- Self-assembly of a benzothiazolone conjugate into panchromatic fluorescent fibres and their application in cellular imaging
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We report the synthesis and characterization of the structures formed by self-assembly of 4-chloro-2(3H)-benzothiazolone (CBT) into panchromatic fibres and their application in cellular imaging. The aggregation properties of the synthesized compound were studied extensively under different solvents and concentrations and their morphologies examined at a supramolecular level by various microscopic techniques such as atomic force microscopy (AFM), fluorescence microscopy, and optical microscopy. Interestingly, the self-assembled structures formed byCBTreveal panchromatic emission properties and show blue, green, and red fluorescence under different excitation wavelengths. The mechanism of structure formation of the self-assemblies was studied through different techniques such as concentration-dependent1H-NMR, ATR-FTIR, UV-visible spectroscopy, and fluorescence spectroscopy. Finally, the utility ofCBTfor cell imaging applications was demonstrated and it can be noted thatCBTwas efficiently taken up by mammalian cells and the cells revealed panchromatic emission in the blue, green, and red channels. The intensities of the fluorescence observed were blue > green > red and the dye interestingly does not exhibit any fluorescence quenching.
- Bhatia, Dhiraj,Gangrade, Ankit,Gour, Nidhi,Haque, Ashadul,Joshi, Khashti Ballabh,Koshti, Bharti,Kshtriya, Vivekshinh,Singh, Ramesh
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p. 17211 - 17221
(2021/10/04)
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- Iodine-catalyzed amination of benzothiazoles with KSeCN in water to access primary 2-aminobenzothiazoles
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A facile and sustainable approach for the amination of benzothiazoles with KSeCN using iodine as the catalyst in water has been disclosed under transition-metal free conditions. The reaction proceeded smoothly to afford various primary 2-amino benzothiazoles in up to 96% yield. A series of control experiments were performed, suggesting a ring-opening mechanism was involved via a radical process. This protocol provides efficient synthesis of primary 2-aminobenzothiazoles
- Chen, Xiran,Fu, Lianrong,Hao, Xin-Qi,Shi, Linlin,Song, Mao-Ping,Zhu, Xinju,Zhu, Yu-Shen
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supporting information
(2021/09/09)
-
- SN-Donor methylthioanilines and copper(II) complexes: Synthesis, spectral properties, and in vitro antimicrobial activity
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Methylthioanilines, a series of sulfur-nitrogen donor ligands substituted with OCH3, CH3, Cl, and Br, and their copper(II) complexes have been synthesized and characterized by 1H and 13C NMR, elemental analysis, FTIR, UV-Vis and EPR spectra, molar conductance, and magnetic susceptibility measurements. The NMR spectra of the ligands revealed that the para/ortho protons and para carbon were sensitive to the electronic effect of substituents. The CHNS analysis presented CuLCl2 (L = OCH3, CH3, Cl) and CuL2Cl2 (L = Br) stoichiometries for the copper complexes. FTIR spectra showed that the bidentate ligands were coordinated to the copper ion through their nitrogen and sulfur atoms. The electronic spectra have suggested square planar and octahedral geometries for these complexes. The EPR spectra demonstrated that the solid state copper(II) complexes possess dx2-y2 orbital ground state and g= > g > 2.0023 in a tetragonal environment. The compounds were evaluated for in vitro antimicrobial activity against S. aureus, B. subtilis, E. coli, and C. albicans. The copper complexes showed higher activity than the parent ligands against S. aureus and B. subtilis; the electron-donating OCH3 and CH3 derivatives were more active than the withdrawing Br- A nd Cl-substituted compounds.
- Olalekan, Temitope E.,Ogunlaja, Adeniyi S.,Watkins, Gareth M.
