Synthesis, Characterization and Biological Activities of Substituted 1-[Benzothiazol-(1H)-2-yl]-3-phenyl-prop-2-en-1-ones

2019 ◽  
Vol 4 (3) ◽  
pp. 144-146
Author(s):  
C. Anuba ◽  
T.F. Abbs Fen Reji

A series of ortho and para substituted 1-[benzothiazol-(1H)-2-yl]-3-phenyl-prop-2-en-1-one derivatives were synthesized from 2-acetyl benzothiazole and ortho and para-substituted benzaldehye using ethanol as solvent. The synthesized compounds were characterized by UV-visible, FT-IR, 1H NMR and mass spectrometry. Antioxidant activities of synthesized compounds have been evaluated by DPPH free radical scavenging activity using ascorbic acid as standard. The standard solution and 1-[benzothiazol- (1H)-2-yl]-3-phenylprop-2-en-1-ones compounds were prepared with different concentrations. Anticancer activity of 1-[benzothiazol-(1H)-2-yl]-3-phenylprop-2-en-1-one and 1-[benzothiazol-(1H)- 2-yl]-3(4-chlorophenyl)prop-2-en-1-one were assigned by MTT assays.

2019 ◽  
Author(s):  
Chem Int

In this study, we determined the chemical composition and antioxidant activities of the essential oils from two different varieties of khat (Catha edulis Forsk) cultivated in Ethiopia. The essential oils were extracted by hydrodistillation using the Clevenger type apparatus, identifications of compounds were made by gas chromatography and gas chromatography-mass spectrometry (GC-MS). Seventy seven different compounds were identified from essential oils of the two different khat cultivars. The essential oils in the samples from Bahir Dar and Wendo were composed of 50 and 34 compounds, respectively. The major compound identified in khat essentials oils include: limonene, 1-phenyl-1,2-propanedione, 1-hydroxy,1-phenyl-2-propanone, camphor, (sulfurous acid)-2-propylundecyl ester, hexadecane, O-mentha-1(7), 8-dien-3-ol, heptadecane, 10-methylnonadecane, (phthalic acid)-isobutyl octadecyl ester, and tritetracontane. The antioxidant and free radical scavenging activity of the oils were assessed by means of 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical assay. The scavenging activities of the oils were 23.5-23.6 μg AAE/kg of fresh khat sample.


2020 ◽  
Vol 10 (2) ◽  
pp. 145-152 ◽  
Author(s):  
Imane Rihab Mami ◽  
Rania Belabbes ◽  
Mohammed El Amine Dib ◽  
Boufeldja Tabti ◽  
Jean Costa ◽  
...  

Background: Carthamus caeruleus belongs to the Asteraceae family. The roots are traditionally used as healing agents. They help to heal burns and treat skin diseases. They are also used against joint inflammation and are very effective against diseases such as irritable bowel syndrome for cancer patients. Objectives: The purpose of this work was i) to study the chemical composition of i) the essential oil and hydrosol extract of Carthamus caeruleus, ii) to isolate the major component of both extracts and iii) to evaluate their antioxidant, antifungal and insecticidal activities. Methods: The essential oil and hydrosol extract obtained from the roots were studied by GC and GC/MS. The antioxidant activities were performed using two different methods i) Radical scavenging activity (DPPH) and ii) the Ferric-Reducing Antioxidant Power (FRAP), using BHT as a positive control. Whereas, the antifungal activity of the essential oil and Carlina oxide was investigated against plant fungi. The fumigation toxicity of C. caeruleus essential oil besides Carlina oxide was evaluated against adults of Bactrocera oleae better known as the olive fly. Results: The essential oil and hydrosol extract were mainly represented by acetylenic compounds such as carline oxide and 13-methoxy carline oxide. Carlina oxide was isolated and identified by 1H and 13C NMR spectroscopic means. The results showed that Carlina oxide presented interesting antioxidant and antifungal properties, while C. caeruleus root essential oil had better insecticidal activity. Furthermore, Carlina oxide has demonstrated promising in vivo antifungal activity to control infection of apples by Penicillium expansum. Conclusion: Carlina oxide can be used as a natural food preservative and alternative to chemical fungicides to protect stored apple against Penicillium expansum.


