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

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.

2006 ◽  
Vol 1 (8) ◽  
pp. 1934578X0600100 ◽  
Author(s):  
Hocine Laouer ◽  
Salah Akkal ◽  
Claire Debarnot ◽  
Bruno Canard ◽  
Uwe J. Meierhenrich ◽  
...  

The chemical composition of the essential oil of Saccocalyx satureioides Coss. et Dur. (Lamiaceae) was analyzed by chiral and achiral GC/MS and 42 components were identified. The main constituents were (+)-α-terpineol (35.9%), thymol (15.6%) and borneol (12.4%). The in vitro antibacterial and antifungal activities of the essential oil were assessed by the disc diffusion method, and were significant on the six microorganisms tested. A moderate inhibitory activity against hepatitis C virus polymerase was also evidenced.


2016 ◽  
Vol 8 (2) ◽  
pp. 209-216
Author(s):  
A. Rahim ◽  
R. Ali ◽  
A. Islam

 2',4',5'- and 2',3',4'-trimethoxy flavanones have been synthesized starting with 2-hydroxyacetophone and substituted aldehyde. Antibacterial activities of the flavanones have been tested along with their corresponding chalcones against two human pathogenic bacteria (Streptococcus-b-haemolyticus and  Klebsiella sp. (G-)). Antifungal activities of the flavanones have also been investigated against  two plants pathogenic mold fungi (Rhizactonia solani Sclerotium rolfsii). The structures of the synthesized compounds have been characterized with the help of  UV, IR and 1H NMR and 13C-NMR spectra. The antibacterial and antifungal screening were performed in vitro by the filter paper disc diffusion method and poisoned food technique. The flavanones showed antibacterial activity while no activity was observed to their corresponding chalcones against the tested bacteria. On the other hand, chalcones and their corresponding flavanones both showed fungicidal activities.


2018 ◽  
Vol 13 (6) ◽  
pp. 1934578X1801300
Author(s):  
Zhe Wang ◽  
Ai-Hong Peng ◽  
Dan-Dan Lu ◽  
Ya-Jie Song ◽  
Cheng-Lei Wang ◽  
...  

Two new manumycin-type derivatives named as cornifronin A and cornifronin B, and one known analogue antibiotic SW-B were isolated from the liquid fermentation of Streptomyces sp. OC1401 obtained from body surface of a meson bee Osmia cornifrons. The structures of all isolates were identified by spectroscopic methods (HRESIMS, IR, 1D and 2D NMR) and comparison with literature data. The antibacterial and antifungal activities of these manumycin-type derivatives were evaluated by disc diffusion method and more accurate data on the antibacterial activity were obtained through the MIC (Minimum Inhibitory Concentration) and MBC (Minimal bactericidal concentration) values.


2007 ◽  
Vol 4 (s1) ◽  
pp. 17-20 ◽  
Author(s):  
Nenad Vukovic ◽  
Tanja Milosevic ◽  
Slobodan Sukdolak ◽  
Slavica Solujic

This study was designed to examine the chemical composition of essential oil and thein vitroantimicrobial activities of essential oil and methanol extract ofTeucrium montanum. The inhibitory effects of essential oil and methanol extracts ofT. montanumwere tested against 13 bacterial and three fungal species by using disc-diffusion method. GC/MS analyses revealed that essential oil contains mainly δ-cadinene (17.19%), β-selinene (8.16%) α-calacorene (4.97%), 1,6-dimethyl-4-(1-methylethyl)-naphthalene (4.91%), caryophyllene (4.35%), copaene (4.23%), torreyol (3.91%), 4-terpineol (3.90%), cadina-1,4-diene (3.39%), β-sesquiphellandrene (3.34%), τ-cadinol (3.12%) and γ-curcumene (3.18%). The essential oil has antibacterial as well as antifungal effect.


2019 ◽  
Vol 16 ◽  
pp. 6313-6324
Author(s):  
Hanaa A. El-Boraey ◽  
Aballah El-domiaty

Four novel Mn(II), Co(II), Cu(II) complexes with nitrogen containing ligand (L) i.e. N,N-((Z)-ethane-1,2-diylidine)bis(2-amino benzo hydrazide) have been synthesized and structurally characterized by elemental analysis, spectral, thermal (TG/DTG), molar conductance and magnetic susceptibility measurements. From the spectroscopic and magnetic studies it has been concluded that all complexes have a six coordinated octahedral geometry. The Schiff base and their metal complexes have also been screened for their antibacterial and antifungal activities by using a modified Kirby-Bauer disc diffusion method.