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-
- Discovery of 18β-glycyrrhetinic acid conjugated aminobenzothiazole derivatives as Hsp90-Cdc37 interaction disruptors that inhibit cell migration and reverse drug resistance
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A series of 18β-glycyrrhetinic acid (GA) conjugated aminobenzothiazole derivatives were designed, synthesized and evaluated for disruption activity of Hsp90-Cdc37 as well as the effects of in vitro cell migration. These compounds exhibited relatively good disruption activity against Hsp90-Cdc37 with IC50 values in low micromolar range. A docking study of the most active compound 11g revealed key interactions between 11g and Hsp90-Cdc37 complex in which the benzothiazole moiety and the amine chain group were important for improving activity. It is noteworthy that further antitumor activity screening revealed that some compounds exhibited better inhibitory activity than the commercial anticancer drug 5-FU and showed potent suppression activity against drug-resistant cancer cells. In particular, compound 11 g appeared to be the most potent compound against the A549 cell line, at least partly, by inhibition of the activity of Hsp90 and apoptosis induction. The treatment of A549 cells with compound 11g resulted in inhibition of in vitro cell migration through wound healing assay and S phase of cell cycle arrested. In addition, 11g-induced apoptosis was significantly facilitated in A549 cells. Thus, we conclude that GA aminobenzothiazole derivatives may be the potential Hsp90-Cdc37 disruptors with the ability to suppress cells migration and reversed drug-resistant.
- Jin, Le,Huang, Rizhen,Huang, Xiaochao,Zhang, Bin,Ji, Min,Wang, Hengshan
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p. 1759 - 1775
(2018/03/01)
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- Compounds for treating spinal muscular atrophy
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Provided herein are compounds, compositions thereof and uses therewith for treating spinal muscular atrophy. In a specific embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN2 into mRNA that is transcribed from the SMN2 gene. In another specific embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN1 into mRNA that is transcribed from the SMN1 gene. In yet another embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN1 and SMN2 into mRNA that is transcribed from the SMN1 and SMN2 genes, respectively.
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Page/Page column 321; 322
(2017/05/02)
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- NOVEL BENZOTHIAZOLE DERIVATIVES WITH ENHANCED BIOLOGICAL ACTIVITY
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The present invention discloses novel conjugates of benzothiazole derivatives with cystine and glucosamine and their method of synthesis. Their method of synthesis is easy and eco-friendly, avoiding the use of hazardous materials or reactions, The compounds offer technical advantages of increased solubility, potency, selectivity and biological activity. The novel compounds show antibacterial, antifungal and anticancer activities. Formula, physico-chemical data and biological activity of the novel derivatives are as given in Tables 1 to 9.
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Page/Page column 9; 12
(2017/03/08)
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- Efficient and facile protocol for one-pot synthesis of 2-amino-substituted benzothiazoles catalyzed by nano-BF3/SiO2 under mild conditions
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Abstract: A highly efficient and simple protocol for the preparation of 2-aminobenzothiazoles through the reaction of potassium thiocyanate and substituted anilines in the presence of nano-BF3/SiO2 as a reusable heterogeneous catalyst is described. In this method, all of the 2-amino-substituted benzothiazoles were obtained in high to excellent yields and short reaction times under mild conditions. The structures of the resulting products were characterized and confirmed by melting point, FT-IR, 1H NMR and 13C NMR techniques. Graphical Abstract: A highly efficient and simple protocol for the preparation of 2-aminobenzothiazoles by reaction of potassium thiocyanate and substituted anilines in the presence of nano-BF3/SiO2 as a reusable heterogeneous catalyst is described.[Figure not available: see fulltext.]
