scholarly journals Design, Synthesis, and Antimicrobial Evaluation of New Annelated Pyrimido[2,1-c][1,2,4]triazolo[3,4-f][1,2,4]triazines

Molecules ◽  
2020 ◽  
Vol 25 (6) ◽  
pp. 1339 ◽  
Author(s):  
Islam H. El Azab ◽  
Nadia A.A. Elkanzi

A series of 34 new pyrimido[2,1-c][1,2,4]triazine-3,4-diones were synthesized and fully characterized using IR, NMR, MS, and microanalytical analysis. In vitro investigation of 12 compounds of this series revealed promising antimicrobial activity of the conjugates 15a and 15f–j that were tagged with electron-withdrawing groups, with sensitivities ranging from 77% to as high as 100% of the positive control. The investigation of antimicrobial activity included Bacillus subtilis ATCC 6633, Staphylococcus aureus ATCC 6535, Pseudomonas aeruginosa ATCC 27853, and Escherichia coli ATCC 8739 (EC), and fungal strains Candida albicans ATCC 10231 and Aspergillus brasiliensis ATCC 16404.

2020 ◽  
Vol 22 (1) ◽  
pp. 43 ◽  
Author(s):  
Т.V. Kharlamova ◽  
R.B. Seidakhmetova ◽  
K.D. Praliyev

The present study is a continuation of the scientific research works for the synthesis of anthraquinonе-containing derivatives with cyclic ring systems by the interaction of 1,2,4-trihydroxyanthraquinone (purpurin) with cyclic carboxylic acid chlorides. Series of purpurin esters containing a saturated cyclic fragment was studied for antibacterial activity about museum strains of microorganisms. The effects of these preparations in vitro about Staphylococcus aureus ATCC 6538, Bacillus subtilis ATCC 6633, Escherichia coli ATCC 25922, Pseudomonas aeruginosa АТСС 27853 and fungus Сandida albicans АТСС 10231 were studied. It has been found that the compounds with the cyclohexane fragment have possess an antimicrobial activity with strains of microorganisms Staphylococcus aureus АТСС 6538 for which the MIC value was 31.25 μg/ml.


2012 ◽  
Vol 13 (1) ◽  
pp. 63
Author(s):  
Taswin Yacob ◽  
Rita Endriani

The benefit and efficacy of ketepeng cina (Senna alata) in the treatment of infection has shown that have antibacterialactivity, inhibiting and killing bacteria that cause infection. The objective of this study was evaluate the antibacterialactivity of ketepeng cina against Staphylococcus aureus dan Escherichia coli in vitro. This study was a laboratoryexperimental research which use completely randomized design with diffusion method. Ethanol extract of Sennaalata leaves devided into 4 doses, i.c. 100, 50, 25 and 12.5. Amoxiclave were used as positive control and aquadestnegative control. The data were analyzed by Analysis of Varian continued with Duncan’s Multiple Range Test. Theresult of this study showed that antimicrobial activity of ethanol extract Senna alata leaves inhibited the growth ofStaphylococcus aureus, but not Escherichia coli. The optimum effect was showed given by the concentration 100at 17.7 mm.


2020 ◽  
Vol 151 ◽  
pp. 15550-15558
Author(s):  
Amégninou Agban ◽  
Yao Hoekou ◽  
Passimna Pissang ◽  
Tchadjobo Tchacondo ◽  
Komlan Batawila

