- Benzothiazole disperse dye monomer compound, synthesis method and application thereof
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The invention discloses a benzothiazole disperse dye monomer compound. The structure of the compound is shown as formula (I) in the specification, wherein X1 and X4 are hydrogen, halogen, nitro, methyl or methoxy independently; X2 and X3 are independently hydrogen, halogen, nitro, methyl, methoxy or cyano; X5 is hydrogen or C1-C4 alkoxy; X6 is hydrogen, C1-C4 alkyl, NHCOR1 or halogen, and R1 is C1-C4 alkyl. The invention also discloses a preparation method of the benzothiazole disperse dye monomer compound and application thereof in preparation of disperse dyes. According to the invention, a phenylthiourea compound is adopted as the starting raw material, and by means of condensation ring closure, diazotization and coupling, a disperse dye filter cake can be obtained. The obtained dispersedye has bright color, high coloring intensity, good dyeing reproducibility, and has excellent promotion performance, dye uptake, dyeing fastness, sunlight resistance and sublimation fastness.
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Paragraph 0076-0082
(2019/10/02)
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- AMINOISOXAZOLINE COMPOUNDS AS AGONISTS OF ALPHA7-NICOTINIC ACETYLCHOLINE RECEPTORS
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The present invention relates to novel aminoisoxazoline compounds, and pharmaceutical compositions of the same, that are suitable as agonists or partial agonists of α7-nAChR, and methods of preparing these compounds and compositions, and the use of these compounds and compositions in methods of maintaining, treating and/or improving cognitive function. In particular, methods of administering the compound or composition to a patient in need thereof, for example a patient with a cognitive deficiency and/or a desire to enhance cognitive function, that may derive a benefit therefrom.
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Paragraph 00319; 00320
(2017/05/19)
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- IMIDAZO[2,1-B]THIAZOLE AND 5,6-DIHYDROIMIDAZO[2,1-B]THIAZOLE DERIVATIVES USEFUL AS S100-INHIBITORS
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A compound of formula (I) or a pharmaceutically acceptable salt thereof. The compound is useful for use in the treatment of cancer, an inflammatory disorder,an autoimmunity disorder or a neurodegenerative disorder.
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Page/Page column 78; 79
(2016/04/09)
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- Synthesis, anti-inflammatory, analgesic, 5-lipoxygenase (5-LOX) inhibition activities, and molecular docking study of 7-substituted coumarin derivatives
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In the present study, 7-subsituted coumarin derivatives were synthesized using various aromatic and heterocyclic amines, and evaluated in vivo for anti-inflammatory and analgesic activity, and for ulcerogenic risk. The most active compounds were evaluated in vitro for 5-lipoxygenase (5-LOX) inhibition. Docking study was performed to predict the binding affinity, and orientation at the active site of the enzyme. In vivo anti-inflammatory and analgesic activity, and in vitro 5-LOX enzyme inhibition study revealed that compound 33 and 35 are the most potent compounds in all the screening methods. In vitro kinetic study of 35 showed mixed or non-competitive type of inhibition with 5-LOX enzyme. Presence of [Formula presented]3 group in 35 and [Formula presented] in 33 at C6-position of benzothiazole ring were found very important substitutions for potent activity.
- Srivastava, Pavan,Vyas, Vivek K.,Variya, Bhavesh,Patel, Palak,Qureshi, Gulamnizami,Ghate, Manjunath
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supporting information
p. 130 - 138
(2016/07/11)
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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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- 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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- 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)
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- Synthesis of some 5-nitro-2-furfurylidene derivatives and their antibacterial and antifungal activities
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A number of new 5-nitro-2-furfurylidene derivatives 9a-k were synthesized by the reaction of 2-methyl-4-(5-nitro-2-furfurylmethyliden)-Δ2-oxazolin-5-one 6 or 2-phenyl-4-(2-furfurylmethyliden)-Δ2-oxazolin-5-one 7 with appropriate 2-aminobenzothiazole. The compounds synthesized were identified by 1H-NMR, IR, MS and micro analysis. All compounds studied in this work were screened for their in vitro antimicrobial and antifungal activities against the standard strains: Bacillus subtilis, Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Salmonella typhimurium, and the yeast Candida albicans.
- Charris, Jaime,Monasterios, Melina,Dominguez, Josee,Infante, Wilson,Castro, Norma De
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p. 275 - 280
(2007/10/03)
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- Monoazo dyestuffs derived from benzothiazole
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A disperse dye of the formula, STR1 wherein R1 is an alkyl group having 5 to 6 carbon atoms, R2 is an alkyl group having 5 to 6 carbon atoms, a cyano-ethyl group, R3 is a hydrogen atom or a lower alkyl, amino or phenyl group, and Y1 and Y2 represent independently a hydrogen atom, a lower alkyl group, a lower alkoxy group, a halogen atom, a nitro group, a cyano group, a thiocyanate group or an alkylsulfonyl group, provided that both Y1 and Y2 are not hydrogen at the same time and Y1 is located at the 4- or 5-position, which is useful for dyeing hydrophobic fibers in brilliant red to violet shade with good fastnesses.
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