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 Photoinduced Synthesis of New Diisochromenochromen-4-ones and Their Antimicrobial Activities

2012 ◽  
Vol 2012 ◽  
pp. 1-8 ◽  
Author(s):  
Mohamad Yusuf ◽  
Indu Solanki ◽  
Payal Jain
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activities ◽  
Significant Activity ◽  
Rigorous Analysis ◽  
H Nmr ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal ◽  
C Nmr

The diisochromenochromen-4-one3a-3b,4a-4c,5a-6a  & 7have been prepared from the photocyclization reaction of bischromen-4-one2a-2e. The later compounds are obtained from the O-alkylation of the suitable 3-hydroxy-2-aryl-4H-chromen-4-one1a-1ewith 4,4′-bischloromethyl-diphenyl in dry acetone, anhydrous K2CO3, and PTC (Bu4N+I−) under refluxing conditions. The structures of compounds2a-2e,3a-3b,4a-4c,5a-6a  & 7have been characterized from the rigorous analysis of their IR,1H-NMR,13C-NMR, ESI-Mass, and elemental analysis. The antibacterial and antifungal activities of the synthesized products were also evaluated against theKlebsiella pneumoniae, Pseudomonas aeruginosa, Escherichia coli, Staphylococcus aureus, Bacillus subtilis, andAspergillus janusandPenicillium glabrum, respectively. Some of the tested compounds showed significant activity against the above-said microorganisms.

scholarly journals Synthesis and In Vitro Antimicrobial Evaluation of New 1,3,4-Oxadiazoles Bearing 5-Chloro-2-methoxyphenyl Moiety

2013 ◽  
Vol 2013 ◽  
pp. 1-6 ◽  
Author(s):  
Basavapatna N. Prasanna Kumar ◽  
Kikkeri N. Mohana ◽  
Lingappa Mallesha ◽  
Kikkeri P. Harish
Keyword(s):  
Mass Spectra ◽  
Significant Activity ◽  
H Nmr ◽  
Antibacterial And Antifungal Activities ◽  
Antimicrobial Studies ◽  
Antimicrobial Evaluation ◽  
Oxadiazole Derivatives ◽  
Ft Ir ◽  
Antibacterial And Antifungal

A series of new 1,3,4-oxadiazole derivatives, 4(a–h), containing 5-chloro-2-methoxy benzohydrazide moiety were synthesized by the reaction of 5-chloro-2-methoxybenzoate with different aromatic carboxylic acids. These newly synthesized compounds were characterized by FT-IR, 1H NMR, mass spectra, and also by elemental analysis. All the newly synthesized compounds were screened for their antibacterial and antifungal activities. Antimicrobial studies revealed that compounds 4c, 4f, and 4g showed significant activity against tested strains.

Substituted 4-Formyl-2H-chromen-2-ones: Their Reaction with N-(2,3,4,6-Tetra-Oacetyl- β-D-galactopyranosyl)thiosemicarbazide, Antibacterial and Antifungal Activity of Their Thiosemicarbazone Products

2020 ◽  
Vol 24 (19) ◽  
pp. 2272-2282
Author(s):  
Vu Ngoc Toan ◽  
Nguyen Minh Tri ◽  
Nguyen Dinh Thanh
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Candida Albicans ◽  
Selenium Dioxide ◽  
Antibacterial And Antifungal Activity ◽  
E Coli ◽  
Antibacterial And Antifungal Activities ◽  
Alkyl Ethers ◽  
Antibacterial And Antifungal

Several 6- and 7-alkoxy-2-oxo-2H-chromene-4-carbaldehydes were prepared from corresponding alkyl ethers of 6- and 7-hydroxy-4-methyl-2-oxo-2H-chromen-2-ones by oxidation using selenium dioxide. 6- and 7-Alkoxy-4-methyl-2H-chromenes were obtained with yields of 57-85%. Corresponding 4-carbaldehyde derivatives were prepared with yields of 41-67%. Thiosemicarbazones of these aldehydes with D-galactose moiety were synthesized by reaction of these aldehydes with N-(2,3,4,6-tetra-O-acetyl-β-Dgalactopyranosyl) thiosemicarbazide with yields of 62-74%. These thiosemicarbazones were screened for their antibacterial and antifungal activities in vitro against bacteria, such as Staphylococcus aureus, Escherichia coli, and fungi, such as Aspergillus niger, Candida albicans. Several compounds exhibited strong inhibitory activity with MIC values of 0.78- 1.56 μM, including 8a (against S. aureus, E. coli, and C. albicans), 8d (against E. coli and A. niger), 9a (against S. aureus), and 9c (against S. aureus and C. albicans).

