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 Characterization of Antimicrobial, Antioxidant, and Leishmanicidal Activities of Schiff Base Derivatives of 4-Aminoantipyrine

Molecules ◽  
2019 ◽  
Vol 24 (15) ◽  
pp. 2696 ◽  
Author(s):  
Teran ◽  
Guevara ◽  
Mora ◽  
Dobronski ◽  
Barreiro-Costa ◽  
...  
Keyword(s):  
Schiff Base ◽  
Schiff Bases ◽  
Antimicrobial Activities ◽  
Drug Candidates ◽  
Development Of Resistance ◽  
Schiff Base Derivatives ◽  
Wide Range ◽  
Derivatives Of

Our main interest is the characterization of compounds to support the development of alternatives to currently marketed drugs that are losing effectiveness due to the development of resistance. Schiff bases are promising biologically interesting compounds having a wide range of pharmaceutical properties, including anti-inflammatory, antipyretic, and antimicrobial activities, among others. In this work, we have synthesized 12 Schiff base derivatives of 4-aminoantipyrine. In vitro antimicrobial, antioxidant, and cytotoxicity properties are analyzed, as well as in silico predictive adsorption, distribution, metabolism, and excretion (ADME) and bioactivity scores. Results identify two potential Schiff bases: one effective against E. faecalis and the other with antioxidant activity. Both have reasonable ADME scores and provides a scaffold for developing more effective compounds in the future. Initial studies are usually limited to laboratory in vitro approaches, and following these initial studies, much research is needed before a drug can reach the clinic. Nevertheless, these laboratory approaches are mandatory and constitute a first filter to discriminate among potential drug candidates and chemical compounds that should be discarded.

scholarly journals Synthesis and Evaluation of Antimicrobial Activities of Novel N-Substituted Indole Derivatives

2020 ◽  
Vol 2020 ◽  
pp. 1-9
Author(s):  
Tanveer MahamadAlli Shaikh ◽  
Habtamu Debebe
Keyword(s):  
Antimicrobial Activities ◽  
New Drugs ◽  
Diffusion Method ◽  
Indole Derivatives ◽  
Disc Diffusion ◽  
Disc Diffusion Method ◽  
Standard Drug ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal

Indole motifs are one of the most significant scaffolds in the discovery of new drugs. We have described a synthesis of new N-substituted indole derivatives (1-3), and their in vitro antimicrobial activities were investigated. The synthesis of titled compounds has been demonstrated by utilizing commercially available starting materials. The antibacterial and antifungal activities were performed using new strains of bacteria Staphylococcus aureus, Escherichia coli, and Candida albicans using the disc diffusion method. Notably, the compound 4-(1-(2-(1H-indol-1-yl) ethoxy) pentyl)-N,N-dimethyl aniline (1) was found to be most potent than the other analogues (2 and 3), which has shown higher inhibition than the standard drug chloramphenicol.

Synthesis, Antimicrobial Evaluation and Docking Study of Novel Thiosemicarbazone clubbed with 1,2,3-Triazoles

2020 ◽  
Vol 16 ◽  
Author(s):  
Adinath D. Badar ◽  
Shubham M. Sulakhe ◽  
Mahesh B. Muluk ◽  
Naziya N. M. A. Rehman ◽  
Prashant P. Dixit ◽  
...  
Keyword(s):  
Binding Affinity ◽  
Biological Activities ◽  
Dna Gyrase ◽  
Docking Study ◽  
Antimicrobial Activities ◽  
Diffusion Method ◽  
Molecular Docking Study ◽  
Triazole Derivatives ◽  
Antibacterial And Antifungal

