scholarly journals Synthesis and Antimicrobial Activity of Novel Benzoxazoles

2012 ◽  
Vol 67 (9-10) ◽  
pp. 466-472 ◽  
Author(s):  
Mustafa Arisoy ◽  
Ozlem Temiz-Arpaci ◽  
Fatma Kaynak-Onurdag ◽  
Selda Ozgen

A series of 2-(p-substituted-benzyl)-5-[[4-(p-chloro/fluoro-phenyl)piperazin-1-yl]ace tamido] -benzoxazoles were synthesized in need of new compounds for the fight against microbial pathogens. Their structures were elucidated by spectral techniques. These new derivatives, along with previously synthesized 2-(p-substituted-benzyl)-5-substituted-benzoxazoles, were evaluated for their antibacterial and antifungal activities against standard strains and drugresistant isolates in comparison with ampicillin, gentamicin sulfate, ofloxacin, vancomycin, fluconazole, and amphotericin B trihydrate. The minimum inhibitory concentration (MIC) of each compound was determined by a two-fold serial dilution technique. The compounds were found to possess a broad spectrum of antimicrobial activities with MIC values of 32 - 256 μg/ml. Although standard drugs were more active against the pathogenes employed in this study, the activities of the new benzoxazoles and reference drugs against drug-resistant isolates of the microorganisms were largely similar

Molecules ◽  
2018 ◽  
Vol 23 (8) ◽  
pp. 2013 ◽  
Author(s):  
Ricardo Murcia ◽  
Sandra Leal ◽  
Martha Roa ◽  
Edgar Nagles ◽  
Alvaro Muñoz-Castro ◽  
...  

In this work, six complexes (2–7) of Cr(III) and Co(II) transition metals with triazole ligands were synthesized and characterized. In addition, a new ligand, 3,5-bis(1,2,4-triazol-1-ylmethyl)toluene (1), was synthesized and full characterized. The complexes were obtained as air-stable solids and characterized by melting point, electrical conductivity, thermogravimetric analysis, and Raman, infrared and ultraviolet/visible spectroscopy. The analyses and spectral data showed that complexes 3–7 had 1:1 (M:L) stoichiometries and octahedral geometries, while 2 had a 1:2 (M:L) ratio, which was supported by DFT calculations. The complexes and their respective ligands were evaluated against bacterial and fungal strains with clinical relevance. All the complexes showed higher antibacterial and antifungal activities than the free ligands. The complexes were more active against fungi than against bacteria. The activities of the chromium complexes against Candida tropicalis are of great interest, as they showed minimum inhibitory concentration 50 (MIC50) values between 7.8 and 15.6 μg mL−1. Complexes 5 and 6 showed little effect on Vero cells, indicating that they are not cytotoxic. These results can provide an important platform for the design of new compounds with antibacterial and antifungal activities.


Molecules ◽  
2018 ◽  
Vol 23 (9) ◽  
pp. 2092 ◽  
Author(s):  
Ibrahim Radini

A novel series of pyrazolyl 1,3,4-thiadiazines 5a–c, 8a–c, 12, 15a–c, 17a–c, and 20 was prepared from the reaction of pyrazole-1-carbothiohydrazide 1a,b with 2-oxo-N′-arylpropanehydrazonoyl chloride, 2-chloro-2-(2-arylhydrazono)acetate, and 3-bromoacetylcoumarin. Moreover, the regioselective reaction of 5-pyrazolone-1-carbothiohydrazide 1a with 4-substituted diazonium salts and 4-(dimethylamino)benzaldehyde gave the corresponding hydrazones 21a–c and 22. The newly prepared compounds were characterized by spectroscopy and elemental analysis. Many new synthesized compounds showed considerable antimicrobial activity against tested microorganisms. Hydrazones 21a–c and 22 showed remarkable antibacterial and antifungal activities. 4-(2-(p-tolyl)hydrazineylidene)-pyrazole-1-carbothiohydrazide 21a displayed the highest antibacterial and antifungal activities with minimum inhibitory concentration (MIC) values lower than standard drugs chloramphenicol and clotrimazole, in the range of 62.5–125 and 2.9–7.8 µg/mL, respectively.


