Design, Synthesis and Antibacterial, Antifungal Activity of Some Coumarin Acetohydrazide Derivatives

2021 ◽  
pp. 3931-3937
Author(s):  
A. R. Chabukswar ◽  
P.V. Adsule ◽  
P.B. Randhave ◽  
Manini Mantri
Keyword(s):  
Antifungal Activity ◽  
Moderate Activity ◽  
Gram Negative Bacteria ◽  
Significant Activity ◽  
Design Synthesis ◽  
E Coli ◽  
Gram Positive Bacteria ◽  
Antibacterial And Antifungal ◽  
Gyrase Inhibitors

We have designed and synthesized (Z)-2-(5-methyl-2-oxo-2H-chromen-7-yl) oxy)-N’-(2-oxoindolin-3-ylidin) acetohydrazide derivatives by reacting 7-hydroxy-4-methyl-coumarin and substituted isatin to afford 12 substituted coumarin acetohydrazide derivatives. The synthesized compounds of coumarin acetohydrazide derivatives were designed and evaluated to study for their possible interactions as DNA gyrase inhibitors. All the synthesized coumarin acetohydrazide compounds have been characterized by spectral analysis IR, 1H NMR and mass spectroscopy. The compounds have been evaluated for In vitro antibacterial and antifungal activity against S. aureus, B. subtilus, E. coli, P. aeruginosa and fungi C. albicans and A. niger. In case of Gram positive bacteria and Gram negative bacteria Compound P5C, M5C, C5C exhibited significant activity. Compounds P5N, M5N, C5N shown moderate activity. Compound P5C, M5C, C5C shown significant Antifungal activity against C. albicans and A. niger. Compounds P5C, M5C, C5C are found to exert significant antibacterial as well as antifungal activity and can serve as potential compound against infectious diseases in future.

scholarly journals Synthesis, Characterization of Biologically Potent Novel Chalcones Bearing Urea, Thiourea and Acetamide Linkages

2014 ◽  
Vol 36 ◽  
pp. 281-294
Author(s):  
Nirali S. Mewada ◽  
Dhruvin R. Shah ◽  
Kishor H. Chikhalia
Keyword(s):  
Antifungal Activity ◽  
Dilution Method ◽  
Gram Negative Bacteria ◽  
Antibacterial And Antifungal Activity ◽  
Gram Positive Bacteria ◽  
H Nmr ◽  
Antibacterial And Antifungal ◽  
Antimicrobial And Antifungal Activities

Three series of some novel chalcone based urea, thiourea and acetamide derivatives were designed, synthesized and screened for their antimicrobial and antifungal activities. All the synthesized compounds are first reported. The structures of the compounds were elucidated with the aid of elemental analysis and spectral methods including IR, 1H-NMR spectral data. The prepared compounds were evaluated for antibacterial activity against two Gram-positive bacteria (Staphylococcus aureus, Staphylococcus pyogenus), two Gram-negative bacteria (Pseudomonas aeruginosa, Escherichia coli). The title compounds were also investigated for their antifungal activity using the broth micro dilution method. The bioassay results showed that compounds a few compounds showed good to superior in vitro antibacterial and antifungal activity.

scholarly journals Design, Synthesis and Antifungal Activity of Novel Benzoylcarbamates Bearing a Pyridine Moiety

2018 ◽  
Vol 8 (12) ◽  
pp. 2577
Author(s):  
Fu-Xian Wan ◽  
Jian-Hua Wang ◽  
Yan-Hua Shi ◽  
Li-Zhi Niu ◽  
Lin Jiang
Keyword(s):  
Antifungal Activity ◽  
High Efficiency ◽  
Plant Diseases ◽  
Moderate Activity ◽  
Significant Activity ◽  
Environmental Friendliness ◽  
Design Synthesis ◽  
Lead Compounds ◽  
Pyridine Moiety

