Antiviral and Antimicrobial Profiles of Selected Isoquinoline Alkaloids from Fumaria and Corydalis Species

2007 ◽  
Vol 62 (1-2) ◽  
pp. 19-26 ◽  
Author(s):  
Ilkay Orhan ◽  
Berrin Özçelik ◽  
Taner Karaoğlu ◽  
Bilge Şener
Keyword(s):  
Rna Virus ◽  
Selective Inhibition ◽  
Antimicrobial Activities ◽  
Isoquinoline Alkaloids ◽  
Antibacterial And Antifungal Activities ◽  
Microdilution Method ◽  
Antibacterial And Antifungal ◽  
Toxic Concentrations ◽  
Derivatives Of

In the current study, 33 isoquinoline alkaloids belonging to protopine-, benzylisoquinoline-, benzophenanthridine-, spirobenzylisoquinoline-, phthalideisoquinoline-, aporphine-, protoberberine-, cularine-, and isoquinolone-types as well as 7 derivatives of them obtained from some Fumaria and Corydalis species growing in Turkey have been evaluated for their in vitro antiviral and antimicrobial activities. Both DNA virus Herpes simplex (HSV) and RNA virus Parainfluenza (PI-3) were employed for antiviral assessment of the compounds using Madine- Darby bovine kidney and Vero cell lines and their maximum non-toxic concentrations (MNTC) and cytopathogenic effects (CPE) were determined using acyclovir and oseltamivir as the references. Antibacterial and antifungal activities of the alkaloids were tested against Escherichia coli, Pseudomonas aeruginosa, Proteus mirabilis, Klebsiella pneumoniae, Acinetobacter baumannii, Staphylococcus aureus, Bacillus subtilis, and Candida albicans by the microdilution method and compared to ampicilline, ofloxacine, and ketocanazole as the references. The alkaloids did not present any notable antibacterial effect, while they had significant antifungal activity at 8 μg/ml concentration. On the other hand, the alkaloids were found to have selective inhibition against the PI-3 virus ranging between 0.5 and 64 μg/ml as minimum and maximum CPE inhibitory concentrations, whereas they were completely inactive towards HSV.

scholarly journals Synthesis,Characterization and Evaluation of the Anticancer and Antimicrobial Activities of Some Novel Benzazole and Benzazine Derivatives

2007 ◽  
Vol 3 (3) ◽  
pp. 252-263
Author(s):  
Wesam Saber Shehab ◽  
Naglaa Z.H. Eleiwa ◽  
Samar.M. Mouneir
Keyword(s):  
Cancer Cells ◽  
Benzimidazole Derivative ◽  
Coupling Reaction ◽  
Antimicrobial Activities ◽  
Spectral Studies ◽  
Design Modification ◽  
Future Design ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal

The present study was designed to synthesize  and develop new useful lead compounds (some novel benzazole and benzazine derivatives ) of simple structure , exhibiting optimal in vitro anticancer  and antimicrobial potency. Phenylenediamine derivative 1 was condensed  with  dithiocarboxylic acid derivatives 2 and produced   benzimidazole derivative 4. The benzotriazepines 8 and 10  were formed by the reaction of 1 with dicarbonyl derivatives followed by intermolecular coupling reaction. The synthesis of benzotriazine12, benzotriazole 14,17, benzimidazole16 and benzothiadiazine 19 from compound 1 was also described. The Synthesized Compounds were characterized by Spectral Studies like IR, H1 – NMR and Analysis Spectra .The title compounds were screened for their possible In vitro anticancer and antimicrobial activities. Among the synthesized compounds, some have shown promisingly remarkable activities against  different  cancer cell lines (MCF-7 human breast cancer cells, HepG2 human hepatocarcinoma cells and PC3 human prostate cancer cells)and moderate  to high antibacterial and antifungal activities. The obtained results showed that the most active compounds could be useful as a template for future design, modification and investigation to produce more active analogs.

