scholarly journals Synthesis and biological evaluation of 1,3,5-triazine-substituted ureido benzenesulfonamides as antioxidant, acetylcholinesterase and butyrylcholinesterase inhibitors

2020 ◽  
Vol 3 (2) ◽  
pp. 22-31
Author(s):  
Nebih Lolak ◽  
Muhammed Tuneğ ◽  
Aslınur Doğan ◽  
Mehmet Boğa ◽  
Suleyman Akocak
Keyword(s):  
Antioxidant Capacity ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Cation Radical ◽  
Biological Evaluation ◽  
Standard Drug ◽  
Lead Compounds ◽  
Current Series ◽  
Free Radical Scavenging Assay ◽  
Synthesis And Biological Evaluation

A series of twenty 1,3,5-triazine-substituted ureido benzenesulfonamides 2 (a-e) and 3 (a-o) were re-synthesized and assayed for antioxidant properties by using several different methods including 1,1-diphenyl-2-picryl hydrazyl (DPPH) free radical scavenging assay, 2,2′-azino-bis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) cation radical decolarization assay, metal chelating and cupric reducing antioxidant capacity (CUPRAC) methods. The inhibitory effects of compounds on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes have been also demonstrated. All compounds showed a greater antioxidant capacity against ABTS assay by having a more potent activity than the standards BHT, BHA and α-TOC. In general, all compounds were non susceptible to against AChE enzyme. On the other hand, several lead compounds were obtained from the current series against BChE enzyme. More specifically, compound 3m showed great inhibition profile against BChE with % inhibition value of 93.77, which is better than the standard drug galantamine (% inhibition value of 87.86).

Synthesis and characterisation of novel 4,6-dimethoxyindole-7- and -2-thiosemicarbazone derivatives: Biological evaluation as antioxidant and anticholinesterase candidates

2019 ◽  
Vol 43 (9-10) ◽  
pp. 399-406 ◽  
Author(s):  
Murat Bingül
Keyword(s):  
Antioxidant Capacity ◽  
Sulfonic Acid ◽  
Condensation Reaction ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Biological Evaluation ◽  
Free Radical Scavenging ◽  
Cupric Ion ◽  
High Yields ◽  
Anticholinesterase Properties

Two sets of novel indole-based thiosemicarbazone systems 8a–d and 9a–d are prepared by the Schiff base condensation reaction of indole carbaldehydes 4 and 6 with a range of thiosemicarbazides 7a–d in high yields and purity. The antioxidant properties of the synthesised compounds 8a–d and 9a–d are determined by employing three different assays, namely 2,2-diphenyl-1-picrylhydrazyl hydrate–free radical scavenging, ABTS [2,2’-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)] cationic radical decolarization and cupric ion reducing antioxidant capacity. The anticholinesterase properties of the products are investigated by acetylcholinesterase and butyrylcholinesterase enzyme inhibition assays. The methyl-substituted compounds 8b and 9b display the highest inhibition for the ABTS assay and absorbance values for the cupric ion reducing antioxidant capacity assay, while compound 9c shows the best activity for 2,2-diphenyl-1-picrylhydrazyl hydrate assay. Moderate inhibition of acetylcholinesterase and butyrylcholinesterase is determined in the case of compound 8b.

Synthesis and Biological Evaluation of the Antimicrobial Natural Product Lipoxazolidinone A

2018 ◽  
Author(s):  
Jonathan J. Mills ◽  
Kaylib R. Robinson ◽  
Troy E. Zehnder ◽  
Joshua G. Pierce
Keyword(s):  
Natural Products ◽  
Natural Product ◽  
Mechanism Of Action ◽  
Marine Natural Products ◽  
Biological Evaluation ◽  
Lead Compounds ◽  
Follow Up Studies ◽  
Initial Resistance ◽  
Synthesis And Biological Evaluation

The lipoxazolidinone family of marine natural products, with an unusual 4-oxazolidinone heterocycle at their core, represents a new scaffold for antimicrobial discovery; however, questions regarding their mechanism of action and high lipophilicity have likely slowed follow-up studies. Herein, we report the first synthesis of lipoxazolidinone A, 15 structural analogs to explore its active pharmacophore, and initial resistance and mechanism of action studies. These results suggest that 4-oxazolidinones are valuable scaffolds for antimicrobial development and reveal simplified lead compounds for further optimization.

scholarly journals Synthesis and biological evaluation of some novel pyrazolopyrimidines incorporating a benzothiazole ring system

