Synthesis, Characterization and Biological Evaluation of Ethyl-4'-(cyclopropane carboxamido-N-yl)-5-ary-3-oxo-3,4,5,6-tetrahydro-biphenyl-4-carboxylate

2019 ◽  
Vol 4 (4) ◽  
pp. 240-243
Author(s):  
P.M. Akbari ◽  
V.R. Shah

A series of new substituted cyclohexenone derivatives have been synthesized by the reaction of various substituted chalcones with ethylacetoacetate. Some new N-(4-(3-aryl-acryloyl)phenyl)cyclopropane carboxamide were prepared by Claisen-Schmidt condensation method in presence of sodium hydroxide in ethanol solvent under stirring. The synthesized compounds were characterized by their spectral (IR, NMR, Mass) data and screened for their antimicrobial activities against Gram-positive and Gram-negative bacteria by using standard antimicrobial drugs.

2000 ◽  
Vol 44 (4) ◽  
pp. 848-852 ◽  
Author(s):  
C. M. Kunin ◽  
W. Y. Ellis

ABSTRACT Mefloquine was found to have bactericidal activity against methicillin- and fluoroquinolone-susceptible and -resistant strains ofStaphylococcus aureus and Staphylococcus epidermidis and gentamicin- and vancomycin-resistant strains ofEnterococcus faecalis and Enterococcus faecium. The MICs were 16 μg/ml, and the minimal bactericidal concentrations (MBCs) were 16 to 32 μg/ml. These concentrations cannot be achieved in serum. Mefloquine was active at a more achievable concentration against penicillin-susceptible and -resistant Streptococcus pneumoniae, with MICs of 0.2 to 1.5 μg/ml. Mefloquine was not active against gram-negative bacteria and yeasts. In an attempt to find more active derivatives, 400 mefloquine-related compounds were selected from the chemical inventory of The Walter Reed Army Institute of Research. We identified a series of compounds containing a piperidine methanol group attached to pyridine, quinoline, and benzylquinoline ring systems. These had activities similar to that of mefloquine against S. pneumoniae but were far more active against other gram-positive bacteria (MICs for staphylococci, 0.8 to 6.3 μg/ml). They had activities similar to that of amphotericin B againstCandida spp. and Cryptococcus neoformans. Combinations of the compounds with gentamicin and vancomycin were additive against staphylococci and pneumococci. The MIC and MBC of gentamicin were decreased by four- to eightfold when this drug was combined with limiting dilutions of the compounds. There was no antagonism with other antimicrobial drugs. The compounds were rapidly bactericidal. They appear to act by disrupting cell membranes. Combinations of the compounds with aminoglycoside antibiotics may have potential for therapeutic use.


1962 ◽  
Vol 8 (5) ◽  
pp. 621-628 ◽  
Author(s):  
W. A. Taber ◽  
B. B. Wiley

The antimicrobial activities of a branched, monoalkyl benzene sulphonate complex (ABS), the active component of a commercial liquid household detergent, and of the detergent have been investigated. Cultures of dermatophytes, Candida albicans, saprophytic phycomycetes, ascomycetes, fungi imperfecti, Gram-positive and Gram-negative bacteria were tested. Only the Fusarium species and the Gram-negative bacteria were not inhibited by a concentration of 0.1 ml of the detergent/50 ml medium. Microgram quantities of ABS inhibited the Gram-positive bacteria and the fungi except Fusarium spp. ABS was lethal in microgram quantities, the effect being detectable within 30 minutes. Inhibition of exogenous respiration of glucose by C. albicans began upon contact and was complete within 50 minutes. A linear and biodegradable ABS was more active than the branched form against C. albicans.


Polymers ◽  
2019 ◽  
Vol 11 (4) ◽  
pp. 670 ◽  
Author(s):  
Alzagameem ◽  
Klein ◽  
Bergs ◽  
Do ◽  
Korte ◽  
...  

The antiradical and antimicrobial activity of lignin and lignin-based films are both of great interest for applications such as food packaging additives. The polyphenolic structure of lignin in addition to the presence of O-containing functional groups is potentially responsible for these activities. This study used DPPH assays to discuss the antiradical activity of HPMC/lignin and HPMC/lignin/chitosan films. The scavenging activity (SA) of both binary (HPMC/lignin) and ternary (HPMC/lignin/chitosan) systems was affected by the percentage of the added lignin: the 5% addition showed the highest activity and the 30% addition had the lowest. Both scavenging activity and antimicrobial activity are dependent on the biomass source showing the following trend: organosolv of softwood > kraft of softwood > organosolv of grass. Testing the antimicrobial activities of lignins and lignin-containing films showed high antimicrobial activities against Gram-positive and Gram-negative bacteria at 35 °C and at low temperatures (0–7 °C). Purification of kraft lignin has a negative effect on the antimicrobial activity while storage has positive effect. The lignin release in the produced films affected the activity positively and the chitosan addition enhances the activity even more for both Gram-positive and Gram-negative bacteria. Testing the films against spoilage bacteria that grow at low temperatures revealed the activity of the 30% addition on HPMC/L1 film against both B. thermosphacta and P. fluorescens while L5 was active only against B. thermosphacta. In HPMC/lignin/chitosan films, the 5% addition exhibited activity against both B. thermosphacta and P. fluorescens.