Many natural and synthetic pyridine derivatives have good biological activity, and are widely used in the fields of pesticides and medicines. On the other hand, carbamate fungicides possess some unique properties, such as high efficiency, strong selectivity, low toxicity, and environmental friendliness, and are often used to control many plant diseases. Therefore, discovering novel pyridine-based carbamates is of great significance. In this paper, we chose the excellent fungicides tolprocarb and picarbutrazox as lead compounds, integrating benzoyl, carbamate, and pyridinyl moieties into a molecule. Thus, we designed and synthesized a series of substituted benzoyl carbamates containing a pyridine ring, and evaluated the in vitro antifungal activity. The target compounds exhibited moderate to strong bioactivity against Botrytis cinerea, among which the compounds 4d, 4f, 4g, and 4h exhibited significant activity with EC50 values (the concentration resulting in a 50% inhibition) of 6.45–6.98 μg/mL, and their activities were near or superior to that of chlorothalonil. Additionally, 4h exhibited moderate activity against Sclerotinia sclerotiorumwith an EC50 value of 10.85 μg/mL.

scholarly journals Synthesis and In Vitro Antibacterial and Antifungal Evaluation of Quinoline Analogue Azetidin and Thiazolidin Derivatives

2014 ◽  
Vol 39 ◽  
pp. 195-210 ◽  
Author(s):  
Shraddha M. Prajapati ◽  
Rajesh H. Vekariya ◽  
Kinjal D. Patel ◽  
Shyamali N. Panchal ◽  
Hitesh D. Patel ◽  
...  
Keyword(s):  
Gram Negative Bacteria ◽  
Aspergillus Clavatus ◽  
Dilution Technique ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
Gram Positive Bacteria ◽  
H Nmr ◽  
Antibacterial And Antifungal ◽  
Broth Dilution

A library of quinoline analog two novel series of azetidin (SH1-5) and thiazolidin (SHa-e) derivatives were designed and synthesized with simple and eco-friendly methodologies. The structures of the compounds were elucidated with the aid of elemental analysis, IR, 1H-NMR and mass spectral data. These novel synthesized compounds were evaluated for antibacterial activity against two gram-positive bacteria (Staphylococcus aureus, Staphylococcus pyogenus) and two gram-negative bacteria (Pseudomonas aeruginosa, Escherichia coli). The title compounds were also studied for their antifungal activity with Candida albicans, Aspergillus niger, Aspergillus clavatus using the broth dilution technique. Most of the compounds were the best bio-active desired antibacterial analog with less MIC value against different tested strains.

Novel 2-(5-Aryl)thiophen-2-yl)benzimidazoles; Design, Synthesis and In vitro Evaluation Against Cercarial Phase of Schistosoma mansoni

2020 ◽  
Vol 17 (11) ◽  
pp. 1432-1438
Author(s):  
Serry Atta El Bialy ◽  
Basem Mansour ◽  
Waleed Abdelhakeem Bayoumi ◽  
Amira Taman ◽  
Hassan Mohammed Eissa
Keyword(s):  
Structural Modification ◽  
Anthelmintic Activity ◽  
Ring System ◽  
Literature Survey ◽  
Moderate Activity ◽  
Significant Activity ◽  
Design Synthesis ◽  
Interesting Class ◽  
Low Activity

Background: Literature survey has pointed out that Benzimidazoles represent an interesting class of anthelmintics, of which several potent members were developed. Objective: Benzimidazoles hybridized with pharmacophoric moieties possessing anthelmintic activity were designed, synthesized to be evaluated against cercaria. Methods: Structural modification was achieved through 2- and 5-positions. Moreover, an in vitro cercarial assay was adopted to evaluate target compounds. Results and Discussion: Biological screening revealed that compound 3h showed significant activity with a survival index of 35% at a 100 μg/mL concentration. Whereas, compounds 3a and 3c showed moderate activity, the rest of the tested compounds exhibited low activity. Conclusion: The current study evidenced that the new hybrids "benzimidazole-thiophen-aryl" are successful as cercacidal agents. Further studies of this novel tri-ring system are suggested on adult worms of S. mansoni.

scholarly journals Antimicrobial Evaluation of Leaf and Stem Extract of Cordia macleodii

2014 ◽  
Vol 1 (1) ◽  
pp. 1-3 ◽  
Author(s):  
Deepkumar Joshi ◽  
Rinku Patel ◽  
Nupur Patel ◽  
Devendra Patel ◽  
Chintan Pandya
Keyword(s):  
Antimicrobial Activities ◽  
Maximum Amount ◽  
Gram Negative Bacteria ◽  
Gram Negative ◽  
E Coli ◽  
Gram Positive Bacteria ◽  
Antifungal Potential ◽  
Stem Extract ◽  
Antimicrobial Evaluation ◽  
Antibacterial And Antifungal

