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.

scholarly journals Synthesis and Biological Effectiveness of Some new Azo Compounds as Derivatives of Nitrogen Bases

2016 ◽  
Vol 13 (2) ◽  
pp. 368-375
Author(s):  
Baghdad Science Journal
Keyword(s):  
Diazonium Salt ◽  
Coupling Reaction ◽  
Hemoglobin Concentration ◽  
Antimicrobial Activities ◽  
Uv Spectra ◽  
Azo Compounds ◽  
Nitrogen Bases ◽  
Antibacterial And Antifungal Activities ◽  
Physiological Tests

In this study the new azo compounds (3compounds) for nitrogen bases (Adenine and Cytosine) are synthesized through two reaction steps (formation of diazonium salt and coupling reaction). The compounds have been characterized by FTIR, melting point, and ultra-violate (UV) spectra. All synthesized compounds have been estimated in vitro for their antimicrobial activities against two species of bacteria(E.coli, S.aureus)and one kind of fungi ( Aspergillus flavus) .The results show that these compounds have very good antibacterial and antifungal activities especially compounds 1 and 3.To study the effect of these compounds were making some physiological tests on rats are made ,the results of hematological study showed decreasing level of total hemoglobin concentration in all treatment groups specially in group (1).The values of Packed in cell volume (P.C.V) are within normal blood range of rats . Total leucocytes count (W.B.C) decrease in all groups.

Infrared, 1H-NMR Spectral Studies of some Methyl 6-O-Myristoyl-α-D-Glucopyranoside Derivatives: Assessment of Antimicrobial Effects

2015 ◽  
Vol 58 ◽  
pp. 122-136 ◽  
Author(s):  
Sarkar M.A. Kawsar ◽  
Khaleda Mymona ◽  
Refat Asma ◽  
Mohammad A. Manchur ◽  
Yasuhiro Koide ◽  
...  
Keyword(s):  
Pathogenic Fungi ◽  
Spectral Studies ◽  
Bacterial Strains ◽  
Substitution Product ◽  
Antifungal Activities ◽  
H Nmr ◽  
Antibacterial And Antifungal Activities ◽  
Fungal Phytopathogens ◽  
Antibacterial And Antifungal

This study was carried out to regioselective myristoylation of methyl α-D-glucopyranoside (1) using the direct acylation method gave the corresponding methyl 6-O-myristoyl-α-D-glucopyranoside (2) in fair yield. A number of 2,3,4-tri-O-acyl derivatives (3-15) of this 6-O-substitution product using a wide variety of acylating agents were also prepared in order to obtain newer derivatives of synthetic and biological importance. The reaction conditions are reasonably simple and yields were very good. The structures of the title compounds (2-15) were established by using analytical, physicochemical techniques and spectroscopic data (IR and 1H-NMR). All the synthesized compounds were employed as test chemicals for in vitro antimicrobial functionality test against Gram-positive Bacillus subtilis, Staphylococcus aureus, Gram-negative Escherichia coli, Pseudomonas aeruginosa bacteria and plant pathogenic fungi Aspergillus niger and Candida albicans. For comparative studies, antimicrobial 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 human bacterial strains. Encouragingly, a number of tested chemicals showed nearest antibacterial and antifungal activities with the standard antibiotics employed.

scholarly journals Synthesis and Antimicrobial Activity of Pyrimidine Salts with Chloranilic and Picric Acids

2013 ◽  
Vol 2013 ◽  
pp. 1-5 ◽  
Author(s):  
C. Mallikarjunaswamy ◽  
D. G. Bhadregowda ◽  
L. Mallesha
Keyword(s):  
Antimicrobial Activity ◽  
The Other ◽  
Spectral Studies ◽  
H Nmr ◽  
Antibacterial And Antifungal Activities ◽  
Elemental Analyses ◽  
Ft Ir ◽  
Uv Visible ◽  
Antibacterial And Antifungal

Pyrimidine salts such as 2-methyl-5-nitro-phenyl-(4-pyridin-3-yl-pyrimidin-2-yl)-amine (1) and 4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-yl-amino)-phenyl-amine (2) with chloranilic and picric acids were synthesized, and theirin vitroantibacterial and antifungal activities were evaluated. The synthesized compounds were characterized by elemental analyses, UV-visible, FT-IR, and1H NMR spectral studies. Compound2aexhibited good inhibition towards antimicrobial activity compared to the other compounds.

