New approach to 5-arylamino-4-(5-aryloxyfuran-2-yl)pyrimidines: synthesis and antibacterial activity

2021 ◽  
Vol 70 (5) ◽  
pp. 937-942
Author(s):  
E. V. Verbitskiy ◽  
S. A. Baskakova ◽  
G. L. Rusinov ◽  
V. N. Charushin
Author(s):  
Messai Amel

The objective of this work is the synthesis of new quinoline molecules which could have some biological activities. This chapter reported a new approach to the synthesis of some quinoline derivatives. The Baylis-Hillman reaction on 2-methoxy-3-formyl quinoléines derivatives have applied in order to obtain Baylis-Hillman adducts. The products are characterized by FTIR, NMR and X-ray single crystal diffraction .Also, a study of the antibacterial activity of the 3-(2-chloro quinoline)-3-hydroxy-2 methylene propanonitrile products synthesized have been explored. This assessment is made by using the disk diffusion method. The results showed that the 3-(2'-chloroquinoline)-3-hydroxy-2-methylenepropanonitril derivatives present a good antibacterial effectiveness against the strains tested Gram-positive and no antibacterial potency was observed against the stains Gram-negative used in the test.


2012 ◽  
Vol 23 (3) ◽  
pp. 265-275 ◽  
Author(s):  
Renata Los ◽  
Marta Wesołowska-Trojanowska ◽  
Anna Malm ◽  
Monika M. Karpińska ◽  
Joanna Matysiak ◽  
...  

Nanomaterials ◽  
2019 ◽  
Vol 9 (11) ◽  
pp. 1579 ◽  
Author(s):  
Yanmei Zhang ◽  
Xin Zhang ◽  
Jie Song ◽  
Liming Jin ◽  
Xiaotong Wang ◽  
...  

Development of antimicrobial nanomaterials is one of the most attractive strategies for eliminating the major threat of pathogenic bacteria to public health. In this work, we developed a simple impregnation-reduction method for the synthesis of Ag-doped hierarchical ZIF-8 (Ag/H-ZIF-8) nanocomposite. The nanocomposite was characterized by several techniques and its antibacterial activity was investigated. The Ag nanoparticles are uniformly dispersed in the porous ZIF-8 with narrow size distribution. Consequently, the resulting Ag/H-ZIF-8 nanocomposite showed significantly enhanced antibacterial activities compared to the single ZIF-8 or Ag nanoparticles. Furthermore, the composite is biocompatible, because no obvious toxicity was observed on Hepatic epithelial cells. This study offers a new approach for the design of hybrid antimicrobial nanomaterials that have great potentials in practical disinfections


2011 ◽  
Vol 66 (7) ◽  
pp. 715-720
Author(s):  
Rajab Abu-El-Halawa ◽  
Mohanad Masad ◽  
Yaser Bathich ◽  
Mahmoud Al-Refai ◽  
Mohammad M. Ibrahim ◽  
...  

A series of 3-(alkylthio)-6-chlorothieno[2,3-e][1,4,2]dithiazine 1,1-dioxides (7a - e) were prepared via interaction of deprotonated 2,5-dichlorothiophene-3-sulfonamide with carbon disulfide under reflux, followed by alkylation with alkyl halides. Employment of dimethyl sulfate afforded the isomeric 2-methyl-3-thione derivative 8 together with the expected 3-(methylthio) derivative 7a in a molar ratio of 1 : 4. Treatment of 7a or 10 with ethylamine, aniline or p-chloroaniline produced the corresponding N-ethyl- (or N-phenyl)-6-chlorothieno[2,3-e][1,4,2]dithiazine-3-amine 1,1-dioxides 3a - c. Likewise, interaction of 7a with methylhydrazine (or phenylhydrazine) gave the respective 3-(1-methylhydrazinyl or 2-phenylhydrazinyl) 1,1-dioxides 9a, b. Desulfonation of 6-chloro-3-(methylthio)thieno[ 2,3-e][1,4,2]dithiazine 1,1-dioxide (7a) with sulfuryl chloride produced 3,6-dichlorothieno[2,3- e][1,4,2]dithiazine 1,1-dioxide (10). The latter compound was used as a substrate for the preparation of N-alkyl- (or aryl)-6-chlorothieno[2,3-e][1,4,2]dithiazin-3-amine 1,1-dioxides 3a - c representing a new approach for the synthesis of similar derivatives. Compounds 7a - e showed modest to low antibacterial activity against E. coli and S. aureus.


2016 ◽  
Vol 34 (No. 3) ◽  
pp. 233-243 ◽  
Author(s):  
Valachová Ivana ◽  
Bučeková Marcela ◽  
Majtán Juraj

We established and evaluated a polyclonal antibody based competitive enzyme-linked immunosorbent assay for the quantification of defensin-1 in honey. The assay showed an inhibitory concentration (IC<sub>50</sub>) value of 111.5 ± 15.41 ng/ml with a detection limit of 7.8125 ng/ml. The regaining of defensin-1 in spiked ‘artificial honey’ was between 87.05 and 112.96% with relative standard deviation less than 9.2%. Sensitivity and specificity of the test were experimentally validated on a sample of 20 different honeys. The antibacterial activity of these honey samples showed a significant concentration-dependent correlation with the production of defensin-1 (n = 20; r = −0.6598; P = 0.0016). The assay provides a specific and sensitive method for the screening of defensin-1 in honey. The method to detect honeybee-derived proteins in honey is a promising approach to verifying the authenticity of honey. The defensin-1 ELISA could also be used for the rapid screening of honeys suitable for medicinal purposes.


ChemInform ◽  
2012 ◽  
Vol 43 (37) ◽  
pp. no-no
Author(s):  
Renata Los ◽  
Marta Wesolowska-Trojanowska ◽  
Anna Malm ◽  
Monika M. Karpinska ◽  
Joanna Matysiak ◽  
...  

Author(s):  
Somaye Rashki ◽  
Neda Shakour ◽  
Zahra Yousefi ◽  
Marzieh Rezaei ◽  
Mina Homayoonfal ◽  
...  

Antibiotic resistant microorganisms have become an enormous global challenge, and are predicted to cause hundreds of millions of deaths. Therefore, the search for novel/alternative antimicrobial agents is a grand global challenge. Cellulose is an abundant biopolymer with the advantages of low cost, biodegradability, and biocompatibility. With the recent growth of nanotechnology and nanomedicine, numerous researchers have investigated nanofibril cellulose to try to develop an anti-bacterial biomaterial. However, nanofibril cellulose has no inherent antibacterial activity, and therefore cannot be used on its own. To empower cellulose with anti-bacterial properties, new efficient nanomaterials have been designed based on cellulose-based nanofibrils as potential wound dressings, food packaging, and for other antibacterial applications. In this review we summarize reports concerning the therapeutic potential of cellulose-based nanofibrils against various bacterial infections


Chemotherapy ◽  
1973 ◽  
Vol 18 (5) ◽  
pp. 297-303 ◽  
Author(s):  
Aurora Sanfilippo ◽  
Giovanna Schioppacassi

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