2020 ◽  
Vol 42 (1) ◽  
pp. 109-109
Author(s):  
Hao Zang Hao Zang ◽  
Qian Xu Qian Xu ◽  
Luyun Zhang Luyun Zhang ◽  
Guangqing Xia Guangqing Xia ◽  
Jiaming Sun and Junyi Zhu Jiaming Sun and Junyi Zhu

A series of hydroxytyrosol (HT) derivatives were synthesized by modification of alcohol hydroxyl group of HT, twenty-five target compounds were obtained and characterized by NMR and HRMS. The antioxidant activities of those compounds were evaluated in three different assays. Except 3e and 3y, all other compounds demonstrated significant 2,2and#39;-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) free radical cation scavenging activity ranging from IC50 3.4 to 24.4 μM, which were more potent than L-ascorbic acid (IC50=24.8 μM). Compounds 3b-3d, 3f-3k, 3m-3x were better than Trolox (18.3 M). Moreover, the ferric reducing antioxidant power (FRAP) of all compounds were discovered to be more potent than L-ascorbic acid (40.7 mmol/g), except 3e, all other compounds (141.5-202.1 mmol/g) were better than Trolox (94.7 mmol/g). Compounds 3a-3d, 3f-3j, 3l-3m, 3o, 3q, 3t, 3v-3y exhibited more potent hydroxyl radical scavenging activity (IC50=245.1-475.1 M) than L-ascorbic acid (554.4 M) and Trolox (500.4 M). Compounds 3q, 3t and 3y exhibited more potent -Glucosidase inhibition activity (39.1-52.4 M) than Acarbose (60.9 M). Compounds 3a, 3d, 3f-3m, 3s-3t, 3v-3y showed some acetylcholinesterase inhibition activities, compounds 3a, 3d, 3f-3j, 3l-3m, 3o-3p, 3s-3t, 3w showed some butyrylcholinesterase inhibition activities.


2017 ◽  
Vol 15 (2) ◽  
pp. 157-167
Author(s):  
Prabhakar Kumar VERMA ◽  
Mukesh KUMAR ◽  
Nelam MALIK ◽  
Priyanka DHIMAN ◽  
Anurag KHATAHAR

A series of 20 new biologically active derivatives of 2-{4, 5-(substituted diphenyl)-4H-1,2,4-triazol-3-ylthio}acetyl chloride has been synthesized, with the aim to investigate antimicrobial, free radical scavenging activity. All the synthesized compounds were characterized by spectroscopic data and elemental analysis. The final compounds were tested for antibacterial activity against Gram-positive bacteria: Staphylococcus aureus MTCC 3160, Bacillus subtilis MTCC 441; Gram-negative bacteria: Escherichia coli MTCC 443, and, for antifungal activity, against Candida albicans MTCC 227 and Aspergillus niger MTCC 281, taking ciprofloxacin as antibacterial and fluconazole as antifungal standard drugs. Compound 7a6 was found to be the most effective antibacterial (MIC = 3.12 µg/ml), and compounds 7a2 and 7d1 (MIC = 3.12 and 6.25 µg/ml) had the most effective antifungal effects on the selected strains, as compared to the standard drugs. The results of antioxidant studies revealed that compound 7b1 was found to be most active antioxidant, with 40.4±0.687 µg/ml, and compounds 7b3, 7d7, and 7d4 also showed promising free radical scavenging activity, as compared with the standard drug ascorbic acid.


