scholarly journals Microwave Assisted Liquid Phase Synthesis of Benzimidazolo Benzothiophenes for Antimicrobial Activity

2009 ◽  
Vol 6 (s1) ◽  
pp. S25-S32 ◽  
Author(s):  
Deepthi Kini ◽  
Harish Kumar ◽  
Manjunath Ghate

Benzimidazolo benzothiophene derivatives were prepared by liquid phase combinatorial synthesis using soluble polymer support PEG 5000 and 4-fluoro-3-nitrobenzoic acid as starting materials with substituted primary amines. All these synthesized compounds were established by the spectral data and tested for antimicrobial activity against gram positive bacteria,i.e. S. aureus, B. subtilisand gram negative bacteria,E.coliandP.aeruginosaand anti fungal activity againstC. albicans. Ampicillin and ciprofloxacin were used as standard for antibacterial activity and cotrimoxazole for anti fungal activity. Compared with standards compounds(1a-h)showed significant activity against bacterial species and1gshowed significant activity against fungal species.

2020 ◽  
Vol 20 (29) ◽  
pp. 2681-2691
Author(s):  
Athina Geronikaki ◽  
Victor Kartsev ◽  
Phaedra Eleftheriou ◽  
Anthi Petrou ◽  
Jasmina Glamočlija ◽  
...  

Background: Although a great number of the targets of antimicrobial therapy have been achieved, it remains among the first fields of pharmaceutical research, mainly because of the development of resistant strains. Docking analysis may be an important tool in the research for the development of more effective agents against specific drug targets or multi-target agents 1-3. Methods: In the present study, based on docking analysis, ten tetrahydrothiazolo[2,3-a]isoindole derivatives were chosen for the evaluation of the antimicrobial activity. Results: All compounds showed antibacterial activity against eight Gram-positive and Gram-negative bacterial species being, in some cases, more potent than ampicillin and streptomycin against all species. The most sensitive bacteria appeared to be S. aureus and En. Cloacae, while M. flavus, E. coli and P. aeruginosa were the most resistant ones. The compounds were also tested for their antifungal activity against eight fungal species. All compounds exhibited good antifungal activity better than reference drugs bifonazole (1.4 – 41 folds) and ketoconazole (1.1 – 406 folds) against all fungal species. In order to elucidate the mechanism of action, docking studies on different antimicrobial targets were performed. Conclusion: According to docking analysis, the antifungal activity can be explained by the inhibition of the CYP51 enzyme for most compounds with a better correlation of the results obtained for the P.v.c. strain (linear regression between estimated binding Energy and log(1/MIC) with R 2 =0.867 and p=0.000091 or R 2 = 0.924, p= 0.000036, when compound 3 is excluded.


2012 ◽  
Vol 7 (5) ◽  
pp. 941-947 ◽  
Author(s):  
Dario Kremer ◽  
Ivna Müller ◽  
Valerija Dunkić ◽  
Dubravka Vitali ◽  
Edith Stabentheiner ◽  
...  

AbstractChemical composition of the essential oil (analysed by GC-FID and GC-MS), the content of macroelements and trace elements (analysed by ICP-AES), and antimicrobial activities were investigated in Teucrium arduini L. from Mt Biokovo (Croatia). Additionally, a study on the types and distribution of glandular trichomes which produce essential oils was investigated. The oil was characterized by a high concentration of sesquiterpene hydrocarbons (68.5%) of which β-caryophyllene (32.9%) and germacrene D (16.4%) being the major compounds. Among the macroelements, the content of calcium was the highest (9772 mg/kg), while the content of sodium was the smallest (117.74 mg/kg). Among the micronutrients, the most represented element was iron (72.07 mg/kg). The content of each investigated toxic metal (As, Hg, Pb, Cd and Cr) was below permissible levels. The essential oils showed antimicrobial activity against bacterial species tested, with MIC values ranging from 6.25 mg/mL to 37.50 mg/mL. Fungal species were susceptible with MIC values from 7.81 mg/mL and 25.00 mg/mL.


