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.

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 Antibacterial and Antifungal Activities of Rumex Confertus Willd

2021 ◽  
Vol 9 (12) ◽  
pp. 855-856
Author(s):  
G. D. Shermatova
Keyword(s):  
Antibacterial Activity ◽  
Ethyl Acetate ◽  
Gram Positive ◽  
Antifungal Activities ◽  
Gram Positive Bacteria ◽  
Root Part ◽  
Fungal Activity ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal

Abstract: The leaves and roots of Rumex confertus Willd were tested in vitro for antibacterial and fungal activity in the fractions of gasoline, chloroform, ethyl acetate and butanol. As a result, it was found that the leaves of the Rumex confertus Willd plant, chloroform and ethyl acetate fractions of the root part have antibacterial activity against fungi and gram-positive bacteria. Keywords: Rumex confertus Willd, fractions, extracts, antibacterial, antifungal

scholarly journals Synthesis, Antibacterial and Antifungal Evlaution of Novel Pyrazoline Derivatives

2018 ◽  
Vol 17 (2) ◽  
pp. 221-226
Author(s):  
BC Revanasiddappa ◽  
MS Jisha ◽  
M Vijay Kumar ◽  
Hemanth Kumar
Keyword(s):  
Good Activity ◽  
Bacterial Strains ◽  
Mass Spectral Data ◽  
Acetic Acid Medium ◽  
Mass Spectral ◽  
Antibacterial And Antifungal Activities ◽  
Alcohol Medium ◽  
Antibacterial And Antifungal ◽  
New Compounds

A new series of chalcones (2a-j) were prepared by reacting substituted aldehydes and substituted ketones in alcohol medium in presence of NaOH. The chalcones underwent selective cyclization with guanicol hydrazide (1) in glacial acetic acid medium to yield the title compounds 1,3,5-trisubstituted pyrazolines (3a-j). The new compounds were characterized on the basis of 1H-NMR, IR and mass spectral data. All the newly synthesized compounds were evaluated for their in-vitro antibacterial and antifungal activities. Some of the tested compounds 3a and 3e showed good activity against bacterial strains and compounds 3d and 3h revealed good activity against fungal strains. Dhaka Univ. J. Pharm. Sci. 17(2): 221-226, 2018 (December)

scholarly journals In vitro Activity of Rambutan Binjai (Nephelium lappaceum) Peel Extract from Indonesia to Methicillin-Resistant Staphylococcus aureus (MRSA)

2018 ◽  
Vol 17 (2) ◽  
pp. 197-203
Author(s):  
Tina Rostinawati ◽  
Ami Tjitraresmi ◽  
Myra Vania Wisnuputri
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Methicillin Resistant Staphylococcus Aureus ◽  
Ethanol Extract ◽  
Diffusion Method ◽  
Methicillin Resistant ◽  
Nephelium Lappaceum ◽  
New Compounds ◽  
Peel Extract

Methicillin-resistant Staphylococcus aureus (MRSA) is the most common bacteria causing nosocomial infections with high levels of resistance to available antibiotics. So, it is necessary to search for new compounds to solve this problem. Various studies showed antibacterial activity of rambutan peel but for Rambutan Binjai peel extract that are from Indonesia has never been studied against the MRSA. This study aims to determine the antibacterial activity, the value of minimum inhibitory concentration (MIC) and the minimum bactericidal concentration (MBC) using agar diffusion method. The concentration of rambutan peel ethanol extract at as much as 62.5 mg/ml showed the inhibitory diameter i.e 21.3 ± 2.4 mm. MIC and MBC were in the same range, which was between 0.98 (mg/ml) to 1.95 (mg/ml). The activity strength of tetracycline against the extract was at 1:50. This revealed that Rambutan Binjai peel extract had great potency as antibacterial agent to MRSA. Dhaka Univ. J. Pharm. Sci. 17(2): 197-203, 2018 (December)

scholarly journals Synthesis and Biological Evaluation of New Pyridothienopyrimidine Derivatives as Antibacterial Agents and Escherichia coli Topoisomerase II Inhibitors

Antibiotics ◽  
2020 ◽  
Vol 9 (10) ◽  
pp. 695
Author(s):  
Eman M. Mohi El-Deen ◽  
Eman A. Abd El-Meguid ◽  
Eman A. Karam ◽  
Eman S. Nossier ◽  
Marwa F. Ahmed
Keyword(s):  
Escherichia Coli ◽  
Antibacterial Activity ◽  
Topoisomerase Ii ◽  
Antibacterial Agents ◽  
Dna Gyrase ◽  
Structural Features ◽  
Biological Evaluation ◽  
Topoisomerase Iv ◽  
Gram Negative