2011 ◽  
Vol 6 (9) ◽  
pp. 1934578X1100600
Author(s):  
Soni A. Singh ◽  
Yogesh A. Potdar ◽  
Rasika S. Pawar ◽  
Sujata V. Bhat

Nine conjugated acid derivatives from monoterpene citral have been synthesized using ester, amide condensations, Wittig, Knoevenagel, Baylis-Hillman reactions and their antimicrobial activities were evaluated through disc diffusion and serial dilution methods. Several derivatives displayed interesting antimicrobial activity. Particularly, the Baylis-Hillman adducts 8-10 were found to have more potent antibacterial and antifungal activities than standard drugs namely chloramphenicol and nystatin respectively.


2010 ◽  
Vol 7 (4) ◽  
pp. 1435-1439 ◽  
Author(s):  
Gopal Krishna Rao ◽  
R. B. Kotnal ◽  
P. N. Sanjay Pai

A series of quinoxaline derivatives was prepared and evaluated for antitubercular, antibacterial and antifungal activities. The title compounds were prepared by condensation of substituted aromatic aldehydes and substituted acetophenones with 2-(3-methyl-2-oxoquinoxalin-1(2H)-yl) acetohydrazide. Structures of all these compounds were confirmed by their spectral studies. Among synthesized compounds (4r, 4t, 4u, 4wand4x) have shown good anti tubercular activity (25 µg mL-1) when compared to reference drugs pyrazinamide (10 µg mL-1) and streptomycin (7.5 µg mL-1). In this study, few derivatives showed broad spectrum of antimicrobial activity at low concentration. The MICs (Minimum inhibitory concentration) of some compounds are 2-4 µg mL-1.


2014 ◽  
Vol 69 (9-10) ◽  
pp. 368-374 ◽  
Author(s):  
Mustafa Arisoy ◽  
Ozlem Temiz-Arpaci ◽  
Fatma Kaynak-Onurdag ◽  
Selda Ozgen

Abstract series of 2-(p-substituted phenyl)-5-(2-{4-[(p-chloro-fluorophenyl)=phenyl] piperazin-1-yl}- acetamido)-benzoxazoles were synthesized and tested for their antimicrobial activities. The structures of the new derivatives were elucidated by spectral techniques. The minimum inhibitory concentrations (MIC) of the new benzoxazoles, along with those of previously synthesized analogues, were determined against standard bacterial and fungal strains and drug-resistant isolates, and compared with those of several reference drugs. The new benzoxazole derivatives were found to possess a broad spectrum of antimicrobial activity with MIC values of 32 - 1024 μg/ml. Although the standard drugs were more active against the tested pathogens, the activities of the new benzoxazoles and the reference drugs were largely similar against the drug-resistant isolates.


2012 ◽  
Vol 58 (1) ◽  
pp. 54-66 ◽  
Author(s):  
Mariana L.A. Vieira ◽  
Alice F.S. Hughes ◽  
Viviane B. Gil ◽  
Aline B.M. Vaz ◽  
Tânia M.A. Alves ◽  
...  

The diversity and antimicrobial activity of endophytic fungi associated with the Brazilian medicinal plant Solanum cernuum Vell. were studied during summer and winter seasons. A total of 246 fungal isolates were obtained, including 225 filamentous fungi and 21 yeasts. They were identified by morphological, physiological, and molecular methods. Fifty-five different taxa represented by the phyla Ascomycota (33 taxa), Basidiomycota (21 taxa), and Zygomycota (one taxon) were identified. The most abundant taxa were closely related to Arthrobotrys foliicola , Colletotrichum gloeosporioides , Coprinellus radians , Glomerella acutata , Diatrypella frostii , Phoma glomerata , Mucor sp., Phlebia subserialis , Phoma moricola , Phanerochaete sordida , and Colletotrichum sp. A total of 265 fungal extracts were screened and 64 (26.01%) displayed antimicrobial activities. Among these extracts, 18 (28.12%) presented antibacterial and antifungal activities, 42 (65.62%) displayed selective antibacterial activity, and four (6.25%) exhibited only antifungal activity. The best values of minimum inhibitory concentration were obtained from extracts of Cryptococcus rajasthanensis , Glomerella acutata, Leptosphaeria sp., and Phoma glomerata ranging from 7.8 to 15.62 µg/mL. This study is the first survey of the endophytic fungi community associated with S. cernuum, and our results show that they can represent a promising source of bioactive compounds.


