Synthesis and Antimicrobial Activity of Novel Oxothiazolidine Derivatives

2020 ◽  
Vol 5 (2) ◽  
pp. 91-96
Author(s):  
Balasaheb P. Pagar

In this article, acid hydrazide 2, a functional group, was synthesized by the reaction of (4-chloro-12- methyl-16,17-dihydro-15-thia-6,11-diaza-cyclopenta[a]phenanthren-7-ylsulfanyl)acetic acid ethyl ester (1) with hydrazine yield (4-chloro-12-methyl-16,17-dihydro-15-thia-6,11-diazacyclopenta[a]- phenanthren-7-ylsulfanyl)acetic acid hydrazide (2) is discussed. The reactive acid hydrazide compound 2 was utilized for the synthesis of amides 3, Schiff’s bases 4 and thiazolidine 5 derivatives. The structures of target compounds were confirmed by elemental analysis and spectral data. The antimicrobial activity of new compounds were studied against Streptococcus sp., Bacillus megaterium, Staphylococcus aureus, Escherichia coli, Bacillus cereus, Bacillus subtilis, Proteus valgaris and Pseudomonas aeroginosa by the agar well diffusion method. Compounds 4b, 5a, 5b and 5c showed good antimicrobial activity

2019 ◽  
Vol 18 (5) ◽  
pp. 262-274
Author(s):  
E. Benyagoub ◽  
N. Nabbou ◽  
S. Boukhalkhel ◽  
I. Dehini

The medicinal value of the plants is due to their chemical components that bring a definite physiological action on the human body to prevent the diseases. In this work, we investigated the antimicrobial activity of leaves’ extracts of Quercus robur L., collected from the Algerian upper highlands, on ten bacterial strains and one fungal strain known to be pathogenic. First, we performed a qualitative phytochemical analysis, and second, antimicrobial activity tests performed by agar diffusion method (disc and well) with the determination of MIC by broth macro-dilution method. Given the results, it appears that obtained macerates of Quercus robur L. were rich in bioactive phytoconstituents such as alkaloids, anthraquinones, saponins, tannins, and other components. The yield of aqueous and methanolic macerates of leaves was 8.5 ± 1.41 and 22.4 ± 4.36%, respectively. The bacterial resistance was relatively important to several antibiotics, namely, ampicillin, amoxicillin + clavulanic acid for strains of Escherichia coli and Salmonella sp. However, Staphylococcus aureus strains were resistant to fusidic acid, penicillin, and oxacillin; while Enterococcus faecalis was resistant to fusidic acid, penicillin, oxacillin, and ticarcillin. The antibacterial activity of the macerates toward tested microbial strains showed that the aqueous and methanolic macerates of the leaves were proportional to the tested concentration and active not only against Gram-positive and Gram-negative bacteria but also on the fungal species Candida albicans. The estimated MIC for Escherichia coli, Enterococcus faecalis, and Staphylococcus aureus was in the order of 10 mg/mL, which seems more effective than toward Salmonella sp., Klebsiella pneumoniae, Pseudomonas aeruginosa, and Candida albicans which were in the order of 30 mg/mL. These preliminary results confirm that the part of the studied plant had a very good antimicrobial activity that was proportional to the serial concentrations of the tested extracts.


2020 ◽  
Vol 22 (97) ◽  
pp. 74-78
Author(s):  
T. I. Stetsko ◽  
Ya. M. Liubenko ◽  
V. N. Padovskyi ◽  
L. L. Ostrovska ◽  
O. Yo. Kalinina ◽  
...  

