Tag: 100-200

Jiao, Peili;Wang, Yuxi;Mao, Beibei;Wang, Bingding;Zhong, Yi;Jin, Hongwei;Zhang, Lihe;Zhang, Liangren;Liu, Zhenming published 《Discovery of 2-(2-aminobenzo[d]thiazol-6-yl) benzo[d]oxazol-5-amine derivatives that regulated HPV relevant cellular pathway and prevented cervical cancer from abnormal proliferation》 in 2020. The article was appeared in 《European Journal of Medicinal Chemistry》. They have made some progress in their research.Computed Properties of C7H5N3O2S The article mentions the following:

Herein, virtual screening was performed and 2-(2-aminobenzo[d]thiazol-6-yl) benzo[d]oxazol-5-amine derivatives I (R¹ = H, NH₂; R² = H, NH₂, NHC(O)NHC₂H₅) were designed, synthesized as antineoplastic agents, and evaluated for their anti-tumor activities. Among them, the most promising compound I (R = R¹ = NH₂) (II) showed specific anti-proliferation ability against HeLa cells (IC₅₀ = 380 nM) as well as excellent inhibition of tumor growth in the HeLa xenograft model without inducing obvious side effects. It is interesting that compound II displayed significant inhibition against HPV18-pos. cervical cell lines (HeLa) but not for HPV16-pos. cervical cell lines (SiHa). Further study demonstrated that a low concentration of compound II could lead to a cell cycle blockage at the G1 phase and promote cell apoptosis slightly (8.77%). Compound II also exhibited transcription repression, especially those associated with the oncoprotein E7 cellular pathway like E7/Rb/E2F-1/DNMT1, which were essential in tumorigenesis. Proteomics anal. revealed that E7 might be degraded through E3 ubiquitin ligases, which aligned with decreasing expression of E7 following the treatment of compound II. Taken together, it indicated that compound II could be a promising potential agent for cervical cancer treatment. 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

Recommanded Product: 6-Nitrobenzo[d]thiazol-2-amine《An efficient green synthesis of new benzothiazoles containing sulfonamide or cyclic imide moieties》 was published in 2020. The authors were Bougheloum, Chafika;Alioua, Sabrina;Belghiche, Robila;Benali, Nesma;Messalhi, Abdelrani, and the article was included in《Journal of Heterocyclic Chemistry》. The author mentioned the following in the article:

An efficient and convenient protocol for one-pot synthesis of new benzothiazoles bearing sulfonamide I (R = 4-methylphenyl, NH(CH₂)₃CH₃, 1,2,3,4-tetrahydroisoquinolin-2-yl, etc.; R¹ = H, 6-Me, 6-NO₂, etc.; X = (CH₂)₂, CH=CH, ClC=CCl, etc.) and 1-N-(1,3-benzothiazol-2-yl)-2-N-[(4-methylbenzene)sulfonyl]benzene-1,2-dicarboxamide or cyclic imide moieties II and 2-(6-methoxybenzo[d]thiazol-2-yl)isoindoline-1,3-dione using cesium salt of Wells-Dawson heteropolyacid (Cs₅HP₂W₁₈O₆₂) as solid catalyst and water as solvent under ultrasound irradiation was reported. The reaction speed was remarkably catalyzed with the aid of ultrasound irradiation Moreover, this approach prepares multiple other benefits such as operational ease, higher yields, and energy performance.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) 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

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

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

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

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

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

Mikherdov, A. S.;Baikov, S. V.;Proskurina, I. K.;Shetnev, A. A.;Kotov, A. D. published 《Synthesis and Properties of C,N-Chelated Carbene Complexes of Palladium(II) with 2-Aminobenzo[d]thiazole Fragment》. The research results were published in《Russian Journal of General Chemistry》 in 2019.Name: 6-Nitrobenzo[d]thiazol-2-amine The article conveys some information:

The reaction of bis(cyclohexylisocyanide) complex of Pd(II) with substituted benzo[d]thiazole-2-amines in the presence of triethanolamine as the base has lead to the formation of deprotonated C,N-chelated carbene complexes with a structure similar to that described previously for the products of the reaction with unsubstituted benzo[d]thiazole-2-amine. The complexes have been isolated and characterized using high-resolution mass spectrometry, IR and NMR spectroscopy (¹H, ¹³C{¹H}, ¹H-¹H COSY, ¹H-¹H NOESY, ¹H-¹³C HSQC, ¹H-¹³C HMBC). The resulting complexes have exhibited moderate antibacterial activity against sensitive strains of gram-neg. bacteria E. coli (C600) and P. fluorescens (P218), gram-pos. bacteria S. aureus (ATCC-25923) and B. subtillis (B-3142D) as well as fungi C. albicans (401/NCTC-885-653).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 Name: 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

Shrivastava, Garima;Shrivastava, Manjul published 《Microwave assisted synthesis and characterization of Schiff base of 2-amino-6-nitrobenzothiazole》 in 2018. The article was appeared in 《International Research Journal of Pharmacy》. They have made some progress in their research.Category: thiazole The article mentions the following:

Synthesis of Schiff base I via microwave-induced condensation reaction of 2-amino-6-nitro benzothiazole and 3,5-diiodosalicylaldehyde was reported. The method used in the study was eco friendly and provided many benefits such as to straightforward work-up procedure, short reaction times, non-hazardous and good yield of product.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) 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