Design, Synthesis, and Antibacterial and Antifungal Activities of Novel Trifluoromethyl and Trifluoromethoxy Substituted Chalcone Derivatives

Despite the availability of many drugs to treat infectious diseases, the problems like narrow antimicrobial spectrum, drug resistance, hypersensitivities and systemic toxicities are hampering their clinical utility. Based on the above facts, in the present study, we designed, synthesized and evaluated the antibacterial and antifungal activity of novel fluorinated compounds comprising of chalcones bearing trifluoromethyl (A1–A10) and trifluoromethoxy (B1–B10) substituents. The compounds were characterized by spectroscopic techniques and evaluated for their antimicrobial activity against four pathogenic Gram-positive (Staphylococcus aureus and Bacillus subtilis) and Gram-negative (Escherichia coli and Bacillus subtilis) bacterial and fungal (Candida albicans and Aspergillus niger) strains. In this study, the compounds with trifluoromethoxy group were more effective than those with trifluoromethyl group. Among the 20 fluorinated chalcones, compound A3/B3 bearing an indole ring attached to the olefinic carbon have been proved to possess the most antimicrobial activity compared to the standard drugs without showing cytotoxicity on human normal liver cell line (L02). Further, the minimum inhibitory concentration (MIC) for A3/B3 was determined by serial tube dilution method and showed potential activity. These results would provide promising access to future study about the development of novel agents against bacterial and fungal infections.

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Manganese (II) and Cobalt (II) Acetylacetonates as Antimicrobial Agents

NIGERIAN ANNALS OF PURE AND APPLIED SCIENCES ◽

10.46912/napas.43 ◽

2019 ◽

Vol 1 ◽

pp. 176-185

Author(s):

S G Yiase ◽

S O Adejo ◽

S T Iningev

Keyword(s):

Antimicrobial Activity ◽

Antifungal Activity ◽

Antimicrobial Agents ◽

Inhibitory Concentration ◽

Dilution Method ◽

Spectroscopic Techniques ◽

Metal Chlorides ◽

Activity Screening ◽

Antibacterial And Antifungal ◽

Broth Dilution

Mn(II) and Co(II) complexes were prepared by reaction of the metal chlorides with acetylacetone in ammonical aqueous medium. The metal complexes were prepared in order to investigate their antimicrobial activity on some selected pathogens. The characterisation of the complexes was on the basis of various spectroscopic techniques like infrared and ultraviolet studies. The compounds were subjected to antimicrobial activity screening using serial broth dilution method. Minimum Inhibitory Concentration (MIC) and Minimum Bactericidal/Fungicidal Concentration (MBC/MFC) were determined. Mn(II) complex has shown significantly both antibacterial and antifungal activity with a MIC of 1.25 μg/mL while Co(II) complex was noticeable for antifungal activity at the same concentration. Whereas Mn(II) acetylacetonate is a more potent bactericide while Co(II) acetylacetonate is a more potent fungicide, both with MBC/MFC value of 2.5 μg/mL. Antimicrobial agent of the ligand has enhanced on complexation with Mn(II) and Co(II) ions. Though, the potency of the prepared antibiotics on the tested microbes is less compared to the standard drugs (Ciprofloxacin and Fulcin).

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Antimicrobial Activity ofLippiaSpecies from the Brazilian Semiarid Region Traditionally Used as Antiseptic and Anti-Infective Agents

Evidence-based Complementary and Alternative Medicine ◽

10.1155/2013/614501 ◽

2013 ◽

Vol 2013 ◽

pp. 1-5 ◽

Cited By ~ 4

Author(s):

Cristiana da Purificação Pinto ◽

Velize Dias Rodrigues ◽

Fernanda da Purificação Pinto ◽

Renata da Purificação Pinto ◽

Ana Paula Trovatti Uetanabaro ◽

...