2013 ◽  
Vol 63 (1) ◽  
pp. 19-30 ◽  
Author(s):  
Mohammed Afzal Azam ◽  
Loganathan Dharanya ◽  
Charu Chandrakant Mehta ◽  
Sumit Sachdeva
Keyword(s):  
Antimicrobial Activity ◽  
Diclofenac Sodium ◽  
Biological Evaluation ◽  
Ring System ◽  
Standard Drug ◽  
Anti Inflammatory ◽  
Pyrimidine Moiety ◽  
Synthesis And Biological Evaluation

In the present study, a series of benzothiazol derivatives 3a-l containing pyrazolo[3,4-d]pyrimidine moiety at the second position were synthesized and characterized by analytical and spectral data. The compounds were tested for their in vitro antimicrobial activity. Compounds 1-(1,3-benzothiazol-2- yl)-3-methyl-4-phenyl-1H-pyrazolo[3,4-d]pyrimidine (3a), 1- (1,3-benzothiazol-2-yl)-4-(4-chlorophenyl)-3-methyl-1H-pyrazolo[ 3,4-d]pyrimidine (3d) and 1-(1,3-benzothiazol-2-yl)- 3-methyl-4-substituted phenyl-1H-pyrazolo[3,4-d]pyrimidines (3h-j) showed significant inhibitory activity against P. aeruginosa whereas compounds 1-(1,3-benzothiazol-2-yl)-4- (2-chlorophenyl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidine (3b), 2-[1-(1,3-benzothiazol-2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidin- 4-yl]phenol (3e), 1-(1,3-benzothiazol-2-yl)-4-(3,4-dimethoxyphenyl)- 3-methyl-1H-pyrazolo[3,4-d]pyrimidine (3h), 4-[1-(1,3-benzothiazol-2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyri midin-4-yl]-N,N-dimethylaniline (3j) and 1-(1,3-benzothiazol- 2-yl)-3-methyl-4-[2-phenylvinyl]-1H-pyrazolo[3,4-d]pyrimidine (3k) were found to be active against C. albicans. Some of these synthesized compounds were evaluated for their in vivo acute toxicity, analgesic, anti-inflammatory, and ulcerogenic actions. The tested compound 4-[1-(1,3-benzothiazol- 2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-4-yl]-N, N-dimethylaniline (3j) exhibited maximum analgesic and anti-inflammatory activities. Compounds 1-(1,3-benzothiazol- -2-yl)-3-methyl-4-(3-nitrophenyl)-1H-pyrazolo[3,4-d]pyrimidine (3i) and 3j showed a significant gastrointestinal protection compared to the standard drug diclofenac sodium.

scholarly journals ANTIDIABETIC AND ANTIOXIDANT ACTIVITIES OF ETHANOLIC EXTRACT OF PIPER BETLE L. LEAVES IN CATFISH, CLARIAS GARIEPINUS

2018 ◽  
Vol 11 (3) ◽  
pp. 194 ◽  
Author(s):  
Kavitha S ◽  
Parthasarathi Perumal
Keyword(s):  
Antioxidant Activities ◽  
Clarias Gariepinus ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Metformin Hydrochloride ◽  
Piper Betle ◽  
Phytochemical Analysis ◽  
Standard Drug ◽  
Antioxidant Agents ◽  
Ic50 Values

 Objective: The present study was undertaken to assess the α-amylase inhibitory activity and antidiabetic experimental catfish model and antioxidant properties of Piper betle L. ethanolic (PBE) extract.Methods: The phytochemical analysis of PBE extract was performed. The PBE extract was tested for their inhibitory effect on the α-amylase assay, which compared to the control, acarbose. The absorbance was read at 540 nm using a spectrophotometer, and IC50 values were calculated. In this present investigation, diabetes mellitus was induced in catfish, Clarias gariepinus by epaxial musculature injection to glucose and standard drug, Metformin hydrochloride. After 24-h incubation, the treated fishes were dissected, and the blood, liver, tissue samples, and epaxial musculature regions were collected. In addition, the antioxidant properties of PBE were determined by 2,2-diphenyl-l-picrylhydrazyl (DPPH) radical scavenging and 2,2’-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) radical scavenging (ABTS) assays.Results: The phytochemical screening of PBE revealed the presence of alkaloid, flavonoids, tannins, phenol, glycosides, sterols, saponins, and quinines. Furthermore, the values of (μg/ml) 3.038 and 7.672 α-amylase enzyme inhibition were excellent activity when compared to the acarbose. Moreover, elevated the glucose level (mg/dl) was estimated in blood 1.9±0.35, liver 0.5±0.25, tissue 0.2±0.25, and epaxial musculature 0.8±0.2 after 24-h incubation. The antioxidant effect of maximum activity was found in PBE; IC50 values (μg/ml) of DPPH and ABTS were 9.362 and 6.606, respectively.Conclusions: These studies might be responsible for the P. betle L. that was used as the new source of antidiabetic and antioxidant agents. 