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.

Synthesis and investigation of 3,5-bis-linear and macrocyclic tripeptidopyridine candidates by using l-valine, N,N′-(3,5-pyridinediyldicarbonyl)bis-dimethyl ester as synthon

2019 ◽  
Vol 74 (6) ◽  
pp. 473-478 ◽  
Author(s):  
Abd El-Galil E. Amr ◽  
Ahmed M. Naglah ◽  
Nermien M. Sabry ◽  
Alhussein A. Ibrahim ◽  
Elsayed A. Elsayed ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Candida Albicans ◽  
Organic Molecules ◽  
Biological Activities ◽  
Dimethyl Ester ◽  
Antimicrobial Activities ◽  
Current Work ◽  
Antifungal Activities ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal

AbstractInterest in the synthesis of heterocyclic organic molecules with peptide moieties has gained attention due to their potential biological activities. The current work aimed at synthesizing new macrocyclic tripeptide imides and evaluating their possible antimicrobial activities. A series of 11 derivatives were prepared from dimethyl 3,5-pyridinevalinyl ester either by NaOH or NH2NH2 treatment, followed by cyclization and further reaction with NaOH or NH2NH2. The majority of synthesized derivatives showed promising antibacterial and antifungal activities in comparison to standard known antibiotics. Compounds 5a and 7b showed the most potential antibacterial against Staphylococcus aureus and antifungal activities against Candida albicans, respectively.

scholarly journals Antibacterial and Antifungal Evaluation of Chloroflavones

2018 ◽  
Vol 10 (1) ◽  
pp. 67-76
Author(s):  
M. A. Rahim ◽  
M. M. H. Bhuiyan ◽  
M. M. Matin ◽  
M. R. Alam
Keyword(s):  
Pathogenic Bacteria ◽  
Salmonella Typhi ◽  
Aspergillus Ochraceus ◽  
Diffusion Method ◽  
Dilution Method ◽  
Significant Activity ◽  
Filter Paper Disc ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal

Two chloroflavones, 6 and 7 along with their corresponding chalcones, 4 and 5 have been tested for antibacterial and antifungal activities against six human pathogenic bacteria viz. Bacillus cereus (G+), Staphylococcus aureus (G+), Escherichia coli (G-), Vibrio choloriae (G-), Pseudomonas aeruginosa (G-), and Salmonella typhi (G-), and four plant as well as mold fungi viz. Aspergillus flavus, Aspergillus ochraceus, Aspergillus niger and Rhizopus spp.. The antibacterial and antifungal screens of the synthesized compounds were performed in vitro by the filter paper disc diffusion method and the poisoned food technique, respectively. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of these synthesized compounds in comparison to ampicillin were also determined by broth micro-dilution method. Some of them were found to possess significant activity, when compared to standard drugs.

scholarly journals Synthesis and Characterization of New Fluoro/Trifluoromethyl-Substituted Acylthiourea Derivatives with Promising Activity against Planktonic and Biofilm-Embedded Microbial Cells

Processes ◽  
2020 ◽  
Vol 8 (5) ◽  
pp. 503 ◽  
Author(s):  
Carmen Limban ◽  
Diana Camelia Nuta ◽  
Alexandru Vasile Missir ◽  
Roxana Roman ◽  
Miron Teodor Caproiu ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Topoisomerase Ii ◽  
Dna Gyrase ◽  
Vitro Assay ◽  
Microbial Cells ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal ◽  
New Compounds

The aim of this study was preparation of new derivatives based on 2-((4-chlorophenoxy)methyl)-N-(arylcarbamothioyl)benzamide structure; the new compounds were characterized by IR, NMR (1H, 13C) spectroscopy, and elemental analysis. The obtained compounds were evaluated for their in vitro antimicrobial activity against planktonic and biofilm-embedded microbial cells (Staphylococcus aureus, Enterococcus faecalis, Escherichia coli, Pseudomonas aeruginosa, Candida albicans), by qualitative and quantitative assays. Some of the compounds revealed promising antibacterial and antifungal activities, with low minimum inhibitory concentration values between 0.15 and 2.5 mg/mL and minimal biofilm eradication concentrations of 0.019–2.5 mg/mL. To investigate the potential target of their antibacterial activity, in silico drug-likeness and molecular docking screenings on Staphylococcus aureus DNA gyrase were performed. The compound with the best antibacterial activity (1g) was docked into topoisomerase II DNA gyrase enzymes (PDB ID: 2XCS) and showed valuable interactions with the target protein along with good docking scores, suggesting that it can act by the inhibition of DNA replication. The tested compounds exhibited only a poor antioxidant activity, as revealed by the in vitro assay using 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay.