The leaf and stem of cordia macleodii plant were investigated for evaluating antibacterial and antifungal properties.Different extracts of leaf and stem viz. double distilled water, methanol, ethyl acetate ane n-hexane were collectedand content was optimized for the maximum amount of extraction with varying time of 6 and 12 h. The extracts weretested for their antimicrobial activities against gram-positive bacteria (B. sutilis), gram-negative bacteria (E. coli) andfungi (A. niger). The extracts were found to be more active against bacteria as compared to fungi. It was also observedthat the antibacterial and antifungal potential of the water extracts were found to be excellent as 1A (38 mm) and 1B (22mm) compared to the other extracts. Graphical Abstract:

scholarly journals Synthesis and Biological Screening of 3-Aryl-5-[(4′-Difluoromethoxy)(3′-Hydroxy)Phenyl]-4,5-Dihydro Isoxazole

2015 ◽  
Vol 47 ◽  
pp. 133-138
Author(s):  
V.N. Bhadani ◽  
H.D. Purohit ◽  
Dipak M. Purohit
Keyword(s):  
Antibacterial Activity ◽  
Candida Albicans ◽  
Antifungal Activity ◽  
Biological Activities ◽  
Gram Negative Bacteria ◽  
Biological Screening ◽  
Gram Negative ◽  
E Coli ◽  
Gram Positive Bacteria ◽  
Therapeutic Activities

Isoxazoline derivatives shows various types of therapeutic activities like antimicrobial[1], anti-inflammatory[2], anticonvulsant[3], Hypoglycemic[4] etc. getting to synthesized in view of 3-Aryl-5-[(4′-difluoromethoxy)(3′-hydroxy)phenyl]-4,5-dihydro isoxazole (4a-4i) have been synthesized. All the newly synthesized compounds were screened for their antibacterial activity against S. aureus, M. luteus (Gram-positive bacteria), E. coli, S. thyphi (Gram-negative bacteria) and antifungal activity against Candida albicans (Fungi). The biological activities (MIC) of the synthesized compounds were compared with known standard drugs.

scholarly journals SYNTHESIS AND ANTIMICROBIAL ACTIVITY OF SOME (2-AMINO-5-THIOL-1, 3, 4-THIADIAZOLE DERIVATIVES

2007 ◽  
Vol 4 (1) ◽  
pp. 89-94 ◽  
Author(s):  
Baghdad Science Journal
Keyword(s):  
Uv Spectroscopy ◽  
Alkyl Halides ◽  
Moderate Activity ◽  
Gram Negative Bacteria ◽  
Good Activity ◽  
Gram Positive Bacteria ◽  
Thiadiazole Derivatives ◽  
Derivatives Of ◽  
Ir And Uv Spectroscopy

Five derivatives of thiadiazole were prepared with aldehydes and alkyl halides, compoundA: 2-amino-5-thiol-1,3,4- thiadiazole, compound B :2-(o-hydroxybenzylidine)amino-5-thiol-1,3,4-thiadiazole, compoundC: 2(2-butan-lidine)amino-5-thiol-1,3,4-thiadiazole, compound E: 2- amino-5-(2-Propanylthio)-1,3,4-thiadiazol) and compound F:2(o-chlorobenzylamino)-5-(2-propanyl thio)-1,3,4 thiadiazol. All prepared compounds were diagnosed by (IR) and (UV) Spectroscopy. All of those compounds were screened for their anti-microbial activity in vitro. The results show that most of the compounds A, B, C exhibited moderate to good activity against Gram-positive bacteria and the same compound exhibit low to moderate activity on most gram-negative bacteria under study. Finally, compound E and F had little or no effect organism.