Background: Thiosemicarbazone, 1,2,3-triazole and their derivatives received great pharmaceutical importance due to their prominent biological activities. In the present study, the molecular hybrid thiosemicarbazone-1,2,3-triazoles derivatives were synthesized and screened for their antimicrobial activities. Methods: A series of thiosemicarbazone clubbed with 1,2,3-triazole derivatives were synthesized via click chemistry approach in good yields. The structures of synthesized compounds were assigned by their spectral data. The in vitro antimicrobial activity was performed by the agar well diffusion method. A molecular docking study was performed to identify the possible mode of action of synthesized derivatives. Results: The compounds 5d, 5h, 5i and 5k have exhibited excellent antimicrobial activities against both antibacterial and antifungal pathogens. The active thiosemicarbazone-1,2,3-triazole derivatives have shown excellent binding affinity towards DNA gyrase. Conclusion: The molecular hybrid thiosemicarbazone-1,2,3-triazole derivatives were synthesized. The newly synthesized compounds were evaluated for their antimicrobial activities. Few of the thiosemicarbazone-1,2,3-triazoles derivatives have exhibited good antimicrobial activities. They have been shown excellent binding affinity towards DNA gyrase.

scholarly journals Synthesis and Evaluation of Schiff Bases of 4-Amino-5-(chlorine substituted phenyl)-4H-1,2,4-triazole-3-thione as Antimicrobial Agents

2020 ◽  
Vol 41 (1) ◽  
pp. 26-35
Author(s):  
Kishor Devkota ◽  
Govinda Pathak ◽  
Bhushan Shakya
Keyword(s):  
Schiff Base ◽  
Schiff Bases ◽  
Antimicrobial Agents ◽  
Triazole Ring ◽  
Antimicrobial Activities ◽  
Biologically Active ◽  
Spectral Techniques ◽  
Schiff Base Derivatives ◽  
Bacteria And Fungi ◽  
Different Strains

Triazole ring system has attracted a continuously growing interest of synthetic organic chemists and those dealing with the medicinal compounds due to its versatile potential to interact with biological systems. Schiff bases are also considered as one of the most biologically active compounds.  The aim of the present study was to synthesize new Schiff bases bearing triazole nucleus and to assess their antimicrobial activities. Four new Schiff base derivatives of 1,2,4-triazole-3-thione were synthesized by combining two different pharmacophores viz. triazole nucleus and Schiff base moiety and were characterized by spectral techniques (UV, FT-IR, and NMR). The Schiff bases were evaluated for antibacterial (Staphylococcus aureus, Escherichia coli, and Klebsiella pneumoniae) and antifungal (Candida albicans) activities. The synthesized compounds exhibited good to moderate activities against different strains of bacteria and fungi tested.

scholarly journals Phytochemical investigation and in vitro antimicrobial activity of Richardia scabra

2016 ◽  
Vol 11 (2) ◽  
pp. 248 ◽  
Author(s):  
Kathirvel Poonkodi ◽  
Subban Ravi
Keyword(s):  
Antimicrobial Activity ◽  
Diffusion Method ◽  
Bacterial Strains ◽  
Weed Species ◽  
Antibacterial And Antifungal Activities ◽  
Agar Plug ◽  
Phytochemical Investigation ◽  
Antibacterial And Antifungal ◽  
Simple Sugar

<p class="Abstract">The present study was aimed to evaluate the phytochemical screening and antimicrobial activity of the petroleum ether and methanol extracts from the mature leaves of <em>Richardia scabra</em> from India. Disc diffusion method was used to determine the zone inhibition of the tested samples for antibacterial and agar plug method was used to determine the antifungal activity, while the microtube-dilution technique was used to determine the minimum inhibitory concentration. Both extracts showed significant antibacterial and antifungal activities when tested against 10 bacterial and four fungal strains. The minimum inhibitory concentrations of the methanol extract of<em> R. scabra</em> ranged between 12.5–100 μg/mL for bacterial strains. Alkaloids, steroids, flavonoids, fatty acids, terpenoids and simple sugar were detected as phytoconstituents of extracts. To the best of our knowledge, this is the first report against antimicrobial activity of common weed species <em>R. scabra</em> found in India.</p><p> </p>

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, Antimicrobial Screening, Homology Modeling, and Molecular Docking Studies of a New Series of Schiff Base Derivatives as Prospective Fungal Inhibitor Candidates

