scholarly journals Antioxidant, biofilm inhibition and mutagenic activities of newly substituted fibrates

2021 ◽  
Vol 18 (6) ◽  
pp. 1227-1234
Author(s):  
Asma Sheikh ◽  
Zia-Ur-Rehman ◽  
Muhammad Imran ◽  
Zaid Mahmood
Keyword(s):  
Mass Spectrometry ◽  
13C Nmr ◽  
Biofilm Inhibition ◽  
Mutagenicity Assay ◽  
Anti Oxidant ◽  
Chloro Group ◽  
Electron Withdrawing Group ◽  
Inhibition Studies ◽  
Methyl Propanoate

Purpose: A series of benzylidene-2-(4-bromophenoxy)-2-methyl propane hydrazides (1-10) were synthesized and assay them for their biofilm inhibition, antioxidant and mutagenic. Methods: All derivatives were prepared by condensation of various substituted benzaldehyde and acetophenones with 2-(4-bromorophenoxy)-2-methyl propane hydrazide, which was itself prepared by hydrazinolysis of ethyl-2-(4-bromophenoxy)-2-methyl propanoate and were characterized by FTIR, 1H NMR 13C NMR, mass spectrometry. They were screened for their in-vitro anti-oxidant, biofilm inhibition and mutagenicity by established methods. Results: Anti-oxidant results revealed that the electron donating group enhanced the scavenging ability of the compounds as seen in compounds 4b, 4h and 4i. In biofilm inhibition studies, all compounds were more active against Gram –ive bacterial strain when compared to gram +ive strain. The mutagenicity assay results indicate that the compound having chloro group substitution is mutagenic. Conclusion: The benzylidine compounds of 2-(4-bromophenoxy)-2-methyl hydrazide possessing electron donating substituents exhibit superior activities to the electron withdrawing group substituents.

scholarly journals Synthesis and Bio-Evaluation of Natural Butenolides-Acrylate Conjugates

Molecules ◽  
2019 ◽  
Vol 24 (7) ◽  
pp. 1304 ◽  
Author(s):  
Longzhu Bao ◽  
Shuangshuang Wang ◽  
Di Song ◽  
Jingjing Wang ◽  
Xiufang Cao ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Antifungal Activity ◽  
13C Nmr ◽  
Pathogenic Fungi ◽  
Phytopathogenic Fungi ◽  
Gibberella Zeae ◽  
Ionization Mass ◽  
Activity Screening ◽  
In Vitro Antifungal Activity

A series of novel 3-aryl-4-hydroxy-2(5H) furanone-acrylate hybrids were designed and synthesized based on the natural butenolides and acrylates scaffolds. The structures of the prepared compounds were characterized by 1H-NMR, 13C-NMR and electrospray ionization mass spectrometry (ESI-MS), and the bioactivity of the target compounds against twelve phytopathogenic fungi was investigated. The preliminary in vitro antifungal activity screening showed that most of the target compounds had moderate inhibition on various pathogenic fungi at the concentration of 100 mg·L−1, and presented broad-spectrum antifungal activities. Further studies also indicated that compounds 7e and 7k still showed some inhibitory activity against Pestallozzia theae, Sclerotinia sclerotiorum and Gibberella zeae on rape plants at lower concentrations, which could be optimized as a secondary lead for further research.

Design and Synthesis of some novel 3-benzylidene-1H-benzo [4,5]imidazo[2,1-c] [1,4]oxazine-1,4(3H)-dione derivatives and evaluation of their biological activity

2021 ◽  
Vol 25 (11) ◽  
pp. 157-169
Author(s):  
Ch. Sunitha ◽  
G. Brahmeshwari
Keyword(s):  
Mass Spectrometry ◽  
Biological Activity ◽  
1H Nmr ◽  
Elemental Analysis ◽  
13C Nmr ◽  
The Other ◽  
Good Activity ◽  
Design And Synthesis ◽  
Anti Oxidant ◽  
Anti Fungal

