scholarly journals SYNTHESIS, CHARACTERIZATION AND ANTIMICROBIAL ACTIVITY OF SOME NOVEL 3,4-DISUBSTITUTED PYRAZOLE DERIVATIVES

2019 ◽  
pp. 129-133
Author(s):  
GANESH AKULA ◽  
KAUSHAL K CHANDRUL ◽  
BHIKSHAPATHI DVRN
Keyword(s):  
Antimicrobial Activity ◽  
Hydrazine Hydrate ◽  
Antimicrobial Agents ◽  
Antibacterial Properties ◽  
Acid Methyl Ester ◽  
Dimethyl Acetal ◽  
Inhibitory Effect ◽  
Dimethyl Formamide ◽  
Highly Sensitive ◽  
Substituted Pyrazoles

Objective: The objective of the current work was to synthesize a series of 3,4-substituted pyrazoles from the cyclization of substituted aryl ethanone and hydrazine hydrate in a two-step process and screen the derivatives for their antimicrobial activity. Methods: The title compounds were derived from the condensation of ethanone intermediate with N, N-Dimethyl formamide-dimethyl acetal and hydrazine hydrate. Ethanone intermediate synthesized from substituted methyl phenylacetate in the presence of potassium t-butoxide with 6-methyl pyridine-2-carboxylic acid methyl ester. Results: The final products were characterized by detailed spectral analysis using Mass, Nuclear Magnetic Resonance, and Infra Red spectroscopy. All the compounds (4a-4j) showed significant antibacterial properties on both Gram-positive and Gram-negative bacteria. Interestingly, the selected microbes were found to be highly sensitive for compound 4a, 4c, 4d, 4h, and 4i. The molecules are also antifungal in nature, and they have a significant inhibitory effect on the growth of Candida albicans and Aspergillus niger. Conclusion: The results suggest that the developed derivatives bearing the pyrazole nucleus could be the lead structures for the development of antimicrobial agents for fatal infections.

scholarly journals Synthesis of progesterone heterocyclic derivatives of potential antimicrobial activity

2008 ◽  
Vol 58 (1) ◽  
pp. 29-42 ◽  
Author(s):  
Rafat Mohareb ◽  
Hanaa Hana
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Dimethyl Acetal ◽  
Dimethyl Formamide ◽  
Gram Positive Bacteria ◽  
Heterocyclic Derivatives ◽  
Bacteria And Fungi ◽  
Derivatives Of ◽  
Potential Antimicrobial Activity

Synthesis of progesterone heterocyclic derivatives of potential antimicrobial activityThe aim of this work was to synthesize steroidal heterocycles and to elucidate the potential role of these compounds as antimicrobial agents. The synthesis of steroidal heterocycles containing the pyrazole, isoxazole, thiazole, pyrane, pyridine, pyridazine, or benzopyrane ring attached to the pregnene nucleus is reported. Progesterone (1) reacts with dimethyl formamide dimethyl acetal to form enamine2. Heterocyclization of2with hydrazines, hydroxylamine, glycine, ethyl acetoacetate or cyanomethylene afforded novel steroidal heterocyclic derivatives. Thein vitroantimicrobial evaluation showed that all synthesized compounds show activity against the used strains of Gram positive bacteria and fungi.

scholarly journals Synthesis and Antimicrobial Activity of Silver-Doped Hydroxyapatite Nanoparticles

2013 ◽  
Vol 2013 ◽  
pp. 1-10 ◽  
Author(s):  
Carmen Steluta Ciobanu ◽  
Simona Liliana Iconaru ◽  
Mariana Carmen Chifiriuc ◽  
Adrian Costescu ◽  
Philippe Le Coustumer ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Pathogenic Bacteria ◽  
Antimicrobial Agents ◽  
Antibacterial Properties ◽  
Major Health Problem ◽  
Major Health ◽  
Wall Structures ◽  
Nanocrystalline Hydroxyapatite ◽  
Qualitative Assay ◽  
Antibacterial And Antifungal