Keyword(s):

Antimicrobial Activity ◽

Fungal Infections ◽

Active Species ◽

Semiarid Region ◽

Antimicrobial Drugs ◽

Promising Alternative ◽

Popular Medicine ◽

Antibacterial And Antifungal Activities ◽

Methanolic Extracts ◽

Antibacterial And Antifungal

Lippia origanoidesKunth,Lippia alnifoliaSchauer, andLippia thymoidesMartius and Schauer are shrubs used in the traditional Brazilian medicine as antiseptics, as well as in the treatment of infectious diseases. This study was designed to investigate the antibacterial and antifungal activities of the methanolic extracts of these species, as new potential sources of antimicrobial drugs. The antimicrobial activity of methanolic extracts was investigated against resistant yeasts and bacteria by agar disk diffusion. Then, the MIC determination of the most active species and its fractions in hexane, dichloromethane, ethyl acetate, and water was performed. By the agar diffusion assay, all species were active against at least two microorganisms, giving evidence to support their use in the popular medicine.L. origanoidesleaves exhibited the widest antimicrobial action, inhibiting the growth of two Gram-positive bacteria and two yeasts; this activity was also confirmed by the MIC evaluation. The fractionation ofL. origanoidescrude extracts improved the activity in spectrum and intensity. The results obtained in this study indicate thatL. origanoidesmay be a promising alternative in the treatment of bacterial and fungal infections and in the seeking of new antimicrobial drugs.

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Antimicrobial potential of 3-hydroxy-2-methylene-3-phenylpropionic acid derivatives

Acta Pharmaceutica ◽

10.2478/v10007-011-0034-2 ◽

2011 ◽

Vol 61 (4) ◽

pp. 447-455 ◽

Cited By ~ 4

Author(s):

Soni Singh ◽

Sujata Bhat

Keyword(s):

Antimicrobial Activity ◽

Low Cost ◽

Aromatic Aldehydes ◽

Dilution Method ◽

Phenylpropionic Acid ◽

Antimicrobial Potential ◽

Antibacterial And Antifungal Activities ◽

Antibacterial And Antifungal ◽

Vinyl Derivatives

Antimicrobial potential of 3-hydroxy-2-methylene-3-phenylpropionic acid derivatives Twenty Baylis-Hillman adducts were synthesized from different aromatic aldehydes and activated vinyl derivatives. The adducts, which are differently substituted 3-hydroxy-2-methylene-3-phenylpropionic acid derivatives, were screened for their antimicrobial activity in vitro by the serial dilution method. Many of these molecules displayed potent antibacterial and antifungal activities. The ease of synthesis from low-cost starting materials along with potent antimicrobial activity of these molecules provide the lead for further improvement of activity and reflect the possibility of therapeutic use.

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Synthesis, Antibacterial, and Antifungal Activities of Hybrid Molecules Based on Alzheimer Disease Drugs and Bearing an Amino Acid Fragment

Proceedings ◽

10.3390/ecsoc-23-06602 ◽

2019 ◽

Vol 41 (1) ◽

pp. 23 ◽

Cited By ~ 1

Author(s):

Radoslav Chayrov ◽

Aleksandra Tencheva ◽

Hristina Sbirkova-Dimitrova ◽

Boris Shivachev ◽

Anna Kujumdzieva ◽

...

Keyword(s):

Antimicrobial Activity ◽

Amino Acid ◽

Alzheimer Disease ◽

Fungal Infections ◽

Biological Properties ◽

X Ray ◽

Antibacterial And Antifungal Activities ◽

Acid Fragment ◽

Hybrid Molecules ◽

Antibacterial And Antifungal

The objective of the current study was to develop novel compounds–memantine derivatives with antimicrobial activity designed for application in treatment of bacterial and fungal infections in patients suffering from Alzheimer’s disease. To realize this objective, a series of six memantine hybrid molecules were synthesized, characterized by 1H NMR, 13C NMR, MS, X-ray, and tested for their biological properties as anti-Alzheimer agents and their antimicrobial potential.

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Chemical Composition and Antimicrobial Activity of the Essential Oil from Flowers of Eryngium triquetrum (Apiaceae) Collected Wild in Sicily

Natural Product Communications ◽

10.1177/1934578x1601100737 ◽

2016 ◽

Vol 11 (7) ◽

pp. 1934578X1601100

Author(s):

Simona Casiglia ◽

Maurizio Bruno ◽

Sergio Rosselli ◽

Felice Senatore

Keyword(s):

Antimicrobial Activity ◽

Chemical Composition ◽

Essential Oil ◽

Antifungal Activities ◽

Antibacterial And Antifungal Activities ◽

Art Works ◽

Main Components ◽

Antibacterial And Antifungal ◽

Historical Art

The chemical composition of the essential oil from flowers of Eringium triquetrum Vahl. collected in Sicily was evaluated by GC and GC-MS. The main components were pulegone (50.6%), piperitenone (30.5%) and menthone (7.0%). Comparison of this oil with other studied oils of Eringium species is discussed. The oil showed good antibacterial and antifungal activities against some microorganisms that infest historical art works.

