scholarly journals Diazole and triazole derivatives of castor oil extract: synthesis, hypoglycemic effect, antioxidant potential and antimicrobial activity

2020 ◽  
Vol 71 (4) ◽  
pp. 378
Author(s):  
F. Taieb Brahimi ◽  
F. Belkhadem ◽  
B. Trari ◽  
A. A. Othman
Keyword(s):  
Castor Oil ◽  
Amylase Activity ◽  
Antioxidant Properties ◽  
Methyl Ricinoleate ◽  
Oil Seeds ◽  
Triazole Derivatives ◽  
Antifungal Effects ◽  
Oil Extract ◽  
Antibacterial And Antifungal ◽  
Derivatives Of

The ricinoleate triglyceride was extracted from castor-oil seeds grown in Algeria and isolated by catalytically methanolyse to methyl ricinoleate. Six diazole and triazole derivatives of ricinoleic acid were synthesized and characterized: 1,3,4-oxadiazole-5-thione (4); 1,3,4-thiadiazole-5-thione (5); 4-N-amino-1,2,4-triazole-5-thiol (7); 1,2,4-triazole-5-thione (9); 5-amino-1,3,4-oxadiazole (10) and 5-amino-1,3,4-thiadiazole (11). The antibacterial and antifungal screening data of synthesized compounds showed appreciable inhibition and among them, 5, 7 and 8 showed more inhibition on Gram positive Enterococcus faecalis than reference ampiciline; while compounds 1, 7, 8, 10 and 11 showed competitive antifungal effects compared to reference amphotericin B. In addition, all synthesized compounds (1-11) showed competitive antioxidant properties, particularly compounds 7 at 125, 250, 500 and 1000 μg/mL and compounds 4, 5 and 9 at a concentration of 1000 μg/mL. The intermediate compounds 1, 2 and 8 showed anti-α-amylase activity at various concentrations in the range of IC50 = (120.25 ± 1.17 - 130.42 ± 2.48). Oxadiazole 4 showed the best α-amylase inhibition by 78.5% at a concentration of 1000 μg/mL.

scholarly journals Review of antibacterial and antifungal activity of 1,2,4-triazole derivatives

2018 ◽  
pp. 63-68
Author(s):  
Т. О. Samura
Keyword(s):  
Antifungal Activity ◽  
Heterocyclic Compounds ◽  
Practical Importance ◽  
Complex Compounds ◽  
Biologically Active ◽  
Alkyl Aryl ◽  
Triazole Derivatives ◽  
Antimicrobial And Antifungal Activity ◽  
Antibacterial And Antifungal ◽  
Derivatives Of

Derivatives of 1,2,4-triazole is a very  perspective class of heterocyclic compounds which have high therapeutic effectiveness. The main direction of research on these derivatives are antifungal, antiviral, antibacterial, soothing, hypnotic, anticonvulsant, anti-inflammatory and other activities. The aim was to analyze literature data and generalize recent advances in the study of antimicrobial and antifungal action of 1,2,4-triazole derivatives which can help to create new biologically active substances of this type of activity. Bibliosemantical method, systems thinking and the results of our own research were used in the work. The results of the literature review of antimicrobial and antifungal activity among new alkyl, aryl and heteryl derivatives of 1,2,4-triazole and among complex compounds, which contain 1,2,4-triazole are as ligands were analyzed and systematized. Some dependence of this type of activity on specialty of chemical structure of heterocyclic system derivatives was specified. Perspective of purposeful synthesis of new derivatives of 1,2,4-triazole and products of their transformation as available object for studying biological activity and expanding knowledge about antimicrobial and antifungal activity of this class of heterocyclic compounds were shown with informational analysis. Topicality and practical importance of finding biologically active compounds and receiving biologically active substance by synthesis of new derivatives of 1,2,4-triazole with high antimicrobial activity in relation to gram-negative and gram-positive bacteria were demonstrated.

