scholarly journals Preparation and Antibacterial Activity of Some New 4-(2-Heterylidenehydrazinyl)-7-chloroquinoline Derivatives

2018 ◽  
Vol 2018 ◽  
pp. 1-7 ◽  
Author(s):  
Trong Duc Le ◽  
Ngoc Nam Pham ◽  
Tien Cong Nguyen
Keyword(s):  
Antibacterial Activity ◽  
Bacillus Subtilis ◽  
Aspergillus Niger ◽  
Cytotoxic Activity ◽  
Growth Inhibitor ◽  
Substituted Anilines ◽  
Chemical Structures ◽  
Phenylhydrazine Hydrochloride ◽  
Good Ability ◽  
C Nmr

N-(4-Substituted phenyl)acetamides, which were prepared from acetic anhydride and p-substituted anilines, were utilized as precursors for reactions to Vilsmeier-Haack reagent to form 6-substituted-2-chloroquinoline-3-carbaldehydes 3a–c. Meanwhile, a similar reagent was applied to 1-[1-(4-substituted phenyl)ethylidene]-2-phenylhydrazines as substrates, which were synthesized from phenylhydrazine hydrochloride and p-substituted acetophenones, and 1,3-diarylpyrazole-4-carbaldehydes 3d–f were observed as a result. Reactions between the aldehydes 3a–f and 7-chloro-4-hydrazinylquinoline 2, obtained from reaction of 4,7-dichloroquinoline 1 and hydrazine hydrate, formed six new hydrazone compounds, namely, 4-{2-[(6-substituted-2-chloroquinolin-3-yl)methylidene]hydrazinyl}-7-chloroquinolines 4a–c and 4-(2-{[3-(4-substituted phenyl)-1-phenyl-1H-pyrazol-4-yl]methylene}hydrazinyl)-7-chloroquinolines 4d–f. The chemical structures of all synthesized compounds were elucidated by the analysis of IR, 1H, 13C-NMR, and HRMS spectral data. Additionally, all of the synthesized hydrazones were evaluated in terms of cytotoxic activity against four strains of bacteria and four strains of fungus at several concentrations of substrates. As a result, three of them, 4a–c, possess the good ability as growth inhibitor of Bacillus subtilis and Aspergillus niger at the concentration of 25 μg/mL and 50 μg/mL, respectively, while compound 4e only shows a cytotoxic activity against Aspergillus niger at the concentration of 25 μg/mL.

Synthesis of Chalcones and Nucleosides Incorporating [1, 3, 4]Oxadiazolenone Core and Evaluation of their Antifungal and Antibacterial Activities

2020 ◽  
Vol 15 (6) ◽  
pp. 665-679
Author(s):  
Alok K. Srivastava ◽  
Lokesh K. Pandey
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Bacillus Subtilis ◽  
Antifungal Activity ◽  
Aspergillus Niger ◽  
Gram Negative ◽  
E Coli ◽  
Gram Positive Bacteria ◽  
Good Antibacterial Activity

