scholarly journals Design, Synthesis and Biological Evaluation of Novel Thiazolidinone Derivatives

2021 ◽  
Vol 33 (10) ◽  
pp. 2379-2385
Author(s):  
Reshma Sathyanarayana ◽  
Boja Poojary ◽  
B. Sukesh Kumar ◽  
Vasantha Kumar ◽  
Rajesh P. Shastry ◽  
...  

In present study, the novel thiazolidinone derivatives were designed and synthesized. The formation of the target compounds was confirmed by the elemental analyses, FT-IR, mass spectroscopy and 1H NMR spectroscopy. These derivatives were subjected to antibacterial and antioxidant activities. The antibacterial results revealed that these derivatives were selectively active against Gram-negative Pseudomonas aeruginosa bacteria. Also, these derivatives displayed a good DPPH radical scavenging effect. Drosophila melanogaster flies were used for evaluating the toxic impact of novel thiazolidinone derivatives.

2019 ◽  
Vol 23 (11n12) ◽  
pp. 1478-1485
Author(s):  
Senem Çolak Yazıcı ◽  
Sibel Kahraman ◽  
Salih Z. Yıldız ◽  
Mahmut D. Yılmaz

Tetra-zwitterionic-substituted nickel(II) phthalocyanine derivatives were newly synthesized starting from nonionic 2(3),9(10),16(17),23(24)-tetrakis-[2-([Formula: see text]-((3-dimethylamino)propyl)carbamate)oxyethyl)phthalocyaninato nickel (II). The novel compounds have been characterized by a combination of UV-vis, FT-IR and mass spectroscopies and elemental analysis. The critical micelle concentrations of the prepared compounds were measured, and the antioxidant activities were analyzed with radical scavenging ability of 1,1-diphenyl-2-picrylhydrazyl (DPPH) and with 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS). The zwitterionic molecules showed aggregated spectra in the UV-vis region, and they might be good surfactant candidates for the detergent industry with their appropriate critical micelle concentration (CMC) properties in water. The compounds exhibited ABTS radical scavenging activity and thus they have antioxidant activity.


2011 ◽  
Vol 183-185 ◽  
pp. 104-109
Author(s):  
Ning Zhang ◽  
Zhen Yu Wang ◽  
Hua Zhang ◽  
Jian Ren ◽  
Xiu Mei Hao

This study aims to evaluate the antioxidative activities of water and alkaline solution pH=8, 50% ethanolic (APP1 or SAPP1), 75% ethanolic (APP2 or SAPP2) and 100% ethanolic (APP3 or SAPP3) extracts of A. auricular. The antioxidant activities, including the ABTS, superoxide anion radical-scavenging effect, hydrogen peroxide radical-scavenging effect and chelating ability on ferrous ions were studied in vitro. A comparison of the 50% effective concentration (EC50) values of different antioxidative reactions revealed that SAPP3 was more effective in scavenging ABTS, hydrogen peroxide and chelating ability on ferrous ions.SAPP2 showed a higher superoxide radical-scavenging activity. The alkali-soluble polysaccharides extracts showed higher radical-scavenging effect than water-soluble polysaccharides.


2018 ◽  
Vol 9 (4) ◽  
pp. 375-381 ◽  
Author(s):  
Mahmoud Al‐Refai ◽  
Mohammad Ibrahim ◽  
Abdullah Al‐Fawwaz ◽  
Armin Geyer

A new series of furo[2,3-b]pyridine derivatives bearing aryl substituents were synthesized in two steps, where, the cyano-(2H)-pyridones (1a-l) were converted to the corresponding nicotinonitriles (2a-l), followed by the Thorpe-Ziegler ring cyclization to the furo[2,3-b]pyridine derivatives (3a-l). All new compounds were characterized by 1D-NMR experiments (1H and 13C) and 2D-NMR experiments (COSY, HMBC and HSQC), as well as ESI-MS and HR-ESI-MS data. The new compounds were screened for their antioxidant activities by 2,2-diphenyl-1-picryl-hydrazylhydrate (DPPH) free radical assay. The highest radical scavenging effect was observed for nicotinonitriles 2d, 2h and 2l and furo[2,3-b]pyridines 3b, 3f and 3j by methanolic solvent at 4.0 mg/mL concentration. Remarkably, all nicotinonitriles and furo[2,3-b]pyridine exhibited a significant radical scavenging activity after 24 and 48 hours compared with 0.5 hour.


Author(s):  
Jatin Vora ◽  
Kartik Vyas

A cogent synthesis of completely new compound series of by 6-(3,5-bis(trifluoromethyl)phenyl)-4-(4-chlorophenyl)-3,4-dihydro pyrimidine-2(1H)-one (Biginelli reaction) was achieved by continue heating of (E)-1-(3,5-bis(trifluoromethyl)phenyl)-3-(substituted phenyl)prop-2-en-1-one and urea for 5 hours with 40% KOH and ethyl alcohol. (E)-1-(3,5-bis(trifluoromethyl)phenyl)-3-(substituted phenyl)prop-2-en-1-one is produced by Claisen-Schmidt Condensation. In this condensation 1-(3,5-bis(trifluoromethyl)phenyl)ethanone and different aldehyde are mixed. All the novel compound series were characterized by infrared and 1H nuclear magnetic resonance and mass spectroscopic techniques and by elemental analyses. The newly synthesized compounds were evaluated for their antibacterial and antifungal activity


2013 ◽  
Vol 781-784 ◽  
pp. 1235-1239
Author(s):  
Qian Nan Guo ◽  
Lei Lv ◽  
Yao Zhou ◽  
Peng Yu ◽  
Yuou Teng

Aurones belong to a class of heterocyclic flavonoids which contains a benzofuran element associated with a benzylidene linked in position 2. Aurones possess a wide range of pharmacological activities and biological activities, such as antitumor, antifungal, phytoalexin and so on. A novel series of 2-ayl-yl (5-methacrylate) aurone analogues were synthesized in six steps with the overall yield of 11%-13% and characterized by 1H NMR. Among the key intermediates and target compounds, 2-(2-furan-ylmethylene)-5-methacrylate-benzofuran-3(2H)-one (7a) and 2-(2-thienyl-ylmethylene)-5-methacrylate-benzofuran-3(2H)-one (7b) have never been reported before. Primary biological activities evaluation showed that 7a exhibited good inhibitory activities against K562 with an IC50 of 2.18 μM and against HepG2 with an IC50 of 3.95μM.


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