Fluoroquinolones are critical antimicrobials for both human and veterinary medicine. Due to their unique mechanism of antimicrobial action and good pharmacokinetic properties, they are often the first choice drugs in the treatment of bacterial infections in animals. The purpose of the investigation was to study the antimicrobial activity of a third-generation fluoroquinolone antibiotic of danofloxacin against bacteria, pathogens of respiratory and intestinal infection in goats. The samples of the nasal outflows (respiratory infection) and fecal masses (intestinal infection) were collected from clinically ill goats for microbiological studies. The sensitivity test of the microflora of the biomaterial, carried out by the disco-diffusion method, showed that the microorganisms of all the samples were sensitive to danofloxacin. Bacteria Streptococcus pneumonia (n = 10), Staphylococcus aureus (n = 4) and Escherichia coli (n = 2) were isolated and identified from nasal exudate samples (n = 10). Pathogenic strains of Escherichia coli were isolated from all faecal samples (n = 12). The degree of bacteriostatic activity of danofloxacin was determined by establishing its minimum inhibitory concentration (MIC) for bacterial isolates by sequential dilutions in a liquid nutrient medium. The average MIC of danofloxacin for Streptococcus pneumoniae isolates was 0.26 ± 0.13 μg/ml and for Staphylococcus aureus isolates – 0.25 ± 0.075 μg/ml. For Escherichia coli strains isolated from faeces of goats suffering from coli infection, the average MIC of danofloxacin was 0.38 ± 0.12 μg/ml (range 0.2 to 0.8 μg/ml). Antimicrobial sensitivity testing have shown a high level of bacteriostatic activity of danofloxacin against bacteria, pathogens of respiratory and intestinal infections in goats. This may be the argument for the use of danofloxacin-based chemotherapeutic agents in the treatment of bacterial infections in goats, especially for the empirical approach to therapy.


Author(s):  
SUNDAR MADASAMY ◽  
SURESH SUNDAN ◽  
LINGAKUMAR KRISHNASAMY

Objective: A simple formulation of cold cream from methanolic extract Caralluma adscendens var. attenuata (MECA) and their antimicrobial activity was tested against various clinical pathogens, namely, Escherichia coli, methicillin-resistant Staphylococcus aureus, vancomycin-resistant Enterococcus faecium, and Candida albicans. Methods: Methanol extract of these plant extract was prepared by the Soxhlet method. We analyzed phytochemical nature of theses plant, and subsequently, a cream was formulated cold-cream C. adscendens var. attenuata (FCA) different concentration such as FCA 50 mg, FCA 100 mg, and FCA 200 mg. In the present study, aimed to the antimicrobial activity of cold cream was measured by agar well diffusion method, and standard antibiotic Neosporin (market available) cream was used as positive control and dummy cold cream (without-MECA) were used as the negative control. Results: Phytochemical screening showed that the plant extracts were found a rich source of secondary metabolites. For more, the efficacy of cold cream from MECA extracts to against the clinical pathogen. Positive control Neosporin and 200 mg FCA cream was a highly significant difference in the zone of inhibition when compared to dummy cream. The 200 mg FCA was activity against Escherichia coli, methicillin-resistant Staphylococcus aureus, vancomycin-resistant E. faecium, and C. albicans highly significantly difference (p<0.05) compared FCA 50 mg and FAC 100 mg creams. Conclusion: The results from this study suggested that the cold cream form base of MECA crude had antimicrobial activity in the different clinical pathogen. They could be used as an alternative source to conventional antimicrobial agents for the treatment of pathological infection.


2020 ◽  
Vol 2020 ◽  
pp. 1-7 ◽  
Author(s):  
Pavithra L. Jayatilake ◽  
Helani Munasinghe

Endophytic and rhizosphere fungi are understood to be aiding the host plant to overcome a range of biotic and abiotic stresses (nutrition depletion, droughts, etc.) hence, they remain to be reservoirs of plethora of natural products with immense use. Consequently, this investigation of endophytic and rhizosphere fungi isolated from Mikania cordata (a perennial vine that is well established in Sri Lanka) for their antimicrobial properties was performed with the aim of future derivation of potential beneficial pharmaceutical products. Leaves, twigs, and roots of M. cordata were utilized to isolate a total of 9 endophytic fungi out of which the highest amount (44%) accounted was from the twigs. A sample of the immediate layer of soil adhering to the root of M. cordata was utilized to isolate 15 rhizosphere fungi. Fusarium equiseti and Phoma medicaginis were endophytes that were identified based on colony and molecular characteristics. The broad spectrum of antimicrobial activity depicted by F. equiseti (MK517551) was found to be significantly greater (p≤0.05, inhibitory against Bacillus cereus ATCC 11778, Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, and Pseudomonas aeruginosa ATCC 25853) than P. medicaginis (MK517550) (inhibitory against Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, and Pseudomonas aeruginosa ATCC 25853) as assessed using the Kirby-Bauer disk diffusion method. Trichoderma virens and Trichoderma asperellum were rhizospere fungi that exhibited remarkable antimicrobial properties against the test pathogens chosen for the study. T. asperellum indicated significantly greater bioactivity against all four bacterial pathogens and Candida albicans ATCC 10231 under study. The ranges of minimum inhibitory concentrations (MICs) of the fungi depicting antimicrobial properties were determined. The results obtained suggest that F. equiseti, P. medicaginis, T. asperellum, and T. virens of M. cordata harness bioprospective values as natural drug candidates. This is the first report on isolation and evaluation of the antimicrobial properties of endophytic and rhizosphere fungi of Mikania cordata.