Objectif : L’objectif de ce travail était d’évaluer in vitro l’activité antimicrobienne des extraits de feuilles et tige de Jatropha multifida sur la croissance de Candida albicans, Escherichia coli et Staphylococcus aureus, puis d’évaluer in vivo la toxicité de cette plante. Méthodologie et résultats : Les méthodes de diffusion en milieu gélosé et de microdilution en milieu liquide ont été utilisées pour évaluer l’effet antimicrobien. Une étude en subaigüe était réalisée afin d’explorer les effets toxiques de l’extrait aqueux des feuilles. Les résultats des tests antimicrobiens montrent une activité des extraits de feuilles et tige de J. multifida sur la croissance des souches utilisées avec des diamètres de zones d’inhibition allant de 8 à 25 mm et des concentrations minimales inhibitrices (CMI) variant de 0,039 mg/mL à 1,25 mg/mL à l’exception des souches de E. coli qui sont résistantes aux extraits de la tige. L’administration en subaigüe de l’extrait aqueux des feuilles de J. multifida à la dose de 600 mg/kg entraîne une perte significative de poids chez les souris. Conclusion et applications des résultats : Les extraits aqueux, éthanolique et hydroéthanolique des feuilles et tige de J. multifida possèdent d’activité antimicrobienne et pourraient être utilisés dans le traitement des Candidoses à C. albicans et des infections à S. aureus. Mais l’essai de toxicité subaigüe montre que l’extrait aqueux de la plante serait toxique. Des études toxicologiques approfondies restent donc nécessaires sur ces extraits afin de mieux élucider leur inocuité. Mots-clés : Jatropha multifida, extraits de feuilles et de tige, activités antifongique et antibactérienne, toxicité. Agban et al., J. Appl. Biosci. 2020 Evaluation du potentiel antimicrobien et de la toxicité des extraits de Jatropha multifida Linn, (Euphorbiaceae) 15551 Evaluation of antimicrobial potential and toxicity of Jatropha multifida Linn, (Euphorbiaceae) extracts ABSTRACT Objective: The objective of this study was to evaluate in vitro the antimicrobial activity of leaves and stem of Jatropha multifida extracts against Candida albicans, Escherichia coli and Staphylococcus aureus, and then to evaluate in vivo the toxicity of this plant. Methodology and Results: The agar well-diffusion and the NCCLS broth microdilution methods were used to assess the antimicrobial effect. A subacute study was carried out to explore the toxic effects of the aqueous extract of the leaves. The results of the antimicrobial tests show an activity of the extracts of leaves and stems of J. multifida on the growth of the strains used with diameters of inhibitory zones ranging from 8 to 25 mm and minimum inhibitory concentrations (MIC) varying from 0.039 mg/mL to 1.25 mg/mL exception E. coli strains which are resistant to extracts from the stem. Subacute administration of the aqueous extract of the leaves of J. multifida at a dose of 600 mg/kg leads to a significant loss of weight in the mice. Conclusion and application of findings : The aqueous, ethanolic and hydroethanolic extracts of the leaves and stem of J. multifida have antimicrobial activity and could be used in the treatment of Candidiasis and bacterial infections due respectively to C. albicans and S. aureus. But the subacute toxicity test shows that the aqueous extract of the plant would be toxic. Extensive toxicological studies therefore remain necessary on these extracts in order to better elucidate their safety. Keywords: Jatropha multifida extracts of leaves and stem, antifungal and antibacterial activities, toxicity


Author(s):  
SUNDAR MADASAMY ◽  
SURESH SUNDAN ◽  
LINGAKUMAR KRISHNASAMY

Objective: A simple formulation of cold cream from methanolic extract Caralluma adscendens var. attenuata (MECA) and their antimicrobial activity was tested against various clinical pathogens, namely, Escherichia coli, methicillin-resistant Staphylococcus aureus, vancomycin-resistant Enterococcus faecium, and Candida albicans. Methods: Methanol extract of these plant extract was prepared by the Soxhlet method. We analyzed phytochemical nature of theses plant, and subsequently, a cream was formulated cold-cream C. adscendens var. attenuata (FCA) different concentration such as FCA 50 mg, FCA 100 mg, and FCA 200 mg. In the present study, aimed to the antimicrobial activity of cold cream was measured by agar well diffusion method, and standard antibiotic Neosporin (market available) cream was used as positive control and dummy cold cream (without-MECA) were used as the negative control. Results: Phytochemical screening showed that the plant extracts were found a rich source of secondary metabolites. For more, the efficacy of cold cream from MECA extracts to against the clinical pathogen. Positive control Neosporin and 200 mg FCA cream was a highly significant difference in the zone of inhibition when compared to dummy cream. The 200 mg FCA was activity against Escherichia coli, methicillin-resistant Staphylococcus aureus, vancomycin-resistant E. faecium, and C. albicans highly significantly difference (p<0.05) compared FCA 50 mg and FAC 100 mg creams. Conclusion: The results from this study suggested that the cold cream form base of MECA crude had antimicrobial activity in the different clinical pathogen. They could be used as an alternative source to conventional antimicrobial agents for the treatment of pathological infection.


2020 ◽  
Vol 4 (1) ◽  
pp. 49
Author(s):  
Gracielle Oliveira Sabbag Cunha ◽  
Ana Paula Terezan ◽  
Andreia Pereira Matos ◽  
Marcela Carmen De Melo Burger ◽  
Paulo Cezar Vieira ◽  
...  

This study evaluated the antimicrobial activity of isolated compounds and semisynthetic derivatives from Miconia ferruginata (Melastomataceae) against five microorganisms: Staphylococcus aureus (ATCC 25923), Escherichia coli (ATCC 25922), Bacillus subtilis (ATCC 6623), Pseudomonas aeruginosa (ATCC 15442), and Candida albicans (ATCC 10231). The isomeric mixture of ursolic and oleanolic acids was active against S. aureus (MIC = 250 μg mL-1) and against E. coli, B. subtilis, and P. aeruginosa (MIC = 500 μg mL-1). The flavone 5,6,7-trihydroxy-4’-methoxyflavone and the methyl esters, semisynthetic derivatives of a mixture of ursolic and oleanolic acids, showed no activity against the tested microorganisms. These results suggest that the carboxyl group present in the triterpenes may contribute to antimicrobial activity.