2020 ◽  
Vol 10 (1-s) ◽  
pp. 62-65
Author(s):  
Fahadul Islam ◽  
A.K. Azad ◽  
Md. Faysal ◽  
Md. A.K. Azad ◽  
Saiful Islam ◽  
...  

Objectives: Present study was designed to evaluate Analgesic, Antidiarrhoeal and Antimicrobial activities of methanol and acetone extracts of fruit peels of Limonia acidissima L. by different methods. Method: The analgesic activity of the samples was studied using acetic acid- induced writhing model in mice. Castor oil-induced antidiarrheal activity was observed by Thomas method and antimicrobial activity was monitored by disc diffusion method. Results: Limonia acidissima L. inhibited 60.53 % and 59.65 % writhing of methanol as well as acetone fruit peels extracts, respectively, compared to standard drug Diclofenac Na inhibited 78.07 % writhing. At higher dose (500 mg/kg) of the methanol and acetone fruit peels extracts, significant inhibition 47.13 and 44.83 % of characteristic diarrhoeal feces was observed, respectively, as well as at lower dose (250 mg/kg) of the both extracts, inhibition 34.45 and35.63 %. Mention able on average 12mm zone of inhibition was observed of both extract at 250µg/disc and 500µg/disc compare to zone of inhibition 36mm of ciprofloxacin at 50µg/disc. Conclusion: From the above results, it will be very much possible source for an isolating lead compound for curing the numerous disorders. Keywords: Limonia acidissima L. Fruit peels, Diclofenac sodium, Loperamide, Ciprofloxacin.


2017 ◽  
Vol 1 (3) ◽  
pp. 230-234 ◽  
Author(s):  
Sefa Durmuş ◽  
Aslıhan Dalmaz ◽  
Görkem Dülger ◽  
Duygu Bircan Kadıoğlu

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.


2009 ◽  
Vol 4 (3) ◽  
pp. 362-368 ◽  
Author(s):  
Joanna Stefańska ◽  
Anna Bielenica ◽  
Marta Struga ◽  
Stafan Tyski ◽  
Jerzy Kossakowski ◽  
...  

AbstractAntibacterial and antifungal activity of 10-(diphenylmethylene)-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione derivatives were examined by the disc-diffusion method (growth inhibition zone diameter in agar medium). The MIC’s for the most active agents were determined. Title compounds were also evaluated in vitro against representatives of different virus classes. Most of the tested compounds exhibit activity against CVB-2 virus.


2014 ◽  
Vol 6 (3) ◽  
pp. 276-281 ◽  
Author(s):  
Tiwalade Adeyemi ADENIYI ◽  
Peter A. ADEONIPEKUN ◽  
Elizabeth A. OMOTAYO

In order to evaluate the medicinal value of notorious sedge weeds, three species:Cyperus esculentus, Cyperus rotundus and Mariscus alternifolius were investigated for their phytochemical constituents and antimicrobial properties. Preliminary qualitative phytochemical constituents and in vitro antimicrobial activities were evaluated against four fungi species: Aspergillus niger, Aspergillus fumigatus, Penicillium chrysogenum and Candida albicans, and three bacteria species: Escherichia coli,Salmonella typhi and Staphylococcus aureus. Two solvents, water and ethanol, were used to produce the extracts and were screened for their antimicrobial activity. Antimicrobial activity evaluation of the extracts against pathogens was carried out at 100 mg/ml concentration by Disc Diffusion method for fungi, Disc Diffusion and Agar Well Diffusion methods for bacteria. Observed activities were related to standard antibiotics, antifungal and antibacterial, which served as controls. Phytochemically, the plant extracts showed the presence of carbohydrates, flavonoids, ketose sugars, steroids, reducing sugars and tannins. The ethanolic extract of C. rotundus exhibited the highest activity against A. niger, E. coli and S. aureus. No extract was active against C. albicans. From these findings, it was concluded that C. rotundus is a potential source of bioactive compounds for new drugs upon isolation and purification for treating infections caused by these pathogens.


2020 ◽  
Vol 16 ◽  
Author(s):  
Adinath D. Badar ◽  
Shubham M. Sulakhe ◽  
Mahesh B. Muluk ◽  
Naziya N. M. A. Rehman ◽  
Prashant P. Dixit ◽  
...  

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.


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