446065-20-9Relevant articles and documents
Based on isoxazole substitution of benzamide derivatives and anti-prostate cancer drug applications
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Paragraph 0065; 0073-0074, (2022/01/10)
The present invention discloses a class (I), formula (II) structure based on isoxazole substituted benzamide derivatives and antiprostate cancer drug applications, such isoxazole substituted benzamide derivatives, can effectively inhibit the activity of a
SUBSTITUTED AMINOTHIAZOLES AS INHIBITORS OF NUCLEASES
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Page/Page column 14-15; 40; 63, (2019/11/12)
The invention provides compounds represented by the structural formula (1): wherein R1, R2, R3, R4, R5, R6 are as defined in the claims. The compounds are inhibitors of nucleases, and are useful in particular in a method of treatment and/or prevention of proliferative diseases, neurodegenerative diseases, and other genomic instability associated diseases.
Method of synthesizing 2-aminothiazole ring compound from ethylbenzene compound
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Paragraph 0036; 0037; 0038, (2018/12/13)
The invention discloses a method of synthesizing 2-aminothiazole ring compound from ethylbenzene compound, and belongs to the technical field of thiazole ring derivative synthesis. The technical scheme of the invention is characterized by adding the ethylbenzene compound, a phase transfer catalyst, N-bromosuccinimide (NBS) and azodiisobutyronitrile (AIBN) into water in sequence, reacting at 60 DEGC, cooling after the reaction, adding inorganic base and a thiourea compound, and reacting at 80 DEG C to obtain the target product. The synthesis method has the advantages of high yield, mild reaction, low cost and environment friendliness.
Method for synthesizing novel 2-aminothiazole ring derivatives
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Paragraph 0042; 0043; 0044, (2018/11/27)
The invention discloses a method for synthesizing 2-aminothiazole ring derivatives and belongs to the technical field of organic synthesis. The method comprises that an ethylbenzene compound, dibromohydantoin DBH and t-butyl hydroperoxide TBHP are sequentially added to water, the solution undergoes a reaction at 60 DEG C, the reaction product is cooled, an inorganic base and a thiourea compound are orderly added into the reaction product and the mixture undergoes a reaction at 80 DEG C to produce desired product 2-aminothiazole ring derivatives. The method has the advantages of high yield, mild reaction, low cost and environmental friendliness.
Synthesis of 2-aminothiazoles from styrene derivatives mediated by 1,3-dibromo-5,5-dimethylhydrantoin (DBH)
Ma, Chunhua,Miao, Yuqi,Zhao, Minghao,Wu, Ping,Zhou, Jianglu,Li, Zhi,Xie, Xilei,Zhang, Wei
, p. 3602 - 3607 (2018/05/26)
An efficient procedure for the synthesis of 2-aminothiazoles via DBH-mediated oxidative cyclization of styrenes and thioureas is reported. Various alkenes were successfully transformed to the corresponding 2-aminothiazoles in yields of 10–81% via a two-step one-pot manner using DBH as both the bromine source and oxidant. The method can be readily carried out in gram-scale and successfully applied to the synthesis of anti-inflammatory drug fanetizole using styrene as starting material.
Method for synthesizing 1,3-substituted thiazole ring compound by styrene compound
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Paragraph 0038; 0039; 0040; 0041, (2018/01/12)
The invention discloses a method for synthesizing a 1,3-substituted thiazole ring compound by a styrene compound, and belongs to the technical field of synthesis of thiazole ring compounds. The method is characterized by comprising the following steps: dissolving the styrene compound and a phase transfer catalyst into water, adding dibromohydantoin DBH, carrying out a reaction at 60 DEG C, spin-drying after the reaction and dissolving into an organic solvent, adding a thiourea compound and performing reflux reaction to prepare a target product 1,3-substituted thiazole ring compound. The synthesis method provided by the invention is high in yield, mild in reaction, low in cost and environmentally friendly.