A novel series of 3-arylbenzylidene-1H-benzo[4,5] imidazo[2,1-c][1,4]oxazine-1,4(3H)-dione (4a-l) was synthesized in moderate to good yields. The structures of the newly synthesized compounds were confirmed by 1H NMR, 13C NMR mass spectrometry and elemental analysis. The synthesized compounds were evaluated for their anti-bacterial and anti-oxidant activities. Among all the derivatives tested, the compound 3-(3,5- dimethoxy benzylidene)-1H-benzo [4,5]imidazo[2,1- c][1,4]oxazine-1,4-(3H)-dione showed more potent activity and 3-(4-methoxybenzylidene)-1H benzo[4,5] imidazo[2,1-c][1,4]oxazine-1,4(3H)-dion exhibited good activity as compared to standard streptomycin. The anti-fungal activity reveals that the compound 3- (3,5-dimethoxy benzylidene)-1H-benzo[4,5]imidazo [2,1-c][1,4]oxazine-1,4-(3H)-dione showed more promising activity as compared to standard Itrazole. The remaining compounds showed moderate to poor activity. Similarly, the anti-oxidant activity results revealed that the compound 3-(3,5-dimethoxy benzylidene)-1H-benzo [4,5] imidazo[2,1-c][1,4] oxazine-1,4-(3H)-dione exhibited potent activity as compared to the other tested compounds.

Synthesis and Evaluation of Chalcone and its Derivatives as Potential Anticholinergic Agents

2019 ◽  
Vol 16 (3) ◽  
pp. 322-332
Author(s):  
Shahzad Murtaza ◽  
Khoula Zubair Mir ◽  
Adina Tatheer ◽  
Raja Summe Ullah
Keyword(s):  
Mass Spectrometry ◽  
13C Nmr ◽  
Radical Scavenging ◽  
Structural Similarity ◽  
Docking Studies ◽  
Antioxidant Potential ◽  
H Nmr ◽  
Methods Of Synthesis ◽  
Anti Oxidant ◽  
Inhibition Potency

Background: Structural similarity in Chalcone and Pyrazoline brought our intention for the analysis of such compounds. This study involved the synthesis of chalcones and their pyrazoline derivatives and their screening as cholinesterase inhibitors. The newly synthesized compounds were also investigated for their antioxidant potential. </P><P> Methods: Chalcones were synthesized by well-established methods of synthesis and their structural elucidation was carried out by H-NMR, 13C-NMR, Mass spectrometry and FTIR. For the determination of inhibition potency of synthesized compounds, spectrophotometric method was applied whereas, DPPH free radical scavenging method was used to check the antioxidant ability. </P><P> Results: Chalcones and their pyrazoline derivatives were synthesized and characterised by 1HNMR, 13C-NMR, Mass spectrometry and FTIR. The compounds were screened for their anti- Alzheimer activity, which exhibited that compounds 1g, 1c and 1h, 1g showed strong inhibitory potency against acetylcholinesterase and butyrylcholinesterase, respectively. DPPH radical scavenging method was applied to check anti-oxidant potential of synthesized compounds and results explored that among all the synthesized compounds only compounds 1c and 1b showed strong scavenging potential. </P><P> Conclusion: Chalcone and their pyrazoline derivatives were synthesized and screened for their anti-Alzheimer and antioxidant potential. The experimental results of anti-Alzheimer activity were compared with molecular docking studies, which showed that compounds 1g, 1c and 1h, 1g were active against AChE and BChE, respectively. Among the synthesized compounds 1c and 1b were found to be most potent antioxidants. These results suggest that compound 1b, 1c, 1g and 1h may further be explored for further developments.

scholarly journals Tooth-Binding Micelles for Dental Caries Prevention

2009 ◽  
Vol 53 (11) ◽  
pp. 4898-4902 ◽  
Author(s):  
Fu Chen ◽  
Xin-Ming Liu ◽  
Kelly C. Rice ◽  
Xue Li ◽  
Fang Yu ◽  
...  
Keyword(s):  
Caries Prevention ◽  
Tooth Surface ◽  
Hydrodynamic Diameter ◽  
Local Concentration ◽  
Binding Ability ◽  
Biofilm Inhibition ◽  
Tooth Surfaces ◽  
Delivery Platform ◽  
Inhibition Studies

