Synthesis of Some Novel Quinolinols with In-vitro Antimicrobial, and Antioxidant Activity

2020 ◽  
Vol 16 (4) ◽  
pp. 514-520
Author(s):  
Marwa A. Sh. Shehab ◽  
Mohamed El-Naggar ◽  
Rabab A. Ismail ◽  
Hala M. El Kafrawy ◽  
Amira Abood ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antioxidant Activity ◽  
Candida Albicans ◽  
Aspergillus Niger ◽  
Mannich Bases ◽  
Klebsiella Pneumonia ◽  
Good Activity ◽  
Penicillium Sp

Background: Amongst the quinolone core structures, 8-hydroxyquinoline (8-HQ or quinolinol) stands out as the greatest frequently used therapeutic moietiy. This includes the most critical molecules in medicinal chemistry. Quinolinol remains a broad-spectrum ligand capable of chelating to a large number of metal ions. Methods: The synthesized quinolinols Mannich bases were screened for their in vitro antimicrobial activity against Staphylococcus aureus (ATTCC 6538), Escherichia coli (ATTCC 7839), Klebsiella pneumonia (ATCC10131). The antifungal activity of the prepared compounds was assessed against Candida albicans (10231), Aspergillus niger and Penicillium sp. The antioxidant activity of the established compounds was assessed by means of α, α-diphenyl-β-picrylhydrazyl (DPPH) free radical scavenging method. Results: The antimicrobial outcomes indicated that all the synthesized compounds excluding 5 and 9b displayed reasonable antibacterial activity against Staphylococcus aureus (ATTCC 6538) and Escherichia coli (ATTCC 7839) with an inhibition zones ranging from 13 to 23 mm. However, in the case of Klebsiella pneumonia (ATCC10131) only compound 6 did not show any activity. The results also indicated that compounds 2b and 3 were the most potent antibacterial compounds against the verified strains with minimum inhibitory concentration (MIC) values ranging from 0.05 to 0.5mg/ml. In the antifungal assay, all compounds showed good activity against Candida albicans (10231) except compounds 5 and 9b. However, in the case of Aspergillus niger and Penicillium sp. only compounds 2b and 3 showed good activity. In the antifungal assay, MIC values for compounds 2b and 3 ranged from 0.25 to 2.5 mg/ml against the specified fungal strains. The antioxidant activity was assessed using the DPPH scavenging activity method. The results indicated that 2b was the most active among all tested compounds, with almost double the antioxidant activity as compared with that of trolox (positive control). Conclusion: In this work, we describe the synthesis of new Mannich bases comprising 8-HQ (1) and its derivative (8). The resulted Mannich bases of type 2 were used in transamination reactions with hydrazine and hydrazine derivatives. The structures of the newly synthesized Mannich bases were confirmed based on the NMR spectroscopic data and elemental analysis. Antimicrobial and antioxidant activities were also assessed.

scholarly journals A Novel Antimicrobial Phenanthrene Alkaloid from Bryopyllum pinnatum

2011 ◽  
Vol 8 (3) ◽  
pp. 1456-1461 ◽  
Author(s):  
Donatus Ebere Okwu ◽  
Fred Uchenna Nnamdi
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Candida Albicans ◽  
Aspergillus Niger ◽  
Ethanolic Extract ◽  
Klebsiella Pneumonia ◽  
Antimicrobial Studies ◽  
Prevention And Treatment ◽  
Kalanchoe Pinnata ◽  
Isolated Compound

Phenenthrene alkaloid identified as 1-ethanamino 7 hex-1-yne-5I-one phenanthrene was isolated from the ethanolic extract of the leaves ofBryophyllum pinnatum(syn. B. calcinum kalanchoe pinnata) a versatile Nigeria medicinal plant. The structure was elucidated using NMR, IR, UV and MS spectral data. Antimicrobial studies showed that the isolated compound successfully inhibitedPsuedomonas aeruginosa, Klebsiella pneumonia, Staphylococcus aureus, Escherichia coli, Candida albicansandAspergillus niger. This result authenticates the use ofbryophyllum pinantumin phytomedicine for disease prevention and treatment of infections.