2021 ◽  
Vol 90 (1) ◽  
pp. 2
Author(s):  
Halyna Hryhoriv ◽  
Illia Mariutsa ◽  
Sergiy M. Kovalenko ◽  
Victoriya Georgiyants ◽  
Lina Perekhoda ◽  
...  

Among all modern antibiotics, fluoroquinolones are well known for their broad spectrums of activity and efficiency toward microorganisms and viruses. However, antibiotic resistance is still a problem, which has encouraged medicinal chemists to modify the initial structures in order to combat resistant strains. Our current work is aimed at synthesizing novel hybrid derivatives of ciprofloxacin and norfloxacin and applying docking studies and biological activity evaluations in order to find active promising molecules. We succeeded in the development of a synthetic method towards 1,2,3-triazole-substituted ciprofloxacin and norfloxacin derivatives. The structure and purity of the obtained compounds were confirmed by 1H NMR, 13C NMR, 19F NMR, LC/MS, UV-, IR- spectroscopy. Docking studies, together with in vitro research against Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, Bacillus subtilis ATCC 6633, Pseudomonas aeruginosa ATCC 27853, Candida albicans NCTC 885-653 revealed compounds in which activity exceeded the initial molecules.


2021 ◽  
Vol 10 (13) ◽  
pp. e329101320579
Author(s):  
Alexandre Horácio Couto Bittencourt ◽  
Jaqueline Souza Machado ◽  
Mariana Garcia da Silva ◽  
Braz Antônio Pereira Cosenza

Devido ao aumento da resistência de patógenos humanos e animais aos medicamentos atuais, pesquisas por novos antimicrobianos têm sido incentivadas, principalmente por meio de plantas medicinais. Eugenia uniflora L., conhecida como pitangueira, é popularmente utilizada com diversas funções terapêuticas, justificando estudos nesta espécie. Assim, os objetivos deste estudo foram avaliar a atividade antibacteriana “in vitro” de extratos de folhas e cascas de Eugenia uniflora L. sobre Escherichia coli e Staphylococcus aureus. Para as etapas de triagem fitoquímica e microbiologia, foram utilizadas as metodologias usuais nessas áreas para obtenção dos extratos e avaliação da atividade antibacteriana com uso de controle positivo e negativo. Os resultados obtidos mostraram que no extrato das folhas foi verificada a presença de saponinas, flavonóides, alcalóides e taninos, enquanto na casca foram obtidos apenas saponinas e alcalóides. Os extratos da folha e da casca foram capazes de inibir o crescimento de Stapylococcus aureus apenas, promovendo halos de inibição de meio de 19,4 mm e 14,4 mm, respectivamente. As análises permitiram concluir que os extratos apresentam metabólitos secundários interessantes e de grande potencial antimicrobiano e que esses extratos foram capazes de inibir apenas as cepas de S. aureus, sendo resistentes às cepas de E. Coli.


2020 ◽  
Vol 2 (2) ◽  
pp. 55-64
Author(s):  
Fajrin Noviyanto ◽  
Siti Nuriyah ◽  
Hadi Susilo

The bacteria Staphylococcus aureus are round bacteria that are shaped like a cocci, and are Gram-positive. These bacteria can be found on the skin, genitals, nasal cavity, mouth and around the anus. One of the pharmaceutical products that can maintain skin health and protect the skin is soap. The leaves of noni (M. citrifolia L.) contain various compounds such as flavonoids, tannins, saponins, alkaloids, and triterpenoids which are capable of being antibacterial. This study aims to make a liquid soap formulation from M. citrifolia L. leaf extract and its activity as an antibacterial to S aureus. The leaves of M. citrifolia L. were extracted using 96% ethanol solvent by maceration method until a thick extract was obtained. Soap formulations are made with a concentration of 20% 40% and 60%. Evaluation of soap quality includes organoleptic test, high foam test and pH test. The method of antibacterial testing is carried out in vitro by means of well diffusion. The results on the quality test of the liquid soap formulation showed that the pH and height of the foam had good results and had met the SNI 1996 Standards. From the results showed that formulation III with an extract content of 60% had a large antimicrobial activity with a value of 16.83 mm which was categorized as strong. In positive control (Dettol) 60% antimicrobial activity showed a value of 14.83 mm. The results of statistical tests were carried out by One-Way ANOVA analysis followed by LSD analysis Post hoc, liquid soap extract of M. citrifolia L. had greater antimicrobial potential than the positive control (Dettol).


2021 ◽  
Vol 11 (2) ◽  
pp. 17-22
Author(s):  
Samsuar Samsuar ◽  
Wasinton Simanjuntak ◽  
Hardoko Insan Qudus ◽  
Yandri Yandri ◽  
Dian Herasari ◽  
...  

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