Synthesis, Characterization and Biological Evaluation of
Novel Triazole Linked Chromone Biheterocycle Analogs

The current work focused on the synthesis of novel chromone biheterocycle analogs followed by its characterization through physico-chemical and spectral techniques like FTIR, mass and NMR spectroscopy. The basic triazole heterocycle and its analogs have different biological properties. At the point when one biological active molecule is connected to another, the resultant shows improved potency (biheterocycles). Chromone and triazole are selected in this study to develop new efficient, simple, economically viable and biologically active synthetic compounds. All the novel derivatives of triazole linked chromone biheterocycles were synthesized via a click chemistry procedure and screened for in vitro antimicrobial, antifungal and antioxidant studies. Among them, the compounds CRN-F (IC50 = 35.97), CRN-H (IC50 = 28.76) and CRN-J (IC50 = 29.72) have significant free radical scavenging activity in comparison with the ascorbic acid as control standard (IC50 = 23.07). Some of these novel derivatives exhibited moderate antimicrobial and antifungal activity compared to that of the reference standards. Hence, the novel chromone biheterocycle analogs played a protective role against oxidative damage.

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Synthesis, Characterization and Biological Evaluation of Indole-Pyrazole Amalgamated α-Cyano Substituted Chalcones

Anti-Cancer Agents in Medicinal Chemistry ◽

10.2174/1871520621666210201095030 ◽

2021 ◽

Vol 21 ◽

Author(s):

Pravin S. Bhale ◽

Sadanand N. Shringare ◽

Amol B. Khade ◽

Hemant V. Chavan

Keyword(s):

Breast Cancer ◽

Cell Line ◽

Radical Scavenging Activity ◽

Radical Scavenging ◽

Safety Margin ◽

Biological Evaluation ◽

Biologically Active ◽

Monkey Cell ◽

Mcf 7

Background: Indole and pyrazole constitute a major class of biologically active scaffolds. The amalgamation of two or more pharmacophores would generate novel molecular templates that are likely to unveil remarkable biological properties. Objective: An efficient and high yielding synthesis of indole-pyrazole integrated α-cyano substituted chalcones and their in vitro antibreast cancer and antioxidant evaluation. Methods: The synthesis of a series of indole-pyrazole amalgamated α-cyano substituted chalcones (6a-o) was achieved by reacting substituted 3-cyanoacetyl indole 2 with substituted pyrazole aldehyde 5 in the presence of piperidine. All the newly synthesized compounds have been characterized by IR, 1H NMR and HRMS spectroscopy. Results: Anti-breast cancer evaluation of the synthesized compounds in vitro against MCF-7 cell line revealed high anti-breast cancer activities. Amongst the compounds screened 6f, 6g, 6h, 6c, 6d, 6e, 6i and 6k unveiled excellent activity against breast carcinoma (GI50 <0.1µM) as good as adriamycin (GI50 <0.1µM). The compounds were also screened against the normal Vero monkey cell line and the results demonstrated more selectivity against MCF-7. In other hand, compounds, 6b, 6c, 6d, 6h and 6i have shown moderate DPPH and NO radical scavenging activity. Conclusion: Most of the synthesized compounds exhibited significant antitumor activities. These results further support its safety margin by studying the activity on normal Vero monkey cell line. These results acclaim the possible use of these compounds for the design and development of potent anti-breast cancer agents.

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Determination of in vitro antioxidant activity of the leaves extracts of Ehretia pubescens

International Journal of Research in Pharmaceutical Sciences ◽

10.26452/ijrps.v11i4.3308 ◽

2020 ◽

Vol 11 (4) ◽

pp. 6262-6267

Author(s):

Krishnamoorthy Meenakumari ◽

Giridharan Bupesh ◽

Mayur Mausoom Phukan

Keyword(s):

Antioxidant Activity ◽

Ethyl Acetate ◽

Radical Scavenging Activity ◽

Antioxidant Properties ◽

Radical Scavenging ◽

Reducing Power ◽

Biological Properties ◽

Scavenging Activity ◽

Reducing Power Assay

The foods from plants were known to ensure against degenerative diseases and maturing because of their antioxidant activitycredited to their high content. Information on antioxidant activity of Indian medicinal plant is abundant. To the best of our knowledge, biological properties have not been accounted in the literature for this species of . As a point, this is the first results to assess the anti-oxidant activity of the plant which belongs to the family . The antioxidant activity of Methanol, , Ethyl acetate and Aqueous extracts of E. was determined using the DPPH free radical scavenging activity, ABTS radical scavenging activity and reducing power assay. The DPPH scavenging activity showed higher activity observed in extract (63%) of E. than (54%), (44%) and aqueous (30%). the ABTS assay inhibition in extract (58%) than (43%), (38%) and aqueous (32%) extracts. The reducing power assay of different extracts was increased in extract (54%) than (40%), (34%) and aqueous (28%) extracts. Overall, the and ethyl acetate extract had higher antioxidant properties than other extract. However, in this study, extracts exhibit great potential for antioxidant activity and may be useful for their nutritional and medicinal functions.