Background: [1, 3, 4]oxadiazolenone core containing chalcones and nucleosides were synthesized by Claisen-Schmidt condensation of a variety of benzaldehyde derivatives, obtained from oxidation of substituted 5-(3/6 substituted-4-Methylphenyl)-1, 3, 4-oxadiazole-2(3H)-one and various substituted acetophenone. The resultant chalcones were coupled with penta-O-acetylglucopyranose followed by deacetylation to get [1, 3, 4] oxadiazolenone core containing chalcones and nucleosides. Various analytical techniques viz IR, NMR, LC-MS and elemental analysis were used to confirm the structure of the synthesised compounds.The compounds were targeted against Bacillus subtilis, Staphylococcus aureus and Escherichia coli for antibacterial activity and Aspergillus flavus, Aspergillus niger and Fusarium oxysporum for antifungal activity. Methods: A mixture of Acid hydrazides (3.0 mmol) and N, Nʹ- carbonyl diimidazole (3.3 mmol) in 15 mL of dioxane was refluxed to afford substituted [1, 3, 4]-oxadiazole-2(3H)-one. The resulted [1, 3, 4]- oxadiazole-2(3H)-one (1.42 mmol) was oxidized with Chromyl chloride (1.5 mL) in 20 mL of carbon tetra chloride and condensed with acetophenones (1.42 mmol) to get chalcones 4. The equimolar ratio of obtained chalcones 4 and β -D-1,2,3,4,6- penta-O-acetylglucopyranose in presence of iodine was refluxed to get nucleosides 5. The [1, 3, 4] oxadiazolenone core containing chalcones 4 and nucleosides 5 were tested to determined minimum inhibitory concentration (MIC) value with the experimental procedure of Benson using disc-diffusion method. All compounds were tested at concentration of 5 mg/mL, 2.5 mg/mL, 1.25 mg/mL, 0.62 mg/mL, 0.31 mg/mL and 0.15 mg/mL for antifungal activity against three strains of pathogenic fungi Aspergillus flavus (A. flavus), Aspergillus niger (A. niger) and Fusarium oxysporum (F. oxysporum) and for antibacterial activity against Gram-negative bacterium: Escherichia coli (E. coli), and two Gram-positive bacteria: Staphylococcus aureus (S. aureus) and Bacillus subtilis(B. subtilis). Result: The chalcones 4 and nucleosides 5 were screened for antibacterial activity against E. coli, S. aureus and B. subtilis whereas antifungal activity against A. flavus, A. niger and F. oxysporum. Compounds 4a-t showed good antibacterial activity whereas compounds 5a-t containing glucose moiety showed better activity against fungi. The glucose moiety of compounds 5 helps to enter into the cell wall of fungi and control the cell growth. Conclusion: Chalcones 4 and nucleosides 5 incorporating [1, 3, 4] oxadiazolenone core were synthesized and characterized by various spectral techniques and elemental analysis. These compounds were evaluated for their antifungal activity against three fungi; viz. A. flavus, A. niger and F. oxysporum. In addition to this, synthesized compounds were evaluated for their antibacterial activity against gram negative bacteria E. Coli and gram positive bacteria S. aureus, B. subtilis. Compounds 4a-t showed good antibacterial activity whereas 5a-t showed better activity against fungi.

scholarly journals Study on the extraction and antibacterial activity of Monascin

2021 ◽  
Vol 251 ◽  
pp. 02061
Author(s):  
Xiaojuan Gao ◽  
Xiaoshi Lu ◽  
Zifeng Wang ◽  
Guangpeng Liu ◽  
Xinjun Li
Keyword(s):  
Escherichia Coli ◽  
Saccharomyces Cerevisiae ◽  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Bacillus Subtilis ◽  
Aspergillus Niger ◽  
Inhibitory Effect ◽  
Ethanol Extraction ◽  
Inhibitory Ability ◽  
Strong Inhibitory Effect

Taking monascin as the research object, monascin was extracted from red kojic rice by ethanol extraction and extracted with 60%, 70% and 80% ethanol respectively. Finally, it was concluded that when the concentration of ethanol was 70%, the extraction rate of monascin was the highest, reached 75.68%. The bacteriostatic experiments of monascin extract and monascin fermentation showed that it had strong inhibitory effect on Staphylococcus aureus and Bacillus subtilis, weak inhibitory ability on Escherichia coli and Aspergillus niger, and no obvious inhibitory effect on the growth of Saccharomyces cerevisiae.

scholarly journals Room Temperature Synthesis and Antibacterial Activity of New Sulfonamides Containing N,N-Diethyl-Substituted Amido Moieties

2012 ◽  
Vol 2012 ◽  
pp. 1-13 ◽  
Author(s):  
Olayinka O. Ajani ◽  
Oluwole B. Familoni ◽  
Feipeng Wu ◽  
Johnbull O. Echeme ◽  
Zheng Sujiang
Keyword(s):  
Antibacterial Activity ◽  
Mass Spectra ◽  
Room Temperature ◽  
Biological Activities ◽  
Chemical Structures ◽  
Wide Range ◽  
Synthetic Routes ◽  
Mic Value ◽  
C Nmr

