scholarly journals Synthesis and Biological Evaluation of Some New Chalcones Containing 2,5-Dimethylfuran Moiety

2011 ◽  
Vol 8 (2) ◽  
pp. 541-546 ◽  
Author(s):  
S. Sridhar ◽  
S. C. Dinda ◽  
Y. Rajendra Prasad

A series of new chalcones(3a-g)were prepared by Claisen-Schmidt condensation of 3-acetyl-2,5-dimethylfuran with various substituted aromatic aldehydes in presence of aqueous solution of potassium hydroxide and ethanol at room temperature. The synthesized chalcones were characterized by means of their IR,1H NMRspectral data and elemental analyses. When these chalcones were evaluated for antimicrobial and anti-inflammatory activities, some of them were found to possess significant activity, when compared to standard drugs.

2008 ◽  
Vol 5 (3) ◽  
pp. 461-466 ◽  
Author(s):  
Y. Rajendra Prasad ◽  
A. Lakshmana Rao ◽  
R. Rambabu

In an effort to develop antimicrobial agents, a series of chalcones were prepared by Claisen-Schmidt condensation of appropriate acetophenones with appropriate aromatic aldehydes in the presence of aqueous solution of potassium hydroxide and ethanol at room temperature. The synthesized compounds were characterized by means of their IR,1H-NMR spectral data and elemental analysis. All the compounds were tested for their antibacterial and antifungal activities by the cup plate method.


2010 ◽  
Vol 7 (1) ◽  
pp. 295-298 ◽  
Author(s):  
B. C. Revanasiddappa ◽  
R. Nagendra Rao ◽  
E. V. S. Subrahmanyam ◽  
D. Satyanarayana

A new series of chalcones (3a-j) were synthesized by condensation of simple aldehydes with substituted acetophenones in presence of alkali. The resulted chalcones upon cyclization in presence of glacial acetic acid with isoniazid (INH) will yields the title compounds (4a-j). The newly synthesized compounds were assigned on the basis of IR,1H NMR, and Mass spectral data. All the final compounds were evaluated for theirin vitroantimicrobial activity.


2009 ◽  
Vol 6 (1) ◽  
pp. 196-200 ◽  
Author(s):  
B. A. Baviskar ◽  
Bhagyesh Baviskar ◽  
M. R. Shiradkar ◽  
U. A. Deokate ◽  
S. S. Khadabadi

Some novel benzimidazolyl chalcones were synthesized by condensation ofN-(4-(1H-benzo[d]imidazol-2-yl)phenyl)acetamide with aromatic aldehydes in presence of aqueous potassium hydroxide solution at room temperature. All the synthesized compounds were characterized on the basis of their IR,1H NMR spectroscopic data and elemental analysis. All the compounds have been screened for antimicrobial activity by the cup-plate method.


2016 ◽  
Vol 2016 ◽  
pp. 1-7 ◽  
Author(s):  
Betül Kaya ◽  
Yusuf Özkay ◽  
Halide Edip Temel ◽  
Zafer Asım Kaplancıklı

Some hydrazone derivatives were synthesized and their potential anticholinesterase activities were examined. A series of eleven new compounds of N′-(2,4-disubstitutedbenzylidene)-2-(4-(4-nitrophenyl)piperazin-1-yl)acetohydrazide derivatives were obtained via reaction of 2-[4-(4-nitrophenyl)piperazin-1-yl]acetohydrazide with aromatic aldehydes. The chemical structures of the compounds were enlightened by FT-IR,1H-NMR,13C-NMR, and HRMS (ESI) spectral data. The inhibition potency of the compounds3a–kagainst AChE and BuChE was measured and evaluated using a modification of Ellman’s spectrophotometric method. Among the tested compounds, compound3cwas assigned to be the most active derivative. Galantamine was used as a standard drug.


1998 ◽  
Vol 63 (3) ◽  
pp. 363-370 ◽  
Author(s):  
Violetta Patroniak-Krzyminiewska ◽  
Wanda Radecka-Paryzek

The template reactions of 2,6-diacetylpyridine with 3,6-dioxaoctane-1,8-diamine in the presence of dysprosium(III), thulium(III) and lutetium(III) chlorides and erbium(III) perchlorate produce the complexes of 15-membered macrocyclic ligand with an N3O2 set of donor atoms as a result of the [1+1] Schiff base cyclocondensation. In contrast, analogous reactions involving the lighter lanthanide ions (lanthanum(III), samarium(III) and europium(III)) yield the acyclic complexes with terminal acetylpyridyl groupings as products of the partial [2+1] condensation. The complexes were characterized by spectral data (IR, UV-VIS, 1H NMR, MS), and thermogravimetric and elemental analyses.