2017 ◽  
Vol 901 ◽  
pp. 124-132
Author(s):  
Artania Adnin Tri Suma ◽  
Tutik Dwi Wahyuningsih ◽  
Deni Pranowo

Some novel N-phenylpyrazolines were synthesized and investigated for their antibacterial activitiy. Chalcones 2-4 which were prepared from acetophenone and veratraldehyde derivatives were reacted with phenylhydrazine to give N-phenylpyrazolines 5-7. All of the synthesized compounds were characterized using FTIR, GC-MS, and NMR spectrometers. Further, antibacterial activity of N-phenylpyrazolines were evaluated by agar well-diffusion method against Staphylococcus aureus, Bacillus cereus, Bacillus subtilis, Escherichia coli, and Shigella flexneri. The highest activity (highest inhibition zone) of compound 5 was 2.6 mm (at 1000 ppm) against B. subtillis, compound 6 was 7.25 mm (at 1000 ppm) against S. aureus, and compound 7 was 6.75 mm (at 500 ppm) against S. aureus. The results indicated that compound 6 and 7 exhibited promising antibacterial activity.


2001 ◽  
Vol 56 (1-2) ◽  
pp. 82-88 ◽  
Author(s):  
Ahmed G. Hegazi ◽  
Faten K. Abd El Hady

Abstract The antimicrobial activity of four propolis samples collected from Upper Egypt against Staphylococcus aureus; Escherichia coli and Candida albicans was evaluated. There was a variation in the antimicrobial activity according to the propolis origin. Banisweif propolis showed the highest antimicrobial activity against Staphylococcus aureus, Escherichia coli and Candida albicans, but Fayoum propolis had moderate activity against all tested pathogens. Propolis collected from Assiut and Souhag gave lower antimicrobial activity. Propolis samples were investigated by GC/MS, 71 compounds were identified, 14 being new for propolis. Banisweif propolis is characterized by the presence of 7 caffeate esters and 4 triterpenoids. Fayoum propolis showed the highest amount of lactic acid and the presence of 3 chalcones. But Assiut propolis is characterized by the presence of 4 prenylated coumar-ates. Souhag propolis is characterized by the presence of 5 aliphatic dicarboxylic acids and some other new compounds to propolis.


2021 ◽  
Vol 10 (25) ◽  
pp. 1899-1903
Author(s):  
Mohsin Ali Khan ◽  
Shadma Yaqoob ◽  
Sharique Ahmad

BACKGROUND Azadirachta indica, commonly known as neem, neem tree or Indian lilac, Limbo, Nim, Nimba, Medusa and Vempu. It is typically grown in tropical and subtropical regions. Neem belongs to family meliaceae. Neem is a native tree of India. It is also called “village pharmacy of south Asia” (India) because of its enormous medicinal properties and people use it most of the time without knowing its multiple advantages. This study was done to know the efficacy of medicinal plant named Azadirachta indica (Neem) against pathogenic microorganisms and about its utility as disinfectant and floor cleaner. METHODS Agar well diffusion method, Culture plate method, inoculum preparation & its subculture methods were used to determine the antimicrobial activity of the neem leaf extract. Different concentrations of neem leaf extracts in culture plates were used for the study. In this method inhibited zones were measured. RESULTS Neem leaf extracts showed considerable antimicrobial activity against four target pathogens. In agar well diffusion method it showed maximum antimicrobial activity against Enterococcus and Staphylococcus aureus. Growth of inhibition was increased as the concentration of the neem extract in agar media increased and was maximum for Staphylococcus aureus. CONCLUSIONS The extract of A. indica, has antimicrobial activity against target pathogens Enterococcus, Staphylococcus aureus, Pseudomonas, and E.coli. With the old medicinal knowledge on neem, better economic and therapeutic utilization can be done by using modern approaches of drug development. KEY WORDS Neem Leaf extract, Antimicrobial Activity, Agar Well Diffusion Test, Zone of Inhibition


