scholarly journals Microwave Assisted Synthesis and Evaluation of Toxicity and Antioxidant Activity of Pyrazoline Derivatives

2019 ◽  
Vol 19 (3) ◽  
pp. 583
Author(s):  
Jasril Jasril ◽  
Hilwan Yuda Teruna ◽  
Aisyah Aisyah ◽  
Nurlaili Nurlaili ◽  
Rudi Hendra

Four pyrazoline analogues, 3-(4-methoxyphenyl)-5-naphthalene-1-yl-1-phenyl-4,5-dihydro-pyrazole (3), 3-(4-methoxyphenyl)-5-naphthalene-1-yl-4,5-dihydro-1H-pyrazole (4), 3-(2-methoxyphenyl)-5-naphthalene-1-yl-1-phenyl-4,5-dihydro-pyrazole (5) and 3-(2-methoxyphenyl)-5-naphthalene-1-yl-4,5-dihydro-1H-pyrazole (6) were synthesized via intermolecular cyclization between substituted chalcones and hydrazine derivatives. The compounds were synthesized in two steps. In the first step, the chalcones were synthesized by Claisen-Schmidt reaction. In the second step, they were cyclized with some hydrazine derivatives to form pyrazolines by using glacial acetic acid as a catalyst and assisted by microwave irradiation. The toxicity analysis showed that compound 1 and 2 were toxic with LC50 values of 11.47 and 0.97 μg/mL, respectively. Furthermore, only compound 6 showed high antioxidant activity by using DPPH with an IC50 value of 4.47 μg/mL.

2012 ◽  
Vol 345 (7) ◽  
pp. 574-583 ◽  
Author(s):  
Adriana Ignat ◽  
Tamas Lovasz ◽  
Mihai Vasilescu ◽  
Eva Fischer-Fodor ◽  
Corina Bianca Tatomir ◽  
...  

2019 ◽  
Vol 43 (44) ◽  
pp. 17231-17240 ◽  
Author(s):  
Munusamy Saravanabhavan ◽  
Vishnu Nayak Badavath ◽  
Siddhartha Maji ◽  
Shabbir Muhammad ◽  
Marimuthu Sekar

Design and synthesis a series of pyrido[2,3-a]carbazoles for their anticancer and antioxidant activity.


ChemInform ◽  
2012 ◽  
Vol 43 (26) ◽  
pp. no-no
Author(s):  
Feng Shi ◽  
Xiao-Ning Zeng ◽  
Fei-Yue Wu ◽  
Shu Yan ◽  
Wei-Fa Zheng ◽  
...  

KOVALEN ◽  
2021 ◽  
Vol 7 (1) ◽  
pp. 42-50
Author(s):  
Imran ◽  
Nurlian ◽  
L.A. Kadir ◽  
La Agusu ◽  
Ruslan

This study was conducted to determine the organic constituents and to test the antioxidant activity and toxicity of gaharu fruit pulp extract (Aquilaria malaccensis Lamk.). Gaharu fruit pulp extract was obtained through Microwave Assisted Extraction (MAE) method and then extracted with a solvent with different polarity, namely ethyl acetate and n-hexane. The obtained yield of ethyl acetate extract of the gaharu fruit pulp was 40.827% w/v, whereas 0% w/v in n-hexane extract, therefore, no further test for n-hexane extract, so that the n-hexane extract was not tested for the next stage. The results of the organic constituents of the ethyl acetate extract of gaharu fruit pulp showed flavonoids, saponins, glycosides, phenols and tannins. Antioxidant activity testing was carried out using the DPPH method with vitamin C as a positive control. The results of the antioxidant activity test showed that IC50 of ethyl acetate extract of gaharu fruit pulp and vitamin C were 143.789ppm and 13.797ppm, respectively. Extracts from microwave-assisted maceration that were partitioned with ethyl acetate solvent were categorized into moderate antioxidants because the IC50 value was between 101-150ppm, while vitamin C was categorized as a strong antioxidant because the IC50 value was between 0-100ppm. Toxicity testing was also carried out on ethyl acetate extract of gaharu fruit pulp using the BSLT method. The results of the toxicity test of the ethyl acetate extract of gaharu fruit pulp showed activity with an LC50 value of 11.282ppm. Based on this research, the ethyl acetate extract of gaharu fruit pulp is considered to have an anticancer potential.