Sulfonamide drugs which have brought about an antibiotic revolution in medicine are associated with a wide range of biological activities. We have synthesized a series of α-tolylsulfonamide, 1–11 and their substituted N,N-diethyl-2-(phenylmethylsulfonamido) alkanamide derivatives, 12–22 in improved and excellent yields in aqueous medium at room temperature through highly economical synthetic routes. The chemical structures of the synthesized compounds 1–22 were confirmed by analytical and spectral data such as IR, 1H- and 13C-NMR, and mass spectra. The in vitro antibacterial activity of these compounds along with standard clinical reference, streptomycin, was investigated on two key targeted organisms. It was observed that 1-(benzylsulfonyl)pyrrolidine-2-carboxylic acid, 2 emerged as the most active compound against Staphylococcus aureus at MIC value of 1.8 μg/mL while 4-(3-(diethylamino)-3-oxo-2-(phenylmethylsulfonamido) propyl)phenyl phenylmethanesulfonate, 22 was the most active sulfonamide scaffold on Escherichia coli at MIC value of 12.5 μg/mL.

scholarly journals Synthesis and comparative study on the antibacterial activity organotin(IV) 3-hydroxybenzoate compounds

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Sutopo Hadi ◽  
Sri Lestari ◽  
Tati Suhartati ◽  
Hardoko Insan Qudus ◽  
Mita Rilyanti ◽  
...  
Keyword(s):  
Pseudomonas Aeruginosa ◽  
Antibacterial Activity ◽  
Bacillus Subtilis ◽  
Comparative Study ◽  
Antibacterial Agents ◽  
Positive Control ◽  
Dilution Method ◽  
Hydroxybenzoic Acid ◽  
C Nmr

Abstract The synthesis and comparative study on the antibacterial activity of three organotin(IV) compounds, namely dibutyltin(IV) bis-(3-hydroxybenzoate), [Bu2Sn(3-HBz)2] (7), diphenyltin(IV) bis-(3-hydroxybenzoate), [Ph2Sn(3-HBz)2] (8), and triphenyltin(IV) 3-hydroxybenzoate, [Ph3Sn(3-HBz)] (9) which were prepared by the reaction of dibutyltin(IV) oxide, [Bu2SnO] (4), diphenyltin(IV) dihydroxide, [Ph2Sn(OH)2] (5), and triphenyltin(IV) hydroxide, [Ph3SnOH] (6) with 3-hydroxybenzoic acid (3-HBz) has successfully been performed. The characterization of these compounds were done using 1H and 13C NMR, IR, UV spectroscopies and their compositions were determined based on microanalytical data. Antibacterial activity of these compounds was demonstrated at concentrations of 1.89 × 10−4, 1.81 × 10−4, and 1.72 × 10−4 M, respectively by dilution method against Pseudomonas aeruginosa. Similarly, the compounds were active at concentration of 1.87 × 10−4, 1.79 × 10−4, and 1.71 × 10−4 M, respectively, against Bacillus subtilis. These activities are comparable to that of streptomycin at a concentration of 1.70 × 10−4 M as a positive control, but the halozone of compounds 7, 8, and 9 were slightly lower than that of streptomycin’s halozone. The results obtained suggest that the compounds synthesized have potential as antibacterial agents.

Antibacterial activity of Celastrol against Bacillus subtilis

Planta Medica ◽  
2008 ◽  
Vol 74 (09) ◽  
Author(s):  
N Padilla-Montaño ◽  
IL Bazzocchi ◽  
L Moujir
Keyword(s):  
Antibacterial Activity ◽  
Bacillus Subtilis

Novel Synthesis of 4-Benzylidene-2-((1-phenyl-3,4-dihydroisoquinoline-2(1H)-yl)methyl) oxazol-5(4H)-one Derivatives Using 1,2,3,Tetrahydroisoquinoline and their Antimicrobial Activity

2020 ◽  
Vol 17 (5) ◽  
pp. 396-403
Author(s):  
Nalla Krishna Rao ◽  
Tentu Nageswara Rao ◽  
Botsa Parvatamma ◽  
Y. Prashanthi ◽  
Ravi Kumar Cheedarala
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Acetic Acid ◽  
Sodium Acetate ◽  
Good Activity ◽  
Activity Profile ◽  
Aryl Aldehydes ◽  
Chemical Structures ◽  
Novel Synthesis ◽  
Target Molecules