The synthesis of nanosized particles of Ag-doped hydroxyapatite with antibacterial properties is of great interest for the development of new biomedical applications. The aim of this study was the evaluation ofCa10−xAgx(PO4)6(OH)2nanoparticles (Ag:HAp-NPs) for their antibacterial and antifungal activity. Resistance to antimicrobial agents by pathogenic bacteria has emerged in the recent years and became a major health problem. Here, we report a method for synthesizing Ag doped nanocrystalline hydroxyapatite. A silver-doped nanocrystalline hydroxyapatite was synthesized at 100°C in deionised water. Also, in this paper Ag:HAp-NPs are evaluated for their antimicrobial activity against Gram-positive and Gram-negative bacteria and fungal strains. The specific antimicrobial activity revealed by the qualitative assay is demonstrating that our compounds are interacting differently with the microbial targets, probably due to the differences in the microbial wall structures.

scholarly journals Antimicrobial Phenolic Compounds from Anabasis Aphylla L

2009 ◽  
Vol 4 (3) ◽  
pp. 1934578X0900400 ◽  
Author(s):  
Hua Du ◽  
Ye Wang ◽  
Xiaojiang Hao ◽  
Chun Li ◽  
Youliang Peng ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Phenolic Compounds ◽  
Benzoic Acid ◽  
Cinnamic Acid ◽  
Antimicrobial Agents ◽  
Inhibitory Concentration ◽  
Control Plant ◽  
Acid Methyl Ester ◽  
Spectrometric Analysis ◽  
Bacterium Bacillus

Bioassay-guided fractionation of an ethyl acetate extract from the aerial parts of Anabasis aphylla, a Chenopodiaceous species widely distributed in the northwest of China, led to the isolation of six phenolic compounds, which were identified by means of spectrometric analysis as 1-(2-hydroxy-4,6-dimethoxyphenyl)-ethanone (1), 3,4-dihydroxy cinnamic acid tetracosyl ester (2), 4-hydroxy-3-methoxy benzoic acid (3), 2-hydroxy benzoic acid (4), 3,4-dihydroxy cinnamic acid methyl ester (5) and 4-hydroxy benzoic acid pentadecane ester (6). These compounds were further screened for their minimum inhibitory concentration (MIC) and median inhibitory concentration (IC50) by use of the microdilution-MTT assay for antimicrobial activity against one Gram-positive bacterium ( Bacillus subtilis), three Gram-negative bacteria ( Agrobacterium tumefaciens, Pseudomonas lachrymans, and Xanthomonas vesicatoria), and one yeast ( Candida albicans). Apart from compound 6, which had no activity against any of the tested microorganisms, the other compounds showed selective inhibitory activity. This is the first report on the antimicrobial activity of the phenolic compounds isolated from A. aphylla. The obtained results provide promising baseline information for the potential use of the extract and some isolated compounds from this plant as antimicrobial agents to control plant and animal diseases.

scholarly journals Algae Polyphenolic Compounds and Modern Antibacterial Strategies: Current Achievements and Immediate Prospects

Biomedicines ◽  
2020 ◽  
Vol 8 (9) ◽  
pp. 342 ◽  
Author(s):  
Natalya N. Besednova ◽  
Boris G. Andryukov ◽  
Tatyana S. Zaporozhets ◽  
Sergey P. Kryzhanovsky ◽  
Tatyana A. Kuznetsova ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Biological Activities ◽  
Antibacterial Properties ◽  
Structural Diversity ◽  
Polyphenolic Compounds ◽  
High Antimicrobial Activity ◽  
Functional Relationships ◽  
Treatment And Prevention ◽  
Polyfunctional Compounds