2014 ◽  
Vol 79 (11) ◽  
pp. 1347-1354 ◽  
Author(s):  
Gavrilo Sekularac ◽  
Jasmina Nikolic ◽  
Predrag Petrovic ◽  
Branko Bugarski ◽  
Boban Djurovic ◽  
...  

The isatin derivatives, Schiff bases, were synthesized by the reaction of isatin and various substituted primary amines and characterized by several spectroscopic methods. Investigation of the antimicrobial activity of the synthesized compounds was performed by the agar dilution method, against different strains of bacteria and one fungi. The antioxidative activity of the synthesized compounds was also determined. Some of the compounds have shown the significant activity against the selected strains of microorganisms and the antioxidative activity.


2021 ◽  
pp. 10-15
Author(s):  
Miloud M. Miloud ◽  
Najma A. Senussi

The present study was aimed to investigate the antimicrobial potential of leaf extracts of Euphorbia paralias and Melilotus sulcatus against four bacterial species Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli and Klebsiella sp. and two fungal species Asperigillus niger and Aspergillus flavus. The agar well diffusion assay was used to evaluate the antimicrobial activity. The effect of these extracts was most effective against the bacterial species compared to the fungal species at a used concentration (100 mg/ml). Methanolic extracts of selected plants displayed good antimicrobial activity against all tested microorganisms species, while, no activity for aqueous extracts against tested fungal species. Methanolic extracts were the most effective plant extracts against all tested bacterial species, with MIC and MBC reached 6.2 and 12.5 mg/ml, except Klebsiella sp. which was less sensitive to M. sulcatus methanolic extract and its MIC and MBC reached 12.5 and 25 mg/ml, respectively. These plant extracts which proved to be potentially effective can be used as bioactive agents to control microorganisms caused for diseases and they can be used naturally in the human and veterinary healthcare systems.


2016 ◽  
Vol 2 (5) ◽  
pp. 109
Author(s):  
Sailaja V. ◽  
Madhu M. ◽  
Neeraja V.

In the present study aqueous, acetone, petroleum ether and chloroform solvents extracts of 6 selected plant seeds (Acacia catechu, Sida cordifolia, Momordica fotida, Albiziz procera, Mesua ferrea and Lantana camare ) are screened for their anti-fungal potential against 4 important fungal species(Candida albicans, Cryptococcus luteotus, Aspergillus niger and Mucor heimalis). Among the six plant seed extracts tested, petroleum ether and acetone extracts showed highest to moderate levels of anti-fungal activity when compared to standard anti-fungal drugs (fluconazole(1mg/ml) and Amphotericin B (150 Units/disc).). The chloroform extracts of Albizia procera seed extract failed to inhibit the growth of Candida and Cryptococcus species. Among the solvent extracts tested, petroleum ether recorded highest significant anti-fungal activity when compared to aqueous, chloroform and acetone extracts.


2020 ◽  
Vol 18 ◽  
Author(s):  
Faheem Hadi ◽  
Tahir Maqbool ◽  
Sameera Khurshid ◽  
Aisha Nawaz ◽  
Saira Aftab ◽  
...  

Background: Fungal infections have always remain a problem and they are getting worse with passage of each year due to their resistance against available antibiotics. Natural ways of treatment with homoeopathic medicines made of mother tinctures of plants have no reported side effects and have been proved effective against many bacterial and fungal infections. Materials & Methods: Preparation of mother tinctures of plants Cressa cretica, Leptadenia pyrotechnica and Pulicaria crispa was done and used to evaluate the anti-fungal potential of these plants against potentially pathogenic fungal species like Aspergillus niger, Aspergillus flavus, Aspergillus ustus and Candida albicans by agar disc diffusion method. Each tincture was evaluated at 0.25 ml, 0.5 ml and 1 ml volume per disc and zone of inhibition was measured in millimetres and compared with commercial drug Fluconazole (2 mg/ml) which was used as standard. Results: The results showed that satisfactory anti-fungal activity of these plants in comparison to standard drug Fluconazole. The ratio of antifungal activity of Cressa cretica measured as the zone of growth inhibition of these cultures against Aspergillus niger, Aspergillus flavus, Aspergillus ustus and Candida albicans was 24 mm / 27 mm, 30mm / 28 mm, 23 mm/ 30 mm and 32 mm/ 30 mm respectively. In the case of Leptadenia pyrotechnica, the mother tincture’s antifungal activity was 32 mm / 27 mm, 30 mm / 28 mm, 17 mm/ 30 mm and 24 mm/ 30 mm. In case of our third plant Pulicaria crispa, antifungal activity came out to be 23 mm/ 27 mm, 26 mm/ 28 mm, 26 mm / 30 mm and 24 mm/ 30 mm. Conclusion: Our study proved that mother tincture of these plants can be a potential new therapy to treat fungal infections and has the potential to rule out fungal problems. Further research using mother tincture of these plants against other fungal species has the potential to prove them a safer and widespread anti-fungal homoeopathic medicine.


