Day: September 15, 2022

Related Products of 55981-09-4《Structure-Activity Study of Nitazoxanide Derivatives as Novel STAT3 Pathway Inhibitors》 was published in 2021. The authors were Lu, Zirui;Li, Xiaona;Li, Kebin;Wang, Cong;Du, Tingting;Huang, Wei;Ji, Ming;Li, Changhong;Xu, Fengrong;Xu, Ping;Niu, Yan, and the article was included in《ACS Medicinal Chemistry Letters》. The author mentioned the following in the article:

We identified nitazoxanide (NTZ) as a moderate STAT3 pathway inhibitor through immunoblot anal. and a cell-based IL-6/JAK/STAT3 pathway activation assay. A series of thiazolide derivatives were designed and synthesized to further validate the thiazolide scaffold as STAT3 inhibitors. Eight out of 25 derivatives displayed potencies greater than that of NTZ, and their STAT3 pathway inhibitory activities were found to be significantly correlated with their antiproliferative activities in HeLa cells. Derivatives 15 and 24 were observed to be more potent than the pos. control WP1066, which is under phase I clin. trials. Compared with NTZ, 15(I) also exhibited much improved in vivo pharmacokinetic parameters in rats and efficacies against proliferations in multiple cancer cell lines, indicating a broad-spectrum effect of these thiazolides as antitumor agents targeted on STAT3. 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.Related Products of 55981-09-4

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

Recommanded Product: 55981-09-4《Sorafenib and nitazoxanide disrupt mitochondrial function and inhibit regrowth capacity in three-dimensional models of hepatocellular and colorectal carcinoma》 was published in 2022. The authors were Ek, Frida;Blom, Kristin;Selvin, Tove;Rudfeldt, Jakob;Andersson, Claes;Senkowski, Wojciech;Brechot, Christian;Nygren, Peter;Larsson, Rolf;Jarvius, Malin;Fryknaes, Maarten, and the article was included in《Scientific Reports》. The author mentioned the following in the article:

Abstract: Quiescent cancer cells in malignant tumors can withstand cell-cycle active treatment and cause cancer spread and recurrence. Three-dimensional (3D) cancer cell models have led to the identification of oxidative phosphorylation (OXPHOS) as a context-dependent vulnerability. The limited treatment options for advanced hepatocellular carcinoma (HCC) and colorectal carcinoma (CRC) metastatic to the liver include the multikinase inhibitors sorafenib and regorafenib. Off-target effects of sorafenib and regorafenib are related to OXPHOS inhibition; however the importance of this feature to the effect on tumor cells has not been investigated in 3D models. We began by assessing global transcriptional responses in monolayer cell cultures, then moved on to multicellular tumor spheroids (MCTS) and tumoroids generated from a CRC patient. Cells were treated with chemotherapeutics, kinase inhibitors, and the OXPHOS inhibitors. Cells grown in 3D cultures were sensitive to the OXPHOS inhibitor nitazoxanide, sorafenib, and regorafenib and resistant to other multikinase inhibitors and chemotherapeutic drugs. Furthermore, nitazoxanide and sorafenib reduced viability, regrowth potential and inhibited mitochondrial membrane potential in an additive manner at clin. relevant concentrations This study demonstrates that the OXPHOS inhibition caused by sorafenib and regorafenib parallels 3D activity and can be further investigated for new combination strategies. 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.Recommanded Product: 55981-09-4

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

Kiehl, Isis G. A.;Riccetto, Eduardo;Salustiano, Ana C. C.;Ossick, Marina V.;Ferrari, Karen L.;Assalin, Heloisa B.;Ikari, Osamu;Reis, Leonardo O. published 《Boosting bladder cancer treatment by intravesical nitazoxanide and bacillus calmette-guerin association》 in 2021. The article was appeared in 《World Journal of Urology》. They have made some progress in their research.COA of Formula: C12H9N3O5S The article mentions the following:

Abstract: Purpose: Nitazoxanide (NTZ) has shown a promising antitumoral effect, the current study compared the anti-neoplastic effects of intravesical NTZ and BCG plus NTZ in NMIBC animal model. Methods: 30 rats, Fisher 344 were instilled with 4 intravesical doses of 1.5 mg/kg of N-methyl-N-nitrosourea (MNU) every 15 days for BC induction. The animals were divided into 3 groups (Group BCG 10⁶ UFC -1 mg of BCG; Group NTZ -300 mg/kg of NTZ; Group NTZ + BCG -simultaneous treatment of BCG and NTZ) and received weekly intravesical treatment for 6 consecutive weeks. Animals were submitted to ultrasound imaging and euthanasia, their bladders were collected and histopathol., immunohistochem. tests (ki67 e c-Myc) and Western Blotting (PI3K, mTOR, and p-4E-BP) were performed. Results: Histopathol. tests showed 66.67%, 62.5% and 37.5% incidence of BC in animals treated with BCG, NTZ, and NTZ + BCG, resp. Nuclear positivity for ki-67 in BC animals were 12.4%, 13.2% and 8.8% in BCG, NTZ and NTZ + BCG group, resp. Between animals with carcinoma, c-Myc strong pos. was 40.10% in NTZ, 32.2% in BCG and 19.90% in the NTZ + BCG group. Blotting has shown mTOR (p =0.0473) and PI3K inhibition (p = 0.0349) in the presence of BCG, added to 4-EBP inhibition in the presence of NTZ. Conclusions: Results show the possible synergy between the gold standard BC treatment BCG and NTZ, in which multiple targets inhibition such as c-Myc and downstream mTOR, p-4E-BP and PI3K might play a role. 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 cellsCOA of Formula: C12H9N3O5S

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

Reference of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetateIn 2021, Ashigbie, Paul G;Shepherd, Susan;Steiner, Kevin L;Amadi, Beatrice;Aziz, Natasha;Manjunatha, Ujjini H;Spector, Jonathan M;Diagana, Thierry T;Kelly, Paul published 《Use-case scenarios for an anti-Cryptosporidium therapeutic.》. 《PLoS neglected tropical diseases》published the findings. The article contains the following contents:

Cryptosporidium is a widely distributed enteric parasite that has an increasingly appreciated pathogenic role, particularly in pediatric diarrhea. While cryptosporidiosis has likely affected humanity for millennia, its recent “emergence” is largely the result of discoveries made through major epidemiologic studies in the past decade. There is no vaccine, and the only approved medicine, nitazoxanide, has been shown to have efficacy limitations in several patient groups known to be at elevated risk of disease. In order to help frontline health workers, policymakers, and other stakeholders translate our current understanding of cryptosporidiosis into actionable guidance to address the disease, we sought to assess salient issues relating to clinical management of cryptosporidiosis drawing from a review of the literature and our own field-based practice. This exercise is meant to help inform health system strategies for improving access to current treatments, to highlight recent achievements and outstanding knowledge and clinical practice gaps, and to help guide research activities for new anti-Cryptosporidium therapies. 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.Reference of 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate

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

Addanki, Hanumantha Rao;Vallabhaneni, Madhava Rao;Chennamsett, Subramanyam;Pullagura, Priyadarshini;Sagurthi, Someswara Rao;Pasupuleti, Visweswara Rao published 《An in silico ADMET, molecular docking study and microwave-assisted synthesis of new phosphorylated derivatives of thiazolidinedione as potential anti-diabetic agents》 in 2022. The article was appeared in 《Synthetic Communications》. They have made some progress in their research.Category: thiazole The article mentions the following:

A series of new phosphorylated derivatives of thiazolidinedione was synthesized for the first time with high yields (92-96%) in short reaction time (7-15 min) by the reaction of 4-{[(5E)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl}phenyl Et phosphorochloridate with various heterocyclic amines by microwave irradiation technique under solvent-free condition. A study on in silico ADMET and mol. docking was performed for all the mols. to acquire an insight on drug likeliness behavior and also their ability to inhibit the enzyme, α-amylase. The mols. with momentous pharmacokinetic properties with substantial binding affinity were synthesized. The synthesized compounds were characterized spectroscopically to confirm their structure and then in vitro α-amylase inhibitory activity was also carried out for all the newly prepared compounds The synthesized compounds were characterized spectroscopically to confirm their structure and then in vitro α-amylase inhibitory activity was also carried out for all the newly prepared compounds All the leftover compounds displayed modest to excellent inhibition in comparison with reference drug, Acarbose. 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 Category: thiazole) 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

