse dyes have potential research value in the development of high light resistant dyes and functional dyes. The experimental procedure involved many compounds, such as 6-Nitrobenzo[d]thiazol-2-amine (cas: 6285-57-0) .

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

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

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

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

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