Molecules ◽  
2019 ◽  
Vol 24 (18) ◽  
pp. 3250 ◽  
Author(s):  
Yahya Toubi ◽  
Farid Abrigach ◽  
Smaail Radi ◽  
Faiza Souna ◽  
Abdelkader Hakkou ◽  
...  
Keyword(s):  
Schiff Base ◽  
Homology Modeling ◽  
Condensation Reaction ◽  
Docking Studies ◽  
Antifungal Effect ◽  
1H And 13C Nmr ◽  
Schiff Base Derivatives ◽  
Ft Ir ◽  
Antibacterial And Antifungal

Twelve new Schiff base derivatives have been prepared by the condensation reaction of different amino substituted compounds (aniline, pyridin-2-amine, o-toluidine, 2-nitrobenzenamine, 4-aminophenol, and 3-aminopropanol) and substituted aldehydes such as nicotinaldehyde, o,m,p-nitrobenzaldehyde, and picolinaldehyde in ethanol using acetic acid as a catalyst. The envisaged structures of the all the synthesized ligands have been confirmed on the basis of their spectral analysis FT-IR, mass spectroscopy, 1H- and 13C-NMR. In vitro screening of their antibacterial and antifungal potential against Escherichia coli bacterium and Fusarium oxysporum f.sp albedinis (F.o.a) fungus, respectively, revealed that all the ligands showed no significant antibacterial activity, whereas most of them displayed good antifungal activity. Homology modeling and docking analysis were performed to explain the antifungal effect of the most and least active compound against two F.o.a fungus proteins.

scholarly journals Synthesis, Characterization and Study of Antimicrobial Activities of Mannich Bases Incorporating 1,2,4-Triazole Nucleus

2021 ◽  
Vol 2 (01) ◽  
pp. 19-27
Author(s):  
Rhambus Rawat ◽  
Prem Shankar Deo ◽  
Bhushan Shakya
Keyword(s):  
Schiff Base ◽  
Heterocyclic Compounds ◽  
Environmental Science ◽  
Biological Activities ◽  
Antimicrobial Activities ◽  
Mannich Bases ◽  
New Drugs ◽  
Spectroscopic Techniques ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal

Heterocyclic compounds containing triazole moiety have great importance in the field of medicine, pharmaceuticals, biochemistry, biology, therapeutics, environmental science, and industry. Triazoles and their derivatives have been extensively used in the development of new drugs. Biological activities of Schiff bases are highly investigated, but Mannich bases are on the verge of their development, and they are being synthesized in large number nowadays. In this work, Mannich bases are synthesized by incorporation 1,2,4-triazole moiety through Schiff base using different amines. Mannich bases are found to exhibit highly effective antibacterial and antifungal activities. The formation of synthesized compounds - 1,2,4-triazole-5-thione, Schiff base (4) and Mannich bases (5a and 5b) - are confirmed and characterized by spectroscopic techniques like UV, FTIR 1H-NMR and 13C-NMR. The activity of the synthesized compounds was tested against bacterial and fungal strain.

scholarly journals Synthesis and Antimicrobial Activities of N-(Heteroaryl-substituted)-p-toluenesulphonamides

2014 ◽  
Vol 2014 ◽  
pp. 1-5
Author(s):  
Ozoh Chinwe Francisca ◽  
Okoro Uchechukwu Chris ◽  
Ugwu David Izuchukwu
Keyword(s):  
Biological Activities ◽  
Condensation Reaction ◽  
Antimicrobial Activities ◽  
Diffusion Method ◽  
Gram Positive Bacteria ◽  
New Class ◽  
Bacteria And Fungi ◽  
Antibacterial And Antifungal ◽  
C Nmr

A new class of N-(heteroaryl-substituted)-p-toluenesulphonamides has been synthesized exhibiting antibacterial and antifungal properties. The condensation reaction of p-toluenesulphonyl chloride 1 with appropriate substituted amino pyridines 2a–g in acetone furnished N-(heteroaryl-substituted)-p-toluenesulphonamides 3a–g. These derivatives were characterized by IR, 1H-, and 13C-NMR spectroscopy and were screened in vitro against gram-positive bacteria, gram-negative bacteria, and fungi organisms using agar-diffusion method. Results indicated improved biological activities over reference drugs such as Tetracycline (TCN) and Fluconazole (FLU).

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