scholarly journals Paralemnolins X and Y, New Antimicrobial Sesquiterpenoids from the Soft Coral Paralemnalia thyrsoide

Antibiotics ◽  
2021 ◽  
Vol 10 (10) ◽  
pp. 1158
Author(s):  
Abdelsamed I. Elshamy ◽  
Tarik A. Mohamed ◽  
Eman M. Elkady ◽  
Ibrahim A. Saleh ◽  
Ahmed A. El-Beih ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Candida Albicans ◽  
Aspergillus Niger ◽  
Spectroscopic Data ◽  
Soft Coral ◽  
2D Nmr ◽  
Organic Extracts

The organic extracts of the Red Sea soft coral Paralemnalia thyrsoides has led to the identification of two neolemnane-type sesquiterpenoids: paralemnolins X and Y (1, 2). In addition to these newly characterized compounds, ten known metabolites (3–12) were isolated. Previously reported compounds were elucidated by literature comparison of spectroscopic data (1D and 2D NMR as well as MS data). In vitro antimicrobial activity was investigated for compounds (1–12) against Staphylococcus aureus, Escherichia coli, Candida albicans and Aspergillus niger. Compound 5 showed antimicrobial activity against all assayed microorganisms.

scholarly journals In-vitro antimicrobial activity of methanolic and aqueous leaf extracts of Chrysophyllum albidum (African star apple) and Garcinia kola (Bitter kola)

2021 ◽  
Vol 14 (03) ◽  
pp. 249-253
Author(s):  
Nicholas Chinedu Ewelike ◽  
Joy Chinyere Okammadu ◽  
Vincent Ezechukwu Ogwudire ◽  
Raymond Ikechukwu Nnadozie
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Candida Albicans ◽  
Klebsiella Pneumonia ◽  
Leaf Extracts ◽  
Garcinia Kola ◽  
Test Organisms ◽  
African Star Apple

Methanolic and aqueous leaf extracts of Chrysophyllum albidum (African star apple) and Garcinia kola (bitter kola) were studied for in-vitro microbial activity using the disc diffusion technique. The aqueous and methanolic leaf extracts of Chrysophyllum albidum showed antimicrobial activity against Escherichia coli, Staphylococcus aureus and Candida albicans but showed no antibacterial activity against Klebsiella pneumonia. The methanolic leaf extract of Garcinia kola inhibited the growth of Escherichia coli, Staphylococcus aureus and Klebsiella pneumonia while the aqueous extract of the leaf inhibited the growth of Staphylococcus aureus and Escherichia coli. Both methanolic and aqueous leaf extracts of the plant showed no antifungal activity against Candida albicans. The minimum inhibitory concentrations of the leaf extracts of Chrysophyllum albidum ranged from 12.5 mgL-1 to 25 mgL-1 while those of Garcinia kola ranged from 25 mgL-1 to 50 mgL-1. The results obtained suggest that the leaves of these plants can be used in treating diseases caused by the test organisms. The further investigation on the crude extracts would characterize bioactive components of the leaves of Chrysophyllum albidum and Garcinia kola.

scholarly journals Actividad antimicrobiana de cuatro plantas del nor-oriente peruano

2009 ◽  
Vol 12 (1) ◽  
pp. 41-47 ◽  
Author(s):  
Julio R. Ruiz Q. ◽  
Mirtha Roque A.
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Bacillus Subtilis ◽  
Candida Albicans ◽  
Aspergillus Niger ◽  
Staphylococcus Epidermidis ◽  
Microsporum Canis ◽  
Terminalia Catappa