Antiviral and Antimicrobial Assessment of Some Selected Flavonoids

2006 ◽  
Vol 61 (9-10) ◽  
pp. 632-638 ◽  
Author(s):  
Berrin Özçelik ◽  
Ilkay Orhan ◽  
Gülnur Toker
Keyword(s):  
Inhibitory Concentration ◽  
Rna Virus ◽  
Antiviral Effect ◽  
Dna Virus ◽  
E Coli ◽  
Antibacterial And Antifungal Activities ◽  
Microdilution Method ◽  
Vero Cell Lines ◽  
Antibacterial And Antifungal ◽  
Cytopathogenic Effect

AbstractIn the current study, the results of antibacterial, antifungal, and antiviral activity tests of four flavonoid derivatives, scandenone (1), tiliroside (2), quercetin-3,7-O-α-ʟ-dirhamnoside (3), and kaempferol-3,7-O-α-ʟ-dirhamnoside (4), are presented. Antibacterial and antifungal activities of these compounds were tested against Escherichia coli, Pseudomonas aeruginosa, Proteus mirabilis, Klebsiella pneumoniae, Acinetobacter baumannii, Staphylococcus aureus, Bacillus subtilis, and Enterococcus faecalis, as well as the fungus Candida albicans by a microdilution method. On the other hand, both DNA virus Herpes simplex (HSV) and RNA virus Parainfluenza-3 (PI-3) were employed for antiviral assessment of the compounds using Madin- Darby bovine kidney and Vero cell lines. According to our data, all of the compounds tested were found to be quite active against S. aureus and E. faecalis with MIC values of 0.5 μg/ml, followed by E. coli (2 μg/ml), K. pneumoniae (4 μg/ml), A. baumannii (8 μg/ml), and B. subtilis (8 μg/ml), while they inhibited C. albicans at 1 μg/ml as potent as ketoconazole. However, only compound 3 displayed an antiviral effect towards PI-3 in the range of 8- 32 μg/ml of inhibitory concentration for cytopathogenic effect (CPE).

Influence of chlorine and methyl substituents and their position on the antimicrobial activities and crystal structures of 4-methyl-1,6-diphenylpyrimidine-2(1H)-selenone derivatives

2021 ◽  
Vol 77 (10) ◽  
Author(s):  
Izabela Korona-Głowniak ◽  
Wojciech Nitek ◽  
Waldemar Tejchman ◽  
Ewa Żesławska
Keyword(s):  
Crystal Structure ◽  
Biological Activity ◽  
Intermolecular Interactions ◽  
Current Knowledge ◽  
Antimicrobial Activities ◽  
Mutual Orientation ◽  
Antibacterial And Antifungal Activities ◽  
Chlorine Substituent ◽  
Antibacterial And Antifungal ◽  
Derivatives Of

Derivatives of 4-methyl-1,6-diphenylpyrimidine-2(1H)-selenone show very strong antimicrobial activity. In order to extend the current knowledge about the features responsible for the biological activity, crystal structure analyses are presented for 4-methyl-1-(2-methylphenyl)-6-phenylpyrimidine-2(1H)-selenone (1), 4-methyl-1-(3-methylphenyl)-6-phenylpyrimidine-2(1H)-selenone (2), 4-methyl-1-(4-methylphenyl)-6-phenylpyrimidine-2(1H)-selenone (3) (all C18H16N2Se) and 1-(4-chlorophenyl)-4-methyl-6-phenylpyrimidine-2(1H)-selenone (4) (C17H13ClN2Se). Furthermore, the antibacterial and antifungal activities of these compounds were evaluated. All the presented derivatives crystallize in the space group P21/c with one molecule in the asymmetric unit. The molecular geometries differ slightly in the mutual orientation of the rings. The packing of molecules in the crystals is dominated by C—H...N and C—H...Se intermolecular interactions. Additionally, in the crystal structure of 4, C—H...Cl intermolecular interactions are observed. The introduction of a methyl or chlorine substituent improves the biological activity, while its position significantly affects biological activity only in case of the chlorine substituent.

scholarly journals Biological evaluation of some octanoyl derivatives of methyl 4,6-O-cyclohexylidene-α-D-glucopyranoside

2013 ◽  
pp. 53-64 ◽  
Author(s):  
Abul KMS Kabir ◽  
Sarkar MA Kawsar ◽  
Mohammad MR Bhuiyan ◽  
Md Safiqur Rahman ◽  
Bilkiss Banu
Keyword(s):  
Pathogenic Bacteria ◽  
Biological Evaluation ◽  
Phytopathogenic Fungi ◽  
Bacterial Strains ◽  
Antibacterial And Antifungal Activities ◽  
Inhibition Concentration ◽  
Fungal Phytopathogens ◽  
Antibacterial And Antifungal ◽  
Derivatives Of