Identification of novel 2-aminothiazole conjugated nitrofuran as antitubercular and antibacterial agents
Ran, Kai,Gao, Chao,Deng, Hongxia,Lei, Qian,You, Xinyu,Wang, Ningyu,Shi, Yaojie,Liu, Zhihao,Wei, Wei,Peng, Cuiting,Xiong, Lu,Xiao, Kunjie,Yu, Luoting
, p. 3669 - 3674 (2016/07/21)
The emergence of antibiotic resistant pathogens is an ongoing main problem in the therapy of bacterial infections. In order to develop promising antitubercular and antibacterial lead compounds, we designed and synthesized a new series of derivatives of 2-aminothiazole conjugated nitrofuran with activities against both Mycobacterium tuberculosis and Staphylococcus aureus. Eight compounds 12e, 12k, 12l, 12m, 18a, 18d, 18e, and 18j emerged as promising antitubercular agents. Structure–activity relationships (SARs) were discussed and showed that the derivatives substituted at the position-3 of benzene of 5-nitro-N-(4-phenylthiazol-2-yl)furan-2-carboxamide exhibited superior potency. The most potent compound 18e, substituted with benzamide at this position, displayed minimum inhibitory concentrations (MICs) of 0.27 μg/mL against Mtb H37Ra and 1.36 μg/mL against S. aureus. Furthermore, compound 18e had no obvious cytotoxicity to normal Vero cells (IC50= 50.2 μM). The results suggest that the novel scaffolds of aminothiazole conjugated nitrofuran would be a promising class of potent antitubercular and antimicrobial agents.
Synthesis and biological evaluation of N-(4-phenylthiazol-2-yl)cinnamamide derivatives as novel potential anti-tumor agents
Luo, Yong,Zhu, Yongxia,Ran, Kai,Liu, Zhihao,Wang, Ningyu,Feng, Qiang,Zeng, Jun,Zhang, Lidan,He, Bing,Ye, Tinghong,Zhu, Shirui,Qiu, Xiaolong,Yu, Luoting
, p. 1036 - 1042 (2015/06/25)
In this study, a series of novel N-(4-phenylthiazol-2-yl)cinnamamide derivatives (7a-8n) were synthesized and evaluated for their anti-proliferative activities in vitro by MTT assay and a possible antitumor mechanism was also explored. SAR analysis showed that steric effects played an important role on the anti-tumor activity. The most potent analogue 8f showed excellent inhibitions on the K562, Bel7402, A549 and Jurkat cells ranging from sub-micromolar to nanomolar concentration. Compound 8f inhibited Jurkat cells with an IC50 value of 0.035 μM with no apparent toxicity in different non-cancerous cells. Furthermore, it was suggested that the possible mechanism of 8f might be associated with inducing cancer cell apoptosis following flow cytometer analysis and Hoechst 33358 staining assays.
Synthesis, characterization and antimicrobial studies of a few novel thiazole derivatives
Praveen, Aletti S.,Yathirajan, Hemmige S.,Narayana, Badiadka,Sarojini, Balladka K.
, p. 259 - 268 (2014/03/21)
A series of novel N-[4-(substituted)-1,3-thiazol-2-yl]-2-(substituted) acetamide (9a-m) and methyl 2-(2-(2-(substituted)acetamido)thiazol-4-yl)acetate (9n-o) derivatives have been synthesized and compounds were characterised by spectral and analytical studies. All compounds were screened for their in vitro antibacterial activity against Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa and Klebsiella pneumonia by disc diffusion method and for antifungal activity against Penicillium marneffei, Trichophyton mentagrophytes, Aspergillus flavus and Aspergillus fumigatus by serial plate dilution method. Compounds 9b, 9e, 9m and 9o exhibited growth inhibition against all the tested bacterial strains, with MIC values varying from 12.5 to 6.25 μg/ml. Among the compounds tested for antifungal activity, 9a, 9b, 9d, 9j, 9k, 9p and 9n showed wide range of activity against all the tested strains. Most of the newly synthesized compounds were effective against fungal strains rather than bacterial strains. However, some of the compounds like 9a, 9e, 9j, 9k and 9i showed selective sensitivity against some of the bacterial strains whereas they were unable to sustain the growth of other strains.
A tandem one-pot aqueous phase synthesis of thiazoles/selenazoles
Madhav,Narayana Murthy,Anil Kumar,Ramesh,Nageswar
, p. 3835 - 3838 (2012/08/14)
The first ever tandem one-pot synthetic protocol for the synthesis of thiazoles/selenazoles from alkynes via the formation of 2,2-dibromo-1- phenylethanone is reported. The reaction is catalyzed by β-cyclodextrin in aqueous medium and resulted in good yields.