scholarly journals Derivatives of 3-Aminopyrazine-2-carboxamides: Synthesis, Antimicrobial Evaluation, and in Vitro Cytotoxicity

Molecules ◽  
2019 ◽  
Vol 24 (7) ◽  
pp. 1212 ◽  
Author(s):  
Ghada Bouz ◽  
Lucia Semelková ◽  
Ondřej Janďourek ◽  
Klára Konečná ◽  
Pavla Paterová ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Three Dimensional ◽  
Cancer Cell Line ◽  
Antimycobacterial Activity ◽  
In Vitro Cytotoxicity ◽  
Antibacterial And Antifungal Activities ◽  
Alkyl Derivatives ◽  
Current Series

We report the design, synthesis, and in vitro antimicrobial activity of a series of N-substituted 3-aminopyrazine-2-carboxamides with free amino groups in position 3 on the pyrazine ring. Based on various substituents on the carboxamidic moiety, the series is subdivided into benzyl, alkyl, and phenyl derivatives. The three-dimensional structures of the title compounds were predicted using energy minimization and low mode molecular dynamics under AMBER10:EHT forcefield. Compounds were evaluated for antimycobacterial, antibacterial, and antifungal activities in vitro. The most active compound against Mycobacterium tuberculosis H37Rv (Mtb) was 3-amino-N-(2,4-dimethoxyphenyl)pyrazine-2-carboxamide (17, MIC = 12.5 µg/mL, 46 µM). Antimycobacterial activity against Mtb and M. kansasii along with antibacterial activity increased among the alkyl derivatives with increasing the length of carbon side chain. Antibacterial activity was observed for phenyl and alkyl derivatives, but not for benzyl derivatives. Antifungal activity was observed in all structural subtypes, mainly against Trichophyton interdigitale and Candida albicans. The four most active compounds (compounds 10, 16, 17, 20) were evaluated for their in vitro cytotoxicity in HepG2 cancer cell line; only compound 20 was found to exert some level of cytotoxicity. Compounds belonging to the current series were compared to previously published, structurally related compounds in terms of antimicrobial activity to draw structure activity relationships conclusions.

scholarly journals Synthesis and Characterization of Some 5-Acetylbarbituric Based Thiosemicarbazone Derivatives

Proceedings ◽  
2019 ◽  
Vol 41 (1) ◽  
pp. 10
Author(s):  
Alfonso Castiñeiras ◽  
Nuria Fernández-Hermida ◽  
Isabel García-Santos ◽  
Lourdes Gómez-Rodríguez
Keyword(s):  
Three Dimensional ◽  
Cancer Cell Line ◽  
In Vitro Cytotoxicity ◽  
Molecular Structures ◽  
Ethyl Sulfate ◽  
X Ray Crystallography ◽  
Elemental Analyses ◽  
Ft Ir

A new series of 5-acetylbarbituric based thiosemicarbazones named 5-acetylbarbituric hydrazine-1-carbothioamide (Acb4NDH, 1), N-methyl-(5-acetylbarbituric)hydrazine- 1-carbothioamide (Acb4NM, 2), N-ethyl-(5-acetylbarbituric)hydrazine-1-carbothioamide (Acb4NE, 3), N,N-dimethyl-(5-acetylbarbituric)hydrazine-1-carbothioamide (Acb4NDM, 4), N′-piperidine- (5-acetylbarbituric)-1-carbothiohydrazide (Acb4Npip, 5) and N′-hexamethyleneimine- (5-acetylbarbituric)-1-carbothiohydrazide (Acb4Nhexim, 6), has been synthesized from 5-acetylbarbituric acid and N-unsubstituted/substituted thiosemicarbazides. The synthesized compounds were well characterized by elemental analyses, FT-IR, 1H, 13C NMR and mass spectroscopic methods. Three-dimensional molecular structures of three compounds (1, 2 and 6) and of N,3-dimethyl-4-(5-(methylamino)-1,3,4λ4-thiadiazol-2-yl)-5-oxo-2,5-dihydro-1H-pyrazole- 1-carbothioamide ethyl sulfate salt (7) were determined by single crystal X-ray crystallography. The compounds were evaluated for their in vitro cytotoxicity against HeLa-229 cancer cell line.

scholarly journals An In Vitro Study on the Antimicrobial Properties of Essential Oil Modified Resin Composite against Oral Pathogens

Materials ◽  
2020 ◽  
Vol 13 (19) ◽  
pp. 4383
Author(s):  
Barbara Lapinska ◽  
Aleksandra Szram ◽  
Beata Zarzycka ◽  
Janina Grzegorczyk ◽  
Louis Hardan ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Antifungal Activity ◽  
Antimicrobial Agents ◽  
Resin Composite ◽  
Antimicrobial Properties ◽  
In Vitro Study ◽  
Diffusion Method ◽  
Oral Pathogens

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.

scholarly journals SYNTHESIS AND CHARACTERIZATION IN VITRO ANTIMICROBIAL AND CYTOTOXICITY TESTING OF OXALIC ACID-DERIVED CADMIUM CHELATING AGENTS

2018 ◽  
Vol 10 (7) ◽  
pp. 80
Author(s):  
Daisy Selasteen F ◽  
Alfred Cecil Raj S ◽  
Alagappa Moses A
Keyword(s):  
Antimicrobial Activity ◽  
Silica Gel ◽  
Optical Conductivity ◽  
Cancer Cell Line ◽  
Uv Spectra ◽  
Diffusion Method ◽  
Spectral Studies ◽  
Cervical Cancer Cell Line ◽  
Cell Line Hela