2012 ◽  
Vol 12 (2) ◽  
pp. 146-151 ◽  
Author(s):  
Elfi Susanti VH ◽  
Sabirin Matsjeh ◽  
Tutik Dwi Wahyuningsih ◽  
Mustofa Mustofa ◽  
Tri Redjeki

Synthesis of flavones and their derivatives has attracted considerable attention due to their significant pharmaceutical effects. 7-hydroxy-3',4'-dimethoxyflavone has been synthesized and its antioxidant activity has been investigated. Flavone was synthesized by oxidative cyclization of chalcone. 2',4'-dihydroxy-3,4-dimethoxychalcone was prepared by Claisen-Schmidt condensation of 2,4-dihydroxyacetophenones with 3,4-dimethoxybenzaldehydes in the presence of aqueous solution of sodium hydroxide and ethanol at room temperature. Oxidative cyclization of 2',4'-dihydroxy-3,4-dimethoxychalcone was done by using I2 catalyst in DMSO to form 7-hydroxy-3',4'-dimethoxyflavone. The synthesized compounds were characterized by means of their UV-Vis, IR, 1H-NMR and 13C-NMR spectral data. The compound was tested for their antioxidant activities by DPPH method.


2020 ◽  
Author(s):  
Lifang Guo ◽  
Benshan Xu ◽  
Zirui Wan ◽  
Lulu Ren ◽  
Jie Zhang ◽  
...  

Abstract Background: A series of aryl-piperazine derivatives of 1,7,8,9-tetrachloro-10,10-dimethoxy-4-azatricyclo [5.2.1.0 2,6 ] dec-8-ene-3,5-dione were synthesized. The chemical structures of the desired compounds were identified by 1 H NMR, ESI-MS and elementary analytical. The anti-cancer and anti-angiogenesis activities of the newly synthesized compounds were evaluated by proliferation and migration assays, respectively. Results: The screening results demonstrated that compounds 2 and 5 showed potent anti-tumor activity (IC 50 values ranging from 7.1 to 15.9μM) with low cytotoxic activities (IC 50 > 79.3μM). Although compound 5 showed little effects on endothelia proliferation (IC 50 =65.3μM), it indeed significantly abrogated endothelia cell migration (IC 50 =6.7μM). Conclusions: This work may impart new direction for the investigations of aryl-piperazine derivatives and lead to the development of potent novel anti-tumor and anti-angiogenesis agents.


INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (05) ◽  
pp. 11-15
Author(s):  
R. R Somani ◽  
◽  
P. K Chaskar ◽  
P. M. Patil

One of the principles of green chemistry emphasises on minimisation of environmental and economic impacts by developing synthetic reactions at ambient temperature and pressure.The rise of resistant strains of microorganisms is an issue of regularly expanding seriousness. Therefore, the development of new antimicrobial agents will remain a challenge for chemists. we herein report room temperature synthesis of newer heterocyclic compounds belonging to 1,3,4-oxadiazole scaffold. Their structures were confirmed using various spectroscopic techniques. These compounds were evaluated for antifungal, antibacterial and antitubercular activities.


2019 ◽  
Vol 31 (10) ◽  
pp. 2389-2393
Author(s):  
Sravanthi Siliveri ◽  
Harinadha Babu Vamaraju ◽  
Shivaraj

In the present work, novel pyrazole fused dihydrofurans synthesized via a chronological addition of N-chloro succinimide and base piperidine to pyrano[3,2-c]pyrazole carbonitrile derivatives in methanol medium. Oxidative difunctionalization was done with the reagent N-chloro succinimide by the addition of both chlorine and alkoxy groups crosswise the chromene double bond. The addition of base results in the construction of dihydrofuran derivatives by ring contraction. The structures of newly synthesized compounds were characterized on the basis of physical and spectral data. Synthesized compounds were evaluated for antibacterial and anti-inflammatory activities. All the compounds exhibited significant antibacterial activity against all the four strains of bacteria and their MICs ranged between 1.56 and 12.55 μg/mL. In anti-inflammatory screening, among all the tested compounds, compounds 7, 8, 9, 11, 12, 13, 14, 16, 17 and 18 exhibited significant protection against the edema formation at a concentration of 100 mg/kg.


2019 ◽  
Vol 42 (1) ◽  
pp. 73-80
Author(s):  
Sayed Masoud Hosseini ◽  
Ali Imani ◽  
Milad Rahimzadegan ◽  
Saeid Mohammadi ◽  
Alireza Golaghaei

Abstract Lead as a potent environmental and occupational pollutant, exerts its toxic effect mainly through oxidative stress induction. Currently, chelation therapy is the only medical management of metal intoxications in clinic, but its administration is associated with various side effects as well. In this study the protective effect of synthetized Piroxicam derivative was evaluated against lead toxicity in vitro. First the chelating activity of Piroxicam derivative was studied through Jobs method and 13C{1H} NMR spectroscopy. Then the cytoprotective effect of Piroxicam derivative (10, 20, 50, 100 and 200 μg/mL) was evaluated and compared with that of EDTA (30 μg/mL) in the presence of lead nitrate (30 μg/mL). The EC50 value of Piroxicam derivative was calculated as well. Finally, the chelation efficacy and antioxidant effects of Piroxicam derivative in EC50 and 2EC50 values was assessed and compared with that of EDTA. Results showed that Piroxicam derivative chelates lead ion as much as EDTA. Moreover, Piroxicam derivative prevented lead-induced cells death more effectively than EDTA which is may due to its potent innate antioxidant activity. In conclusion, the synthetized Piroxicam derivative with possessing potent chelating activity as well as potent antioxidant activity, could be considered as potential drug target in management of toxic metals poisoning.


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