2021 ◽  
Author(s):  
Mbarga Manga Joseph Arsene ◽  
Podoprigora Irina Viktorovna ◽  
Anytoulou Kitio Linda Davares ◽  
Mouafo Hippolyte Tene ◽  
Irma Aurelia Monique Manga ◽  
...  

Background and aim: The Cameroonian flora abounds in plants with multidimensional therapeutic virtues which can play an important role in the fight against resistance to antibiotics and the search for new antimicrobials. This study aimed to screen the antimicrobial potential of aqueous and ethanolic extracts of thirteen (13) samples (Bark, leaf, seed) of eight (8) plants from Cameroon against 3 reference pathogens and to evaluate their synergy with conventional antibiotics against eleven (11) multiresistant uropathogenic (MRU) bacteria. Method: Bioactive compounds were extracted from leaves of Leucanthemum vulgare, Cymbopogon citratus (DC.) Stapf, Moringa oleifera Lam and Vernonia amygdalina Delile; barks of Cinchona officinalis and Enantia chlorantha Oliv; barks and seeds of Garcinia lucida Vesque and leaves and seeds of Azadirachta indica (Neem) using distilled water and ethanol as solvents. The extracts were tested against Escherichia coli ATCC 25922, Staphylococcus aureus ATCC 6538 and Candida albicans 10231 using the well diffusion method and the microdilution method. The synergistic effect was assessed (using disc diffusion method and the checkerboard method) against MRU bacteria namely Achromobacter xylosoxidans 4892, Citrobacter freundii 426, Enterococcus avium 1669, Escherichia coli 1449, Klebsiella oxytoca 3003, Kocuria rizophilia. 1542, Moraxella catarrhalis 4222, Morganella morganii 1543, Pseudomonas aeruginosa 3057, Staphylococcus aureus 1449 and Streptococcus agalactiae 3984. Results: We found that distilled water extracted a more important mass of phytochemical compounds (7.9-21.2%) compared to ethanol (5.8-12.4%). Except C. officinalis and G. lucida leaves, the rest of extracts were active with inhibition diameters (ID) ranging from 5 to 36 mm. Both ethanolic (EE) and aqueous extract (AE) of E. chloranta bark (ECB) were the most active against all pathogens with the mean ID of 17 and 36 mm vs S. aureus ATCC 6538, 23 and 14 mm vs E. coli ATCC 25922 and 36 and 19 mm vs C. albicans ATCC 10231. Only the EE of E. chloranta bark (ECB) had a strong activity against all the microorganisms tested (MIC <2 mg / ml); L. vulgare leaves (LVL) and G. lucida seed (GLS) had moderate (average MIC of 8 mg/ml) while all other extracts showed very weak antimicrobial activity. In addition, the fractional inhibitory concentration (FIC) ranged from 0.125 to 0.750. No antagonism (FIC> 4) or indifference (1≤ FIC≤4) was noted between the extracts and the antibiotics, but the best synergies were found with ECB which well-modulated Kanamycin (FIC = 0.125 against S. aureus and 0.250 against E. coli), nitrofurantoin (FIC = 0.250 against S. aureus and 0.188 against E. coli) and ampicillin (FIC = 0.125 against E. coli). Similarly, compared to other extracts, ECB, LVL and GLS also well-modulated ampicillin, ceftazidime, tetracycline, nitrofurantoin, and trimethoprim against all the above-mentioned resistant uropathogenic bacteria with important increase in fold area (IFA). Conclusion: This study show that E. chlorantha bark, L. vulgare leaves G. lucida seed, have good antimicrobial activity against both bacteria (Gram positive and Gram negative) and fungi (C. albicans); and should be more investigated for their possible use to the fight against MDR and MRU microorganisms.