2011 ◽  
Vol 322 ◽  
pp. 160-163
Author(s):  
Yin Lu ◽  
Hong Chen

A medicinal wild kiwi in China, Actinidia valvata Dunn, has been well known for its activities against leprosy and cancers. The compositions and the antimicrobial activity of its leaf oil were reported for the first time. The oil obtained by hydrodistillation and analyzed by GC and GC-MS, was characterized by the high content of monoterpenes. Linalool (48.14%) is the major component identified, followed by 1,2-dimethyl-lindoline (7.94%), linolenic acid methylester (6.57%) and (E)-phytol (5.29%). The antimicrobial activity of the oil was evaluated against four bacterial and three fungal species. The results showed that it exhibited a mild antibacterial activity against two Gram-positive bacteria (Staphylococcus aureus and Bacillus subtilis), a significant activity against Gram-negative bacteria (Escherichia coli), and no activity on Pseudomonas aeruginosa. The test fungi were more sensitive to the oil, with a MIC range of 0.78~1.56 μL/mL than bacteria in the range which were significantly higher from 0.78 to 25.50 μL/mL.


2005 ◽  
Vol 2 (1) ◽  
pp. 86-90
Author(s):  
C. D. Shelat ◽  
R. T. Vashi

A new quinazolinone derivative namely 2-(4-phenylpiperazinyl)methyl-3-(8-quinolinol-5-yl)- 4(3h)-quinazolinone(HL) was prepared and characterized. Various transition metal (Cu2+, Co2+, Ni2+, Zn2+, Mn2+) chelates of HL were prepared and characterized by metal ligand (M:L) ratio, IR and reflectance spectral studies, magnetic moment, and antimicrobial activity.


Author(s):  
Nurliana Nurliana ◽  
Mirnawati Sudarwanto ◽  
Lisdar I. Sudirman ◽  
Angelina W. Sanjaya

Antimicrobial activity of pliek u crude extracts was evaluated against five bacterial species (Staphylococcus aureus, Bacillus cereus, Escherichia coli, Salmonella enterica serovar Enteritidis and Pseudomonas aeruginosa,)and one fungal species (Candida albicans). Pliek u has been consumed as spices and hot sauce and poultry feed. These foods were collected from household industry at Reudep village in Aceh Besar, Province of Aceh. The ethanol extract of pliek u were obtained by standard method. The antimicrobial activity was detected using paper disc method. The concentration of ethanol crude extract of pliek u (EEP) was determined with the dilution method. The lethality initial test has been detected by using Artemia salina L. bioassay to determine the toxic concentration based on the LC value of EEP. The ethanol crude extract (EEP) was active against all microbial strains. EEP showed 50 antimicrobial activity at a minimum inhibitory concentration (MIC) and a minimum microbicidal concentration (MMC) at 2.5-10 mg/ml and 10-20 mg/ml, respectively. The lethality concentration EEP gave the LC value of 3.36 50 mg/ml. It was concluded that ethanol crude extract (EEP) shows significant antimicrobial activity and it is not toxic.


Author(s):  
Hitesh Makwana ◽  
Yogesh T. Naliapara

Some new N’-benzylidene-5-bromothiophene-2-carbohydrazide derivatives possessing thiophene nucleus were synthesized and characterized by IR, NMR and mass spectral analysis. All synthesized compounds were screened for antimicrobial activity using cup plate method. All the compounds showed moderate to good antimicrobial activity and anti fungal activity


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