Related Products of 6285-57-0In 2018, Kumari, Bhawana;Chauhan, Kalpana;Trivedi, Jalpa;Jaiswal, Varun;Kanwar, Shamsher S.;Pokharel, Yuba Raj published 《Benzothiazole-Based-Bioconjugates with Improved Antimicrobial, Anticancer and Antioxidant Potential》. 《ChemistrySelect》published the findings. The article contains the following contents:

Micro-organism resistance to the drugs has made it necessary to explore novel antibacterial drugs that have significant toxicities. Herein, we report the bioconjugates of N-acetyl-D-glucosamine with benzothiazole derivatives via ester linkage, which display potent effect against pathogenic micro-organisms (E. coli, S. aureus and C. albicans). These newly synthesized compounds have also been evaluated for anticancer (Hep-2 and caco cell lines) and antioxidant activities. The results supported that bioconjugates suppress pathogenic infections (in-vitro) more effectively in comparison to equivalent dosage of non-conjugated benzothiazole. Specifically, bioconjugates of Schiff derivative of methoxy-benzothiazol (compound 8) and nitro- benzothiazole (compound 9) showed MIC value of 1.25 μg/mL against C. albicans. The above proved potent compound 9, furthermore, revealed significant activity against Hep-2 and caco cell lines. In conclusion, this study proved that integration of biocomponent enhances the competence in biol. application and the results can be explored as a lead for further improvization for commercialization. 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

Formula: C7H5N3O2SIn 2022, Moodley, Rashmika;Mashaba, Chakes;Rakodi, Goitsemodimo H.;Ncube, Nomagugu B.;Maphoru, Mabuatsela V.;Balogun, Mohammed O.;Jordan, Audrey;Warner, Digby F.;Khan, Rene;Tukulula, Matshawandile published 《New Quinoline-Urea-BenzΞothiazole Hybrids as Promising Antitubercular Agents: Synthesis, In Vitro Antitubercular Activity, Cytotoxicity Studies, and In Silico ADME Profiling》. 《Pharmaceuticals》published the findings. The article contains the following contents:

A series of 25 new benzothiazole-urea-quinoline hybrid compounds, I (X = H, Me, F, NO₂, etc.) and II (n = 0, 2, 3, 4, and 6) were synthesized successfully via a three-step synthetic sequence involving an amidation coupling reaction as a critical step. In vitro evaluation of these hybrid compounds for their antitubercular inhibitory activity against the Mycobacterium tuberculosis H37Rv pMSp12::GPF bioreporter strain was undertaken. Of the 25 tested compounds, 17 compounds exhibited promising anti-TB activities of less than 62.5μM (MIC90) and 13 compds showed promising activity with MIC90 values in the range of 1-10μM, while compound I(X = CF₃), being the most active, exhibited sub-micromolar activity (0.968μM) in the CAS assay. In addition, minimal cytotoxicity against the HepG2 cell line (cell viability above 75%) in 11 of the 17 compounds, at their resp. MIC90 concentrations, was observed, with compound I(X = CF₃), exhibiting 100% cell viability. The hybridization of the quinoline, urea, and benzothiazole scaffolds demonstrated a synergistic relationship because the activities of resultant hybrids were vastly improved compared to the individual entities. In silico ADME predictions showed that the majority of these compounds have drug-like properties and are less likely to potentially cause cardiotoxicity (QPlogHERG > -5).6-Nitrobenzo[d]thiazol-2-amine (cas: 6285-57-0) were involved in the experimental procedure.