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Synthesis, Characterization and Biological Evaluation of Fe(III) and Cu(II) Complexes with 2,4-Dinitrophenyl hydrazine and Thiocyanate Ions

Asian Journal of Chemistry ◽

10.14233/ajchem.2019.21719 ◽

2019 ◽

Vol 31 (4) ◽

pp. 780-784

Author(s):

P. Manimaran ◽

S. Balasubramaniyan

Keyword(s):

Antioxidant Activity ◽

Metal Complexes ◽

Radical Scavenging Activity ◽

Radical Scavenging ◽

Free Ligand ◽

Antimicrobial Activities ◽

Biological Evaluation ◽

Diffusion Method ◽

Spectral Studies

The metal complexes of Fe(III) and Cu(II) were prepared by using 2,4-dinitrophenyl hydrazine (DNPH) and thiocyanate (SCN) with stirrer refluxed for about 6 h. The prepared Fe(III) and Cu(II) complexes were characterized by elemental analysis, molar conductance, magnetic susceptibility and electronic spectrum, FT-IR spectral studies. The result suggested the octahedral geometry for Fe(III) and Cu(II) complexes. Powder X-ray diffraction indicate the crystalline nature of the metal complexes. The antimicrobial activities of the Fe(III) and Cu(II) complexes were tested with various micro organisms by disc diffusion method. The antimicrobial results indicate that the metal complexes are highly active with compared to the free ligand. The in vitro antioxidant activity of the free ligand and its metal complexes was assayed by radical scavenging activity (DPPH). The result proposed that Fe (III) and Cu(II) complexes exhibited strong antioxidant activity than that of the ligand.

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SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL THIAZOLE-PYRAZOLE INTEGRATED CHALCONES AS ANTIOXIDANT AND ANTI-INFLAMMATORY AGENTS

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2019.v12i7.34143 ◽

2019 ◽

pp. 311-315

Author(s):

DNYANESHWAR SIRSAT ◽

PRADEEP KATE ◽

MADHUSUDAN BACHUTE

Keyword(s):

Radical Scavenging Activity ◽

Radical Scavenging ◽

Biological Evaluation ◽

Schmidt Reaction ◽

Chemical Structures ◽

1H Nuclear Magnetic Resonance ◽

Anti Inflammatory ◽

Synthesis And Biological Evaluation ◽

Substituted 1

Objective: The objective of the present study was to synthesize the thiazole-pyrazole integrated chalcones and their in vitro antioxidant and anti- inflammatory evaluation. Methods: The designed hybrid thiazole-pyrazole integrated chalcones (3a-j) were synthesized by Claisen–Schmidt reaction of substituted 1-(4-methyl-2-phenylthiazol-5-yl) ethanone and substituted pyrazole aldehyde in the presence of 10% NaOH in ethanol solvent under reflux condition. The chemical structures of synthesized compounds were confirmed by IR, 1H nuclear magnetic resonance (NMR), 13C NMR, and high- resolution mass spectra. Results: All the title compounds were screened for their in vitro antioxidant and anti-inflammatory activity. The screening data indicated that tested compounds showed potent antioxidant activity with moderate anti-inflammatory potential. Conclusion: Antioxidant screening data reveal that most of the synthesized compounds possess excellent 1,1-diphenyl-2-picrylhydrazyl and NO radical scavenging activity. Most of the compounds found to possess marked anti-inflammatory potential by effectively inhibiting the heat-induced albumin denaturation.

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Feijoa Fruit Peel: Micro-morphological Features, Evaluation of Phytochemical Profile, and Biological Properties of Its Essential Oil

Antioxidants ◽

10.3390/antiox8080320 ◽

2019 ◽

Vol 8 (8) ◽

pp. 320 ◽

Cited By ~ 3

Author(s):

Antonella Smeriglio ◽

Marcella Denaro ◽

Clara De Francesco ◽

Laura Cornara ◽

Davide Barreca ◽

...