scholarly journals Study of the Biological Activity of Alkyl Derivatives of Tetrahydroisoquinolines

2021 ◽  
pp. 238-246
Author(s):  
Umida Khamidova ◽  
Ekaterina Terenteva ◽  
Mukaddas Umarova ◽  
Jaloliddin Abdurakhmanov ◽  
Sabirdjan Sasmakov ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Biological Activity ◽  
Cancer Cells ◽  
Cytotoxic Effect ◽  
Normal Cells ◽  
Alkyl Derivatives ◽  
Antifungal Effects ◽  
Low Toxicity ◽  
Antibacterial And Antifungal ◽  
Derivatives Of

A row of 1-alkyne (C6-C17) derivatives against tetrahydroisoquinoline have been synthesized. 1-alkyne (C6-C17) derivatives cytotoxicity against three lines of cancer cells and two lines of normal cells was studied. It was found that 1-tridecyl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline exhibits a high cytotoxic effect with low toxicity to healthy cells. Antimicrobial activity of 1-alkyne (C6-C17) derivatives against 5 strains of bacteria and fungus was studied. It has been found that 1-nonyl-6,7-dimethoxy-1,3,4-tetrahydroisoquinoline exhibits strong antibacterial and antifungal effects.

Synthesis, characterization and biological activities of 1,3,4-oxadiazole derivatives of nalidixic acid and their copper complexes

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Nalidixic Acid ◽  
Copper Complexes ◽  
Biological Activities ◽  
Bidentate Coordination ◽  
Antibacterial And Antifungal Activities ◽  
Elemental Analyses ◽  
Oxadiazole Derivatives ◽  
Antibacterial And Antifungal ◽  
Derivatives Of ◽  
Substituted 1

A series of novel 1, 3, 4-oxadiazole analogues was synthesized from cyclization of hydrazones of substituted 1-ethyl-1,4-dihydro-7-methyl-4-oxo-1,8-naphthyridine-3-carbohydrazides were prepared from nalidixic acid. The structures of synthesized oxadiazole derivatives and their copper complexes were elucidated on the basis of FTIR, elemental analyses, 1H-NMR and atomic absorption spectral analysis. It was observed from spectral data that metal ligand ratio was 1:1 in all copper complexes and they were bidentate, coordination was found to be done through oxygen of 4-oxo group and nitrogen of oxadiazole ring. The synthesized compounds were further evaluated with biological activities and compared with parent hydrazones. Copper complexes possess antibacterial and antifungal activities better than the oxadiazoles while they have better antioxidant activity then copper complexes. Parent hydrazones were better in all biological activities than synthesized oxadiazoles.

Copper-catalyzed Convenient Synthesis and SAR Studies of Substituted-1,2,3-triazole as Antimicrobial Agents

2018 ◽  
Vol 16 (1) ◽  
pp. 3-10
Author(s):  
Aniket P. Sarkate ◽  
Kshipra S. Karnik ◽  
Pravin S. Wakte ◽  
Ajinkya P. Sarkate ◽  
Ashwini V. Izankar ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antifungal Activity ◽  
Antimicrobial Agents ◽  
Cycloaddition Reaction ◽  
Dipolar Cycloaddition ◽  
One Pot ◽  
Triazole Derivatives ◽  
Sar Studies ◽  
Convenient Synthesis ◽  
Antibacterial And Antifungal

Background:A novel copper-catalyzed synthesis of substituted-1,2,3-triazole derivatives has been developed and performed by Huisgen 1,3-dipolar cycloaddition reaction of azides with alkynes. The reaction is one-pot multicomponent.Objective:We state the advancement and execution of a methodology allowing for the synthesis of some new substituted 1,2,3-triazole analogues with antimicrobial activity.Methods:A series of triazole derivatives was synthesized by Huisgen 1,3-dipolar cycloaddition reaction of azides with alkynes. The structures of the synthesized compounds were elucidated and confirmed by 1H NMR, IR, MS and elemental analysis. All the synthesized compounds were tested for their antimicrobial activity against a series of strains of Bacillus subtilis, Staphylococcus aureus and Escherichia coli for antibacterial activity and against the strains of Candida albicans, Aspergillus flavus and Aspergillus nigar for antifungal activity, respectively.Results and Conclusion:From the antimicrobial data, it was observed that all the newly synthesized compounds showed good to moderate level of antibacterial and antifungal activity.