- Naeimi, Hossein,Heidarnezhad, Arash
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p. 7855 - 7868
(2016/11/25)
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- Novel Piperine Derivatives with Antidiabetic Effect as PPAR-γ Agonists
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Piperine is an alkaloid responsible for the pungency of black pepper. In this study, piperine isolated from Piper nigrum L. was hydrolyzed under basic condition to obtain piperic acid and was used as precursor to carry out the synthesis of twenty piperine derivatives containing benzothiazole moiety. All the benzothiazole derivatives were evaluated for their antidiabetic potential by OGT test followed by assessment of active derivatives on STZ-induced diabetic model. It was observed that nine of twenty novel piperine analogues (5b, 6a-h), showed significantly higher antidiabetic activity in comparison with rosiglitazone (standard). Furthermore, these active derivatives were evaluated for their action as PPAR-γ agonists demonstrating their mechanism of action. The effects on body weight, lipid peroxidation, and hepatotoxicity after administration with active derivatives were also studied to further establish these derivatives as lead molecules for treatment of diabetes with lesser side-effects.
- Kharbanda, Chetna,Alam, Mohammad Sarwar,Hamid, Hinna,Javed, Kalim,Bano, Sameena,Ali, Yakub,Dhulap, Abhijeet,Alam, Perwez,Pasha, M. A. Qadar
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p. 354 - 362
(2016/10/19)
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- COMPOUNDS FOR TREATING SPINAL MUSCULAR ATROPHY
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Provided herein are compounds, compositions thereof and uses therewith for treating spinal muscular atrophy. In a specific embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN2 into mRNA that is transcribed from the SMN2 gene. In another specific embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN1 into mRNA that is transcribed from the SMN1 gene. In yet another embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN1 and SMN2 into mRNA that is transcribed from the SMN1 and SMN2 genes, respectively.
- -
-
Paragraph 00586; 00587
(2013/07/19)
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- Synthesis, cytotoxic evaluation, and in silico studies of substituted N-alkylbromo-benzothiazoles
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In efforts to develop a new class of anticancer agents with improved efficacy and selective action, a series of N-alkylbromo-benzothiazoles were synthesized and evaluated for in vitro cytotoxic activity against various human cancer cell lines such as lung (A-549), prostate (PC-3), leukemia (THP-1), and colon (Caco-2). They were found to be highly active against prostate (PC-3) and leukemia (THP-1) cancer cells, moderately active against colon (Caco-2) cancer cells and less active against lung (A-549) cancer cells. Of the 12 compounds, two (11d, 11j) exhibit IC50 values of ≤ 1 μM against leukemia (THP-1) cancer cell lines. Compound 11l showed significant cytotoxic activity against the PC-3 (IC50 = 0.6 μM), THP-1 (IC50 = 3 μM) and Caco-2 cell lines (IC50 = 9.9 μM), respectively. Docking study of the synthesized ligand was done on epidermal growth factor receptor using ArgusLab flexible docking, to determine their observed activity. Further QSAR investigations with stepwise multiple linear regression analysis were applied to find correlation between various physicochemical parameters and anticancer activity. The QSAR results showed that anticancer activity could be modeled with descriptors. The predictive ability of models was cross-validated by observation of the low residual activity values and adjusted coefficient of variation (radj2) obtained by leave-one-out technique.
- Gill, Rupinder Kaur,Singh, Gagandeep,Sharma, Anuradha,Bedi,Saxena
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p. 4211 - 4222
(2013/09/02)
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- Design, synthesis and anticonvulsant evaluation of N-(benzo[d]thiazol-2- ylcarbamoyl)-2-methyl-4-oxoquinazoline-3(4H)-carbothioamide derivatives: A hybrid pharmacophore approach
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Novel N-(benzo[d]thiazol-2-ylcarbamoyl)-2-methyl-4-oxoquinazoline-3(4H)- carbothioamide derivatives were synthesized and evaluation of their anticonvulsant effects was done using various models of experimental epilepsy. Initial anticonvulsant activities of the compounds were investigated using intraperitoneal (i.p.) maximal electroshock shock (MES), subcutaneous pentylenetetrazole (scPTZ) seizure models in mice. The quantitative assessment after oral administration in rats showed that the most active was 2-methyl-4-oxo-N-(6-(trifluoromethoxy)benzo[d]thiazol-2-ylcarbamoyl) quinazoline-3(4H)-carbothioamide (SA 24) with ED50 values of 82.5 μmol/kg (MES) and 510.5 μmol/kg (scPTZ). This molecule was more potent than phenytoin and ethosuximide which were used as reference antiepileptic drugs. To explain the possible mechanism for anticonvulsant action, some of the selected active compounds were subjected to GABA (γ-amino butyric acid) assay and AMPA ((S)-2-amino-3-(3-hydroxyl-5-methyl-4-isoxazolyl) propionic acid) induced seizure test.