Keyword(s):

Essential Oil ◽

Radical Scavenging Activity ◽

Radical Scavenging ◽

Antimicrobial Properties ◽

Biological Properties ◽

Fruit Peel ◽

Cytoprotective Activity ◽

Phytochemical Profile ◽

Acca Sellowiana

Acca sellowiana (O. Berg) Burret (Feijoa) is an evergreen shrub, belonging to the Mirtaceae family. The aim of this study was to investigate the micromorphological features of the feijoa fruit peel and to evaluate the phytochemical profile, as well as the antioxidant, cytoprotective, and antimicrobial properties of its essential oil (EO), by several in vitro cell-free and cell-based assays. The micromorphological analysis showed several schizogenic secretory cavities, immediately below the epidermal layer. Forty compounds were identified and quantified by GC-FID and GC-MS analyses. Sesquiterpenes were the most abundant ones (76.89%), followed by monoterpene hydrocarbons (3.26%), and oxygenated monoterpenes (0.34%). The main compounds were γ-Selinene (17.39%), α-Cariophyllene (16.74%), β-Cariophyllene (10.37%), and Germacene D (5.32%). The EO showed a strong and dose-dependent antioxidant, and free-radical scavenging activity. Furthermore, it showed cytoprotective activity on the lymphocytes, that have been pre-treated with 100 μM tert-butyl-hydroperoxide (t-BOOH), as well as a decrease in intracellular reactive oxygen species (ROS), induced by t-BOOH on erythrocytes. A preliminary antimicrobial screening against GRAM+ and GRAM− bacteria, as well as on fungi highlighted that EO showed the best activity against S. aureus and C. albicans (MIC 2.7 mg/mL). In light of these results, feijoa fruit EO could find various applications, especially in the food, nutraceutical, and pharmaceutical fields.

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A Face Serum Containing Bakuchiol, Palmitoyl Tripeptide-38, Hydrolyzed Hyaluronic Acid and a Polyherbal and Vitamin Blend Improves Skin Quality in Human Volunteers and Protects Skin Structure In vitro

10.20944/preprints202106.0580.v1 ◽

2021 ◽

Author(s):

Brett J West ◽

Ifedayo Alabi ◽

Shixin Deng

Keyword(s):

Patch Test ◽

Radical Scavenging Activity ◽

Radical Scavenging ◽

Quality Parameters ◽

Biologically Active ◽

Efficacy Trial ◽

Dermatological Examination ◽

The Face ◽

Skin Quality

A face serum composed of a combination of biologically active compounds was evaluated for safety and efficacy in vitro, in a repeat insult patch test and in a human clinical efficacy trial. The serum inhibited tyrosinase activity modestly, decreased collagenase activity and exhibited notable free radical scavenging activity in vitro. It is gentle to the skin, as the serum did not irritate the skin or produce symptoms of allergic contact dermatitis in the 55 healthy adults that participated in the repeat insult patch test. In the efficacy trial, daily application of the face serum for 30 days significantly increased skin hydration, with all 35 volunteers experiencing improvement. Substantial improvements in skin elasticity, roughness (fine lines and wrinkles), and brightness also occurred during the trial. Dermatological examination also revealed a trend for reduced comedone count with use of the serum. Self-assessment responses revealed that all volunteers experienced improvements in multiple skin quality parameters and that participant perceptions are consistent with the results of the instrumental analyses. These findings indicated that the measured improvements in skin quality are not only statistically significant but are also clinically relevant as they were great enough for users of the face serum to feel and recognize.

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Contribution of Resveratrol in the Development of Novel Urease Inhibitors: Synthesis, Biological Evaluation and Molecular Docking Studies

Combinatorial Chemistry & High Throughput Screening ◽

10.2174/1386207322666190410150216 ◽

2019 ◽

Vol 22 (4) ◽

pp. 245-255 ◽

Cited By ~ 1

Author(s):

Ritu Kataria ◽

Anurag Khatkar

Keyword(s):

Radical Scavenging Activity ◽

Radical Scavenging ◽

Docking Studies ◽

Biological Evaluation ◽

Vilsmeier Reaction ◽

Parent Molecule ◽

Ic50 Value ◽

Urease Enzyme ◽

Protein Pocket

Aims and Objective: A new library of resveratrol derivatives was designed and synthesized in excellent yield via two-step reaction utilizing Vilsmeier reaction as the first step and subsequent addition of substituted aromatic amine in the second step. Methods: Synthesized compounds were investigated for their antioxidant as well as for in vitro inhibition activity against jack bean urease enzyme. Compounds R3b and R4 with IC50 value 18.85±0.15 and 21.60±0.19µM against urease enzyme and 6.01±0.07 and 7.52±0.14µM in vitro- DPPH free radical scavenging activity have emerged as most active molecules from the selected library. Molecular simulation studies were also carried out for determining the interaction detail of newly synthesized compounds within a protein pocket. Results and Conclusion: Newly synthesized compounds were found to possess better docking score (-5.941 to -6.894) and binding energy (-46.854 to -56.455) as compared to the parent resveratrol (-5.45 and -20.155) which revealed that the newly synthesized compounds bind in a better way as compared to the parent molecule

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Design, Synthesis, and Biological Evaluation of Novel Tetramethylpyrazine- nitrone Derivatives as antioxidants

Letters in Drug Design & Discovery ◽

10.2174/1570180817999201117145311 ◽

2020 ◽

Vol 17 ◽

Author(s):

Haiyun Chen ◽

Chunyan Yan ◽

Jie Cao ◽

Zheng Liu ◽

Yewei Sun ◽

...