6-Nitrobenzo[d]thiazol-2-amine(cas:6285-57-0Formula: 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

Hedvat, Jessica;Salerno, David M.;Kovac, Danielle;Scheffert, Jenna L.;Corbo, Heather;Chen, Justin K.;Choe, Jason Y.;Jennings, Douglas L.;Anamisis, Anastasia;Liu, Esther C.;Lee, Jennifer H.;Shertel, Tara;Lange, Nicholas W. published 《Nitazoxanide treatment for norovirus infection in solid organ transplant recipients》. The research results were published in《Clinical Transplantation》 in 2022.Recommanded Product: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate The article conveys some information:

A review. This was an IRB-approved, single-center retrospective study of all SOT recipients with GI PCR pos. for acute NV who either received nitazoxanide for NV or did not receive nitazoxanide between Jan., 2015 and August, 2019. A total of 195S OT recipients with GIPCR pos. for NV infection were screened; 52 patients who received nitazoxanide (nita+) were matched on the basis of transplant type and time post-transplant to 52 patients who had GIPCR pos. NV but did not receive nitazoxanide (nita-). These results suggest that nitazoxanide may improve symptoms from NV 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), 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

Category: thiazole《Design, synthesis and biological evaluation of some 2-(6-nitrobenzo[d]thiazol-2-ylthio)-N-benzyl-N-(6-nitrobenzo[d]thiazol-2-yl)acetamide derivatives as selective DprE1 inhibitors》 was published in 2019. The authors were Gawad, Jineetkumar;Bonde, Chandrakant, and the article was included in《Synthetic Communications》. The author mentioned the following in the article:

In the present study, pharmacophore model was developed using single ligand by ligand-based drug discovery approach. The key features responsible for DprE1 inhibitory activity were taken into consideration for developing pharmacophore. After the virtual screening, top 1000 hits were further subjected to docking study using GLIDE module, Schrodinger. Docking studies have shown promising interaction with amino residues with better glide score. Ligand-based drug design approach yielded a series of 15, 2-(6-nitrobenzo[d]thiazol-2-ylthio)-N-benzyl-N-(6-nitrobenzo[d]thiazol-2-yl)acetamide derivatives I(R¹ = H, Me, COMe, NH₂, etc.; R² = H, Br, NO₂, Me, etc.). The synthesized compounds were screened for In vitro antitubercular activity against Mycobacterium tuberculosis (H₃₇Rv). Four compounds, I (R¹ = H; R² = OMe) (MIC-1.01 μM); I (R¹ = Cl; R² = H) (MIC-0.91 μM); I (R¹ = R² = H) (MIC-0.82 μM); and I (R¹ = H; R² = Br) (MIC-1.04 μM) have shown promising activity compared to MIC of standard isoniazid (INH) and DprE1 enzyme inhibition was compared to BTZ043. Two halogen-substituted compounds have exhibited drastic enzyme inhibition. 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

Millet, Antoine;Filho, Mauro Safir;Hamouda-Tekaya, Nedra;Cavazza, Elisa;Abbe, Patricia;Ruediger, Johanna;Plaisant, Magali;Mayen, Julie;Rocchi, Stephane;Ronco, Cyril;Benhida, Rachid published 《Development and in vivo evaluation of fused benzazole analogs of anti-melanoma agent HA15》. The research results were published in《Future Medicinal Chemistry》 in 2021.Application In Synthesis of 6-Nitrobenzo[d]thiazol-2-amine The article conveys some information:

In line with our recent discovery of an efficient anticancer thiazolebenzenesulfonamide framework HA15 (1) based on a remarkable endoplasmic reticulum stress inducement mode of action, we report herein a series of innovative constrained HA15 analogs, featuring four types of bicylic derivatives The structure-activity relationship anal., using a cell line assay, led us to identify a novel version of HA15: a new benzothiazole derivative (10b) exhibiting important anti-melanoma effect against sensitive and resistant melanoma cells. Meanwhile, compound 10b induced a significant tumor growth inhibition in vivo with no apparent signs of toxicity. These results consistently open new directions to improve and develop more powerful anticancer therapeutics harboring this type of fused framework. 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 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