The increasing drug resistance of pathogenic microorganisms raises concern worldwide and necessitates the search for new natural compounds with antibacterial properties. Marine algae are considered a natural and attractive biotechnological source of novel antibiotics. The high antimicrobial activity of their polyphenolic compounds is a promising basis for designing innovative pharmaceuticals. They can become both a serious alternative to traditional antimicrobial agents and an effective supplement to antibiotic therapy. The present review summarizes the results of numerous studies on polyphenols from algae and the range of biological activities that determine their biomedical significance. The main focus is put on a group of the polyphenolic metabolites referred to as phlorotannins and, particularly, on their structural diversity and mechanisms of antimicrobial effects. Brown algae are an almost inexhaustible resource with a high biotechnological potential for obtaining these polyfunctional compounds. An opinion is expressed that the effectiveness of the antibacterial activity of phlorotannins depends on the methods of their extraction aimed at preserving the phenolic structure. The use of modern analytical tools opens up a broad range of opportunities for studying the metabolic pathways of phlorotannins and identifying their structural and functional relationships. The high antimicrobial activity of phlorotannins against both Gram-positive and Gram-negative bacteria provides a promising framework for creating novel drugs to be used in the treatment and prevention of infectious diseases.

scholarly journals Evaluation of Antibacterial Properties of Different Leaf Extracts of Hyptis suaveolens (L) Poit

2021 ◽  
pp. 40-44
Author(s):  
B. A. Erinle ◽  
A. O. Ajayi ◽  
O. T. Osuntokun
Keyword(s):  
Antimicrobial Activity ◽  
Folk Medicine ◽  
Antibacterial Properties ◽  
Extraction Process ◽  
Inhibitory Effect ◽  
Diffusion Method ◽  
Aqueous Extracts ◽  
Bacterial Strains ◽  
Leaf Extracts ◽  
Hyptis Suaveolens

Aim: Hyptis suaveolens is well known for its immense medicinal properties and are beneficial as folk medicine. The objective of the study is to investigate the efficacy of the leaves for it antimicrobial activity. Material and Methods: The leaves of Hyptis suaveolens was  subjected to extraction process using n-hexane, ethanol and distilled water as solvents and the antimicrobial activity was analyzed against different bacterial strains viz.; Escherichia coli, Proteus mirabilis, Streptococcus pneumoniae, Staphylococcus aureus, Klebsiella aerogenes, Pseudomonas aeruginosa, Salmonella typhi, Enterococcus faecalis by agar well diffusion method. Results: Aqueous extracts showed inhibitory effect against the different tested bacteria organisms with variable zone of inhibitory range 6 -21 mm. Conclusion: The aqueous extracts of Hyptis suaveolens exhibited the presence of highly effective bio-active compounds in these extracts. These can further be evaluated and characterize to improve upon what has been done to create a novel compound that can be useful for various medicinal purposes.

Design, Synthesis, Evaluation of Antimicrobial Activity and Docking Studies of New Thiazole-based Chalcones

2019 ◽  
Vol 19 (5) ◽  
pp. 356-375 ◽  
Author(s):  
Christophe Tratrat ◽  
Michelyne Haroun ◽  
Iakovos Xenikakis ◽  
Konstantinos Liaras ◽  
Evangelia Tsolaki ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Antimicrobial Agents ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Bacterial Species ◽  
Antibacterial Properties ◽  
Docking Studies ◽  
In Vivo Evaluation ◽  
Better Than

