Synthesis, Characterization, Antimicrobial and Antioxidant Activities of 1,2,4-triazolyl-isoxazole Moieties via Dehydration Reactions of Carbohydrazides

2021 ◽  
Vol 18 ◽  
Author(s):  
Asma K. Alshamari ◽  
Mahmoud A. Al-Qudah ◽  
Fedaa Hamadeh ◽  
Lo’ay A. Al-Momani ◽  
Sultan T. Abu-Orabi

: For the reason of distinct place in the field of medicinal and pharmaceutical chemistry of 1,2,4-triazole derivatives, a new class of fused 1,2,4-triazolyl-isoxazole moieties was prepared from 3-(2,4,6-trimethoxyphenyl)isoxazolo-4,5-bis[carbonyl-(4̍-phenyl) thiosemicarbazide via dehydration reactions of carbohydrazides by using the appropriate chemical reagents. The structures of the compounds were elucidated by both elemental and spectral (IR, NMR and MS) analyses. The in vitro antioxidant activity of the new compounds was determined by free radical scavenging and metal chelating activity. All the synthesized compounds showed good activity according to free radical scavenging and metal chelating activity compared with standards. The new compounds were screened in vitro antibacterial activity against three gram-positive bacteria and three gram-negative bacteria.

2015 ◽  
Vol 2015 ◽  
pp. 1-9 ◽  
Author(s):  
Maira Rubi Segura Campos ◽  
Jorge Ruiz Ruiz ◽  
Luis Chel-Guerrero ◽  
David Betancur Ancona

The flora of Latin America attracts gaining interest as it provides a plethora of still unexplored or underutilized fruits that can contribute to human well-being due to their nutritional value and their content of bioactive compounds. Antioxidant compounds are now of considerable interest due to their effect of preventing or delaying aging and their apparent involvement in prevention of numerous human diseases, including cancer, atherosclerosis, Alzheimer’s disease, inflammation, and rheumatoid arthritis. In this work, the fruit ofCoccoloba uvifera(L.) was investigated for theirin vitroantioxidant capacity using two assays based on reactions with a relatively stable single reagent radical (Trolox equivalent antioxidant capacity, TEAC; and DPPH free radical scavenging assay, DPPH), two assays based on chelating of metallic cations, and one based on the reduction of oxidized species. The TEAC value on ABTS radical, DPPH scavenging activity, ion chelation, and reducing power were found to be 897.6 μM of Trolox/100 g of sample, 22.8% of DPPH free radical scavenging, 11.3% of Cu2+-chelating activity, 23.9% of Fe2+-chelating activity, and a Fe2+-reducing power of 0.76 mg/mL, respectively. The free radical scavenging and antioxidant characteristics ofC. uviferamay be due to the presence of diverse phytochemicals in the fruit as anthocyanins, ascorbic acid, phenolic compounds, and flavonoids.


2013 ◽  
Vol 2013 ◽  
pp. 1-7 ◽  
Author(s):  
G. Kiran ◽  
T. Maneshwar ◽  
Y. Rajeshwar ◽  
M. Sarangapani

A series of β-Isatin aldehyde-N,N′-thiocarbohydrazone derivatives were synthesized and assayed for theirin vitroantimicrobial and antioxidant activity. The new compounds were characterized based on spectral (FT-IR, NMR, MS) analyses. All the test compounds possessed a broad spectrum of activity having MIC values rangeing from 12.5 to 400 μg/ml against the tested microorganisms. Among the compounds3e,3jand3nshow highest significant antimicrobial activity. The free radical scavenging effects of the test compounds against stable free radical DPPH (α,α-diphenyl-β-picryl hydrazyl) and H2O2were measured spectrophotometrically. Compounds3j,3n,3l, and3e, respectively, had the most effective antioxidant activity against DPPH and H2O2scavenging activity.