The growing resistance of bacteria to many antibiotics that have been in use for several decades has generated the need to discover new antibacterial agents with structural features qualifying them to overcome the resistance mechanisms. Thus, novel pyridothienopyrimidine derivatives (2a,b–a,b) were synthesized by a series of various reactions, starting with 3-aminothieno[2,3-b]pyridine-2-carboxamides (1a,b). Condensation of compounds 1a,b with cyclohexanone gave 1’H-spiro[cyclohexane-1,2’-pyrido[3’,2’:4,5]thieno[3,2-d]pyrimidin]-4’(3’H)-ones (2a,b), which in turn were utilized to afford the target 4-substituted derivatives (3a,b–8a,b). In vitro antibacterial activity evaluations of all the new compounds (2a,b–8a,b) were performed against six strains of Gram-negative and Gram-positive bacteria. The target compounds showed significant antibacterial activity, especially against Gram-negative strains. Moreover, the compounds (2a,b; 3a,b; 4a,b; and 5a,b) that exhibited potent activity against Escherichia coli were selected to screen their inhibitory activity against Escherichia coli topoisomerase II (DNA gyrase and topoisomerase IV) enzymes. Compounds 4a and 4b showed potent dual inhibition of the two enzymes with IC50 values of 3.44 µΜ and 5.77 µΜ against DNA gyrase and 14.46 µΜ and 14.89 µΜ against topoisomerase IV, respectively. In addition, docking studies were carried out to give insight into the binding mode of the tested compounds within the E. coli DNA gyrase B active site compared with novobiocin.

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 Synthesis and Antimicrobial Properties of Naphthylamine Derivatives Having a Thiazolidinone Moiety

Medicina ◽  
2011 ◽  
Vol 47 (6) ◽  
pp. 47
Author(s):  
Vilma Petrikaitė ◽  
Eduardas Tarasevičius ◽  
Alvydas Pavilonis
Keyword(s):  
Antibacterial Activity ◽  
Minimum Inhibitory Concentration ◽  
Antifungal Activity ◽  
Inhibitory Concentration ◽  
Antimicrobial Properties ◽  
Microbiological Analysis ◽  
Antibacterial And Antifungal Activity ◽  
Antibacterial And Antifungal ◽  
New Compounds

Objective. The aim of this study was to evaluate the influence of pharmacophores having naphthylamine and nitro groups on the antimicrobial (antibacterial and antifungal) activity of thiazolidinone derivatives. Materials and Methods. The initial 5-substituted-2-methylmercaptothiazolidin-4-ones were subjected to S-demethylation to yield 2-amino-substituted thiazolidinones. 4-Nitro-1-naphthylamine, nitrofuran aldehydes, and nitrobenzene aldehydes were used as pharmacophoric compounds having amino or aldehyde groups. Antimicrobial (antibacterial and antifungal) activity of the new compounds was tested in vitro against bacterial cultures – Staphylococcus aureus, Escherichia coli, Bacillus subtilis, Klebsiella pneumoniae – and fungal cultures – Candida albicans, Candida glabrata, Candida krusei, Candida kefyr, Candida tropicalis, and Candida parapsilosis. Results. Microbiological analysis showed that all new thiazolidinone derivatives with nitronaphthylamine substituent possessed antibacterial and antifungal properties. New compounds 2a-b showed similar antibacterial activity in vitro against S. aureus and B. subtilis as aminopenicillins. The lowest antibacterial activity of all newly synthesized compounds was against capsule-forming bacteria K. pneumoniae and against gram-negative bacteria E. coli (minimum inhibitory concentration range, 500–1000 μg/mL). Conclusions. The minimum inhibitory concentration of naphthylamine derivatives varied in the range of 0.4–1000 μg/mL, and activity of some newly synthesized compounds was similar to the activity of aminopenicillins and fluconazole, an antifungal preparation. Based on the results, it is possible to separate the perspective group of potential antimicrobial compounds.

scholarly journals Synthesis, Structural Characterization and Biological Studies of Metal Complexes with (E)-4-oxo-4-(thiazol-2-ylamino)but-2-enoic Acid

