Conventional and microwave assisted synthesis of small molecule based biologically active heterocyclic amidine derivatives

2010 ◽  
Vol 45 (3) ◽  
pp. 902-908 ◽  
Author(s):  
Sham M. Sondhi ◽  
Reshma Rani ◽  
Partha Roy ◽  
S.K. Agrawal ◽  
A.K. Saxena
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.


Materials ◽  
2019 ◽  
Vol 12 (23) ◽  
pp. 3825 ◽  
Author(s):  
Janus ◽  
Piątkowski ◽  
Radwan-Pragłowska

Carbon nanomaterials in the form of quantum dots have a high potential due to their luminescent properties and low cytotoxicity which allows their use in optical probes for use in bioimaging and biodetection. In this article, we present a novel type of nanomaterials and their obtainment method under microwave-assisted conditions using poly(L-lysine) as a raw material. The ready products were characterized over their chemical structure, pH-dependent fluorescence properties and cytotoxicity on human dermal fibroblasts. Moreover, their antioxidant activity as well as ability to biologically active molecules (vitamins) and heavy metal ions detection was evaluated. The results confirmed the obtainment of biocompatible nanomaterials with advanced properties and good water solubility according to sustained development principles.


2006 ◽  
Vol 3 (4) ◽  
pp. 307-312 ◽  
Author(s):  
Prashant Kriplani ◽  
Pawan Swarnkar ◽  
Rinku Maheshwari ◽  
K. G. Ojha

Synthesis of some biologically active benzothiazolotriazine derivatives by microwave irradiation is reported. 2-Amino-6-substituted benzothiazoles1on treatment with benzaldehyde in anhydrous ethanol afforded 2-benzylidenoimino-6-substitutedbenzothiazoles2which underwent cyclisation with ammoniumthiocyanate in dioxane to give 2-phenyl benzothiazolo [3,2-α]-s-triazine-4-[3H] thiones3.These both steps were carried out in microwave. Compound3with benzoyl chloride in anhydrous pyridine gave 2-phenyl-3-(benzoyl) benzothiazolo [3,2-α]-s-triazine-4-thiones4in good yields. The structure of all these compounds have been supported by their elemental analysis and their spectral data. All synthesized compounds were tested for their antibacterial activity using standard drug.


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