Comparison of ameliorative effects of Taraxacum syriacum and N-acetylcysteine against acetaminophen-induced oxidative stress in rat liver and kidney

2020 ◽  
Author(s):  
Reza Eshrati ◽  
Mahvash Jafari ◽  
Saeed Gudarzi ◽  
Afshen Nazari ◽  
Esmaeil Samizadeh ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Ethanol Extract ◽  
Control Group ◽  
Standard Drug ◽  
Ameliorative Effect ◽  
Male Wistar Rats ◽  
Liver And Kidney ◽  
Serum Biochemical

Abstract Taraxacum syriacum (TS) with natural antioxidant and pharmacological activities may be considered for treatment of oxidative stress induced by acetaminophen (APAP). The aim of this study was to evaluate the ameliorative effects of the ethanol extract of TS root against hepatorenal toxicity induced by APAP in comparison to N-acetylcysteine (NAC) as a standard drug. Thirty male Wistar rats were randomly divided into five groups. Control group; APAP (1 g/kg) group; APAP–NAC (160 mg/kg) group and APAP-TS100 and APAP-TS200 groups: APAP plus 100 and 200 mg/kg of TS extract, respectively. After 7 days treatment, serum and liver and kidney tissues were prepared and evaluated. TS extract ameliorated the increased lipid peroxidation level and decreased antioxidant enzymes activities and glutathione level in liver and kidney of APAP-treated rats. Moreover, treatment with the TS extract caused significant reduction in the histopathological damages and high levels of serum biochemical markers of hepatic and renal functions after APAP treatment. This study suggests that the extract of TS roots has dose-dependent ameliorative effect against APAP-induced oxidative damage in liver and kidney due to its free radical scavenging and antioxidant properties. The overall efficacy of the extract at 200 mg/kg dose is comparable with NAC.

scholarly journals Antioxidant Properties of a Yogurt Beverage Enriched with Salal (Gaultheria shallon) Berries and Blackcurrant (Ribes nigrum) Pomace during Cold Storage

Beverages ◽  
2018 ◽  
Vol 5 (1) ◽  
pp. 2 ◽  
Author(s):  
Vassilios Raikos ◽  
He Ni ◽  
Helen Hayes ◽  
Viren Ranawana
Keyword(s):  
Phenolic Compounds ◽  
Antioxidant Capacity ◽  
Cold Storage ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Total Phenol ◽  
Total Phenol Content ◽  
Anthocyanin Content ◽  
Total Period ◽  
Scavenging Effect

Aqueous extracts (20% w/w) of dried berry fruits and skins were used as sources of phenolic compounds to fortify yogurt beverages. The total phenol and anthocyanin content of the reformulated yogurts were determined, and the antioxidant properties were compared to plain yogurt (C) during storage at 4 °C for a total period of four weeks. Yogurt beverages fortified with salal berry (SB) extracts contained higher amounts of phenolic compounds (>69.9 μg GAE/mL) and anthocyanins (>19.12 mg C3G/L) compared to drinks supplemented with blackcurrant pomace (BC) extract (>50.13 μg GAE/mL and >10.80 mg C3G/L respectively). Storage affected the stability of anthocyanins, whereas total phenol content remained unaffected. Yogurts with SB displayed the highest antioxidant capacity followed by samples with BC, which is attributed to the radical scavenging effect of the bioactive compounds present with antioxidant properties. The antioxidant capacity of the yogurt beverages fortified with fruit extracts was maintained during cold storage. Findings of this study indicate that SB and BC pomace can be used as functional ingredients to increase the antioxidant potential of yogurt beverages.

scholarly journals Antioxidant capacity, phenolic and vitamin C contents of quinoa (Chenopodium quinoa Willd.) as affected by sprouting and storage conditions

2017 ◽  
Vol 12 (1) ◽  
Author(s):  
Maura N. Laus ◽  
Mariagrazia P. Cataldi ◽  
Carlo Robbe ◽  
Tiziana D'Ambrosio ◽  
Maria L. Amodio ◽  
...  
Keyword(s):  
Vitamin C ◽  
Antioxidant Capacity ◽  
Peroxyl Radical ◽  
Radical Scavenging Activity ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Chenopodium Quinoa ◽  
Storage Conditions ◽  
Trolox Equivalent Antioxidant Capacity ◽  
Reducing Activity