ABSTRACT Maintenance of the effective local concentration of antimicrobials on the tooth surface is critical for the management of cariogenic bacteria in the oral cavity. We report on the design of a simple tooth-binding micellar drug delivery platform that would effectively bind to tooth surfaces. To achieve tooth-binding ability, the chain termini of biocompatible Pluronic copolymers were modified with a biomineral-binding moiety (i.e., alendronate). The micelles formulated with this polymer were shown to be able to swiftly (<1 min) bind to hydroxyapatite (HA; a model tooth surface) and gradually release the encapsulated model antimicrobial (farnesol). These tooth-binding micelles were negatively charged and had an average effective hydrodynamic diameter of less than 100 nm. In vitro biofilm inhibition studies demonstrated that the farnesol-containing tooth-binding micelles were able to provide significantly stronger inhibition of Streptococcus mutans UA159 biofilm formation on HA discs than the untreated blank control micelles (P < 0.0001). Upon further optimization, this delivery platform could provide an effective tool for caries prevention and treatment.

Protective Effect of Vitamin E on Immune Triggered, Granulocyte Mediated Endothelial Injury

1984 ◽  
Vol 51 (01) ◽  
pp. 089-092 ◽  
Author(s):  
M A Boogaerts ◽  
J Van de Broeck ◽  
H Deckmyn ◽  
C Roelant ◽  
J Vermylen ◽  
...  
Keyword(s):  
Vitamin E ◽  
Protective Effect ◽  
Umbilical Vein ◽  
Endothelial Damage ◽  
Endothelial Injury ◽  
Mediated Effects ◽  
Anti Oxidant ◽  
Endothelial Cell Cultures ◽  
Vitro Model

SummaryThe effect of alfa-tocopherol on the cell-cell interactions at the vessel wall were studied, using an in vitro model of human umbilical vein endothelial cell cultures (HUEC). Immune triggered granulocytes (PMN) will adhere to and damage HUEC and platelets enhance this PMN mediated endothelial injury. When HUEC are cultured in the presence of vitamin E, 51Cr-leakage induced by complement stimulated PMN is significantly decreased and the enhanced cytotoxicity by platelets is completely abolished (p <0.001).The inhibition of PMN induced endothelial injury is directly correlated to a diminished adherence of PMN to vitamin E- cultured HUEC (p <0.001), which may be mediated by an increase of both basal and stimulated endogenous prostacyclin (PGI2) from alfa-tocopherol-treated HUEC (p <0.025). The vitamin E-effect is abolished by incubation of HUEC with the irreversible cyclo-oxygenase inhibitor, acetylsalicylic acid, but the addition of exogenous PGI2 could not reproduce the vitamin E-mediated effects.We conclude that vitamin E exerts a protective effect on immune triggered endothelial damage, partly by increasing the endogenous anti-oxidant potential, partly by modulating intrinsic endothelial prostaglandin production. The failure to reproduce vitamin E-protection by exogenously added PGI2 may suggest additional, not yet elucidated vitamin E-effects on endothelial metabolism.

In-Vitro Anti-oxidant And Antimicrobial Study Of Ficus hispida

2015 ◽  
Vol 3 (2) ◽  
pp. 153-166
Author(s):  
Atanu Chatterjee ◽  
Jayita Mondal ◽  
Rudranil Bhowmik ◽  
Anshuman Bhattachayra ◽  
Hirak Roy ◽  
...  
Keyword(s):  
Antimicrobial Study ◽  
Anti Oxidant ◽  
Ficus Hispida

Synthesis and Spectral Characterization of New S-Alkylated 1,2,4-Triazoles as Potential Biological Agents

2017 ◽  
Vol 68 (10) ◽  
pp. 2436-2439
Author(s):  
Stefania Felicia Barbuceanu ◽  
Laura Ileana Socea ◽  
Constantin Draghici ◽  
Elena Mihaela Pahontu ◽  
Theodora Venera Apostol ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Spectral Data ◽  
1H Nmr ◽  
Elemental Analysis ◽  
13C Nmr ◽  
Ethyl Bromide ◽  
Spectral Characterization ◽  
Basic Medium ◽  
Phenacyl Bromide

In the work we presented the behavior of 5-(4-(4-X-phenylsulfonyl)phenyl)-4-(n-propyl)-2H-1,2,4-triazole-3(4H)-thiones (X= Cl or Br) with some alkylation agents. Thus, new S-alkylated 1,2,4-triazole derivatives were synthesized by reaction of the corresponding 1,2,4-triazole-3-thione derivatives with different �-halogenated compounds (ethyl bromide, ethyl chloroacetate or phenacyl bromide), in basic medium. The structures of synthesized compounds were elucidated by spectral data (1H-NMR, 13C-NMR, mass spectrometry) and elemental analysis.