- Malik, Sachin,Bahare, Radhe Shyam,Khan, Suroor Ahmad
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supporting information
p. 1 - 13
(2013/10/01)
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- A novel system for the synthesis of 2-aminobenzthiazoles using sodium dichloroiodate
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2-Aminobenzthiazole is a privileged scaffold with a range of biological activities. However, to date, an efficient protocol for the synthesis of this ring system using aniline as a starting material has been lacking. Herein, for the first time, we describe a highly efficient and mild protocol for the synthesis of 2-aminiobenzthiazole using NaICl Georg Thieme Verlag Stuttgart ? New York.
- Telvekar, Vikas N.,Bachhav, Harshal M.,Bairwa, Vinod Kumar
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p. 2219 - 2222
(2012/10/30)
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- Antiviral Compounds
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Novel compounds, methods, and compositions for treating various viral infections are described. In some embodiments the novel compounds of the invention are 3-oxo-phenothiazine derivatives; more specific embodiments include 3-oxo-phenothiazine derivatives having substituents at the 1-, 7-, and 9-positions of the phenothiazine parent ring. In other embodiments, the invention provides compositions and methods for treating viral infections, especially HIV.
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- Synthesis and antimicrobial activity of new pyridine derivatives-I
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2-Amino substituted benzothiazoles 2a-l and 2-chloropyridine-3-carboxylic acid 3 were used to prepare 2-[N-(substitutedbenzothiazolyl)amino]pyridine-3- carboxylic acids (4a-l) in 2-ethoxy ethanol. Acid chlorides (5a-l) were condensed with 2-hydroxyethyl piperazine (6) and 2,3-dichloropiperazine (7) to prepare amide derivatives 2-[N-(substituted benzothiazolyl)amino]pyridin-3-yl (4-(2-hydroxyethyl)piperazin-1-yl)methanones (8a-l) and 2-[N-(substituted benzothiazolyl) amino]pyridin-3-yl(2,3- dichloropiperazine-1-yl)methanones (9a-l), respectively. The structures of new compounds have been established on the basis of elemental analysis and spectral (IR, 1H NMR, and Mass spectra) studies. The in vitro antimicrobial activity was screened for all the synthesized compounds. Variable and modest activity were observed against the investigated strains of bacteria and fungi. Springer Science+Business Media, LLC 2010.
- Patel, Navin B.,Agravat, Suresh N.,Shaikh, Faiyazalam M.
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experimental part
p. 1033 - 1041
(2012/05/04)
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- Synthesis of 1,2,4-triazole derivatives containing benzothiazoles as pharmacologically active molecule
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In attempt to make significant pharmacologically active molecule, we report here the synthesis and in vitro antimicrobial and antitubercular activity of various series of 3-(3-pyridyl)-5-(4-nitrophenyl)-4-(N-substituted-1,3- benzothiazol-2-amino)-4H-1,2,4-triazole. The antimicrobial activity of title compounds were examined against two Gram-positive bacteria (Staphylococcus aureus, Streptococcus pyogenes), two Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa), and three fungi (Candida albicans, Aspergillus niger, Aspergillus clavatus) using the broth microdilution method and antitubercular activity H37Rv using Lowenstein-Jensen agar method.
- Patel, Navin B.,Khan, Imran H.