Author(s):  
Pooja Pisal ◽  
Meenakshi Deodhar ◽  
Amol Kale ◽  
Ganesh Nigade ◽  
Smita Pawar

Objective: A new series 2-phenyl-3-(substituted benzo[d] thiazol-2-ylamino)-quinazoline-4(3H)-one was prepared by the fusion method by reacting 2-phenyl benzoxazine with 2-hydrazino benzothiazole and it was evaluated for their antimicrobial activity against gram positive, gram negative bacteria and fungi.Methods: Titled compounds were synthesized by fusion reactions. These compounds were evaluated by in vitro antibacterial and antifungal activity using the minimum inhibitory concentration and zone of inhibition methods. The synthesized compounds were characterized with the help of infrared, NMR and mass spectral studies. The benzothiazole moiety and the quinazoline ring have previously shown DNA gyrase inhibition and target related antibacterial activity. Thus, molecular docking studies of synthesized compounds were carried out (PDB: 3G75) to study the possible interaction of compounds with the target. The batch grid docking was performed to determine the probable.Results: These compounds showed significant activity against gram positive and gram negative bacteria as well against the fungi. The compound A5 was found to be active against B. subtilis, P aeruginosa and C. albican at 12.5 µg/ml MIC. The compound A3 was found to be active against all microbial strains selected at 25 and 12.5 µg/ml MIC.Conclusion: Though the relationship between the activities shown by these compounds in, the antimicrobial study is still to be established, the docking studies conducted found to be consistent with antimicrobial results. Thus the results indicate that the designed structure can be a potential lead as an antimicrobial agent.


2016 ◽  
Vol 34 (2) ◽  
pp. 35
Author(s):  
Prayna P. P. Maharaj ◽  
Riteshma Devi ◽  
Surendra Prasad

Fiji is highly populated with plants containing essential oils (EO). The essential oils extracted from the leaves of the selected Fijian leafy plants were screened against two Gram-negative bacteria (Salmonella typhimurium, Pseudomonas aeruginosa) and three Gram-positive bacteria (Staphylococcus aureus, Enterococcus faecalis and Bacillus subtilis). The agar diffusion method was used to examine the antimicrobial activities of the extracted EO. All the EO tested showed antibacterial properties against one or more strains while none of the EO was active against Pseudomonas aeruginosa. Viburnum lantana (Wayfaring tree), Annona muricata (Soursop), Coleus amboinicus (Spanish thyme) and Cinnamomum zeylancium (Cinnamon) showed good inhibition against both Gram-positive and Gram-negative bacteria and proved as worthy source of antimicrobial agent. These findings will help the Pacific population to use the studied plants leaves as antimicrobial agent.


2004 ◽  
Vol 59 (5-6) ◽  
pp. 373-378 ◽  
Author(s):  
El-Sayed S. Mansour ◽  
Galal T. Maatooq ◽  
Ashraf T. Khalil ◽  
El-Sayed M. Marwan ◽  
Amal A. Sallam

The composition of the essential oil of the fruits, leaves and stems of Daucus glaber Forssk has been studied by GC/MS. It was found that, the essential oil of the fruits consists of monoterpene hydrocarbons (limonene and sylvestrene are the majors) and phenylpropanoids (elemicin is the major). Sylvestrene has never been reported before in the essential oil of any Daucus species. The study of the essential oil of the leaves revealed the presence of monoterpene hydrocarbons; limonene and γ-terpinene are the majors and a small amount of sylvestrene. The essential oil of stems consists of monoterpene hydrocarbons (γ-terpinene is the major), terpene alcohols (mainly 4-terpineol) and phenylpropanoids (myristicin and elemicin are the majors). It is interesting that, the essential oil of the fruits is free from any oxygenated terpenes while that of the stems is free from limonene and sylvestrene which are present in the essential oil of the fruits and leaves in fairly large amounts. The essential oil of the fruits, leaves and stems shows broad antimicrobial activities against both gram positive and gram negative bacteria. In addition, the volatile oil of the stem, particularly, show activi­ties against Candida albicans (yeast). Also, the prepared oils have variable cytotoxic activities with LC50 21.52, 36.01 and 42.34 μrg/ml. respectively.


2021 ◽  
Vol 4 (4) ◽  
pp. 348-354
Author(s):  
Aliyu Shehu ◽  
Ahmed Salisu ◽  
Nura S. Gwaram