Author(s):  
Sridevi Chigurupati ◽  
Shantini Vijayabalan ◽  
Kesavanarayanan Krishnan Selvarajan ◽  
Ahmad Alhowail ◽  
Fatema Kauser

AbstractObjectivesResearch on endosymbionts is emerging globally and is considered as a potential source of bioactive phytochemicals. The present study examines the antioxidant and antidiabetic of the endophytic crude extract isolated from Leucaena leucocephala leaves.MethodsEndophytic bacteria were isolated from the leaves of L. leucocephala and 16S rRNA gene sequencing was used to establish their identity. The in vitro antioxidant effect of endophytic crude extract (LL) was evaluated using 2-diphenyl-1-picrylhydrazyl (DPPH) and 2, 2′-azino-bis-3-ethylbenzthiazoline-6-sulphonic acid (ABTS) free radical scavenging methods. The in vitro antidiabetic properties of LL were evaluated using α-amylase and α-glucosidase enzyme inhibition assay.ResultsThe isolated endophytic bacteria were identified as Cronobacter sakazakii. LL displayed potent free radical scavenging effect against ABTS and DPPH radicals with an inhibitory concentration 50% (IC50) value of 17.49 ± 0.06 and 11.3 ± 0.1 μg/mL respectively. LL exhibited α-amylase and α-glucosidase inhibition with an IC50 value of 23.3 ± 0.08 and 23.4 ± 0.1 μg/mL respectively compared to the standard drug (acarbose). Both glucose loaded normoglycemic rats and STZ induced diabetic rats treated with LL (200 mg/kg) exhibited a considerable reduction in blood glucose levels p<0.01 after 8 h of treatment when compared to normal and diabetic control rats respectively.ConclusionsThus, the study shows that LL has a wellspring of natural source of antioxidants, and antidiabetic agents and phytoconstituents present in endophytes could be the rich source for bioactive compounds.


Antioxidants ◽  
2019 ◽  
Vol 8 (8) ◽  
pp. 309
Author(s):  
Olukayode O. Aremu ◽  
Adebola O. Oyedeji ◽  
Opeoluwa O. Oyedeji ◽  
Benedicta N. Nkeh-Chungag ◽  
Constance R. Sewani Rusike

Oxidative stress has gained attention as one of the fundamental mechanisms responsible for the development of hypertension. The present study investigated in vitro and in vivo antioxidant effects of 70% ethanol-water (v/v) leaf and root extracts of T. officinale (TOL and TOR, respectively). Total phenolic and flavonoid content of plant extracts were assessed using Folin Ciocalteau and aluminium chloride colorimetric methods; while, 2,2-diphenyl-1-picrlhydrazyl (DPPH), 2,2-azinobis (3-ethylbenzothiazoline-6-sulfonic acid (ABTS) and ferric reducing antioxidant power (FRAP) protocols were used to determine the free radical scavenging and total antioxidant capacities (TAC), respectively. The in vivo total antioxidant capacity and malondialdehyde acid (MDA) levels for lipid peroxidation tests were performed on organ homogenate samples from Nω-nitro-L-arginine methyl ester (L-NAME)-induced hypertensive rats treated with leaf extract, TOL (500 mg/kg/day) and TOR (500 mg/kg/day) for 21 days. Results showed that compared to TOR, TOL possessed significantly higher (p < 0.01) polyphenol (4.35 ± 0.15 compared to 1.14 ± 0.01) and flavonoid (23.17 ± 0.14 compared to 3 ± 0.05) content; free radical scavenging activity (EC50 0.37 compared to 1.34 mg/mL) and total antioxidant capacities (82.56% compared to 61.54% ABTS, and 156 ± 5.28 compared to 40 ± 0.31 FRAP) and both extracts showed no toxicity (LD50 > 5000 mg/kg). TOL and TOR significantly (p < 0.01) elevated TAC and reduced MDA levels in targets organs. In conclusion, T. officinale leaf extract possesses significant anti-oxidant effects which conferred significant in vivo antioxidant protection against free radical-mediated oxidative stress in L-NAME-induced hypertensive rats.


2012 ◽  
Vol 554-556 ◽  
pp. 1357-1360
Author(s):  
Zhong Li Jiang ◽  
Ai Li Wang ◽  
Xi Hong Li ◽  
Min Peng Zhu ◽  
Jun Wei Wang

The present study investigated the effect of 1-MCP on bioavailability of Lingwu long jujube stored at 0 °C for 60 days. At the end of the storage, compared with the control samples, Lingwu long jujube treated with 1-MCP exhibited higher Vc bioaccessibility, total phenolic content and free radical scavenging capacity, which demonstrated that 1-MCP treatment could provide a better effect on maintaining the bioavailability of Lingwu long jujube.


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