2020 ◽  
Vol 71 (6) ◽  
pp. 75-81
Author(s):  
Summia Rehman ◽  
Muhammad Imran ◽  
Ayesha Kanwal ◽  
Shoomaila Latif ◽  
Fiza Akbar ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Metal Complexes ◽  
1H Nmr Spectroscopy ◽  
Conductivity Measurements ◽  
Antibacterial And Antifungal Activities ◽  
Biological Studies ◽  
Uv Visible ◽  
Antibacterial And Antifungal ◽  
Structural Aspects

Carboxylate functionalized ligand (LH) was synthesized as a result of reaction between maleic anhydride and 2�aminothiazole. This ligand was further reacted with Co(II), Ni(II), Cu(II), Zn(II) and Bi(III) ions to yield respective metal complexes. The structural aspects were studied using FTIR, UV�Visible and 1H-NMR spectroscopy. Non-electrolytic behavior was revealed by the conductivity measurements. Except Bi(III) being octahedral, all other complexes prepared are tetrahedral in geometry. Ligand (LH) and its metal complexes were also investigated for their in vitro antibacterial and antifungal activities. All the complexes exhibited significant antibacterial activity but non-significant antifungal activity.

Synthesis and Evaluation of Demethoxyviridin Derivatives as Potential Antimicrobials

2005 ◽  
Vol 60 (9-10) ◽  
pp. 686-692
Author(s):  
Ismail Kiran ◽  
Semra Ilhan ◽  
Tamer Akar ◽  
Lacine Tur ◽  
Erdinc Erol
Keyword(s):  
Antibacterial Activity ◽  
Antifungal Activity ◽  
Geotrichum Candidum ◽  
Diffusion Method ◽  
Dilution Method ◽  
Agar Dilution Method ◽  
Antibacterial And Antifungal Activities ◽  
Agar Dilution ◽  
Antibacterial And Antifungal

Abstract The in vitro antibacterial and antifungal activities of demethoxyviridin and some synthetic analogues were evaluated by the agar diffusion method. The minimum inhibitory concentrations (MIC) of the active compounds were also determined by the agar dilution method. Demethoxyviridin (1) showed moderate antibacterial activity against most of the strains tested. 1α-Hydroxydemethoxyviridin (3) showed antibacterial activity and the most potent in vitro antifungal activity with MIC of 20 μg/ml (0.062 mm) against Aspergillus niger, A. fumigatus, A. flavus, A. parasiticus, Fusarium solani, F. graminarum, Geotrichum candidum whereas 5′-methylfuro-(4′,3′,2′-4,5,6)androst-5-ene-3,17-dione (7) exhibited very weak antifungal activity against Candida albicans only.

scholarly journals SYNTHESIS AND CHARACTERIZATION OF 3-ARYL-5H,13AH-QUINOLINO(3,2-F) (1,2,4)TRIAZOLO(4,3-B)(1,2-DIAZA-4-SULPHO)AZEPINES: IN VITRO ANTIFUNGAL AND ANTIBACTERIAL ACTIVITY

2011 ◽  
Vol 11 (2) ◽  
pp. 148-153
Author(s):  
Hemant Panwar ◽  
Shishupal Singh
Keyword(s):  
Antibacterial Activity ◽  
Antifungal Activity ◽  
Synthesis And Characterization ◽  
Mass Analysis ◽  
Antibacterial And Antifungal Activity ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal ◽  
Ampicillin Trihydrate

3-Aryl-5H,13aH-quinolino(3,2-f)(1,2,4)triazolo(4,3-b)(1,2-diaza-4-sulpho)azepines [2a-i] have been prepared by the cyclisation of 5-aryl-4-amino-3-mercapto-1,2,4-triazole by reaction with 2-chloro-3-formylquinoline in catalytic presence of p-toluene sulphonic acid. All the synthesized compounds have been characterized by elemental and spectral (IR, 1H- NMR and Mass) analysis. Furthermore, all compounds were evaluated for their antibacterial and antifungal activities against selected panel of pathogenic strains. Ampicillin trihydrate and fluconazole were used as standard drugs for antibacterial and antifungal activity, respectively. 3-(2-Chloro)phenyl-5H,13aH-quinolino(3,2-f)(1,2,4)triazolo(4,3-b)(1,2-diaza-4-sulpho)azepine [2h] was found, one of the most potent with lesser toxicity among the all prepared thiazepine derivatives.

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