2017 ◽  
Vol 72 (4) ◽  
pp. 249-256 ◽  
Author(s):  
Hanan A. Al-Hazam ◽  
Zeki A. Al-Shamkani ◽  
Najim A. Al-Masoudi ◽  
Bahjat A. Saeed ◽  
Christophe Pannecouque

AbstractThe development of new HIV non-nucleoside reverse transcriptase inhibitors offers the possibility of generating structures of increased potency. To this end, coupling of mefenamic acid (4) with 4-amino-acetophenone (6) in the presence of dicyclohexylcarbodiimide and dimethylaminopyridine (DMAP) reagents afforded 4-(acetyphenyl)-2-((2,3-dimethylphenyl)amino)benzamide (7). Analogously, treatment of mefenamyl chloride (5) prepared from 4 with 6 under microwave irradiation (MWI) afforded 7. A new series of substituted chalconyl-incorporated amide derivatives of mefenamic acid 8–13 were synthesized from condensation of 7 with various substituted benzaldehydes via the Claisen–Schmidt reaction. Treatment of 8 and 11 with thiourea in a basic medium afforded the thiopyrimidine analogues 14 and 15, respectively. The newly synthesized compounds were assayed against HIV-1 and HIV-2 in MT-4 cells. Compounds 9 and 11 showed cytotoxicity values of 2.17 and 2.06 μm, respectively, against mock-infected MT-4 cells (C type adult T leukemia cells), which considered to be promising antileukemic agents.


Molecules ◽  
2021 ◽  
Vol 26 (12) ◽  
pp. 3761
Author(s):  
Thi-Thuy-Dung Nguyen ◽  
Quoc-Duy Nguyen ◽  
Thi-Van-Linh Nguyen

Polyscias fruticosa (L.) leaves contain significant bioactive compounds with high antioxidant activity such as chlorophylls, total polyphenols, etc. but these have still been underutilized. In this study, the kinetics of chlorophyll and antioxidant activity extraction from P. fruticosa leaves by microwave-assisted extraction (MAE) were investigated. Microwave power was 300, 450, or 600 (W); the ratio of material/solvent varied from 1:40 to 1:80 (g/mL). In this study, the second-order kinetic model successfully predicted the change of chlorophyll and antioxidant activity during MAE. The increase of microwave power or/and the solvent amount increased saturated extraction efficiency and the extraction rate constant. However, the saturated concentration of chlorophyll and antioxidant activity increased with the increment of microwave power and the decrease in solvent amount.


2021 ◽  
Vol 8 (1) ◽  
pp. 31
Author(s):  
Zahra Hasna Fadhilah ◽  
Farid Perdana ◽  
Raden Aldizal Mahendra Rizkio Syamsudin

Katekin merupakan senyawa bioaktif dengan kerangka flavan-3-ol dan menjadi senyawa utama penentu mutu serta dapat memberikan rasa pahit yang khas pada teh. Senyawa turunan katekin yang memiliki aktivitas sebagai antioksidan paling kuat dan melimpah yaitu epigalokatekin galat. Tujuan dari review artikel ini yaitu untuk mengetahui kandungan senyawa katekin dan epigalokatekin galat sebagai antioksidan pada berbagai jenis teh berdasarkan nilai IC50.Metode penulisan review artikel ini dilakukan dengan mencari serta menganalisis studi pustaka dari beberapa jurnal yang berkaitan dengan aktivitas antioksidan pada berbagai jenis teh dengan penelusuran terhadap senyawa katekin, khususnya epigalokatekin galat. Hasil review menunjukkan bahwa aktivitas antioksidan pada pengolahan jenis teh seperti teh hijau, teh oolong, dan teh hitam memiliki perbedaan yang cukup signifikan yang dapat dilihat dari kandungan senyawa katekin dan EGCG dimana semakin besar kandungan senyawa tersebut, maka aktivitas antioksidannya semakin tinggi. Selain itu, tingginya aktivitas antioksidan dapat dilihat dari nilai IC50. Semakin rendah nilai IC50, maka aktifitas antioksidan akan semakin tinggi. Teh hijau terbukti memiliki aktivitas antioksidan yang paling tinggi diantara teh lainnya dengan kandungan katekin sebesar 10,04% dan epigalokatekin galat sebesar 3,28% serta nilai IC50 yang paling rendah yaitu 58,61 µg/mL. Kata Kunci: Katekin, Teh Hijau, Teh Oolong, Teh Hitam, Antioksidan Catechins are bioactive compounds with a flavan-3-ol structure and become a major determinant of quality compounds and can give a distinctive bitter taste of tea. Catechin derivative compounds that have the antioxidant activity as the strongest and abundant are epigallocatechin gallate. The purpose of this article review was to determine the content of catechins and epigallocatechin gallate compounds as an antioxidant in various types of tea based on the IC50 value. The method of writing of this article review was carried out by searching and analyzing literature studies from several journals related to antioxidant activity in various types of tea by tracing catechin compounds, especially the epigallocatechin gallate. The results of the review showed that the antioxidant activity in the processing of types of tea such as green tea, oolong tea, and black tea has significant differences which could be seen from the content of catechins and EGCG compounds where the greater the content of the compounds, the higher the antioxidant activity. Also, the high antioxidant activity can be seen from the IC50 value. The lower the IC50 value, the higher the antioxidant activity. Green tea shows to have the highest antioxidant activity among other teas with a catechin content of 10.04% and an epigallocatechin gallate of 3.28% and the lowest IC50 value of 58.61 µg/mL.


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