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Phytochemical investigation and in vitro antimicrobial activity of Richardia scabra

Bangladesh Journal of Pharmacology ◽

10.3329/bjp.v11i2.24666 ◽

2016 ◽

Vol 11 (2) ◽

pp. 248 ◽

Cited By ~ 1

Author(s):

Kathirvel Poonkodi ◽

Subban Ravi

Keyword(s):

Antimicrobial Activity ◽

Diffusion Method ◽

Bacterial Strains ◽

Weed Species ◽

Antibacterial And Antifungal Activities ◽

Agar Plug ◽

Phytochemical Investigation ◽

Antibacterial And Antifungal ◽

Simple Sugar

The present study was aimed to evaluate the phytochemical screening and antimicrobial activity of the petroleum ether and methanol extracts from the mature leaves of Richardia scabra from India. Disc diffusion method was used to determine the zone inhibition of the tested samples for antibacterial and agar plug method was used to determine the antifungal activity, while the microtube-dilution technique was used to determine the minimum inhibitory concentration. Both extracts showed significant antibacterial and antifungal activities when tested against 10 bacterial and four fungal strains. The minimum inhibitory concentrations of the methanol extract of R. scabra ranged between 12.5–100 μg/mL for bacterial strains. Alkaloids, steroids, flavonoids, fatty acids, terpenoids and simple sugar were detected as phytoconstituents of extracts. To the best of our knowledge, this is the first report against antimicrobial activity of common weed species R. scabra found in India.

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Synthesis and Antimicrobial Activity of Some Chalcone Derivatives

E-Journal of Chemistry ◽

10.1155/2008/876257 ◽

2008 ◽

Vol 5 (3) ◽

pp. 461-466 ◽

Cited By ~ 24

Author(s):

Y. Rajendra Prasad ◽

A. Lakshmana Rao ◽

R. Rambabu

Keyword(s):

Aqueous Solution ◽

Antimicrobial Activity ◽

Potassium Hydroxide ◽

Room Temperature ◽

Antimicrobial Agents ◽

Aromatic Aldehydes ◽

Plate Method ◽

H Nmr ◽

Antibacterial And Antifungal Activities ◽

Antibacterial And Antifungal

In an effort to develop antimicrobial agents, a series of chalcones were prepared by Claisen-Schmidt condensation of appropriate acetophenones with appropriate aromatic aldehydes in the presence of aqueous solution of potassium hydroxide and ethanol at room temperature. The synthesized compounds were characterized by means of their IR,1H-NMR spectral data and elemental analysis. All the compounds were tested for their antibacterial and antifungal activities by the cup plate method.

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Design, Synthesis, and Antimicrobial Evaluation of Novel Pyrazoles and Pyrazolyl 1,3,4-Thiadiazine Derivatives

Molecules ◽

10.3390/molecules23092092 ◽

2018 ◽

Vol 23 (9) ◽

pp. 2092 ◽

Cited By ~ 10

Author(s):

Ibrahim Radini

Keyword(s):

Antimicrobial Activity ◽

Minimum Inhibitory Concentration ◽

Elemental Analysis ◽

Inhibitory Concentration ◽

Diazonium Salts ◽

Design Synthesis ◽

Antifungal Activities ◽

Antibacterial And Antifungal Activities ◽

Antimicrobial Evaluation ◽

Antibacterial And Antifungal

A novel series of pyrazolyl 1,3,4-thiadiazines 5a–c, 8a–c, 12, 15a–c, 17a–c, and 20 was prepared from the reaction of pyrazole-1-carbothiohydrazide 1a,b with 2-oxo-N′-arylpropanehydrazonoyl chloride, 2-chloro-2-(2-arylhydrazono)acetate, and 3-bromoacetylcoumarin. Moreover, the regioselective reaction of 5-pyrazolone-1-carbothiohydrazide 1a with 4-substituted diazonium salts and 4-(dimethylamino)benzaldehyde gave the corresponding hydrazones 21a–c and 22. The newly prepared compounds were characterized by spectroscopy and elemental analysis. Many new synthesized compounds showed considerable antimicrobial activity against tested microorganisms. Hydrazones 21a–c and 22 showed remarkable antibacterial and antifungal activities. 4-(2-(p-tolyl)hydrazineylidene)-pyrazole-1-carbothiohydrazide 21a displayed the highest antibacterial and antifungal activities with minimum inhibitory concentration (MIC) values lower than standard drugs chloramphenicol and clotrimazole, in the range of 62.5–125 and 2.9–7.8 µg/mL, respectively.