Synthesis, Antimicrobial Evaluation and Docking Study of Novel Thiosemicarbazone clubbed with 1,2,3-Triazoles

2020 ◽  
Vol 16 ◽  
Author(s):  
Adinath D. Badar ◽  
Shubham M. Sulakhe ◽  
Mahesh B. Muluk ◽  
Naziya N. M. A. Rehman ◽  
Prashant P. Dixit ◽  
...  
Keyword(s):  
Binding Affinity ◽  
Biological Activities ◽  
Dna Gyrase ◽  
Docking Study ◽  
Antimicrobial Activities ◽  
Diffusion Method ◽  
Molecular Docking Study ◽  
Triazole Derivatives ◽  
Antibacterial And Antifungal

Background: Thiosemicarbazone, 1,2,3-triazole and their derivatives received great pharmaceutical importance due to their prominent biological activities. In the present study, the molecular hybrid thiosemicarbazone-1,2,3-triazoles derivatives were synthesized and screened for their antimicrobial activities. Methods: A series of thiosemicarbazone clubbed with 1,2,3-triazole derivatives were synthesized via click chemistry approach in good yields. The structures of synthesized compounds were assigned by their spectral data. The in vitro antimicrobial activity was performed by the agar well diffusion method. A molecular docking study was performed to identify the possible mode of action of synthesized derivatives. Results: The compounds 5d, 5h, 5i and 5k have exhibited excellent antimicrobial activities against both antibacterial and antifungal pathogens. The active thiosemicarbazone-1,2,3-triazole derivatives have shown excellent binding affinity towards DNA gyrase. Conclusion: The molecular hybrid thiosemicarbazone-1,2,3-triazole derivatives were synthesized. The newly synthesized compounds were evaluated for their antimicrobial activities. Few of the thiosemicarbazone-1,2,3-triazoles derivatives have exhibited good antimicrobial activities. They have been shown excellent binding affinity towards DNA gyrase.

scholarly journals Avocado-Derived Biomass: Chemical Composition and Antioxidant Potential

Proceedings ◽  
2020 ◽  
Vol 70 (1) ◽  
pp. 100
Author(s):  
Minerva C. García-Vargas ◽  
María del Mar Contreras ◽  
Irene Gómez-Cruz ◽  
Juan Miguel Romero-García ◽  
Eulogio Castro
Keyword(s):  
Chemical Composition ◽  
Phenolic Content ◽  
Antioxidant Properties ◽  
Total Phenolic ◽  
Nutritional Properties ◽  
Aqueous Fraction ◽  
Extraction Solvent ◽  
Main Components ◽  
A Minor ◽  
Derivatives Of

Avocado has become fashionable due to its great organoleptic and nutritional properties. It is consumed as a fresh product and it is also processed to obtain salad oil and guacamole. In all cases, the only usable portion is the pulp. Therefore, to be a more sustainable and profitable agribusiness, it is important to recognize which compounds from the peel and the stone waste can be converted into valuable bio-products. Therefore, their chemical composition was determined according to the National Renewable Energy Laboratory, the total phenolic content by the Folin-Ciocalteu method and the antioxidant properties by the FRAP and TEAC assays. The main components of the peel and stone were acid-insoluble lignin (35.0% and 15.3%, respectively), polymeric sugars (23.6% and 43.9%, respectively), and the aqueous extractives (15.5% and 16.9%, respectively). Both biomasses contain lipids and protein, but a minor proportion (<6%). The valorization of lignin and sugars is of interest given the high content; stones are a rich source of glucose (93.2% of the polymeric fraction), which could be used to obtain biofuels or derivatives of interest. The extractive fraction of the peel contained the highest number of phenolic compounds (4.7 g/100 g biomass), mainly concentrated in the aqueous fraction (i.e., 87%) compared to the ethanol one, which was subsequently extracted. It correlated with major antioxidant activity and, therefore, the peel can be applied to obtain antioxidants and water can be used as an environmentally friendly extraction solvent.

