scholarly journals Synthesis and antibacterial screening of new N-Substituted-9H-β-carboline 6-amine derivatives

2020 ◽  
Vol 11 (3) ◽  
pp. 4146-4151
Author(s):  
Alivelu Samala ◽  
Srinivasa Murthy M ◽  
Krishna Mohan Gottumukkala

β-Carboline is also known as nor-harmane. It is a nitrogen-containing heterocyclic compound formed in plants and animals as Maillard reaction products between amino acids and reducing sugars or aldehydes. These tricyclic nitrogen heterocyclics play a vital role in medicinal chemistry, due to significant biological activities of their derivatives. It is also a key pharmacophore present in a large number of natural tricyclic alkaloids. Current work is reported with the synthesis and antibacterial activity screening of a new series of N-Substituted-9H-β-carboline-6-amine derivatives. The title compounds were synthesized according to the well known Pictet Spengler reaction in three steps by taking 5-Chlorotryptamine and glyoxalic acid as starting materials. This is an acid-catalyzed intramolecular condensation of an iminium ion and an aromatic C-nucleophile which resulted in the formation of 6-Chloro-1,2,3,4-tetrahydro-9H-pyrido[3,4-b]indol-2-ium-1-carboxylate (3). Oxidative decarboxylation and aromatization of compound 3 with iodobenzene diacetate led to the 6-Chloro-β–carboline (4) which were treated with different mono substituted amines gave the title compounds (5 a-J). Structures of the synthesized entities were confirmed spectroscopically (FT-IR, 1H NMR and Mass) and screened for antibacterial activity against various pathogenic bacterial strains ( Streptococcus pyogenes, Bacillus subtilis, Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa) by disc diffusion method. The title compounds showed moderate to good antibacterial activity.

Antibiotics ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 717
Author(s):  
Rita Abou Nader ◽  
Rawan Mackieh ◽  
Rim Wehbe ◽  
Dany El El Obeid ◽  
Jean Marc Sabatier ◽  
...  

Honeybees are one of the most marvelous and economically beneficial insects. As pollinators, they play a vital role in every aspect of the ecosystem. Beehive products have been used for thousands of years in many cultures for the treatment of various diseases. Their healing properties have been documented in many religious texts like the Noble Quran and the Holy Bible. Honey, bee venom, propolis, pollen and royal jelly all demonstrated a richness in their bioactive compounds which make them effective against a variety of bacterial strains. Furthermore, many studies showed that honey and bee venom work as powerful antibacterial agents against a wide range of bacteria including life-threatening bacteria. Several reports documented the biological activities of honeybee products but none of them emphasized on the antibacterial activity of all beehive products. Therefore, this review aims to highlight the antibacterial activity of honey, bee venom, propolis, pollen and royal jelly, that are produced by honeybees.


2020 ◽  
Vol 21 (2) ◽  
Author(s):  
Magdalena Woźniak ◽  
Lucyna Mrówczyńska ◽  
Anna Sip ◽  
Izabela Ratajczak

Introduction. Herbal bee products, including honey, propolis and pollen, are wide applied in various branches of industry due to their natural origin and biological activities. Bee products exhibit e.g. antioxidant, antibacterial and antifungal activity. In addition, honey, propolis and pollen characterize diverse and complex chemical composition. Aim. The aim of the study was to determine antioxidant and antibacterial activity of honey, propolis and pollen from the Sowie Mountains. Material and methods. In the study, honey, propolis and pollen collected from an apiary located in the Sowie Mountains were used. The tested bee products were extracted with ethanol, and the obtained extracts from bee products were used to determine their antioxidant and antibacterial activity. The antioxidant potential of bee products were evaluated applying DPPH· free radical scavenging activity assay. The antimicrobial activity of the tested bee products was determined by the point-diffusion method against 13 strains of pathogenic and potentially pathogenic bacteria. In addition, the total content of phenolic compounds in the tested bee products was determined by the Folin-Ciocalteu method. Results. Among the tested bee products, propolis exhibited the highest antioxidant activity. The antiradical activity of propolis was equal to 96% approx. activity of Trolox, the standard antioxidant used in this study. Propolis had the highest total phenol content. All bee products showed antagonistic activity against all tested bacterial strains, however, propolis was characterized by the highest antibacterial activity. Conclusions. The obtained results indicate that among the tested bee products (honey, propolis and pollen), the highest antioxidant and antibacterial activity showed propolis. The high biological activity of propolis is associated with the high content of phenolic compounds.