2020 ◽  
Vol 38 ◽  
Author(s):  
M. AKBAR ◽  
I.N. SHERAZI ◽  
M.S. IQBAL ◽  
T. KHALIL ◽  
H.M. WAQAS

ABSTRACT: In the present study, antibacterial and antioxidant [1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging activity] activities of a weed, slender amaranth (Amaranthus viridis L.) were investigated. Extracts of different plant parts were prepared in n-hexane, chloroform and ethyl acetate. Antibacterial activity was measured by using 100 mg mL-1 concentration extracts against 4 deadly phytopathogenic bacterial species viz. Pseudomonas syringae Van Hall, Ralstonia solanacearum Smith, Erwinia carotovora (Jones), Holland and Xanthomonas axonopodis Hasse. In antioxidants assays, 10, 20 and 30 mg mL-1 extracts were used keeping DPPH as control. In these bioassays, ethyl acetate fraction of A. viridis leaf exhibited the best antibacterial and antioxidants activity. Ethyl acetate leaf fraction showed the highest inhibition zone diameter (IZD) where it caused 21 mm IZD against P. syringae and 19 mm IZD against E. carotovora. This extract also showed 22, 52 and 84% antioxidant activity at 10, 20 and 30 mg mL-1 concentrations, respectively. Previously there is no report available that describes antibacterial activity of root extract of A. viridis against P. syringae. Moreover, antioxidant activity of stem and root extracts in n-hexane, chloroform and ethyl acetate was investigated first time in the world. It was concluded that the biological activities observed during the present investigation may be due to the presence of bioactive constituents that can be harnessed as natural antibacterials and antioxidants.


2019 ◽  
Vol 31 (11) ◽  
pp. 2448-2452
Author(s):  
Somashekara Bhadrachar ◽  
Giriyapura R. Vijayakumar ◽  
Kittappa M. Mahadevan ◽  
Thippeswamy Basavaraja

A series of 1,2,4,5-tetrasubstituted imidazoles (2a-g) were synthesized using 1,2-diketone, 1-naphthaldehyde, substituted aromatic amine and ammonium acetate in the presence of ceric ammonium nitrate as a catalyst. The synthesized compounds were characterized by FT-IR, 1H NMR, Mass spectra and explored for their antioxidant activity by DPPH free radical scavenging assay method. Among the synthesized compounds 2a, 2e and 2f exhibit good antioxidant activities. Molecular docking study was also been performed to know the possible interactions between the synthesized compound and antioxidant receptor 3MNG.


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.


2020 ◽  
Vol 18 (4) ◽  
pp. 386-391
Author(s):  
Yonghun Kim ◽  
Ang Li ◽  
Junyu Wang ◽  
Wancong Yu ◽  
Fang Wan ◽  
...  

Yinchenhao (Artemisia capillaris Thunb.) is a pharmaceutical agent that not only shows therapeutic effects against hepatobiliary diseases but also offers various physiological benefits. This study examined the extraction rates of antioxidant extracts from Yinchenhao leaves using different solvents. The extraction rates using different solvents were as follows: ethanol (12.1 ± 0.87%) > water (7.7 ± 0.45%) > n-butanol (1.3 ± 0.16%) ethyl acetate > (1.3 ± 0.14%) > n-hexane (1.1 ± 0.15%). The n-butanol and ethyl acetate extracts showed higher 1,1-Diphenyl-2 picrylhydrazyl radical free radical scavenging activity, 2,2′-azinobis-(3-ethylbenzothiazoline-6-sulphonate) free radical scavenging activity and ferric ion reducing antioxidant activity, while n-hexane extracts showed weak antioxidant activity. In conclusion, Yinchenhao leaf has potential as a natural antioxidant, and n-butanol and ethyl acetate may be effective extraction solvents for studying its antioxidant activities.


2012 ◽  
Vol 2012 ◽  
pp. 1-8 ◽  
Author(s):  
Shang-Tse Ho ◽  
Yu-Tang Tung ◽  
Yong-Long Chen ◽  
Ying-Ying Zhao ◽  
Min-Jay Chung ◽  
...  

The objective of this study is to assess antioxidant activities of methanolic extracts from the leaves of 18 indigenous tree species in Taiwan. Results revealed that, among 18 species,Acer oliverianumexhibited the best free radical scavenging activities. The IC50values were 5.8 and 11.8 μg/mL on DPPH radical and superoxide radical scavenging activities, respectively. In addition,A. oliverianumalso exhibited the strongest ferrous ion chelating activity. Based on a bioactivity-guided isolation principle, the resulting methanolic crude extracts ofA. oliverianumleaves were fractionated to yield soluble fractions of hexane, EtOAc, BuOH, and water. Of these, the EtOAc fraction had the best antioxidant activity. Furthermore, 8 specific phytochemicals were isolated and identified from the EtOAc fraction. Among them, 1,2,3,4,6-O-penta-galloyl-β-D-glucopyranose had the best free radical scavenging activity. These results demonstrate that methanolic extracts and their derived phytochemicals ofA. oliverianumleaves have excellent antioxidant activities and thus they have great potential as sources for natural health products.


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