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Antimicrobial activity of methanol extracts of Fontinalis antipyretica, Hypnum cupressiforme, and Ctenidium molluscum

Archives of Biological Sciences ◽

10.2298/abs0902225v ◽

2009 ◽

Vol 61 (2) ◽

pp. 225-229 ◽

Cited By ~ 8

Author(s):

M. Veljic ◽

Aleksandra Djuric ◽

Marina Sokovic ◽

Ana Ciric ◽

Jasmina Glamoclija ◽

...

Keyword(s):

Escherichia Coli ◽

Antimicrobial Activity ◽

Salmonella Enteritidis ◽

Trichoderma Viride ◽

Fontinalis Antipyretica ◽

Moss Species ◽

Methanol Extracts ◽

Hypnum Cupressiforme ◽

Antibacterial And Antifungal Activities ◽

Antibacterial And Antifungal

Antibacterial and antifungal activities of methanol extracts of the moss species Fontinalis antipyretica Hedw. var. antipyretica, Hypnum cupressiforme Hedw., and Ctenidium molluscum (Hedw.) Mitt. were analyzed. Antimicrobial activity was tested against Gram (+) (Bacillus subtilis, Micrococcus flavus, and Staphylococcus epidermidis) and Gram (-) (Escherichia coli and Salmonella enteritidis) bacteria. Antifungal activity of extracts was tested using the following micromycetes: Trichoderma viride, Penicillium funiculosum, P. ochrochloron, Aspergillus fumigatus, A. flavus, and A. niger. The methanol extract of Fontinalis antipyretica showed the strongest activity against the tested bacteria and micromycetes. The antibacterial effect of methanol extracts was higher against the G (-) (Escherichia coli and Salmonella enteritidis) than against the G (+) bacteria tested.

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Evaluation of the antimicrobial activity of Gooseberry and Wild Apple fruit juices of the northeast region of India

Journal of Medicinal Herbs and Ethnomedicine ◽

10.19071/jmhe.2017.v3.3160 ◽

2017 ◽

Vol 3 ◽

pp. 1 ◽

Cited By ~ 1

Author(s):

Kapil Punjabi ◽

Vidushi K. Chitalia ◽

Tehmeena Mukadam ◽

Jaishankar Sharma ◽

Jinesh Maniar ◽

...

Keyword(s):

Antimicrobial Activity ◽

Apple Fruit ◽

Fruit Juices ◽

Diffusion Method ◽

Eastern Region ◽

The North ◽

Antibacterial And Antifungal Activities ◽

Wild Fruits ◽

North Eastern ◽

Antibacterial And Antifungal

A large number of wild fruits belonging to the North Eastern region of India are considered to be nutritionally abundant and traditionally used for the treatment of various ailments. In the present study, juices of Gooseberry and Wild Apple have been evaluated for their antimicrobial activity in its consumable form as a potential source of natural anti-infective agent. The fruit juices were screened for their antibacterial and antifungal activities qualitatively, using the agar well diffusion method followed by quantitative assessment by determining the Minimum Inhibitory Concentration (MIC) and Minimum Bactericidal Concentration (MBC). The study revealed that both the fruit juices exhibited broad spectrum antibacterial activity. Considerable activity against drug resistant pathogens such as Methicillin Resistant Staphylococcus aureus (MRSA), Vancomycin Resistant Enterococci (VRE) and Extended Spectrum Î²-Lactamases (ESBL) producing Gram Negative bacteria (GNB) was observed. Thus, this study highlights the antibacterial efficacy of Wild Apple and Gooseberry fruit juices and augments the beneficiary properties of highly nutritional fruit juices that are specific to the Indian region.

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