Background:Thiazole derivates as well as chalcones, are very important scaffold for medicinal chemistry. Literature survey revealed that they possess wide spectrum of biological activities among which are anti-inflammatory and antimicrobial.Objectives:The current studies describe the synthesis and evaluation of antimicrobial activity of twenty eight novel thiazole-based chalcones.Methods:The designed compounds were synthesized using classical methods of organic synthesis. The in vivo evaluation of antimicrobial activity was performed by microdilution method.Results:All compounds have shown antibacterial properties better than that of ampicillin and in many cases better than streptomycin. As far as the antifungal activity is concerned, all compounds possess much higher activity than reference drugs bifonazole and ketoconazole. The most sensitive bacterial species was B. cereus (MIC 6.5-28.4 µmol × 10-2/mL and MBC 14.2-105.0 µmol × 10-2/mL) while the most resistant ones were L. monocytogenes (MIC 21.4-113.6 µmol × 10-2/mL) and E. coli (MIC 10.7- 113.6 µmol × 10-2/mL) and MBC at 42.7-358.6 µmol × 10-2/mL and 21.4-247.2 µmol × 10-2/mL, respectively. All the compounds exhibited antibacterial activity against the three resistant strains, MRSA, P. aeruginosa and E.coli. with MIC and MBC in the range of 0.65-11.00 µmol/mL × 10-2 and 1.30-16.50 µmol/mL × 10-2. Docking studies were performed.Conclusion:Twenty-eight novel thiazole-based chalcones were designed, synthesized and evaluated for antimicrobial activity. The results showed that these derivatives could be lead compounds in search of new potent antimicrobial agents. Docking studies indicated that DNA gyrase, GyrB and MurA inhibition may explain the antibacterial activity.

scholarly journals A Review on Antibacterial, Antiviral, and Antifungal Activity of Curcumin

2014 ◽  
Vol 2014 ◽  
pp. 1-12 ◽  
Author(s):  
Soheil Zorofchian Moghadamtousi ◽  
Habsah Abdul Kadir ◽  
Pouya Hassandarvish ◽  
Hassan Tajik ◽  
Sazaly Abubakar ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Water Solubility ◽  
Curcuma Longa ◽  
Antimicrobial Activities ◽  
Inhibitory Effect ◽  
Polyphenolic Compound ◽  
Future Studies ◽  
Chemical Derivatives ◽  
Antimicrobial Studies

Curcuma longaL. (Zingiberaceae family) and its polyphenolic compound curcumin have been subjected to a variety of antimicrobial investigations due to extensive traditional uses and low side effects. Antimicrobial activities for curcumin and rhizome extract ofC. longaagainst different bacteria, viruses, fungi, and parasites have been reported. The promising results for antimicrobial activity of curcumin made it a good candidate to enhance the inhibitory effect of existing antimicrobial agents through synergism. Indeed, different investigations have been done to increase the antimicrobial activity of curcumin, including synthesis of different chemical derivatives to increase its water solubility as well ass cell up take of curcumin. This review aims to summarize previous antimicrobial studies of curcumin towards its application in the future studies as a natural antimicrobial agent.

Synthesis of 8,10-disubstituted-triazoloperimidines from (E)-3-(dimethylamino)-1-(8- phenyl-8H-[1,2,4]triazolo[4,3-a]perimidin-10-yl)prop-2-en-1-one and Their Antimicrobial Activity

2018 ◽  
Vol 15 (1) ◽  
pp. 126-136 ◽  
Author(s):  
Ghada S. Masaret ◽  
Thoraya A. Farghaly
Keyword(s):  
Antimicrobial Activity ◽  
Acetic Acid ◽  
Hydrazine Hydrate ◽  
Spectral Data ◽  
Organic Compounds ◽  
The Novel ◽  
Hydrazonoyl Chlorides ◽  
Elemental Analyses ◽  
Different Types ◽  
Substituted Pyrazoles

Aim and Objective: Enaminones belay to be extremely stable compounds and constitute a versatile group of salutary precursors for the synthesis of enormous classes of organic compounds. So, in this context, we synthesized a new enaminone, namely, (E)-3-(dimethylamino)-1-(8-phenyl-8H-[1,2,4]triazolo[4,3- a]perimidin-10-yl)prop-2-en-1-one (enaminone 2). Materials and Methods: The reaction of enaminone 2 with different types of hydrazonoyl chlorides or hydrazine hydrate afforded new substituted pyrazoles. Also, the reaction of enaminone with 6-amino-2- thioxopyrimidin-4-one in acetic acid under reflux produced 2-thioxopyridopyrimidinone derivative. The latter thione derivative reacts with hydrazonoyl chlorides to give pyridotriazolopyrimidines. 5-(8-Phenyl-8H- [1,2,4]triazolo[4,3-a]perimidin-10-yl)isoxazole was produced from the reaction of enaminone 2 with hydroxylamine. Results & Conclusion: The structure of all the novel perimidine derivatives was confirmed on the basis of spectral data and elemental analyses. The enaminone and the newly synthesized compounds were tested for their antimicrobial activity, and the results obtained revealed that some derivatives are more potent than the reference drugs used.