Keyword(s):

Ischemic Stroke ◽

Neurite Outgrowth ◽

Radical Scavenging Activity ◽

Radical Scavenging ◽

Iodoacetic Acid ◽

Biological Evaluation ◽

Protective Effects ◽

Neuroprotective Effects ◽

Design Synthesis

Background: Thrombolysis and endovascular thrombectomy acted as two mainly therapeutic strategies for the ischemic stroke in clinic. However, reperfusion injury caused oxidative stress leading overproduction of reactive oxygen species, mitochondrial dysfunction and subsequent cell death. Methods: We designed and synthesized two tetramethylpyrazine-nitrone derivatives (T-003 and T-005) and investigated their abilities for scavenging free radicals and protective effects as well as neurite outgrowth promotion in vitro. Results and Discussion: Both of them showed potent radical-scavenging activity and neuroprotective effects against iodoacetic acid-induced cells injury. Furthermore, T-003 and T-005 significantly promoted neurite outgrowth in PC12 cells. Conclusion: Our results suggest that compound T-003 and T-005 could be potent antioxidants for the treatment of neurological disease, particularly ischemic stroke.

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Phytochemical characterization of phenolics by LC-MS/MS and biological evaluation of Ajuga orientalis from Turkey

Bangladesh Journal of Pharmacology ◽

10.3329/bjp.v10i3.23500 ◽

2015 ◽

Vol 10 (3) ◽

pp. 639 ◽

Cited By ~ 6

Author(s):

Fatih Göger ◽

Yavuz Bülent Köse ◽

Gamze Göger ◽

Fatih Demirci

Keyword(s):

Radical Scavenging Activity ◽

Radical Scavenging ◽

Biological Evaluation ◽

Trolox Equivalent Antioxidant Capacity ◽

Bacterial Strains ◽

Trolox Equivalent ◽

Anticandidal Activity ◽

Antioxidant And Antimicrobial Activity ◽

Mic Value

The aim of this study was to reveal the phytochemical constituents, antioxidant and antimicrobial activity of Ajuga orientalis. According to the antimicrobial results, the methanol extract of A. orientalis showed a MIC value of 312.5 µg/mL against the tested pathogenic bacterial strains. Anticandidal activity of extract was found as 156.3 µg/mL both against Candida albicans and C. parapsilosis strains. Whereas the extract was more effective against C. tropicalis with the MIC value of 78.1 µg/mL. The in vitro DPPH radical scavenging activity of the extract was determined as IC50=0.4 ± 0.02 mg/mL whereas the standard BHT IC50 was 0.01 ± 0.00 mg/mL. Trolox Equivalent Antioxidant Capacity (TEAC) of extract was determined 1.3 mM TEAC, while BHT, 1.9 mM TEAC.

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Protective effect of Aurelia aurita against free radicals and streptozotocin-induced diabetes

Bangladesh Journal of Pharmacology ◽

10.3329/bjp.v13i3.36907 ◽

2018 ◽

Vol 13 (3) ◽

pp. 287 ◽

Cited By ~ 1

Author(s):

Mallikarjuna Rao Talluri ◽

Alekhya Ketha ◽

Ganga Rao Battu ◽

Rajananda Swamy Tadi ◽

Vinay Bharadwaj Tatipamula

Keyword(s):

Free Radicals ◽

Radical Scavenging Activity ◽

Radical Scavenging ◽

Aurelia Aurita ◽

Biologically Active ◽

Chemical Profiling ◽

Streptozotocin Induced Diabetes ◽

Anti Oxidant ◽

Profiling Analysis

The present work was carried out to identify the anti-oxidant and anti-diabetic activities of Aurelia aurita. The chemical profiling analysis showed that it possess different biologically active secondary metabolites like phenols, alakoids, steroids etc. The methanolic extract showed different free radical scavenging activity as ascorbic acid with IC50 values 202, 205, 153 µg on DPPH, hydroxyl and superoxide free radicals. The extract significantly reduced the hyperglycemic conditions with percentage of reduction 18.7 ± 1.3 to 53.5 ±1.5 of streptozotocin-induced animals and the positive result of in-vitro aldose reductase enzyme inhibition with IC50 value 163 µg suggests that A. aurita have potential to cure the diabetic complications.

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