2014 ◽  
Vol 1 (1) ◽  
pp. 45-53 ◽  
Author(s):  
Yared Wasihun ◽  
Tesfalem Adraro ◽  
Solomon Ali

There are quite large numbers of traditionally used medicinal plants that are used to treat skin disorder in the ethno medical system of Ethiopia. Medicinal plants namely L. adoensis, was screened for antibacterial activity against different strains of bacteria which are known to cause various types of skin infections and food poisoning Anti bacterial effect of the plant species was evaluated against different bacterial strains. The leaves of plant species were extracted by maceration and soxhelt extraction technique for preparation of crude and fractional extract respectively. And anti bacterial screening of different concentration of both crude and fractional extract of the plant species were determined using agar well diffusion method. The test organisms were one gram positive (S.aures) and three gram negative (Salmonella typhi, E.coli and P.aeruginosa) standard organisms. The results of the initial antibacterial screening test indicated the potential of these herbal drugs in treating bacterial infections of the skin and food poisoning. Among the different fractions (petroleum ether, chloroform, acetone and methanol) tested for antibacterial activity, the non-polar fractions were found to be more active than the polar fractions. The Phytochemical screening tests carried out on L. adoensis indicated the presence of tannins, flavonoids and saponins. Different extracts L.adoensis were showed significant antibacterial activity against the S.aueres, P.aeroginosa, E.coli and S.typhi. Hence further study is recommended to identify the specific active ingredient and potential formulation of effective antibiotic.  


2016 ◽  
Vol 15 (1) ◽  
Author(s):  
Mohammed Dahiru Ahmed ◽  
Mohamed Imad Mustafa Mahmoud ◽  
Muhammad Taher

Introduction: The leaves of Glochidion superbum and other similar plants had been in use as a folk medicine by indigenous people in South East Asia for treatment of wound infections and diarrhoea. As recommended by WHO, studies on medicinal plants should include both identification of the chemical constituents and determination of their biological activities. Thus, the study aims to screen various local plant extracts for antibacterial activity and determine the extract fraction showing the highest antibacterial activity. Methods: In this study, Glochidion superbum leaves methanol extract was selected after preliminary antibacterial screening of this extract alongside extracts of Rennellia elliptica (leaves and roots) and Uncaria acida (stem and leaves) by the agar disc diffusion method against Escherichia coli ATCC 35218, Pseudomonas aeruginosa ATCC 27853, Staphylococcus aureus ATCC 25923, and Bacillus subtilis ATCC 11778. Furthermore, methanol leave extract of Glochidion superbum was subjected to a qualitative phytochemical screening. The extract was fractionated using Vacuum Liquid Chromatography (VLC) method and the following fractions were obtained: methanol 2.2 g (4.7%), ethylacetate 38.3 g (81.4%) and ethylacetate:methanol 5.0 g (10.6%). Results: The ethylacetate:methanol 1:1 fraction showed the highest in vitro dose-dependent inhibitory activity at concentrations of 25, 50, 100 and 150 mg/mL against the growth of E. coli ATCC 35218, and S. aureus ATCC 25923. Conclusions: This research has demonstrated proof of concept that the plant extract of Glochidion superbum leaves has antibacterial activity against both gram-positive and gram-negative bacteria.


2019 ◽  
Vol 16 (3) ◽  
pp. 245-248
Author(s):  
Hummera Rafique ◽  
Aamer Saeed ◽  
Ehsan Ullah Mughal ◽  
Muhammad Naveed Zafar ◽  
Amara Mumtaz ◽  
...  