scholarly journals Design, Synthesis and Biological Assessment of Thiazole Derivatives as Possible Antioxidant and Antimicrobial Agents

2021 ◽  
pp. 24-32
Author(s):  
. Isha ◽  
Neetu Sachan
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Therapeutic Potential ◽  
Antibacterial Properties ◽  
Antimicrobial Properties ◽  
Molecular Structures ◽  
Biological Assessment ◽  
Thiazole Derivatives ◽  
Antioxidant And Antimicrobial Activity

Aims: To synthesize thiazole derivatives and evaluate their therapeutic potential to continue our quest for new antibacterial and antioxidant drugs. Place and Duration of Study: Institute of Pharmaceutical Research, GLA University, Mathura, Uttar Pradesh, between January 2021 and July 2021. Methodology: The target compounds in this investigation were synthesized in the search for new molecules having antioxidant and antimicrobial activity. Physicochemical and spectroanalytical studies validated the derivatives molecular structures. Antioxidant and antimicrobial properties of the synthesized molecules were evaluated in vitro using the DPPH and tube dilution methods, respectively. Results: The majority of the synthesized derivatives displayed antioxidant and antimicrobial activity. The efficacy of the derivatives varied based upon the substituent. Compound 7c exhibited significant antioxidant and antibacterial activity, according to the results of the study. Conclusion: Our results showed the antioxidant and antibacterial properties of novel thiazole compounds, implying the probability of their utilization in the development of new therapeutics.

Lemongrass and cinnamon oil nanoemulsions: Formulation and study of their physical stability and activity against Zygosaccharomyces bailii

2021 ◽  
Vol 27 (6) ◽  
pp. 485-498
Author(s):  
Malena M González ◽  
Aldana L Zalazar ◽  
Julieta D Pedreira ◽  
Carmen A Campos ◽  
María F Gliemmo
Keyword(s):  
Antimicrobial Activity ◽  
Essential Oils ◽  
High Speed ◽  
Antimicrobial Agents ◽  
Physical Stability ◽  
Inhibitory Effect ◽  
Additive Interaction ◽  
Cinnamon Oil ◽  
Zygosaccharomyces Bailii ◽  
Food And Beverage

The optimal conditions for elaborating oil/water nanoemulsions of lemongrass (LG), cinnamon bark (CB) and cinnamon leaves (CL) essential oils and their antimicrobial activity against Zygosaccharomyces bailii at pH 4.00 were studied. The effect of the emulsification methodology on the physical stability and antimicrobial activity of the nanoemulsions were also evaluated. Furthermore, the sensory impact of nanoemulsions added to an apple juice was tested. LG and CL nanoemulsions were elaborated by ultrasonication and CB nanoemulsion, by high-speed homogenization. They were stable for at least 120 days at 25 °C. They exhibited antimicrobial activity against Z. bailii being CB the most effective since it showed the smallest MIC value (156.3 mg/l), followed by LG (468.8 mg/l) and CL (1250.0 mg/l). A slight increase in growth rate was observed due to ultrasonication. An additive interaction in relation to the inhibitory effect between LG and CB nanoemulsions against Z. bailii was observed. While nanoemulsions obtained would be used as natural antimicrobial agents in food and beverage products, only LG nanoemulsion at MIC concentration diluted was acceptable in juice showing the sensory impact of essential oils on foods.

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