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scheme or table
p. 527 - 534
(2012/05/20)
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- Synthesis and pharmacological screening of novel (2-(4-Methyl-2-oxo-2H- chromen-7-yloxy)-N-(benzo[d]thiazol-2-yl))acetamide derivatives
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A new series of 2-(4-methyl-2-oxo-2H-chromen-7-yloxy)-N-(benzo[d]thiazol-2- yl)acetamide derivatives (4a-k) was synthesized and evaluated for their D 2 and 5HT2 antagonistic activity as a measure of atypical antipsychotic property. Compounds (4a-k) were synthesized by refluxing various N-(benzothiazol-2-yl)-2-chloroacetamides substituted derivatives (3a-k) with 7-hydroxy-4 methyl-2H-chromen-2-one (1) in acetonitrile and anhydrous K 2CO3. N-(Benzothiazol-2-yl)-2-chloroacetamides substituted derivatives (3a-k) were prepared from the chloroacetyl chloride with various 2-amino benzothiazole substituted derivatives (2a-k). The synthesized compounds were characterized with the help of spectral and analytical data. Most of these compounds showed dopamine D2 receptor antagonistic activity from moderate to high affinity along with serotonin 5-HT2 receptor blockage activity: a property that has been suggested as necessary for atypicality. The D 2 and 5-HT2 receptor blockage activity was evaluated by inhibition of apomorphine-induced climbing behaviour and 5HTP induced head twitches in mice, respectively.
- Gawai, Ashish,Das, Sanjib,Nemade, Mahesh,Wathore, Sandeep
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experimental part
p. 3969 - 3974
(2012/01/13)
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- Microwave-assisted synthesis of benzothiazoleurea derivatives
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A simple and efficient method has been developed for the synthesis of 1-substituted-3-(4-chlorobenzo[d]thiazol-2-yl) ureas (5), from substituted aromatic or aliphatic amino compounds and phenyl 4-chlorobenzo[d]thiazol-2-yl carbamate 4 using microwave irradiation without phosgene in good yields. The title products were characterised by 1H NMR, ESI-MS, and elemental analysis.
- Chen, Wenbin,Li, Kejian,Wang, Yong,Xi, Zhen
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experimental part
p. 75 - 79
(2010/06/16)
-
- Pharmacological evaluation and characterizations of newly synthesized 1,2,4-triazoles
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The triazole analogs were obtained via. multistep synthesis sequence beginning with ethyl nicotinoate 3 which on treatment with hydrazine hydrate yields nicotinoyl hydrazide 4. Intermolecular cyclisation of 4 with 4-methylbenzoic acid in presence of phosphorous oxy chloride affords 2-(3-pyridyl)-5-(4-methylphenyl)-1,3,4-oxadiazole 5. Condensation of 5 with various substituted 2-hydrazino benzothiazole 2a-j results in 3-(3-pyridyl)-5-(4-methylphenyl)-4-(N-substituted-1,3-benzothiazol-2-amino) -4H-1,2,4-triazole 6a-j analogs. All the compounds have been characterized by elemental analysis, IR, 1H NMR, 13C NMR and mass spectral data. In vitro antitubercular activity was carried out against Mycobacterium tuberculosis H37Rv strain using Lowenstein-Jensen medium and antimicrobial activity against various bacteria and fungi using broth microdilution method. Compounds 2e, 6a, 6b, 6c, 6d, 6g, 6h and 6i emerged as promising antimicrobials. It was also observed that the promising antimicrobials have proved to be better antituberculars. Compound 6j showed better antitubercular activity compared to rifampicin. 3-(3-Pyridyl)-5-(4-methylphenyl) -4-(N-substituted-1,3-benzothiazol-2-amino)-4H-1,2,4-triazole 6a-j were synthesized and their antitubercular activity against H37Rv and antimicrobial activities have been tested.
- Patel, Navin B.,Khan, Imran H.,Rajani, Smita D.