Some acylated derivatives of methyl 4,6-O-cyclohexylidene-?-D-glucopyranoside, including the precursor, were employed as test compounds for in vitro antimicrobial functionality test against ten human pathogenic bacteria and six phytopathogenic fungi. For comparative studies, biological activity of standard antibiotics, Ampicillin and Nystatin were also carried out against these microorganisms. The study revealed that the tested samples exhibited moderate to good antibacterial and antifungal activities. It was also observed that the test substances were more effective against fungal phytopathogens than those of the bacterial strains. Encouragingly, a good number of test compounds exhibited better antimicrobial activity than the standard antibiotics employed. Minimum Inhibition Concentration (MIC) test of methyl 4,6-O-cyclohexylidene-3-Odecanoyl- 2-O-octanoyl-?-D-glucopyranoside was conducted against INABA ET (Vibrio) and MIC was found to be 12.5 ?g/disc. DOI: http://dx.doi.org/10.3329/cujbs.v3i1.13406 The Chittagong Univ. J. B. Sci.,Vol. 3(1&2):53-64, 2008

scholarly journals DESIGN, SYNTHESIS OF BIOLOGICALLY ACTIVE HETEROCYCLES CONTAINING INDOL- THIAZOLYL- THIAZOLIDINONE DERIVATIVES

2018 ◽  
Vol 11 (3) ◽  
pp. 113 ◽  
Author(s):  
Prabhakar Walmik ◽  
Basavaraj S Naraboli ◽  
Swathi B ◽  
Somashekhar Ghanti
Keyword(s):  
Analytical Data ◽  
Biologically Active ◽  
Design Synthesis ◽  
Mass Spectral ◽  
Antibacterial And Antifungal Activities ◽  
Microdilution Method ◽  
13C Nuclear Magnetic Resonance ◽  
Broth Microdilution Method ◽  
Antibacterial And Antifungal

 Objective: The present study envisage a novel series of thiazole, indole and thiazolidine derivatives, namely, N-((5-Substituted-2-phenyl-1 H-indol-3-yl)methylene)-4,5,6,7-tetrahydro-5,7,-dimethylbenzo [d]thiazole-2-amine (4a-c), 2-(5-substituted-2-phenyl-1H-indol-3-yl)-3-(4,5,6,7- trimethylbenzo[d]thiazol-2-yl)-thiazolidin-4-one (5a-c) and 5-benzylidine-2-(5-substituted-2phenyl-1H-indol-3yl)-3-(4,5,6,7-tetrahydro-5,5,7- trimethylbenzo[d]thiazol-2-yl) thiazolidin-4-one (6a-c).Methods: All the newly synthesized compounds were characterized by infrared, 1H, 13C nuclear magnetic resonance and mass spectral data and elemental analysis and evaluated for in vitro antimicrobial activity.Results: Novel compounds N-((5-Substituted-2-phenyl-1H-indol-3-yl)methylene)-4,5,6,7-tetrahydro-5,7,-dimethylbenzo [d]thiazole-2-amine (4a-c), 2-(5-substituted-2-phenyl-1H-indol-3-yl)-3-(4,5,6,7-trimethylbenzo[d]thiazol-2-yl)-thiazolidin-4-one (5a-c) and 5-benzylidine-2-(5-substituted- 2phenyl-1H-indol-3yl)-3-(4,5,6,7-tetrahydro-5,5,7-trimethyl benzo[d]thiazol-2-yl)thiazolidin-4-one (6a-c) have been made and characterized using spectral and analytical data. The results of antibacterial and antifungal activities showed that some of the synthesized compounds exhibited promising activities.Conclusion: All the newly synthesized compounds were carried out by the broth microdilution method (NCCLS. 2002) in a DMF concentration of 500, 250, 125, and 62.5 μg/ml. Gentamycin and fluconazole are used as reference standards for antibacterial and antifungal activity, respectively. The final results revealed that compounds 4b, 5b, and 6b exhibited potent antimicrobial activity when compared to the standard drugs. 

scholarly journals In vitro Antimicrobial Potential of Samples From the Leaves and Fruits of Medicinally Important Melia azedarach