Background: (±)-6,8-Dihydroxy-3-undecyl-3,4-dihydroisochromen-1-one is one of the structural analog of several substituted undecylisocoumarins isolated from Ononis natrix (Fabaceae), has been successfully synthesized by direct condensation of homopthalic acid (1) with undecanoyl chloride yields isochromen-1-one (2). Methods: Alkaline hydrolysis of (2) gave the corresponding keto-acid (3), which is then reduced to hydroxy acid (4) then its cyclodehydration was carried out with acetic anhydride to afford 3,4- dihydroisochromen-1-one (5). Followed by demethylation step, the synthesis of target 6,8- dihydroxy-7-methyl-3-undecyl-3,4-dihydroisocoumarin (6) was achieved. Results: In vitro antibacterial screening of all the synthesized compounds were carried out against ten bacterial strains by agar well diffusion method. Conclusion: Newly synthesized molecules exhibited moderate antibacterial activity and maximum inhibition was observed against Bacillus subtilus and Salmonella paratyphi.


Author(s):  
Selvarani Murugan

Objective: Resistance to antibacterial agents by pathogenic bacteria has emerged in recent years and is a major challenge for the healthcare industry. Copper nanoparticles (CuNPs) are known to be one of the multifunctional inorganic nanoparticles with effective antibacterial activity. Hence the present investigation has been focused on synthesizing and evaluating the bactericidal effect of copper nanoparticles.Methods: CuNPs were synthesized by reducing the aqueous solution of copper sulfate with sodium borohydride. The synthesized particles were characterized by x-ray diffractogram (XRD), scanning electron microscopy (SEM) and energy dispersive spectroscopy (EDS) techniques to analyze size, morphology and quantitative information respectively. The antibacterial activity of CuNPs was examined by agar well diffusion method. Synergistic effect of CuNPs with broad-spectrum antibiotics was determined by the agar disc diffusion method.Results: Color change of reaction mixture from blue to dark brown indicated the formation of CuNPs. SEM image clearly demonstrated that the synthesized particles were spherical in shape and its size was found to be 17.85 nm. EDS report confirmed the presence of elemental copper in the resultant nanoparticles and its accounts for major proportion (96%) of the mass of nanoparticles. Bacterial effect of CuNPs revealed that Pseudomonas aeruginosa showed the highest antibacterial sensitivity (16.00±1.63 mm), whereas least susceptibility (9.67±0.47 mm) was noticed against Staphylococcus aureus. An enhanced antibacterial activity of commercial antibiotics was also noticed when it combined with CuNPS. A minimum zone of inhibition was increased from 0.67±0.47 mm to 10.66±0.24 mm when the nanoparticles and antibiotics were given together.Conclusion: It was observed that copper nanoparticles exhibited profound activity against all the tested bacterial strains which shows that CuNPs may serve as a better option for use in medicine in the future.


2021 ◽  
Vol 13 (1) ◽  
pp. 106-112
Author(s):  
Sri Kasmiyati ◽  
Elizabeth Betty Elok Kristiani ◽  
Maria Marina Herawati ◽  
Andreas Binar Aji Sukmana

The medicinal plant-derived bioactive compounds have a potential for many biological activities, including antimicrobial activity. Artemisia cina is a medicinal plant from the Compositae family with the potential of having antitumor, antifungal, and antibacterial activity. This study aimed to determine the antibacterial activity and the flavonoid content of A. Cina’s ethyl acetate extract. Plants samples were extracted by ethyl acetate maceration method. Antibacterial activity was tested against Gram-negative bacteria (Escherichia coli and Pseudomonas aeruginosa) and Gram-positive bacteria (Bacillus subtilis and Staphylococcus aureus) by a disk diffusion method using 25, 50, and 100 mg/l extract concentrations. The flavonoid contents (quercetin and kaempferol) were measured using High-Performance Liquid Chromatography. The extracts of diploid and polyploid A. cina displayed some antibacterial activity, with the Gram-negative bacteria being more resistant than the Gram-positive counterpart. However, no significant difference was observed between the diploid and polyploid extracts. As for the flavonoid content, the highest quercetin content (0.5501 mg/ml) was found in the polyploid A. cina (J), while the highest kaempferol content (0.5818 mg/ml) was observed in the diploid A. cina (KJT). Although A. cina is widely grown in Indonesia, compared to other Artemisia species, A. cina has not been widely studied, especially its antibacterial  potential and in related to its flavonoid content and the use of ethyl acetate as the extraction solvent.  This study reveals the potential of A. cina as a natural antibacterial agent. 


