Tag: 100-200

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

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

Synthetic Route of C7H5N3O2S《Cyclic (Alkyl)(amino)carbene Ligand-Promoted Nitro Deoxygenative Hydroboration with Chromium Catalysis: Scope, Mechanism, and Applications》 was published in 2021. The authors were Zhao, Lixing;Hu, Chenyang;Cong, Xuefeng;Deng, Gongda;Liu, Liu Leo;Luo, Meiming;Zeng, Xiaoming, and the article was included in《Journal of the American Chemical Society》. The author mentioned the following in the article:

Transition metal catalysis that utilizes N-heterocyclic carbenes as noninnocent ligands in promoting transformations has not been well studied. We report here a cyclic (alkyl)(amino)carbene (CAAC) ligand-promoted nitro deoxygenative hydroboration with cost-effective chromium catalysis. Using 1 mol % of CAAC-Cr precatalyst, the addition of HBpin to nitro scaffolds leads to deoxygenation, allowing for the retention of various reducible functionalities and the compatibility of sensitive groups toward hydroboration, thereby providing a mild, chemoselective, and facile strategy to form anilines, as well as heteroaryl and aliphatic amine derivatives, with broad scope and particularly high turnover numbers (up to 1.8 x 10⁶). Mechanistic studies, based on theor. calculations, indicate that the CAAC ligand plays an important role in promoting polarity reversal of hydride of HBpin; it serves as an H-shuttle to facilitate deoxygenative hydroboration. The preparation of several com. available pharmaceuticals by means of this strategy highlights its potential application in medicinal chem. 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) 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

SDS of cas: 6285-57-0《Development of β-carboline-benzothiazole hybrids via carboxamide formation as cytotoxic agents: DNA intercalative topoisomerase IIα inhibition and apoptosis induction》 was published in 2021. The authors were Tokala, Ramya;Mahajan, Surbhi;Kiranmai, Gaddam;Sigalapalli, Dilep Kumar;Sana, Sravani;John, Stephy Elza;Nagesh, Narayana;Shankaraiah, Nagula, and the article was included in《Bioorganic Chemistry》. The author mentioned the following in the article:

In quest of promising anticancer agents, the pharmacophores of natural (β-carboline) and synthetic origin (benzothiazole) were adjoined by a carboxamide bridge and three-point diversification was accomplished. The in vitro cytotoxic ability of the compounds was established on adherent and suspension human cancer cell lines and compounds I and II advanced as pre-eminent mols. with IC₅₀ values of 1.46 and 1.81μM resp. in A549 cell line. The cytospecificity was entrenched for potent compounds I and II by evaluating against normal human lung epithelial cells and selectivity index was calculated Furthermore, EtBr displacement, relative viscosity and gel-based topoisomerase II target assays unveiled the intercalative topo-II inhibitory capability and DNA binding studies (absorbance) revealed the dissociation constant (K_d) for compounds I and II as 98 and 103μM resp. Addnl., cell-based flow cytometric assays like Annexin-V/PI dual staining aids in the quantification of apoptosis induced and JC-1 staining disclosed the depolarization of mitochondrial membrane potential by compound I in A549 cells in a dose-dependent manner. Moreover, wound healing assay established the inhibition of in vitro cell migration by compound I on A549 cells. In addition, mol. docking studies proved the binding of compounds I and II in the active site of DNA complexed with topo IIα and stabilized by interactions with DNA base pairs and amino acid residues. Remarkably, the compounds I and II follow Lipinski’s rule of five and are in the recommended range for Jorgensen’s rule of three with a minimal violation and other pharmacokinetic parameters revealing druggability of the synthesized hybrids. 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

Name: 6-Nitrobenzo[d]thiazol-2-amine《Lemon juice mediated multicomponent reactions for the synthesis of fused imidazoles》 was published in 2018. The authors were Saha, Argha;Jana, Asim;Choudhury, Lokman H., and the article was included in《New Journal of Chemistry》. The author mentioned the following in the article:

A one-pot three component reaction mediated by lemon juice in an aqueous medium for the synthesis of diverse pharmaceutically important tricyclic fused imidazoles tethered with aryl and various cyclic 1,3-dicarbonyls was reported. The reaction of arylglyoxals with cyclic 1,3-diacarbonyls such as N-methyl-4-hydroxyquinolone, 2,4-dihydroxyquinoline, 4-hydroxycoumarin or 4-hydroxy-6-methyl-2-pyrone with various 1,3-N,N-binucleophiles such as 2-aminobenzothiazoles or 2-aminobenzimidazoles provided medicinally important diverse tricyclic fused imidazoles having aryl and cyclic 1,3-dicarbonyl substituents under metal-free conditions. This method is a natural acid catalyzed multicomponent reaction in an aqueous medium for the synthesis of diverse tricyclic fused imidazoles in good to excellent yields.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

Upadhyay, Neha;Tilekar, Kalpana;Safuan, Sabreena;Kumar, Alan P.;Schweipert, Markus;Meyer-Almes, Franz-Josef;Ramaa, Cs published 《Development and investigation of thiazolidinedione and pyrazoline compounds as antiangiogenic weapons targeting VEGFR-2》 in 2021. The article was appeared in 《Future Medicinal Chemistry》. They have made some progress in their research.Category: thiazole The article mentions the following:

Angiogenesis deregulation is often linked to cancer and is thus an essential target. Twenty-nine compounds were developed as VEGFR-2 inhibitors. Compounds were evaluated to determine their antiangiogenic activity. B1, PB11 and PB16 showed HUVEC′s IC₅₀ scores in the submicromolar range. B1, B2 and PB16 reduced cellular migration and capillary tube formation of HUVECs. VEGFR-2 inhibitory activity was found in the nanomolar range: 200 nM of B1, 500 nM of B2 and 600 nM of PB16. B1 and PB16 suppressed the formation of new capillaries on growing CAMs. B1 and PB16 occupied the ATP site and allosteric pocket of VEGFR-2 in docking studies. These compounds can target VEGFR-2 and are endowed with in vitro and in vivo antiangiogenic activity. 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) 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

Kallur, H. J.;Mathapati, Prabhudev S.;C., Kishore Singh;Malpani, Ashok published 《Synthesis, characterization and anthelmintic screening of some new benzothiophene derivatives》 in 2020. The article was appeared in 《World Journal of Pharmaceutical Research》. They have made some progress in their research.Recommanded Product: 6285-57-0 The article mentions the following:

The proposed work was carried out by following Schemes. In the Scheme-I the starting material cinnamic acid was reacted with thionyl chloride, in presence of pyridine in chlorobenzene medium to yield 3- chlorobenzo[b]thiophene-2-carbonylchloride. Where as in the Scheme-II the 2-amino-6-substituted benzothiazoles I (R = Me, COOEt, Cl, OMe, F, nitro) was prepared by the reaction of 4-substituted anilines 4-RC₆H₄NH₂ and potassium thiocyanate in presence of bromine in acetic acid. In the scheme-III, the compound N-(6-substituted-1,3-benzothiazol-2-yl)-3-chloro-1-benzothiophene-2-carboxamides II was prepared by reacting 3-chlorobenzo[b]thiophene-2-carbonylchloride and 2-amino-6-substituted benzothiazoles I in pyridine medium refluxed for 10-15 h. The synthesized compounds II were evaluated for the anthelmintic activity. 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 Recommanded Product: 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

Quality Control of 6-Nitrobenzo[d]thiazol-2-amineIn 2020, Pugh, Kyler W.;Zhang, Zheng;Wang, Jian;Xu, Xiuzhi;Munthali, Vitumbiko;Zuo, Ang;Blagg, Brian S. J. published 《From Bacteria to Cancer: A Benzothiazole-Based DNA Gyrase B Inhibitor Redesigned for Hsp90 C-Terminal Inhibition》. 《ACS Medicinal Chemistry Letters》published the findings. The article contains the following contents:

Heat shock protein 90 (Hsp90) is a mol. chaperone that is responsible for the folding and maturation of client proteins that are associated with all ten hallmarks of cancer. Hsp90 N-terminal pan inhibitors have experienced unfavorable results in clin. trials due to induction of the heat shock response (HSR), among other concerns. Novobiocin, a well characterized DNA gyrase B inhibitor, was identified as the first Hsp90 C-terminal inhibitor that manifested anticancer effects without induction of the HSR. In this letter, a library of Hsp90 C-terminal inhibitors derived from a benzothiazole-based scaffold, known to inhibit DNA gyrase B, was designed, synthesized, and evaluated. Several compounds were found to manifest low micromolar activity against both MCF-7 and SKBr3 breast cancer cell lines via Hsp90 C-terminal inhibition.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 Quality Control 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

Kachare, Snehal D.;Baheti, Kamalkishor G.;Yasar, Qazi;Jangam, Sampada S. published 《Design, synthesis and evaluation of benzothiazole urea derivatives as an anticonvulsant agent》 in 2021. The article was appeared in 《Pharma Chemica》. They have made some progress in their research.Application In Synthesis of 6-Nitrobenzo[d]thiazol-2-amine The article mentions the following:

A series of 1-((-6-substituted-2-yl)-3-(4H-1,2,4 triazole-3-yl))ureas I (R = H, OMe, Cl, NO₂, etc.) and (1-((3-(6-substituted-2-yl)ureido)methyl)cyclohexyl)acetic acids II were designed, synthesized using appropriate synthetic route and screened for CNS depressant and anticonvulsant activities. The synthesized compounds I and II were also analyzed for ADME properties. The results of In-Silico ADME Screening showed that compounds I and II could be exploited as an oral drug candidate. Mol. docking studies were performed for all the synthesized compounds I and II against γ-amino butyric acid amino transferase enzyme (1OHV), and all the compounds I and II exhibited docking score in the range of -7.5 to -8.4, among which compound II (R = Cl) had shown the highest docking scores as compared to the standard drug phenytoin. Animal study for anticonvulsant indicated that compounds I (R = NO₂, H) and II (R = Cl) were exhibited significant activity at a dose 200 mg/kg. All these compounds I and II were also evaluated for CNS depressant activity using actophotometer. The results of CNS depressant and anticonvulsant activities and docking study showed that synthesized compounds I and II had potential CNS depressant and anticonvulsant activities and can be further optimized and developed as a lead compound 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 Application In Synthesis 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

Formula: C7H5N3O2SIn 2021, Mikherdov, Alexander S.;Popov, Roman A.;Kinzhalov, Mikhail A.;Haukka, Matti;Polukeev, Valeriy A.;Boyarskiy, Vadim P.;Roodt, Andreas published 《Reaction mechanism of regioisomerization in binuclear (diaminocarbene)Pd^II complexes》. 《Inorganica Chimica Acta》published the findings. The article contains the following contents:

A series of binuclear Pd^II carbene complexes were synthesized via the treatment of cis-[PdCl₂(CNXyl)₂] (1) with benzo-1,3-thiazol-2-amines (2–6) and structurally characterized. In every case the reaction leads to the mixture of two regioisomers, which are able to interconvert. The study of the regioisomerization of the binuclear diaminocarbene species showed that it is a first-order reaction, i.e., it occurs intramolecularly, and was analyzed with the Hammett function. Electron-withdrawing substituents in the benzothiazole moiety of the complexes as well as increasing the solvent polarity accelerate the reaction. The solvent donor strength correlates less well with the isomerization rates. Based on the obtained activation parameters the studied regioisomerization could be defined as the interchange/dissociative process type. A combined approach including kinetic and mass spectrometric studies allowed the conclusion that the rate-determining step of the isomerization is breaking the carbon-nitrogen bond in the carbene fragment of the binuclear complex. 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 Formula: C7H5N3O2S) 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