scholarly journals Design, Synthesis, Antimicrobial, and Antioxidant Activities of Novel-{4, 5-(substituted diphenyl)-4H-1, 2, 4-triazol-3-ylthio} Acetyl Chloride

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.

Author(s):  
Md Raihan Sarkar ◽  
Moynul Hasan ◽  
Md Sariful Islam Howlader ◽  
Mohammad Saydur Rahman ◽  
Shubhra Kanti Dey

In the present study, the antioxidant and analgesic potential of the ethanolic extract of the leaves of Derris trifoliata was evaluated. The free radical scavenging activity of the crude extract on the stable radical 1, 1-diphenyl-2-picrylhydrazyl (DPPH) was determined by comparing the DPPH inhibitory capacity of the extract. In the quantitative assay, Derris trifoliata extract displayed a free radical scavenging activity in the DPPH assay (IC50 = 19 ?g/ml) which is comparable to that of ascorbic acid (IC50 = 7.80 ?g/ml), a well-known standard antioxidant. The analgesic responses of the given samples of extracts were evaluated using the Tail immersion method. In the analgesic activity test, extract at dose of 200 mg/kg and 400 mg/kg exhibited significant (P<0.05 and P<0.001 respectively) inhibition of pain by 166.82 and 184.95 after 120 and 180 minutes respectively while the standard drug Diclofenac Na inhibition was found to be 217.67 after 180 minutes at a dose of 25 mg/kg body weight DOI: http://dx.doi.org/10.3329/ijpls.v1i2.12951 International Journal of Pharmaceutical and Life Sciences Vol.1(2) 2012


2021 ◽  
Vol 64 (2) ◽  
pp. 233-237
Author(s):  
Milena Nikolova ◽  
Ana Dobreva ◽  
Strahil Berkov

Distillation wastewater, by-products from steam and water distillation as well as raw material used as control of flower heads of Helichrysum italicum were comparative analyzed for content of the biologically active compounds by GC/MS. Acetone exudates, methanol extracts and ethyl acetate fractions obtained after alkaline hydrolyze of the studied materials were received. The three types of extraction products as well as the distillation wastewater were examined for free radical scavenging activity by DPPH assay. Phenol, fatty- and organic acids, sterols, triterpenes, sugars and sugar alcohols were identified. Succinic acid and myo-inositol were identified as main components of distillation wastewater. Hydroxycinnamic acid, caffeic acid and 4(p)-hydroxybenzoic acid were dominant compounds of the ethyl acetate fractions. Triterpenes and fatty acids, sterols and flavonoids are among the main biologically active substances in the methanolic extracts and acetone exudates. The ethyl acetate fractions were found to possess the highest free radical scavenging activity (IC50 < 50 µg/mL). Significant differences in the activity between wastes and raw materials were not found. The results showed that the waste products after distillation of H. italicum contain important biologically active substances and the extracts with high antioxidant activity can be obtained from them.


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.


2013 ◽  
Vol 477-478 ◽  
pp. 1340-1344
Author(s):  
Cheng Hua Yu ◽  
Ji Cheng Pei ◽  
Fang Dong Zhang

Heterogeneous method for grafting of syringaldehyde (SD) onto chitosan by laccase oxidation, yielding a product with improved antioxidant activities. The results showed that about 1.1% amino groups participated in this reaction. The FTIR showed that the absorption of amino groups were decreased, the absorption of benzene ring structures were disappeared and a new band appeared at 1637 cm-1 corresponding to C=N vibrations that were due to the Schiff base reaction between the chitosan and syringaldehyde. Additionally, the chitosan had insignificant reducing power and DPPH free radical scavenging activity, SD-chitosan had reducing power of A700=0.684, DPPH free radical scavenging activity of 53.2%. SD-chitosan presented improved antioxidant properties.


Crystals ◽  
2021 ◽  
Vol 11 (8) ◽  
pp. 989
Author(s):  
Adnan Shahzad ◽  
Ezzat Khan ◽  
Muhammad Said ◽  
Gul Shazada Khan ◽  
Mian Gul Syed ◽  
...  

The reaction of 1,3-Diisobutyl thiourea (Tu) with metal salts, {[CuX (X = Cl, I)], [ZnCl2] and [HgI2] in an appropriate stoichiometric ratio afforded the corresponding metal complexes [Tu2CuCl] (1), [Tu3CuI] (2), [Tu2ZnCl2] (3) and [Tu2HgI2] (4) in good yields. The FT-IR data show typically broad signals (3278–3288 cm−1) attributed to the involvement of NH bonds in extensive hydrogen bonding. The structures of complexes were proposed based on a spectroscopic data set. Compounds 1 and 2 were additionally characterized by single-crystal X-ray analysis. Complexes 1–4 were tested for their free radical scavenging efficiency using 2,2-diphenyl-1-picrylhydrazyl free radical (hereafter abbreviated as DPPH). The free radical scavenging activity was a function of decrease in the resultant absorption of DPPH solution after the mixing of an appropriate concentration of the respective complex. The activity of complexes was determined to be dose dependent and increased concentration of the complex resulted in improved antioxidant activity. Compound 1 was found to be the most efficient, with 79.9% free radical scavenging activity. Complexes were also tested for their efficiency against selected strains of bacteria (E. coli, S. flexneri, S. typhi, and P. aeruginosa) and the activities were compared to commercially available standard drug cephradine. Compound 1 was more active against P.aeruginosa (ZI 13.25), while compound 4 was found to be more active against E. coli (ZI 11.0), S. flexneri (ZI 11.2), and S. typhi (ZI 10.5).