Objective: The aim of this study is to investigate the growth, structure, spectral, solubility and biological activity of sodium cadmium oxalate dehydrate (NaCdOx) and cadmium oxalate trihydrate (CdOx) crystals prepared by a single diffusion method in the silica gel medium.Methods: The present crystals were grown using single diffusion methods and tested for XRD, UV absorption (190 to 1100 mm) and solubility (distilled water at 20-29 °C) studies. The antimicrobial efficacy of the grown samples at various concentrations (25, 50, 75 and 100 μg/ml) was studied against Streptococcus, (G+Ve), Pseudomonas aeruginosa (G-Ve) and Candida albicans (antifungal). The cytotoxicity evolution was carried out against human cervical cancer cell line (HeLa) using MTT assays.Results: The existing single crystals were successfully grown by silica gel technique. The solubility of sodium cadmium oxalate dehydrate (NaCdOx) was moderately good in deionized warm water. The FTIR spectral studies confirmed the chelating bands of the present samples and UV spectra showed the better the optical conductivity of as-grown crystals. The complexes showed good antimicrobial activity against all tested microbial strains and they exhibited a decrease in cytotoxicity activity.Conclusion: The gel method was suitable to grow metal complexes of legend crystals. The modification of structural properties of cadmium oxalate trihydrate (CdOx) by sodium doping was much improved the solubility, anticancer, antimicrobial activity and polarization by the high optical conductivity of sodium cadmium oxalate dehydrate (NaCdOx) compound. Hence sodium cadmium oxalate dehydrate (NaCdOx) might be a candidate for biomedical applications. 

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 A new group of compounds derived from 4-, 5-, 6- and 7-aminoindoles with antimicrobial activity

2018 ◽  
Vol 4 (3) ◽  
pp. 27-36 ◽  
Author(s):  
Irina Stepanenko ◽  
Semen Yamashkin ◽  
Yuliya Kostina ◽  
Alyona Batarsheva ◽  
Mikhail Mironov
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Antibiotic Resistance ◽  
Biologically Active ◽  
Diffusion Method ◽  
Significant Activity ◽  
Clinical Strains ◽  
Causative Agents ◽  
New Compounds

Introduction. The problem of antibiotic resistance of microorganisms is becoming more urgent in the twenty-first century. Microorganisms possess an evolutionary adaptive capacity. Non-adherence to the basic principles of rational antibiotic therapy leads to menacing consequences. More and more pathogenic microbes are becoming resistant to two or more antibiotics. The search for new compounds with antimicrobial activity is one of the principles for overcoming the antibiotic resistance of microorganisms. Materials and methods. Eighteen test-strains of microorganisms and more than 2000 clinical strains of microorganisms, representating the families Micrococcaceae, Streptococcaceae, Enterobacteriaceae, Moraxellaceae, Pseudomonadaceae, Sphingomonadaceae, Xanthomonadaceae were studied for sensitivity to the compounds derived from 4-, 5-, 6- and 7-aminoindoles. A method of serial dilutions to determine the minimal inhibitory concentration (MIC) of the compounds under study was used in the study, as well as a disc diffusion method. Results and discussion. Sensitivity of the test-strains and of clinical strains of microorganisms to the resulting compounds was studied. The compounds based on substituted 4-, 5-, 6-, 7-aminoindoles showed different activity against the test strains and experimental strains of microorganisms in vitro. It was found that the marked antibacterial activity was exhibited by the compounds containing a trifluoromethyl group. The most significant activity was noted in amides and pyrroloquinolones based on 4-aminoindole, 6-aminoindole and 7-aminoindole.The most effective compounds with laboratory codes 5D, 7D, 39D, S3, HD, 4D showed a pronounced antibacterial activity. Conclusion. Antimicrobial activity of the substituted amides and pyrroloquinolines on the basis of 4-, 5-, 6-, 7-aminoindoles was etermined in our study, as well as the spectra of their action against Gram-positive and Gram-negative microorganisms, which are causative agents of non-specific and certain specific human infectious diseases. Moreover, we evaluated the synthetic potentials of the substituted 4-, 5-, 6-, 7-aminoindoles as the starting compounds for synthesizing a series of indolylamides and pyrroloquinolines. Also, the prospects for targeted synthesis of biologically active compounds based on indole-type aromatic amines were determined.

Synthesis and in vitro cytotoxicity evaluation of ruthenium polypyridyl-sensitized paramagnetic titania nanoparticles for photodynamic therapy

RSC Advances ◽  
2016 ◽  
Vol 6 (53) ◽  
pp. 47520-47529 ◽  
Author(s):  
Mohammad H. Sakr ◽  
Najeeb M. Halabi ◽  
Leen N. Kalash ◽  
Sara I. Al-Ghadban ◽  
Mayyasa K. Rammah ◽  
...  
Keyword(s):  
A549 Cells ◽  
Cancer Cell Line ◽  
In Vitro Cytotoxicity ◽  
Lung Cancer Cell Line ◽  
Titania Nanoparticles ◽  
Human Lung Cancer ◽  
Type I ◽  
Dye Sensitized ◽  
Photo Dynamic Therapy

We demonstrate the effective cytotoxic properties of a dye-sensitized metal oxide in an in vitro model of a human lung cancer cell line (A549 cells) upon light irradiation, where a type I mechanism photo-dynamic therapy is realized exclusively.

Sign in / Sign up

Export Citation Format

Share Document