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scheme or table
p. 4293 - 4299
(2010/10/02)
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- Antimycobacterial and antimicrobial study of new 1,2,4-triazoles with benzothiazoles
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In this study, we report the antimycobacterial and antimicrobial evaluation of newly synthesized 3-(3-pyridyl)-5-(4-methoxyphenyl)-4-(N-substituted-1,3- benzothiazol-2-amino)-4H-1,2,4-triazole 6a-j in good yields. All the synthesized compounds have been established by elemental analysis, IR, 1H NMR, 13C-NMR and Mass spectral data. In-vitro antimycobacterial activity was carried out against (Mycobacterium tuberculosis) H37Rv strain using Lowenstein-Jensen medium and antimicrobial activity against two Gram positive bacteria (Staphylococcus aureus, Streptococcus pyogenes), two Gram negative bacteria (Escherichia coli, Pseudomonas aeruginosa) and three fungal species (Candida albicans, Aspergillus niger, Aspergillus clavatus) using the broth microdilution method. Compounds 2e, 6a, 6g, 6h, and 6j exhibited promising antimicrobial activity whereas compound 6j showed very good antimycobacterial activity. The antimycobacterial and antimicrobial evaluation of newly synthesized 3-(3-pyridyl)-5-(4-methoxyphenyl)-4-(N-substituted-1,3-benzothiazol- 2-amino)-4H-1,2,4-triazoles is reported in detail. Compounds 2e, 6a, 6g, 6h, and 6j exhibited promising antimicrobial activity whereas compound 6j showed very good antimycobacterial activity. Copyright
- Patel, Navin B.,Khan, Imran H.,Rajani, Smita D.
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scheme or table
p. 692 - 699
(2011/09/15)
-
- Synthesis and antimicrobial studies of new pyridine derivatives
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2-(p-Acetylaminobenzenesulfonylamido)-substituted benzothiazoles were prepared from 2-amino-substituted benzothiazoles and p-acetamidobenzenesulfonyl chloride using a mixture of pyridine and Ac2O, which formed an electrophilic N-acetyl- pyridinium complex facilitating condensation to give the desired products by removal of HCl. 2-[4-(Substituted benzothiazol-2-yl) aminosulfonylanilino]pyridine-3-carboxylic acids (synthesized from 2-chloropyridine-3-carboxylic acid and the corresponding substituted 2-(p-aminobenzenesulfonylamido)benzothiazole in 2-ethoxyethanol using Cu-powder and K2CO3) were then converted to acid chlorides, which on further reaction with piperazine and 4-methoxyphenylpiperazine yielded the corresponding 2-[4-(substituted benzothiazol-2-yl)amino-sulfonyl]anilino-3- (piperazinocarbonyl) pyridine and 2-[4-(substituted benzothiazol-2-yl)amino- sulfonyl]anilino-3-[(4-methoxyphenyl)piperazin-1-yl-carbonyl]pyridine. The structures of the new compounds have been established on the basis of their elemental analyses as well as IR, 1H NMR, and mass-spectral data. All the compounds have been screened for antimicrobial activity and found to possess considerable antibacterial activity.
- Patel,Agravat
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experimental part
p. 1343 - 1353
(2010/05/02)
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- ANTIBACTERIAL AGENTS
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Compounds of formula (I) have antibacterial activity wherein R represents hydrogen or 1, 2 or 3 optional substituents; W is =C(R1)- or =N-; R1 is hydrogen or an optional substituent and R2 is hydrogen, methyl, or fluorine; or R1 and R2 taken together are -CH2-, -CH2CH2-, -O-, or, in either orientation, -O- CH2- Or -OCH2CH2-; R3 is a radical of formula -(Alk1)m-(Z)p-(Alk2)n-Q wherein m, p and n are independently 0 or 1, provided that at least one of m, p and n is 1, Z is -O-, -S-, -S(O)-, -S(O2)-, -NH-, -N(CH3)-, -N(CH2CH3)-, -C(=O)-, -O-(C=O)-, -C(=O)-O-, or an optionally substituted divalent monocyclic carbocyclic or heterocyclic radical having 3 to 6 ring atoms; or an optionally substituted divalent bicyclic heterocyclic radical having 5 to 10 ring atoms; Alk1 and Alk2 are optionally substituted C1C6 alkylene, C2-C6 alkenylene, or C2-C6 alkynylene radicals, which may optionally terminate with or be interrupted by -O-, -S-, -S(O)-, -S(O2)-, -NH-, -N(CH3)-, or -N(CH2CH3)-; and Q is hydrogen, halogen, nitrile, or hydroxyl or an optionally substituted monocyclic carbocyclic or heterocyclic radical having 3 to 6 ring atoms; or an optionally substituted bicyclic heterocyclic radical having 5 to 10 ring atoms.
