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

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.

2009 ◽  
Vol 63 (5) ◽  
Author(s):  
Gülşah Kurt ◽  
Fatih Sevgi ◽  
Bedrettin Mercimek

AbstractIn this study, new benzoylthiourea derivatives, (E)-N-[(2-benzamidomethyleneamino)ethylcarbamothioyl]benzamide H3L′, N-(1-(3-benzoylthioureido)propan-2-ylcarbamothioyl)-benzamide H4L″, (E)-N-[4-(benzamidomethyleneamino)phenylcarbamothioyl]benzamide H3L‴, were synthesized. Structures of the compounds were identified by spectroscopic techniques. In addition, all synthesized compounds were evaluated for in vitro antibacterial and antifungal activity. Compound H3L‴ exhibited antibacterial activity.


2015 ◽  
Vol 80 (7) ◽  
pp. 839-852 ◽  
Author(s):  
Nina Bozinovic ◽  
Irena Novakovic ◽  
Sladjana Kostic-Rajacic ◽  
Igor Opsenica ◽  
Bogdan Solaja

A series of new 5H-pyridobenzazepine and pyridobenzothiepine derivatives was synthesized by Pd-catalyzed formation of C-N and C-S bonds. All synthesized compounds were tested for their in vitro antimicrobial activity. The 5H-pyridobenzazepine derivatives showed better antibacterial and antifungal activity than corresponding 5H-dipyridoazepine analogs. Among the synthesized azepines, derivative 8 displayed potent activity against tested bacteria (MIC = 39-78 ?g/mL), while azepine 12 showed promising antifungal activity (MIC = 156-313 ?g/mL). The synthesized thiepine derivatives exhibited weak antibacterial activity, but showed pronounced antifungal activity.


2011 ◽  
Vol 11 (2) ◽  
pp. 148-153
Author(s):  
Hemant Panwar ◽  
Shishupal Singh

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.


2016 ◽  
Vol 5 (04) ◽  
pp. 4512
Author(s):  
Jackie K. Obey ◽  
Anthoney Swamy T* ◽  
Lasiti Timothy ◽  
Makani Rachel

The determination of the antibacterial activity (zone of inhibition) and minimum inhibitory concentration of medicinal plants a crucial step in drug development. In this study, the antibacterial activity and minimum inhibitory concentration of the ethanol extract of Myrsine africana were determined for Escherichia coli, Bacillus cereus, Staphylococcus epidermidis and Streptococcus pneumoniae. The zones of inhibition (mm±S.E) of 500mg/ml of M. africana ethanol extract were 22.00± 0.00 for E. coli,20.33 ±0.33 for B. cereus,25.00± 0.00 for S. epidermidis and 18. 17±0.17 for S. pneumoniae. The minimum inhibitory concentration(MIC) is the minimum dose required to inhibit growth a microorganism. Upon further double dilution of the 500mg/ml of M. africana extract, MIC was obtained for each organism. The MIC for E. coli, B. cereus, S. epidermidis and S. pneumoniae were 7.81mg/ml, 7.81mg/ml, 15.63mg/ml and 15.63mg/ml respectively. Crude extracts are considered active when they inhibit microorganisms with zones of inhibition of 8mm and above. Therefore, this study has shown that the ethanol extract of M. africana can control the growth of the four organisms tested.


Materials ◽  
2020 ◽  
Vol 13 (19) ◽  
pp. 4383
Author(s):  
Barbara Lapinska ◽  
Aleksandra Szram ◽  
Beata Zarzycka ◽  
Janina Grzegorczyk ◽  
Louis Hardan ◽  
...  

Modifying the composition of dental restorative materials with antimicrobial agents might induce their antibacterial potential against cariogenic bacteria, e.g., S.mutans and L.acidophilus, as well as antifungal effect on C.albicans that are major oral pathogens. Essential oils (EOs) are widely known for antimicrobial activity and are successfully used in dental industry. The study aimed at evaluating antibacterial and antifungal activity of EOs and composite resin material (CR) modified with EO against oral pathogens. Ten EOs (i.e., anise, cinnamon, citronella, clove, geranium, lavender, limette, mint, rosemary thyme) were tested using agar diffusion method. Cinnamon and thyme EOs showed significantly highest antibacterial activity against S.mutans and L.acidophilus among all tested EOs. Anise and limette EOs showed no antibacterial activity against S.mutans. All tested EOs exhibited antifungal activity against C.albicans, whereas cinnamon EO showed significantly highest and limette EO significantly lowest activity. Next, 1, 2 or 5 µL of cinnamon EO was introduced into 2 g of CR and microbiologically tested. The modified CR showed higher antimicrobial activity in comparison to unmodified one. CR containing 2 µL of EO showed the best antimicrobial properties against S.mutans and C.albicans, while CR modified with 1 µL of EO showed the best antimicrobial properties against L.acidophilus.


2011 ◽  
Vol 4 (1) ◽  
pp. 22-25 ◽  
Author(s):  
M Bashir ◽  
I Yusuf ◽  
AS Kutama

Five traditional herbal preparations were sampled between May-June, 2009 in Kano. The samples were investigated for invitro antibacterial activities against clinical isolates of Staphylococcus aureus. Likewise, phytochemical screening tests were conducted to determine some of the phytochemicals present in the ethanolic and water extracts of the samples. Various concentrations of the extracts were prepared using serial doubling dilutions (5000=l/ml, 2500=g/ml, 1250=g/ml, 625=g/ml and 312.5=g/ml). All the test extracts showed slight antibacterial activity against the test organism, with ethanolic extract of sample E having the highest zone diameter of inhibition, while sample H had the lowest diameter of inhibition. The standard antibiotic disc (Gentamicin) had demonstrated the highest activity on the test organisms. The results of the Phytochemical screening revealed the presence of steroid in all the samples, tannin in samples A, C, D and E, reducing sugars in sample A, D and E respectively. The result of the minimum inhibitory concentration (MIC) was found to be above 312.5=g/ml for samples C, D and E. Keywords: Staphylococcus aureus, Herbal preparations, antibacterial activity, Phytochemical screening and minimum inhibitory concentration.


2019 ◽  
Vol 31 (4) ◽  
pp. 528-533 ◽  
Author(s):  
Nagarjuna Reddy Desam ◽  
Abdul Jabbar Al-Rajab ◽  
Mukul Sharma ◽  
Mary Moses Mylabathula ◽  
Ramachandra Reddy Gowkanapalli ◽  
...  

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