Mycobacterial DNA GyrB Inhibitors: Ligand Based Pharmacophore Modelling and In Vitro Enzyme Inhibition Studies

2014 ◽  
Vol 14 (17) ◽  
pp. 1990-2005 ◽  
Author(s):  
Shalini Saxena ◽  
Janupally Renuka ◽  
Variam Jeankumar ◽  
Perumal Yogeeswari ◽  
Dharmarajan Sriram
Keyword(s):  
Enzyme Inhibition ◽  
Pharmacophore Modelling ◽  
Inhibition Studies

α-Glucosidase Inhibition, Antioxidant and Docking Studies of Hydroxycoumarins and their Mono and Bis O-alkylated/acetylated Analogs

2018 ◽  
Vol 15 (2) ◽  
pp. 127-135 ◽  
Author(s):  
Parvesh Singh ◽  
Nomandla Ngcoya ◽  
Ramgopal Mopuri ◽  
Nagaraju Kerru ◽  
Neha Manhas ◽  
...  
Keyword(s):  
In Silico ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Catalytic Site ◽  
Docking Simulations ◽  
In Silico Docking ◽  
Anti Oxidant

Background: Diabetes Mellitus (DM) is a complex metabolic disease illustrated by abnormally high levels of plasma glucose or hyperglycaemia. Accordingly, several α-glucosidase inhibitors have been developed for the treatment of diabetes and other degenerative disorders. While, a coumarin ring has the privilege to represent numerous natural and synthetic compounds with a wide spectrum of biological activities e.g. anti-cancer, anti-HIV, anti-viral, anti-malarial, anti-microbial, anti-convulsant, anti-hypertensive properties. Besides this, coumarins have also shown potential to inhibit α-glucosidase leading to a generation of new promising antidiabetic agents. However, the testing of O-substituted coumarins for α-glucosidase inhibition has evaded the attention of medicinal chemists. Methods: For O-alkylation/acetylation reactions, the hydroxyl coumarins (A-B) initially activated by K2CO3 in dry DMF were reacted with variedly substituted haloalkanes at room temperature under nitrogen. The synthesized compounds were tested for their α-glucosidase (from Saccharomyces cerevisiae) inhibitory activity and anti-oxidant activity using DPPH radical scavenging activity. In silico docking simulations were conducted using CDocker module in DS (Accelrys) to explore the binding modes of the representative compounds in the catalytic site of α-glucosidase. Results: All the coumarin analogues (A1, B1, A2-A10, B2-B8) including their precursors (A-B) were evaluated for their in vitro α-glucosidase inhibition using acarbose as a standard inhibitor. All the mono O-alkylated coumarins (except A1) showed significant (p <0.05) α-glucosidase inhibition relative to the hydroxyl coumarin (A) with IC50 values ranging between 11.084±0.117 to 145.24± 29.22 µg/mL. Compound 7-(benzyloxy)-4, 5-dimethyl-2H-chromen-2-one (A9) bearing a benzyl group (Ph-CH2-) at position 7 showed a remarkable (p <0.05) increase in the activity (IC50 = 11.084±0.117 µg/mL), almost four-fold more than acarbose (IC50 = 40.578±5.999 µg/mL). The introduction of –NO2 group dramatically improved the anti-oxidant activity of coumarin, while the O-alkylation/acetylation decreased the activity. Conclusion: The present study describes the synthesis of functionalized coumarins and their evaluation for α-glucosidase inhibition and antioxidant activity under in vitro conditions. Based on IC50 data, the mono O-alkylated coumarins were observed to be stronger inhibitors of α-glucosidase with respect to their bis O-alkylated analogues. Coumarin (A9) bearing O-benzyloxy group displayed the strongest α-glucosidase inhibition, even higher than the standard inhibitor acarbose. The coumarin (A10) bearing –NO2 group showed the highest anti-oxidant activity amongst the synthesized compounds, almost comparable to the ascorbic acid. Finally, in silico docking simulations revealed the role of hydrogen bonding and hydrophobic forces in locking the compounds in catalytic site of α-glucosidase.

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