Author(s):  
Messai Amel

The objective of this work is the synthesis of new quinoline molecules which could have some biological activities. This chapter reported a new approach to the synthesis of some quinoline derivatives. The Baylis-Hillman reaction on 2-methoxy-3-formyl quinoléines derivatives have applied in order to obtain Baylis-Hillman adducts. The products are characterized by FTIR, NMR and X-ray single crystal diffraction .Also, a study of the antibacterial activity of the 3-(2-chloro quinoline)-3-hydroxy-2 methylene propanonitrile products synthesized have been explored. This assessment is made by using the disk diffusion method. The results showed that the 3-(2'-chloroquinoline)-3-hydroxy-2-methylenepropanonitril derivatives present a good antibacterial effectiveness against the strains tested Gram-positive and no antibacterial potency was observed against the stains Gram-negative used in the test.


2019 ◽  
Vol 2019 ◽  
pp. 1-4
Author(s):  
Yohannes Kelifa Emiru ◽  
Ebrahim Abdela Siraj ◽  
Tekleab Teka Teklehaimanot ◽  
Gedefaw Getnet Amare

Objective. To evaluate the antibacterial effects of the leaf latex of Aloe weloensis against infectious bacterial strains. Methods. The leaf latex of A. weloensis at different concentrations (400, 500, and 600 mg/ml) was evaluated for antibacterial activities using the disc diffusion method against some Gram-negative species such as Escherichia coli (ATCC 14700) and Pseudomonas aeruginosa (ATCC 35619) and Gram-positive such as Staphylococcus aureus (ATCC 50080) and Enterococcus fecalis (ATCC 4623). Results. The tested concentrations of the latex ranging between 400 and 600 mg·mL−1 showed significant antibacterial activity against bacterial strain. The highest dose (600 mg/ml) of A. weloensis leaf latex revealed the maximum activity (25.93 ± 0.066 inhibition zone) followed by the dose 500 mg/ml against S. aureus. The lowest antibacterial activity was observed by the concentration 400 mg/ml (5.03 ± 0.03) against E. coli. Conclusion. The results of the present investigation suggest that the leaf latex of A. weloensis can be used as potential leads to discover new drugs to control some bacterial infections.


2019 ◽  
Vol 31 (9) ◽  
pp. 1905-1912 ◽  
Author(s):  
Kummara Srinivasulu ◽  
Katreddi Hussain Reddy ◽  
K. Anuja ◽  
D. Dhanalakshmi ◽  
Golla Ramesh

Metal complexes having the composition M(Bipy)Cl2 (where, M = Cu(II), Ni(II) and Co(II); Bipy = 2,2-bipyridyl) are reacted with 2-acetylthiophene thiosemicarbazone (ATT) to produce heteroleptic transition metal complexes with molecular formula [M(Bipy)ATT]. The complexes are characterized by mass spectra, molar conductivity, infrared and electronic spectra. Electrochemical behaviour of these metal complexes was investigated by cyclic voltammetric studies. The metal complexes show quasi reversible cyclic voltammetric responses for the Cu(II)/Cu(I) couple. The binding properties of these complexes with calf-thymus DNA have been investigated by using absorption spectrophotometry. Metal complexes are screened for their antibacterial activity by using agar well diffusion method against pathogenic bacterial strains viz. Escherichia coli and Staphylococcus aureus. Antibacterial activity of the present complexes are comparable with the activity of ciprofloxacin. The Cu(Bipy)Cl2 complex inhibits bacteria more strongly than any other complex. The Ni(Bipy)ATT complex shows more activity than the parent complex, Ni(Bipy)Cl2.


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