Design, Synthesis and Antimicrobial Activity of Some Triazine Chalcone Derivatives

2021 ◽  
Vol 18 (4) ◽  
pp. 332-338
Author(s):  
Ravindra Sandipan Shinde ◽  
Satish Ashruba Dake ◽  
Rajendra Pundalikrao Pawar
Keyword(s):  
Escherichia Coli ◽  
Candida Glabrata ◽  
Gram Negative Bacteria ◽  
Antibacterial And Antifungal Activity ◽  
Design Synthesis ◽  
Gram Negative ◽  
Chalcone Derivatives ◽  
Gram Positive Bacteria ◽  
Target Molecules ◽  
Antibacterial And Antifungal

Background: A series of Triazine Chalcone derivatives were synthesized by the condensation of 1-(4-((4,6-dimethoxy-1,3,5-triazin-2-yl)amino)phenyl)ethanone with substituted benzaldehyde in methanol solvent. Methods: All the synthesized derivatives (3a-l) were screened for their anti-bacterial evaluation against Gram negative bacteria Escherichia coli (NCIM 2137) and Pseudomonas aeruginosa (NCIM 2036); Gram positive bacteria Staphylococcus aureus, Bacillus subtilis (NCIM 2250) and four fungal stains. Candida albicans (MTCC 227), Aspergillus niger (NCIM 545), Candida tropicalis (NCIM 3110) and Candida glabrata (NCIM 3236). Results and Conclusion: Several target molecules throughout the series showed good antibacterial and antifungal activity against tested stains.

Design, synthesis, and antibacterial activity of novel 8-methoxyquinoline-2-carboxamide compounds containing 1,3,4-thiadiazole moiety

2018 ◽  
Vol 73 (3-4) ◽  
pp. 117-122 ◽  
Author(s):  
Tengfei Qu ◽  
Lailiang Qu ◽  
Xiaoguang Wang ◽  
Ting Xu ◽  
Xiao Xiao ◽  
...  
Keyword(s):  
Antibacterial Activities ◽  
Combination Method ◽  
Gram Negative Bacteria ◽  
Antibacterial Efficacy ◽  
Design Synthesis ◽  
Reference Drug ◽  
Gram Positive Bacteria ◽  
Structure Activity ◽  
Antibacterial Assay

AbstractA series of novel 8-methoxyquinoline-2-carboxamide compounds containing 1,3,4-thiadiazole moiety was designed and synthesized by using an active substructure combination method. Then, the antibacterial activities of all the target compounds were evaluated in vitro against three Gram-positive bacteria and three Gram-negative bacteria. The antibacterial assay showed that some target compounds displayed moderate to good antibacterial efficacy in comparison with the reference drug Chloromycin. Some interesting results of structure-activity relationships were also discussed.

scholarly journals In VitroAntimicrobial Activity and Effect on Biofilm Production of a White Grape Juice (Vitis vinifera) Extract

2015 ◽  
Vol 2015 ◽  
pp. 1-5 ◽  
Author(s):  
Angela Filocamo ◽  
Carlo Bisignano ◽  
Giuseppina Mandalari ◽  
Michele Navarra
Keyword(s):  
Aspergillus Niger ◽  
Grape Juice ◽  
Antimicrobial Effect ◽  
Gram Negative Bacteria ◽  
Respiratory Pathogens ◽  
Gram Positive ◽  
Gram Negative ◽  
E Coli ◽  
Gram Positive Bacteria

Background. The aim of the present study was to evaluate the antimicrobial effect of a white grape juice extract (WGJe) against a range of Gram-positive and Gram-negative bacteria, yeasts, and the fungusAspergillus niger. WGJe was also tested on the production of bacterial biofilmsin vitro.Results. WGJe inhibitedin vitromost Gram-positive bacteria tested,Staphylococcus aureusATCC 6538P being the most sensitive strain (MIC values of 3.9 μg/mL). The effect was bactericidal at the concentration of 500 μg/mL. Amongst the Gram-negative bacteria,Escherichia coliwas the only susceptible strain (MIC and MBC of 2000 μg/mL). No effect on the growth ofCandidasp. and the fungusAspergillus nigerwas detected (MIC values > 2000 μg/mL). WGJe inhibited the biofilms formation ofE. coliandPseudomonas aeruginosawith a dose-dependent effect.Conclusions. WGJe exerted both bacteriostatic and bactericidal activityin vitro. The presented results could be used to develop novel strategies for the treatment of skin infections and against potential respiratory pathogens.

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