scholarly journals Antibacterial and antifungal effects of fired scallop shell - glass composites fabricated by a simple process

2008 ◽  
Vol 116 (Supplement) ◽  
pp. S1-S4 ◽  
Author(s):  
Yoshihiro MIHARA ◽  
Tomoya TAKADA ◽  
Naotsugu UNO ◽  
Iwao TOGASHI ◽  
Keisuke SUGIMOTO
Keyword(s):  
Scallop Shell ◽  
Simple Process ◽  
Glass Composites ◽  
Antifungal Effects ◽  
Antibacterial And Antifungal

scholarly journals Kinetic and regulatory properties of cytosolic pyruvate kinase from germinating castor oil seeds

1991 ◽  
Vol 279 (2) ◽  
pp. 495-501 ◽  
Author(s):  
F E Podestá ◽  
W C Plaxton
Keyword(s):  
Pyruvate Kinase ◽  
Castor Oil ◽  
Mixed Type ◽  
Competitive Inhibition ◽  
Ricinus Communis ◽  
Cytosolic Ph ◽  
Oil Seeds ◽  
Saturation Kinetics ◽  
Regulatory Properties

The kinetic and regulatory properties of cytosolic pyruvate kinase (PKc) isolated from endosperm of germinating castor oil seeds (Ricinus communis L.) have been studied. Optimal efficiency in substrate utilization (in terms of Vmax/Km for phosphoenolpyruvate or ADP) occurred between pH 6.7 and 7.4. Enzyme activity was absolutely dependent on the presence of a bivalent and a univalent metal cation, with Mg2+ and K+ fulfilling this requirement. Mg2+ binding showed positive and negative co-operativity at pH 6.5 (h = 1.6) and pH 7.2 (h = 0.69) respectively. Hyperbolic saturation kinetics were observed with phosphoenolpyruvate (PEP) and K+, whereas ADP acted as a mixed-type inhibitor over 1 mM. Glycerol (10%, v/v) increased the S0.5(ADP) 2.3-fold and altered the pattern of nucleotide binding from hyperbolic (h = 1.0) to sigmoidal (h = 1.79) without modifying PEP saturation kinetics. No activators were identified. ATP, AMP, isocitrate, 2-oxoglutarate, malate, 2-phosphoglycerate, 2,3-bisphosphoglycerate, 3-phosphoglycerate, glycerol 3-phosphate and phosphoglycolate were the most effective inhibitors. These metabolites yielded additive inhibition when tested in pairs. ATP and 3-phosphoglycerate were mixed-type inhibitors with respect to PEP, whereas competitive inhibition was observed for other inhibitors. Inhibition by malate, 2-oxoglutarate, phosphorylated triose sugars or phosphoglycolate was far more pronounced at pH 7.2 than at pH 6.5. Although 32P-labelling studies revealed that extensive phosphorylation in vivo of soluble endosperm proteins occurred between days 3 and 5 of seed germination, no alteration in the 32P-labelling pattern of 5-day-germinated endosperm was observed after 30 min of anaerobiosis. Moreover, no evidence was obtained that PKc was a phosphoprotein in aerobic or anoxic endosperms. It is proposed that endosperm PKc activity of germinating castor seeds is enhanced after anaerobiosis through concerted decreases in ATP levels, cytosolic pH and concentrations of several key inhibitors.

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