scholarly journals MICROWAVE-ASSISTED SYNTHESIS OF SOME BIOLOGICALLY ACTIVE PYRAZOLE DERIVATIVES

2014 ◽  
Vol 3 (5) ◽  
pp. 463-467 ◽  
Author(s):  
Deepak Swarnkar ◽  
Rakshit Ameta ◽  
Ritu Vyas
Author(s):  
Hadis Khodadad ◽  
Farhad Hatamjafari ◽  
Khalil Pourshamsian ◽  
Babak Sadeghi

Aim and Objective: Microwave-assisted condensation of acetophenone 1 and aromatic aldehydes 2 gave chalcone analogs 3, which were cyclized to pyrazole derivatives 6a-f via the reaction with hydrazine hydrate and oxalic acid in the presence of the catalytic amount of acetic acid in ethanol. Materials and Methods: The structural features of the synthesized compounds were characterized by melting point, FT-IR, 1H, 13C NMR and elemental analysis. Results: The antibacterial activities of the synthesized pyrazoles was evaluated against three gram-positive bacteria such as Enterococcus durans, Staphylococcus aureus, Bacillus subtilis and two gram-negative bacteria such as Escherichia coli and Salmonella typhimurium. Conclusion: All the synthesized pyrazoles showed relatively high antibacterial activity against S. aureus strain and none of them demonstrated antibacterial activity against E. coli.


2020 ◽  
Vol 20 (5) ◽  
pp. 2917-2929
Author(s):  
Ahmed F. M. EL-Mahdy ◽  
Hassan A. H. EL-Sherief ◽  
Zeinab A. Hozien ◽  
Shiao-Wei Kuo

A rapid and efficient one-pot protocol has been developed for the synthesis of s-triazolo[3,4-b][1,3,4]thiadiazine and s-triazolo[3,4-b][1,3,4]thiadiazole nanoarchitectonics through the reaction of s-triazoles with ketones and nitriles in acetic acid containing a catalytic amount of sulfuric acid under microwave irradiation in excellent yields. With this catalytic reaction, the cheap sulfuric acid as well as other acids were examined as catalysts and the highly toxic and irritating haloketones and halonitriles were avoided to form. The effects of microwave power, temperature, time, solvent and catalyst were examined. This method achieved a better performance; e.g., higher yields, shorter reaction time and easier work-up as compared to other conventional methods. Therefore, the proposed method will be readily applicable to the synthesis of biologically important compounds containing s-triazolo[3,4-b][1,3,4]thiadiazine and s-triazolo[3,4-b][1,3,4]thiadiazole framework.


Author(s):  
Venkat Swamy Puli ◽  
Vukoti Kiran Kumar ◽  
Venkata Reddy Regalla ◽  
Anindita Chatterjee

Objective: The aim of the present study is to synthesize novel phenylacrylamide derivatives as potent bioactive agents.Methods: Novel N-(3-(4H-1,2,4-triazol-4-ylamino)-3-oxo-1-arylidene prop-2-yl) benzimidic acids (7a-c) have been synthesized by the reaction of 4-(arylidene)-2-phenyloxazol-5(4H)-ones (5a-c) with 4-amino-1, 2, 4-triazole (6) in the presence of anhydrous sodium acetate in glacial acetic acid. Titled compounds (7a-c) were obtained in good yields using microwave technology which resulted in dramatic reductions in reaction times leading to the formation of phenylacrylamide derivatives (7a-c) at a faster rate.Results: The structures of the newly synthesized compounds were characterized by Fourier-transform infrared, 1H NMR, 13C NMR, and mass spectral studies. This method can be an efficient method for the synthesis of phenylacrylamide derivatives (7a-c).Conclusion: All the final compounds were screened for their antimicrobial and antioxidant activities and found to be biologically active. Among all the compounds, 7b was found to be potent antimicrobial and antioxidant.


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