scholarly journals Synthesis, structural characterization and antimicrobial evaluation of some novel piperidin-4-one oxime esters

2015 ◽  
Vol 80 (9) ◽  
pp. 1101-1111 ◽  
Author(s):  
Gokula Krishnan ◽  
R. Sivakumar ◽  
V. Thanikachalam
Keyword(s):  
Biologically Active ◽  
Good Activity ◽  
Mass Spectral ◽  
Antibacterial And Antifungal Activities ◽  
Xrd Study ◽  
Antimicrobial Evaluation ◽  
Ft Ir ◽  
Antibacterial And Antifungal

Fifteen novel biologically active piperidin-4-one oxime esters (8-22) have been synthesized with good yields. These compounds were prepared from in-situ activated carboxylic acids using POCl3 and pyridine with piperidin-4- one oximes. The structure of the title compounds were elucidated on the basis of FT-IR, NMR (1D and 2D) and mass spectral analyses. The single crystal XRD study of compounds 12 and 20 were the further evidence for the proposed structure unambiguously. All the synthesized compounds were tested for in vitro antibacterial and antifungal activities. Many of these derivatives exhibited good activity against Bacillus subtilis, Pseudomonas aeruginosa, Escherichia coli, Trigoderma veride and Aspergillus flavus.

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.  

SYNTHSIS, CHARACTERISATION AND ANTI MICROBIAL EVALUATION OF NOVEL 2-SUBSTITUTED QUINOXALINE DERIVATIVES

INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (05) ◽  
pp. 5-10
Author(s):  
G. R Kamala ◽  
◽  
A. K. Velagaleti
Keyword(s):  
Pseudomonas Aeruginosa ◽  
Bacillus Subtilis ◽  
Candida Albicans ◽  
Bacillus Pumilus ◽  
Biological Activities ◽  
Significant Activity ◽  
Antibacterial And Antifungal Activities ◽  
Quinoxaline Derivatives ◽  
Weak Activity ◽  
Antibacterial And Antifungal

literature survey indicates that 2-substituted quinoxaline derivatives possess different pharmacological and biological activities, of which most potent activities are anti-bacterial, anti-fungal, anti-inflammatory, and analgesic activity. In view of above literature, we planned to synthesize novel 2-Substituted quinoxaline derivatives. The final synthesised were characterized by physical (M.P, TLC) and spectral analysis (1HNMR, IR). The 2-substituted quinoxaline nucleus was constructed by condensation of o-phenylene diamine and diethy loxalate in equimolar quantities which upon heating yielded quinoxaline -2, 3-diol moiety. The quinoxaline -2,3-diol was treated with POCl3 to furnish 2,3-di chloro quinoxaline (2). Further the 2-chloro-3-hydrazinoquinoxaline (3) was synthesized by the reaction of 2,3- dichloroquinoxaline (2) and hydrazine hydrate in methanolic medium upon refluxing for 60 min. different Schiff’s bases of 2-chloro-3- hydrazine quinoxaline were obtained by refluxing the appropriate substituted benzaldehyde and 2-chloro-3-hydrazinoquinoxaline (3) in acetic medium for 3 h. All the synthesized compounds were screened for their antibacterial and antifungal activities by using cup plate method against Bacillus subtilis, Bacillus pumilus, Escherichia coli, Pseudomonas aeruginosa, Aspergillus niger and Candida albicans at 100, 50 μg/mL concentration using ciprofloxacin and clotrimazole as reference standard drugs respectively. Compounds 4e and 4f showed significant activity against Pseudomonas aeruginosa, 4a and 4d showed significant activity against Bacillus subtilis, the compound 4c showed good activity against the organism Bacillus pumilus, whereas the compound 4a shown moderate antifungal activity against Candida albicans. The rest of the compounds showed weak activity when compared to the standard ciprofloxacin and clotrimazole.

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