Se investigó la actividad antimicrobiana in vitro de los extractos metanólicos, etanólicos e hidroalcohólicos de cuatro plantas del nor-oriente peruano: Cassia reticulata (planta entera), Ilex guayusa Loes (hojas), Piper lineatum (hojas), y Terminalia catappa (hojas). Las especies fueron recolectadas en el departamento de Cajamarca, excepto Terminalia catappa (Amazonas). La actividad antimicrobiana se evaluó mediante el método de difusión en agar. Los microorganismos utilizados fueron las bacterias Staphylococcus aureus, Staphylococcus epidermidis, Pseudomonas aeruginosa, Bacillus subtilis y Escherichia coli; y los hongos Candida albicans, Aspergillus niger y Microsporum canis. De doce extractos investigados, ocho (67%) presentaron actividad antimicrobiana significativa frente a Staphylococcus aureus y Staphylococcus epidermidis y uno (8%) frente a Escherichia coli. De doce extractos investigados, diez (83%) presentaron actividad significativa frente a Candida albicans, y seis (50%) contra Microsporum canis. Los extractos con la mejor actividad actimicrobiana fueron los tres extractos del Piper lineatum; el extracto hidroalcohólico de Cassia reticulata y el hidroalcohólico de Terminalia catappa.

scholarly journals Novel Diazenyl Containing Phenyl Styryl Ketone Derivatives As Antimicrobial Agents

2018 ◽  
Vol 17 (1) ◽  
pp. 28-38
Author(s):  
L. Sivasankerreddy ◽  
B. Nagamani ◽  
T. Rajkumar ◽  
M.S. Babu ◽  
N.Y. Subbaiah ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Mycobacterium Tuberculosis ◽  
Candida Albicans ◽  
Aspergillus Niger ◽  
Antimicrobial Agents ◽  
Klebsiella Pneumonia ◽  
Spectroscopic Techniques ◽  
Standard Drug ◽  
Chemical Structures

Background: Antibiotics play an important role in the treatment of infections to the humans and at the same time, irrational, frequent prescription of higher antibiotics, change in gene composition of microorganisms are all the reasons behind the development and introduction of new antibiotics against different microorganisms. Objective: In this project, an attempt has been made to synthesize some derivatives of diazenyl containing phenyl styryl ketones and also their in vitro screening was conducted against Mycobacterium tuberculosis, Escherichia coli, Klebsiella pneumonia, Bacillus subtilis, Staphylococcus aureus, Aspergillus niger and Candida albicans. Methods: Ten molecules were synthesized which are diazenyl containing chalcones. 4- aminoacetophenone was diazotised and piperidine was coupled with the formed diazonium chloride. Further, the acetoxy group underwent Claisen-Schmidt condensation with differently substituted aldehydes to form the final compounds- the chalcones. The proposed chemical structures were confirmed by different spectroscopic techniques like FTIR, 1H NMR and Mass spectroscopy. TLC was used to know that the reactants were exhausted and the formation of the product occurred. Sharp melting point of the compounds concludes the purity. Results: The MIC of the compounds 3CP, 3DP, 3EP and 3GP is 20 times the MIC of the standard fluconazole drug against Aspergillus niger. The compound 3GP is as equipotent as the standard drug Pyrazinamide with MIC of 3.12 µg/ml against Mycobacterium tuberculosis. Conclusion: The results are quite promising which on further studies may lead to drug molecules against different microorganisms. Especially, 3EP can be considered as a broad spectrum agent due to its potent activity against different microorganisms like Staphylococcus aureus, Escherichia coli, Klebsiella pneumonia and Candida albicans.

scholarly journals Atividade antimicrobiana in vitro do rizoma em pó, dos pigmentos curcuminóides e dos óleos e dos essenciais da Curcuma longa L.