2021 ◽  
Vol 64 (2) ◽  
pp. 109-115
Author(s):  
Jehan Bakht ◽  
Ayesha Bukhari ◽  
Arshad Iqbal ◽  
Mohammad Shafi
Keyword(s):  
Escherichia Coli ◽  
Bacillus Subtilis ◽  
Antimicrobial Activities ◽  
Melia Azedarach ◽  
Klebsiella Pneumonia ◽  
Gram Negative ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal ◽  
Micro Organisms

Different solvent extracted samples obtained from the leaves and fruits of Melia azedarach were investigated for their antibacterial and antifungal activities. All the extracts from both tissues sources showed varying degrees of antimicrobial activities. Ethyl acetate and n-butanol extracts of both tissues inhibited the growth of the tested micro-organisms at all concentrations. N-hexane extracted fractions of the leaves reduced the activity of Bacillus subtilis, Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa at all concentrations, while no growth inhibition was recorded against Klebsiella pneumonia and Candida albicans. Crude methanolic extract from the leaves tissues showed activity against all the tested microbial species and highest susceptibility was noted against Bacillus subtilis. In case of leaves, the most susceptible bacteria were Bacillus subtilis (gram positive) and Klebsiella pneumonia (gram negative) was the most resistant one. In case of fruits extracts, the most susceptible bacteria were Klebsiella pneumonia (gram negative) and Escherichia coli (gram negative) was the most resistant one.  

scholarly journals Synthesis and antimicrobial evaluation of 3-hydrazino-quinoxaline derivatives and their cyclic analoaues

2004 ◽  
Vol 72 (2) ◽  
pp. 175-185 ◽  
Author(s):  
E. R. EI-Bendary ◽  
F. E. Goda ◽  
A. R. Maarouf ◽  
F. A. Badria
Keyword(s):  
Staphylococcus Aureus ◽  
Antimicrobial Activities ◽  
Significant Activity ◽  
Chloroacetyl Chloride ◽  
Antibacterial And Antifungal Activities ◽  
Piperazine Derivatives ◽  
Quinoxaline Derivatives ◽  
Antimicrobial Evaluation ◽  
Antibacterial And Antifungal

A series of quinoxaline derivatives has been synthesized by reacting 3-hydrazinoquinoxalines 1a,b with many bifunctional reagents. Reaction of 1a,b with chloroacetyl chloride and ethyl chloroacetate afforded 1-chloromethyl[1,2,4]tnazoIo[4,3-a]quinoxalines 2a,b and dihydro[1,2,4]triazino[4,3-a]quinoxalin-2-ones 3a,b respectively. Condensation of 1a,b with ethyl acetoacetate and acetylacetone yielded 2-quinoxalinylhydrazonobutanoates 4a,b and 2-quinoxalinylhydrazono-2-pentanones 5a,b respectively. Cyclization of 5a,b gave 3,5-dimethylpyrazolylquinoxalines 6a,b. Moreover, reaction of compounds 2a,b with N-phenyl piperazine derivatives afforded 4-(4-Arylpiperazin-1-yl)-1-[(4-arylpiperazin-1-yl) methyl)]triazoloquinoxalines 7a−e. The prepared compounds were screened for in vitro antibacterial and antifungal activities. None of the tested compounds showed significant activity towards Pseudomonas aeruginosa. However, remarkable activities were noticed for compounds 5a and 5b against Eschenchia coli. Staphylococcus aureus and Candida albicans. Compounds 6a and 6b lacked any antimicrobial activities against the tested microorganisms.

scholarly journals Chemical Composition and Antimicrobial Activities of the Essential Oil From Salvia mirzayanii Leaves

2017 ◽  
Vol 22 (4) ◽  
pp. 770-776 ◽  
Author(s):  
Kamiar Zomorodian ◽  
Mahmoodreza Moein ◽  
Keyvan Pakshir ◽  
Forough Karami ◽  
Zahra Sabahi
Keyword(s):  
Chemical Composition ◽  
Essential Oil ◽  
Chemical Constituents ◽  
Antimicrobial Activities ◽  
Gas Chromatography Mass Spectrometry ◽  
Antifungal Activities ◽  
Global Challenge ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal

Resistance of many pathogens to available drugs is a global challenge and is leading to growing interest in natural alternative products. In this study, chemical composition and in vitro antibacterial and antifungal activities of the essential oil from Salvia mirzayanii were investigated. The chemical constituents of essential oil from S mirzayanii were analyzed by gas chromatography–mass spectrometry. The antimicrobial activity was determined by broth microdilution. The main identified compounds were 1,8-cineole (41.2 ± 1.3%), linalool acetate (11.0 ± 0.5%), and α-terpinyl acetate (6.0 ± 0.4%) (mL of essential oil/g of plant material). The MIC95 were 0.03 to 0.5 µL/mL and 16 to 128 µL/mL for gram-positive and gram-negative bacteria, respectively. These results indicated that Salvia mirzayanii essential oil significantly inhibited the growth of standard and clinically isolated tested yeasts by MIC50 0.03 to 1 µL/mL. Potent antibacterial and antifungal activities of Salvia mirzayanii essential oil may be considered in future study, particularly against antibiotic-resistant cases.

scholarly journals Synthesis of disulphide-Schiff base derivatives and investigations of in vitro antimicrobial activities against some human pathogens

2017 ◽  
Vol 1 (3) ◽  
pp. 230-234 ◽  
Author(s):  
Sefa Durmuş ◽  
Aslıhan Dalmaz ◽  
Görkem Dülger ◽  
Duygu Bircan Kadıoğlu
Keyword(s):  
Schiff Base ◽  
Schiff Bases ◽  
Antimicrobial Activities ◽  
Diffusion Method ◽  
Control Group ◽  
Human Pathogens ◽  
Antibacterial And Antifungal Activities ◽  
Schiff Base Derivatives ◽  
Antibacterial And Antifungal

Abstract Thio-Schiff bases are becoming increasingly widespread in various branches such as the preparation of certain medicines, cosmetic products, and polymer production. In particular, the presence of antibacterial, antifungal, antiviral, antitumor and antimalarial properties of Schiff bases containing sulfur in the structure has made these compounds attractive in different disciplines. In this study, different derivatives of dimeric disulfide-Schiff bases have been synthesized. The antibacterial and antifungal activities of the synthesized these compounds were investigated in vitro against some human pathogens (Acinetobacter baumannii, Escherichia coli, Klebsiella pneumoniae, Staphylococcus aureus and Candida albicans, C. tropicalis, C. guilliermondii and C. glabrata). Test microorganisms were isolated from the patients appyling to Medical Faculty Hospital of Duzce University were used. Diffusion method was used to determine the antimicrobial activities of the compounds.standard antibacterial (Cefotaxime, Amoxicillin/clavulanicacid) and antifungal (Posaconazole) antibiotics were used as the control group and the results were compared. The result indicated that antimicrobial activity of Disulphide-Schiff Base Derivatives exhibited less activity against bacteria as compared to AMC30 (Amoxicillin/clavulanicacid), but highly effective against bacteria as compared to CTX30 (Cefotaxime). In addition, the compounds exhibited less activity against yeast.

scholarly journals Antimicrobial activity of secondary metabolites isolated from Centaurea spruneri Boiss.& Heldr.

2011 ◽  
Vol 76 (1) ◽  
pp. 27-34 ◽  
Author(s):  
Ana Ciric ◽  
Anastasia Karioti ◽  
Jasmina Glamoclija ◽  
Marina Sokovic ◽  
Helen Skaltsa
Keyword(s):  
Antimicrobial Activity ◽  
Protocatechuic Acid ◽  
Bacterial Species ◽  
Fungal Species ◽  
Antibacterial And Antifungal Activities ◽  
Fungistatic Activity ◽  
Microdilution Method ◽  
Aerial Parts ◽  
Antibacterial And Antifungal

Two coumarins, scopoletin (1) and isoscopoletin (2), two simple phenolic acids, protocatechuic acid (3) and isovanillic acid (4) and one flavonoid, eriodictyol (5) were isolated from the aerial parts of Centaurea spruneri. The structure of the compounds was established by spectroscopic methods. The in vitro antimicrobial activity of the isolated compounds was tested against eight bacteria and eight fungal species, using a microdilution method. All compounds tested showed moderate antibacterial and antifungal activities. Their minimum inhibitory concentrations were in the range 0.655 - 2.38 ?mol ml-1 and their minimal bactericidal concentrations ranged from 0.694 to 4.15 ?mol ml-1 against the tested bacterial species. All compounds showed fungistatic activity at 0.259 - 2.38 ?mol ml-1 and fungicidal at 0.69 - 2.6 ?mol ml-1 against all fungi tested.

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