Antioxidant capacity (AC) of quinoa (<em>Chenopodium quinoa</em> Willd. cv. Real) seeds and sprouts obtained after 4 days of seed germination at 20°C and 70% humidity was evaluated using trolox equivalent antioxidant capacity (TEAC) and oxygen radical absorbance capacity (ORAC) assays, able to highlight reducing activity and peroxyl radical scavenging capacity, respectively; phenolic content (PC) was also measured. Both TEAC and ORAC assays revealed a significantly higher (about 2- and 2.8-fold, respectively) AC of 4-day-old sprouts compared to seeds; consistently, also PC values of sprouts resulted about 2.6 times higher than seeds. In order to investigate the influence of storage on AC and PC, as well as on vitamin C content (VCC), 4-day-old sprouts were subjected for 7 days at 5°C to three different conditions of controlled atmosphere storage (CAS) compared with air. Interestingly, whatever the CAS conditions, storage of quinoa sprouts up to 7 days induced an increase of AC evaluated in terms of reducing activity by TEAC assay. Consistently, an increase of PC and VCC was measured during storage, positively correlated to TEAC values. Moreover, a decrease of peroxyl radical scavenging activity, measured by ORAC, was observed after 7 days of storage, in accordance with a shift of AC towards the reducing activity component. Overall, these findings indicate that sprouting approach using quinoa may provide highly antioxidant-enriched seedlings that may improve nutritional quality of diet or of functional foods. Interestingly, antioxidant properties of quinoa sprouts may be deeply influenced by storage, able to increase reducing activity by increasing phenols and vitamin C.

scholarly journals Synthesis and Biological Evaluation of 1,3,4-Oxadiazolyl benzenesulphonyl benzimidazole derivatives

2018 ◽  
Vol 6 (02) ◽  
pp. 64-71
Author(s):  
Vivek Kumar Gupta ◽  
Baljeet Kaur ◽  
Amandeep Kaur ◽  
Amanpreet Kaur ◽  
Monika Gupta
Keyword(s):  
Inhibitory Effect ◽  
Biological Evaluation ◽  
Benzimidazole Derivatives ◽  
Growth Inhibitory Effect ◽  
Standard Drug ◽  
Growth Inhibitory ◽  
Anti Cancer ◽  
Synthesis And Biological Evaluation ◽  
Membered Heterocycle ◽  
Cancer Activity

Oxadiazoles are a class of heterocyclic aromatic chemical compound of azole family. Oxadiazole is five membered heterocycle having two carbons, two nitrogen, one oxygen and two double bonds. Oxadiazole exists in four isomeric forms depending upon the position of nitrogen atom in the ring. Benzimidazole is a heterocyclic aromatic compound. This bicyclic compound consists of fusion of benzene and imidazole. Benzimidazole may also be considered as cyclic analogues of imidines due to tautomerism effect. In the present study involves synthesis of1,3,4-oxadiazolyl benzenesulphonylbenzimidazole derivatives. All the synthesized compounds were screened against HepG-2 cell line to determine the growth inhibitory effect of compounds.All the synthesized compounds possessed good to moderate anti-cancer activity as compare to standard drug Adriamycin. Two of the synthesized compounds i.e. 8a and 8f were found to possess maximum anti-cancer activity.The structures of the synthesized compounds were established by IR and 1HNMR.

scholarly journals Synthesis, spectral studies and biological activity of 2, 3-disubstituted imidazo [2, 1-b] benzothiazole derivatives

2018 ◽  
Vol 6 (01) ◽  
pp. 01-08
Author(s):  
Yashveer Singh ◽  
Baljeet Kaur ◽  
Amandeep Kaur ◽  
Vivek Kumar Gupta ◽  
Monika Gupta
Keyword(s):  
Antimicrobial Activity ◽  
Catalytic Domain ◽  
Biological Evaluation ◽  
Spectral Studies ◽  
Thiazole Ring ◽  
Standard Drug ◽  
Atp Binding Site ◽  
Benzothiazole Derivatives ◽  
Antibacterial And Antifungal ◽  
Synthesis And Biological Evaluation

Benzothiazole is a heterocyclic compound formed by the fusion of benzene and thiazole ring. The moiety had been reported to act via competing with ATP binding site at the catalytic domain of tyrosine kinase. The present work involves the synthesis and biological evaluation of 4, 5 disubstituted imidazo [2, 1-b] benzothiazole derivatives. The antimicrobial activity of the synthesized derivatives was carried out against Gram + ve bacteria Staphylococcus aureus (MTCC 3160) and Gram –ve bacteria Bordetella bronchiseptica (MTCC 6838), Pseudomonas aeruginosa (T11) and fungal strains Candida albicans (MTCC 1637). Ciprofloxacin and Fluconazole were used as standard drug for antibacterial and antifungal activity respectively. The compounds 6a1, 6a2, 6a3, 6b1 and 8a1 exhibited good antimicrobial activity against all the strains. The derivative 8a1 was further screened for anticancer activity against MCF-7 cell line using Doxorubicin as standard. The structures of the synthesized compounds were established by IR and NMR spectral studies.

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