2008 ◽  
Vol 32 (3) ◽  
pp. 875-881 ◽  
Author(s):  
Lúcia Péret-Almeida ◽  
Cristina da Cunha Naghetini ◽  
Elzíria de Aguiar Nunan ◽  
Roberto Gonçalves Junqueira ◽  
Maria Beatriz Abreu Glória
Keyword(s):  
Escherichia Coli ◽  
Saccharomyces Cerevisiae ◽  
Staphylococcus Aureus ◽  
Bacillus Subtilis ◽  
Candida Albicans ◽  
Aspergillus Niger ◽  
Curcuma Longa ◽  
E Coli ◽  
Salmonella Choleraesuis

Este trabalho teve como objetivo avaliar a atividade antimicrobiana da cúrcuma em pó, da curcumina disponível no comércio, dos pigmentos curcuminóides purificados e dos óleos essenciais da cúrcuma. As amostras foram analisadas quanto aos teores de pigmentos curcuminóides por cromatografia líquida de alta eficiência. O óleo essencial foi também analisado quanto à densidade, índice de refração e perfil das substâncias voláteis por cromatografia gasosa e detector de ionização de chamas. A atividade antimicrobiana in vitro foi determinada pelo método de difusão em ágar com discos de papel estéreis, impregnados com os extratos, sendo os diâmetros dos halos de inibição medidos com paquímetro. Os extratos etanólicos da cúrcuma, da curcumina comercial, e dos pigmentos curcumina e desmetoxicurcumina não inibiram o crescimento de Staphylococcus aureus, Bacillus subtilis, Salmonella choleraesuis, Escherichia coli, Aspergillus niger, Saccharomyces cerevisiae, e Candida albicans. Apenas o extrato etanólico da bisdesmetoxicurcumina apresentou atividade antimicrobiana em relação ao B. subtilis. O óleo essencial da cúrcuma apresentou atividade antimicrobiana para o B. subtilis, S. choleraesuis, E. coli, A. niger e S. cerevisiae, sendo que essa atividade aumentou em função do aumento da concentração. Os halos de inibição, obtidos com o óleo essencial, foram significativos, quando comparados aos respectivos antibióticos tradicionais, cloranfenicol e anfotericina, indicando ser o óleo essencial da cúrcuma um agente antimicrobiano em potencial.

Substituted 4-Formyl-2H-chromen-2-ones: Their Reaction with N-(2,3,4,6-Tetra-Oacetyl- β-D-galactopyranosyl)thiosemicarbazide, Antibacterial and Antifungal Activity of Their Thiosemicarbazone Products

2020 ◽  
Vol 24 (19) ◽  
pp. 2272-2282
Author(s):  
Vu Ngoc Toan ◽  
Nguyen Minh Tri ◽  
Nguyen Dinh Thanh
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Candida Albicans ◽  
Selenium Dioxide ◽  
Antibacterial And Antifungal Activity ◽  
E Coli ◽  
Antibacterial And Antifungal Activities ◽  
Alkyl Ethers ◽  
Antibacterial And Antifungal

Several 6- and 7-alkoxy-2-oxo-2H-chromene-4-carbaldehydes were prepared from corresponding alkyl ethers of 6- and 7-hydroxy-4-methyl-2-oxo-2H-chromen-2-ones by oxidation using selenium dioxide. 6- and 7-Alkoxy-4-methyl-2H-chromenes were obtained with yields of 57-85%. Corresponding 4-carbaldehyde derivatives were prepared with yields of 41-67%. Thiosemicarbazones of these aldehydes with D-galactose moiety were synthesized by reaction of these aldehydes with N-(2,3,4,6-tetra-O-acetyl-β-Dgalactopyranosyl) thiosemicarbazide with yields of 62-74%. These thiosemicarbazones were screened for their antibacterial and antifungal activities in vitro against bacteria, such as Staphylococcus aureus, Escherichia coli, and fungi, such as Aspergillus niger, Candida albicans. Several compounds exhibited strong inhibitory activity with MIC values of 0.78- 1.56 μM, including 8a (against S. aureus, E. coli, and C. albicans), 8d (against E. coli and A. niger), 9a (against S. aureus), and 9c (against S. aureus and C. albicans).

scholarly journals Evaluation du potentiel antimicrobien et de la toxicité des extraits de Jatropha multifida Linn, (Euphorbiaceae)