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.

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 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 Spectroscopic Characterization and Antimicrobial Activities of Some Heavy Metals Complexes of 2-hydroxy phenyl piperonalidene

2013 ◽  
Vol 10 (3) ◽  
pp. 627-637
Author(s):  
Baghdad Science Journal
Keyword(s):  
Spectroscopic Characterization ◽  
Antimicrobial Activities ◽  
Heat Of Formation ◽  
Molar Ratio ◽  
Ratio Method ◽  
Spectral Studies ◽  
In Vitro Tests ◽  
Tetrahedral Geometry ◽  
Antibacterial And Antifungal

An antibacterial and antifungal piperonal-derived compound and its Rh(III), Pd(II), Pt(IV), and Cd(II) metal complexes were synthesized and characterized by spectroscopic methods, conductivity, metal analyses and magnetic moment measurements. The nature of the complexes formed in ethanolic solution was studied following the molar ratio method. From the spectral studies, octahedral geometry was suggested for rhodium (III) and platinum (IV) complexes, while a square planer structure was suggested for palladium (II) complex and a tetrahedral geometry for cadmium (II) complex. Structural geometries of these compounds were also suggested in gas phase by using hyperchem-8 program for the molecular mechanics and semi-empirical calculations. The heat of formation and binding energy for the prepared compounds was calculated by using PM3 and AMBER methods. The theoretically vibration spectra for the imine and its starting material was evaluated by using PM3 method. Preliminary in vitro tests for antibacterial and antifungal activity showed that most of the prepared compounds display a good activity to (Staphylococcus aureus), (Escherichia coli) and (Candida albicans).

scholarly journals Antimicrobial and Anticancer Activities of Some Partially Acylated Thymidine Derivatives

2021 ◽  
pp. 11-22
Author(s):  
SC Tasneem ◽  
J Ferdous ◽  
MZH Bulbul ◽  
MMH Misbah ◽  
D Sujan ◽  
...  
Keyword(s):  
Pathogenic Bacteria ◽  
Antimicrobial Agents ◽  
Antimicrobial Activities ◽  
Phytopathogenic Fungi ◽  
Bacterial Strains ◽  
Anticancer Activities ◽  
Antibacterial And Antifungal Activities ◽  
Ic50 Values ◽  
Antibacterial And Antifungal

The principal cause of human deaths in the world is primarily due to harmful pathogenic microbes as bacteria, a virus, and fungi. Searching for antimicrobial agents to prevent deaths with new structures and modes of action is an essential strategy of the research. Therefore, in the present study has been undertaken of thymidine and of its eleven acylated derivatives were employed as test chemicals for in vitro antibacterial evaluation against five human pathogenic bacteria. The compounds were also screened for antifungal functionality tests against two phytopathogenic fungi. It was observed that a good number of tested compounds exhibited moderate to good antimicrobial activities. It was also observed that these acylated compounds were more effective against the phytopathogenic fungi than those of the bacterial strains. Encouragingly, several tested chemicals showed better antibacterial and antifungal activities than the standard antibiotics employed. The minimum inhibition concentration (MIC) values of the compounds 3 (5´-O-butyrylthymidine), 7 (5´-O-palmitoylthymidine) and 12 (5´-O-4- dichloroacetylthymidine) were found to be 0.32 mg/ml and minimum bactericidal concentrations (MBC) values were found to be 0.63 mg /ml in each case. On the other hand, the minimum fungal concentration (MFC) was found to be (1.25 mg/ml) in the case of compound 7 (i.e., palmitoyl derivative) which may be used as antifungal active drug providing further investigation. In vitro MTT assays revealed that compounds 4 (5´-O-hexanoylthymidine) and 7 (5´-O-palmitoylthymidine) were effective against Ehrlich’s ascites carcinoma (EAC) cells and IC50 values were found to be 920.88 μg/ml and 792.90 μg/ml, respectively. So these compounds may be targeted for future studies for their usage as broad-spectrum antibiotics. J. Bio-Sci. 29(1): 11-22, 2021 (June)

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