Author(s):  
GANDONOU Dossa Clément ◽  
BAMBOLA Bouraïma ◽  
TOUKOUROU Habib ◽  
GBAGUIDI Ahokannou Fernand ◽  
DANSOU Christian ◽  
...  

Present study involves the study of the chemical composition of the essential oils extracted from the leaves by gas chromatography and gas chromatography coupled with mass spectrometry of Lippia multiflora harvested in the regions of Kétou, Savalou, Bohicon and Mono and tested by the well diffusion method against pathogenic microorganisms. The essential oils studied are terpene compounds, aromatic compounds, aliphatic compounds and other natural substances. The inhibition zone diameters determined allowed us to evaluate their degree of germ sensitivity of the strains tested. Essential oils extracted from Lippia multiflora harvested in these areas have the most pronounced antimicrobial activity. In total, the essential oils tested have different and specifically a degree of sensitivity against Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, Proteus mirabilis A24974, Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae and Pseudomonas aeruginosa except that harvested in the Savalou who does not have no degree of sensitivity on Pseudomonas aeruginosa. This work paves the way for food preservation with extracted natural substances and also the formulation of natural antimicrobials for this fact.


2019 ◽  
Vol 12 (2) ◽  
Author(s):  
Gino Nemesio Cepeda ◽  
Meike Meilan Lisangan ◽  
Isak Silamba ◽  
Nitia Nilawati ◽  
Eka Syartika

ABSTRACT  Akway (Drimys piperita) is a woody, evergreen and aromatic plant that belongs to family winteraceae. This plant is used by Sougb tribe lived in Sururey village, District of Anggi, to enhance the vitality of body. The objectives of the research were to determine antimicrobial stability of akway bark extracts influenced by heating time of 100OC, levels of acidity (pH) and salt contents.. Antimicrobial assays were done by using agar well diffusion method against four species of bacteria, i.e.  Escherichia coli ATCC25922, Bacillus cereus ATCC10876, Pseudomonas aeruginosa ATCC27853 and Staphylococcus aureus ATCC25923. The results showed that ethanolic extracts of akway bark only inhibited growth of B. cereus and S. aureus with minimum inhibitory concentration 0,99% and 0,89% . The levels of concentration and acidity of ethanol extracts  influenced the antimicrobial capacity of extracts.. Whereas heating time on 100OC during 25 minutes and salt contents  up to 5% of extract solution did not influence the antimicrobial stability of  akway bark extracts. Key words : akway, extracts, antimicrobe, pH, Heating, salt ABSTRAK Akway (Drimys piperita) adalah tumbuhan berkayu, aromatik dan hijau sepanjang tahun dan tergolong dalam suku winteraceae. Tumbuhan ini digunakan oleh Suku Sougb yang bermukim di desa Sururey Distrik Anggi, untuk mengobati malaria dan meningkatkan vitalitas tubuh. Tujuan dari penelitian ini adalah untuk menentukan stabilitas antimikroba ekstrak kulit kayu akway pada waktu pemanasan ekstrak pada 100OC, tingkat keasaman (pH) dan kandungan garam. Pengujian antimikroba dilakukan dengan menggunakan metode difusi agar terhadap empat spesies bakteri yaitu Escherichia coli ATCC25922, Bacillus cereus ATCC10876, Pseudomonas aeruginosa ATCC27853 and Staphylococcus aureus ATCC25923. Hasil menunjukkan bahwa ekstrak etanol kulit kayu akway hanya dapat menghambat bakteri Bacillus cereus dan Staphylococcus aureus dengan konsentrasi hambat minimum masing-masing adalah 0,99% dan 0,89%. Tingkat konsentrasi dan keasaman (pH) mempengaruhi kapasitas antimikroba ekstrak etanol kulit kayu akway. Sedangkan perlakuan pemanasan pada suhu 100OC dengan lama pemanasan sampai dengan 25 menit dan penambahan garam NaCl sampai konsentrasi 5%  tidak berpengaruh pada stabilitas antimikroba ekstrak etanol kulit kayu akway.  


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