2020 ◽  
Vol 151 ◽  
pp. 15550-15558
Author(s):  
Amégninou Agban ◽  
Yao Hoekou ◽  
Passimna Pissang ◽  
Tchadjobo Tchacondo ◽  
Komlan Batawila
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Candida Albicans ◽  
Aqueous Extract ◽  
E Coli ◽  
Toxicological Studies ◽  
Jatropha Multifida

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

Synthesis and Antimicrobial Screening of Some Novel 5-Substituted-1,10b-dihydroimidazole[1,2-c]quinazoline Derivatives

2021 ◽  
Vol 14 (2) ◽  
pp. 5406-5411
Author(s):  
Haribhai Rabari ◽  
Hetal Vankar ◽  
Beenkumar Prajapati
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Candida Albicans ◽  
Antifungal Activity ◽  
Aspergillus Niger ◽  
Antifungal Compound ◽  
Bacterial Strains ◽  
Standard Drug ◽  
Quinazoline Derivatives

The emergence of multidrug microbial resistance is the main challenges that the modern scientists have so far been facing in the recent era. In this respect, new series of drug classes having potential to give antimicrobial effect have been synthesized. A new series of 5- substituted-1,10 b-dihydroimidazole[1,2-c]quinazoline derivatives 8a-e have been synthesized and screened for antibacterial activity and antifungal activity. Synthesized derivatives were characterized by IR, MASS and 1H-NMR spectroscopy. Synthesized compounds show good activity, which was comparable to the standard drug and it can be useful for the further clinical study. Antibacterial activity was evaluated against four different pathogenic bacterial strains like Staphylococcus aureus, Enterococcus faecalis, Escherichia coli and Pseudo-monas aeruginosa. Among the screened compounds, 8e show good antibacterial activity against Staphylococcus aureus and Escherichia coli with MIC of 50 and 100 μg/ml respectively. Antifungal activity was evaluated  against two strains of fungi. Among the synthesized derivates, compound 8c was emerged out as the potent antifungal compound against Candida albicans and Aspergillus niger with MIC of 25 μg/ml and 75μg/ml respectively. Compound 8e also shows good antifungal activity with MIC of 50 μg/ml against both Candida albicans and Aspergillus niger. The overall results of this study indicated that  synthesized quinazoline derivatives had the potential to act as an antibacterial and antifungal agent, hence further investigation is warranted.

scholarly journals Pengaruh Pemanasan pada Proses Pembuatan Ekstrak Kulit Buah Manggis (Garcinia mangostana Linn) terhadap Aktivitas Antimikroba

2010 ◽  
Vol 13 (2) ◽  
pp. 46-50
Author(s):  
Dini Kurnia Wisatya ◽  
Purbowatiningrum Ria Sarjono ◽  
Nies Suci Mulyani
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Candida Albicans ◽  
Aspergillus Niger ◽  
Garcinia Mangostana

Telah dilakukan penelitian tentang pengaruh pemanasan pada proses pembuatan ekstrak kulit buah manggis (Garcinia mangostana Linn) terhadap aktivitas antimikroba. Metode yang digunakan adalah metode pemanasan pada proses pembuatan ekstrak kulit buah manggis sedangkan metode cakram kertas dan metode berat kering digunakan pada uji antimikroba. Mikroba yang diuji menggunakan, bakteri Escherichia coli, Staphylococcus aureus, khamir Candida albicans, dan jamur Aspergillus niger. Metode cakram kertas untuk mengidentifikasi aktivitas antimikroba pada bakteri Escherichia coli, Staphylococcus aureus, khamir Candida albicans, sedangkan metode berat kering digunakan untuk identifikasi aktivitas antimikroba dari jamur Aspergillus niger. Konsentrasi Hambat Minimum pada metode cakram kertas pada mikroba bakteri Escherichia coli, Staphylococcus aureus, khamir Candida albicans yaitu 5 % (w/v), dengan rata-rata luas zona hambat masing-masing 0,043 cm2, 0,018 cm2, 0,013 cm2. Sedangkan pada jamur Aspergillus niger pada konsentrasi 0,5% (w/v), dengan berat kering 0,06 gram.

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