Aims: A series of six 4-benzylidene-2-((1-phenyl-3,4-dihydro isoquinoline-2(1H)-yl)methyloxazol- 5(4H)-one derivatives were synthesized by condensation of substituted aryl aldehydes with 2-(2-(1-phenyl-3,4- dihydro isoquinoline-2(1H)-acetamido)acetic acid in the presence of sodium acetate, acetic anhydride and zinc oxide as catalysts. Background: Novel Synthesis of 4-Benzylidene-2-((1-phenyl-3,4-dihy droisoquinoline-2(1H)-yl)methyl)oxazol- 5(4H)-one derivatives using 1,2,3,Tetrahydroisoquinoline and their antimicrobial activity. Objective: The title compounds can be synthesized from 1,2,3,4-tetrahydroisoquinoline. Methods: The target molecules, i.e., 4-benzylidene-2-((1-phenyl-3, 4-dihydro isoquinoline-2(1H)-yl) methyl) oxazol-5(4H)-one derivatives (8a-8f) have been synthesized from 1,2,3,4-tetrahydroisoquinoline which was prepared from benzoic acid in few steps. Results: All the six compounds were evaluated based on advanced spectral data (1H NMR, 13C NMR & LCMS), and the chemical structures of all compounds were determined by elemental analysis. Conclusion: Antibacterial activity of the derivatives was examined for the synthesized compounds and results indicate that compound with bromine substitution has a good activity profile.

Lysis and biological control of Aspergillus niger by Bacillus subtilis AF 1

1996 ◽  
Vol 42 (6) ◽  
pp. 533-538 ◽  
Author(s):  
A. R. Podile ◽  
A. P. Prakash
Keyword(s):  
Biological Control ◽  
Bacillus Subtilis ◽  
Aspergillus Niger ◽  
Fungal Growth ◽  
Dry Weight ◽  
Crown Rot ◽  
Fungal Mycelium ◽  
Infested Soil ◽  
Dual Culture ◽  
Bacterial Cells

A biocontrol rhizobacterial strain of Bacillus subtilis AF 1 grown for 6 h was coinoculated with Aspergillus niger at different time intervals and microscopic observations revealed adherence of bacterial cells to the fungal mycelium. Bacterial cells multiplied in situ and colonized the mycelial surface. Growth of AF 1 resulted in damage to the cell wall, followed by lysis. AF 1 inoculation into media containing A. niger at 0, 6, and 12 h suppressed >90% fungal growth, while in 18- and 24-h cultures fungal growth inhibition was 70 and 56%, respectively, in terms of dry weight. In dual culture the fungal growth was not accompanied by formation of spores. The mycelial preparation of A. niger as principal carbon source supported the growth of B. subtilis, as much as chitin. Extracellular protein precipitate from B. subtilis culture filtrate had a significant growth-retarding effect on A. niger. Groundnut seeds bacterized with B. subtilis showed a reduced incidence of crown rot in A. niger infested soil, suggesting a possible role of B. subtilis in biological control of A. niger.Key words: mycolytic bacteria, Bacillus subtilis, Aspergillus niger, biological control.

scholarly journals Synthesis and Antibacterial Activity of Some New Phenothiazine Derivatives

2007 ◽  
Vol 4 (1) ◽  
pp. 14-20 ◽  
Author(s):  
Pawan Kumar Swarnkar ◽  
P. Kriplani ◽  
G. N. Gupta ◽  
K. G. Ojha
Keyword(s):  
Antibacterial Activity ◽  
Elemental Analysis ◽  
Spectral Studies ◽  
Phenothiazine Derivatives ◽  
Substituted Anilines ◽  
Conventional Methods