2020 ◽  
Author(s):  
Sanita Vucane ◽  
◽  
Martins Sabovics ◽  
Lauris Leitans ◽  
Ingmars Cinkmanis ◽  
...  

Free radicals can rapidly and irreversibly oxidize various structures, including unsaturated fatty acids in vegetable oils, which affect the sensory properties. Spectrophotometry is the most widely used method for the determination of free radical scavenging activity (RSA) using 2,2-diphenyl-1-picrylhydrazyl (DPPH). Barrier to the further use of classical analytical methods to analyze biologically active compounds in foodstuffs is that equipment requires high cost and has limited mobility. One of solutions is to replace classical methods, such as spectroscopy, with smartphonebased colorimetry. Huawei P30 Lite smartphone was used for colorimetric detection. The free radical scavenging activity (RSA) in vegetable oil was detected using an application ‘Color Picker’, with image matching algorithm for red, green, and blue (RGB) model. RSA was expressed as percentage and measured by the DPPH method. The aim of the study was to determinate the total free radical scavenging activity with smartphone-based colorimetry. For the data comparison and accuracy spectrophotometer as analytical optical instrument was used. Eleven vegetable oils: sea buckthorn, sunflower, rice, macadamia nut, hemp, corn, grape, linseed, rapeseed, olive and milk thistle oils were selected for analysis. The best results with no significant differences (p>0.05) compared to smartphone-based colorimetry from spectrophotometry were determined using RG values. The poor results were detected by using B value (p<0.05) and were not suitable for determination of RSA. Smartphone-based colorimetry can be used in the determination of the RSA in vegetable oils.


2020 ◽  
Vol 21 (2) ◽  
pp. 267-277 ◽  
Author(s):  
Ananta Swargiary ◽  
Akalesh K. Verma ◽  
Sweta Singh ◽  
Mritunjoy K. Roy ◽  
Manita Daimari

Background: The use of medicinal plants for general wellbeing and disease treatment is a common practice among tribal communities of Kokrajhar districts of Assam. However, little works have been done to study the pharmacological aspect of the plants. Objectives: The present study intends to study the antioxidant and antiproliferative properties of selected medicinal plants used by the tribal communities of Kokrajhar district of Assam since ancient times. Methods: Five traditionally important medicinal plants namely, Cassia fistula, Citrus grandis, Lindernia crustacea, Sacciolepis myosuroides, and Zingiber zerumbet were investigated for antioxidant, antiproliferative (cytotoxic) and apoptosis-inducing potential in the malignant cancer cell line. Phytochemical content such as phenolic and flavonoid content were estimated following standard protocol. The methanolic extract of plants were investigated following phosphomolybdate method (TAC), FRAP, DPPH, ABTS, and TBARS assays. Antiproliferative activities of the plants were carried out by MTT assay in DL and PBMC cells. The apoptotic study was carried out following the acridine orange and ethidium bromide staining method and fluorescent microscopic imaging. Based on the significant (P≤0.05) high apoptotic inducing potential of the plant and to further dissect the molecular mode of action including downstream biological action, major phytochemicals derived from L. crustacea were investigated for its prospective binding affinity with antiapoptotic cancer target proteins. Results: Antioxidant studies by FRAP, DPPH, ABTS, and TBARS assay revealed that all the five plants contain considerable free radical scavenging activity. C. fistula showed the strongest free radical scavenging activity while the fruit peel extract of C. grandis showed poor activity. The overall antioxidant activities of plants such as TAC, FRAP, DPPH, ABTS, and TBARS may be arranged in decreasing activity as C. fistula > Z. zerumbet > L. crustacea > S. myosuroides > C. grandis. MTT based cell proliferation study showed that all the plants extract significantly (P≤0.05) inhibited cell viability with negligible cytotoxicity (~5-12%) in normal cells. Moreover, L. crustacea showed promising antiproliferative and apoptosis-inducing ability against Dalton’s lymphoma. It is worth mentioning that the major bioactive compounds of the most potent plant extract, L. crustacea interacted with anti-apoptotic proteins (cancer target) with higher affinity and the results are compared with reference inhibitors. Conclusion: It is worth noting that these plants have the potential to consider for further scientific studies in different cell lines and animal models. Furthermore, isolation and characterization of bioactive compound(s), may promise the discovery of new and valuable drugs candidate to tackle various human diseases.


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