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Page/Page column 93-94
(2010/11/28)
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- Thiazole, imidazole and oxazole compounds and treatments of disorders associated with protein aging
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Provided are, among other things, compounds of formula I or IA, . Also provided are methods of treatment with such compounds.
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-
- Method for treating glaucoma IIB
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Provided is a method of decreasing intraocular pressure or improving ocular accommodation in an animal, including a human, comprising administering an intraocular pressure decreasing amount or ocular accommodation improving amount of a compound of the formula I or IA, wherein J is oxygen, sulfur, or N—Rd.
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- Substituted 2-aminobenzothiazoles and derivatives useful as cerebrovascular agents
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A series of substituted 2-aminobenzothiazoles and derivatives useful for treating cerebrovascular disorders are disclosed. Also disclosed is a new method for treating such disorders.
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-
- Electrochemical Behaviour of some Benzothiazolyl-hydrazonobarbituric Acids and Effect of Substituents on Redox-Mechanism
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Polarographic and cyclic voltammetric behaviour of twelve titled compounds have been studied in the pH range 2.0-11.2 at dropping mercury electrode, pyrolytic graphite electrode and platinum electrode.The effect of substituents, covering wide range of Hammett substituents constant values, has been evaluated quantitatively.
- Goyal, R. N.
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p. 281 - 284
(2007/10/02)
-
- A CONVENIENT AND SINGLE STEP SYNTHESIS OF SUBSTITUTED 4H-BENZOTHIAZINES.
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A simple one step synthesis is reported for substituted 4H-benzothiazines involving the condensation of 5-(chloro, bromo, methyl, methoxy, ethoxy)-, 4-methyl- and 3-(chloro and methoxy)-2-aminobenzenethiols with acetylacetone/ethyl acetoacetate/dibenzoylmethane in DMSO.
- Gupta, R. R.,Ojha, K. G.,Kalwania, G. S.,Kumar, M.
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p. 1145 - 1149
(2007/10/02)
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- ETUDE DE LA FRAGMENTATION PAR IMPACT ELECTRONIQUE DE DERIVES DU BENZOTHIAZOLE
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The mass spectra of eighteen substituted benzothiazoles are reported and discussed.All these compounds are thermodynamically stable and give an intense molecular ion, which undergoes different types of fragmentation depending on the nature of the substituent which is rarely eliminated directly. β-Cleavage with respect to the heterocyclic double bond is often obseved.Specific 2H-, 13C-, 15N- and 34S-labelling have been used in order to confirm the fragmentation patterns.
- Claude, Saturnin,Tabacchi, Raffaele,Duc, Laurent,Fuchs, Rudolf,Boosen, Karl-Josef
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p. 682 - 692
(2007/10/02)
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- Process for the production of 2-amino-benzothiazoles
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A process for the production of a 2-amino-benzothiazole having the formula: STR1 wherein R1, R2, R3 and R4 are the same or different and are hydrogen, halogen, alkyl or alkoxy. A phenylthiourea having the formula: STR2 wherein R1, R2, R3 and R4 are defined as above, is added to a cyclization agent in the absence of a solvent and allowing the phenylthiourea to cyclize to form 2-amino-benzothiazole in salt form. Filtering the salt of the 2-amino-benzothiazole out of the reaction mixture.
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