A series of some new phenothiazine derivatives were synthesized with the objective for evaluation as antimicrobials. The title compounds were prepared by a five step synthesis scheme. 2-Amino-6-substituted benzothiazoles (1) on diazotization afford 6-substituted benzothiazolyl-2-diazonium chlorides (2). Reaction of 2 with cold solution ofβ-naphthol in dilute NaOH furnishesα-(2-diazo-6-substituted benzothiazolyl)-β-sodionaphthoxides (3) which on acidification with concentrated HCl givesα-(2-diazo-6-substituted benzothiazolyl)-β-naphthols (4). Reaction of 4 with p-substituted anilines givesα-(2-diazo-6-substituted benzothiazolyl)-β-(p-substituted anilino) naphthalenes (5). This synthesis besides by using conventional methods was also attempted using microwave. Fusion of 5 with sulphur in presence of iodine results inα-(2-diazo-6-substituted benzothiazolyl)-6- substituted [2, 3-b] benzophenothiazines(6). The structures of all these compounds have been supported by elemental analysis and their spectral studies. All synthesized compounds were tested for their antibacterial activity using standard drugs.

scholarly journals PHYTOCHEMICAL ANALYSIS AND ANTIBACTERIAL ACTIVITY OF SWIETENIA MAHAGONI – A HIGHLY MEDICINAL PLANT IN INDIA

2016 ◽  
Vol 9 (6) ◽  
pp. 62
Author(s):  
Dhanapaul Vinoth Kumar
Keyword(s):  
Antibacterial Activity ◽  
Bacillus Subtilis ◽  
Leaf Extract ◽  
Phytochemical Analysis ◽  
Zone Of Inhibition ◽  
Volatile Oils ◽  
Medicinal Uses ◽  
Antibacterial Study ◽  
Active Constituents ◽  
Swietenia Mahagoni

The present study was designed to evaluate the phytochemical analysis and antibacterial activity of Swietenia mahagoni leaf extract. The leaf extract was subjected to a variety of phytochemical analysis. The qualitative phytochemical tests exhibited the presence of common phytocompounds like alkaloids, tannins, saponins, phlobatannins, flavanoids, terpenoids and volatile oils as major active constituents. The plant (Swietenia mahagoni) leaf has valuable medicinal uses, hence petroleum ether (18.2g) was found to be a good solvent for the phytochemical and antibacterial study. Similarly, the Methanolic leaf extract of Swietenia mahagoni has highest zone of inhibition on Bacillus subtilis.

scholarly journals SYNTHESIS AND ANTIMICROBIAL EVALUATION OF QUINAZOLINONE PEPTIDE DERIVATIVES

2017 ◽  
Vol 10 (16) ◽  
pp. 7 ◽  
Author(s):  
Bhupinder Kapoor ◽  
Arshid Nabi ◽  
Reena Gupta ◽  
Mukta Gupta
Keyword(s):  
Antibacterial Activity ◽  
Amino Acid ◽  
Antimicrobial Agents ◽  
Methyl Esters ◽  
Standard Drug ◽  
Amino Acid Peptide ◽  
Chemical Structures ◽  
1H Nuclear Magnetic Resonance ◽  
Peptide Derivatives ◽  
Derivatives Of

  Objective: The increased microbial resistance against commercially available drugs initiated the development of novel and safe antimicrobial agents in last few decades. In this view, a series of amino acid/dipeptide derivatives of quinazolin-3(4H)-one was synthesized and was evaluated for their antimicrobial potential.Method: Synthesis of amino acid/peptide derivatives were carried out by coupling 5-(2-(2-chlorophenyl)-4-oxoquinazolin-3(4H)-yl)-2-hydroxy benzoic acid with amino acid/dipeptide methyl esters in the presence of dicyclohexylcarbodiimide and N-methylmorpholine. The chemical structures of synthesized compounds were characterized by 1H nuclear magnetic resonance and infrared spectroscopy and were screened for antibacterial activity by disc diffusion method.Results: All the synthesized derivatives exhibited moderate to significant antibacterial activity against both Gram-positive and Gram-negative bacteria. The potency of compound 5d was comparable to standard drug ciprofloxacin in all the strains of bacteria used. The compound 5a was found to be more active against Streptococcus pyogenes and Staphylococcus aureus while compound 5c against Pseudomonas aeruginosa and Escherichia coli. Conclusion: Peptide derivatives of quinazolinone are promising antimicrobial agent and can be used for the synthesis of other novel compounds.

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