In this study, the antimicrobial and physicochemical properties of translucent antimicrobial soap prepared using two medicinal plants, Aloe vera gel and Ziziphus jujube leaf extract   was evaluated. The results of the physicochemical analysis showed the pH (7.52±0.02), hardness(1.3 cm±0.02), solubility (0.82 g±0.02) and foamability (6.80 cm±0.03) of the prepared soap and these values were within the acceptable limit  set by WHO/SON which make the prepared soap skin-friendly. Similarly, the antimicrobial screening was carried out on selected Gram-positive and gram-negative bacteria as well as on fungi species using disc diffusion methods and the results showed varying antimicrobial activity at different concentrations ranging from 62.5-500 mg/ml. However, the susceptibility of test bacteria in terms of the zone of inhibition at 500mg/ml of the soap was observed on Staphylococcus lentus (22 mm), Staphylococcus aureus (20mm), Escherichia coli (15 mm), Raoltella ornithinolytica (12mm). The result of antifungal properties was as follows,  Candida albicans (12 mm), Trichophyton rubrum (12 mm), and Aspergillus nigar (10 mm)  at 500 mg/ml concentration. The results when compared to other antimicrobial soap in the market indicate good quality by inhibiting the growth of both Gram-positive, gram-negative bacteria and fungi. The antimicrobial activities exhibited by the soap in this study could be attributed to the presence of phytochemical constituents in the plant extracts, which signify the potential of the soap as an antimicrobial agent. Therefore, these findings confirmed the efficacy of Aloe vera gel and Zizipus jujube extract in traditional medicine.


2018 ◽  
Vol 29 (1) ◽  
pp. 107 ◽  
Author(s):  
Hadeel Majed ◽  
Firyal W. Askar

Agroup of benzimidazole derivatives bearing different heterocyclic moieties such as Schiff bases, 2-azetidinone and  4-thiazolidinone were efficiently prepared. The structures of the newly compounds were characterized by FTIRand ¹H NMR spectra. The synthesized compounds were evaluated for their antimicrobial activities against gram-positive and gram negative bacteria and fungi using the microdilution procedure.


1970 ◽  
Vol 18 ◽  
pp. 128-133 ◽  
Author(s):  
MTH Molla ◽  
MS Ahsan ◽  
MT Alam ◽  
ME Haque

Context: Development of resistance in human pathogens against conventional antibiotic necessitates searching indigenous medicinal plants having antibacterial property. Seven medicinal plants used actively in folklore, ayurvedic and traditional system of medicine were selected for the evaluation of their antimicrobial activity for this study.   Objectives: Evaluation of the effectiveness of some medicinal plant extracts against four Gram-positive and five Gram-negative bacteria.  Materials and Methods: The antibacterial activity of the crude ethanolic extracts obtained from the leaves of seven medicinal plants; viz., Andrographis paniculata, Catharanthus roseus, Adhatoda vasica, Vitex vegundo, Aloe vera, Flacortia ramontchi and Nyctanthes arbortristis were tested against nine bacteria at concentrations of 300-, 400- and 500 μg/ml. Standard antibiotic disc kanamycin (30μg/ml) was used for comparison. The minimum inhibitory concentration (MIC) of ethanolic extracts of the leaves of these medicinal plants were determined by testing the extracts on four Gram-positive and five Gram-negative bacteria by serial tube dilution method.   Results: All the extracts have notable antimicrobial activities against the test organisms. The ethanolic extracts of the leaves showed the highest antimicrobial activities against Bacillus megaterium and Shigella dysenteriae for An. paniculata, Ad. vasica and Al. vera; Bacillus subtilis and Salmonella typhi for C. roseus and N. arbortristis; Staphylociccus aureus and Salmonella typhi for V. vegundo; and Bacillus subtilis and Shigella sonnei for F. ramontchi respectively. The extract of the plants had MIC values ranging from 32 to 128 mg/ml. All plant extracts showed no MIC against Shigella shiga and against Sarcina lutea only C. roseus showed MIC 128 mg/ml.   Conclusion: The results revealed that the ethanolic extracts of the plants under present investigation have notable antimicrobial activities.   Keywords: medicinal plants; antimicrobial screening; MIC; bacteria. DOI: http://dx.doi.org/10.3329/jbs.v18i0.8788 JBS 2010; 18(0): 128-133


2007 ◽  
Vol 2 (4) ◽  
pp. 1934578X0700200 ◽  
Author(s):  
Leopold Jirovetz ◽  
Gerhard Buchbauer ◽  
Thomas Schweiger ◽  
Zapriana Denkova ◽  
Alexander Slavchev ◽  
...  

The chemical composition of a sample of Jasminum grandiflorum L. absolute from India was analyzed by GC and GC/MS. The major compounds identified were benzyl acetate (23.7%), benzyl benzoate (20.7%), phytol (10.9%), linalool (8.2%), isophytol (5.5%), geranyl linalool (3.0%), methyl linoleate (2.8%) and eugenol (2.5%). The odor of this absolute sample was olfactorically evaluated as intense and heavy floral-flowery, with penetrant-animalic and fruity side-notes. Some main and minor compounds were found to be responsible for the aroma impression of this sample. The antimicrobial activities of the J. grandiflorum sample and of some of its main and minor compounds were tested against Gram-positive and Gram-negative bacteria, as well as against the yeast Candida albicans, using agar dilution and agar diffusion methods. The jasmine absolute showed medium to high activity (reference compounds: eugenol and three synthetic antibiotics) against the Gram-positive bacterium Enterococcus faecalis, against the Gram-negative bacteria Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae and Salmonella sp., as well as against the yeast Candida albicans. A comparison of these biological data with those of some constituents of the jasmine absolute is also given.


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