2020 ◽  
Vol 32 (4) ◽  
pp. 783-788
Author(s):  
Panneerselvam Kalaivani ◽  
Jayaraman Arikrishnan ◽  
Mannuthusamy Gopalakrishnan

A series of tosyl carbamates have been synthesized and screened for their antibacterial and antifungal activities. All the synthesized compounds were characterized by spectral techniques (IR, 1H, 13C NMR and mass) and elemental analysis. in silico Molecular docking method was performed to study their antimicrobial activity against the target protein 1T9U. Compound 27 showed good antibacterial activity against Gram-positive and Gram-negative bacterial strains and compound 19 showed good antifungal activity. Molecular docking results revealed that the compound 19 exhibits minimum CDOCKER energy. Tosyl carbamate derivatives having good antimicrobial activities compared to that standard and all the synthesized compounds exhibits moderate CDOCKER scores.


2011 ◽  
Vol 66 (7-8) ◽  
pp. 340-344 ◽  
Author(s):  
Hanif Shirinzadeh ◽  
Nurten Altanlar ◽  
Nihal Yucel ◽  
Seckin Ozden ◽  
Sibel Suzen

There has been an increasing importance of drug-resistant pathogens in clinical microbiological and antibacterial research. Indoles and hydrazone-type compounds constitute important classes of compounds in the search for effective agents against multidrug-resistant microbial infections. In this study a series of 1-methylindole-3-carboxaldehyde hydrazone derivatives were evaluated for their in vitro antimicrobial activities using the two-fold serial dilution technique against Staphylococcus aureus, methicillin-resistant S. aureus, methicillinresistant S. aureus isolate, Escherichia coli, Bacillus subtilis, and Candida albicans. The minimum inhibitory concentration (MIC) of the test compounds and the reference standards sultamicillin, ampicillin, fluconazole, and ciprofloxacin was determined. All compounds possessed a broad spectrum of activity having MIC values of 6.25 - 100 μg/ml against the tested microorganisms. Aromaticity and disubstitution of the phenyl ring with especially fluorine and chlorine atoms were found to be significant for the antimicrobial activity


1970 ◽  
Vol 24 (1) ◽  
pp. 73-75 ◽  
Author(s):  
M Shafiqur Rahman ◽  
M Nural Anwar

Ethanolic extract of Plumbago zeylanica root was investigated for its antimicrobial activities against 11 human pathogenic bacteria and 6 phytopathogenic fungi using disc diffusion method and poisoned food technique respectively. The extract exhibited good antibacterial and antifungal activities against the test organisms. Among the test bacteria, Vibrio cholerae was found to be the most sensitive to the extract showing the highest diameter of zone of inhibition and lowest minimum inhibitory concentration (MIC) value (200 μg/ml). The extract was also very effective against Escherichia coli and Pseudomonas aeruginosa showing MIC value of 250 μg/ml. Among the phytopathogenic fungi tested, Curvularia lunata exhibited the highest sensitivity to the extract with an MIC value of 150 μg/ml, which was followed next by Colletotrichum corchori and Fusarium equiseti (MIC value 250 μg/ml). The root extract from P. zeylanica seems promising since it showed both antibacterial and antifungal activities.  Keywords: Antimicrobial activity, Plumbago zeylanica, Ethanolic extract, Minimum inhibitory concentration (MIC)DOI: http://dx.doi.org/10.3329/bjm.v24i1.1244  Bangladesh J Microbiol, Volume 24, Number 1, June 2007, pp73-75


2013 ◽  
pp. 333-340 ◽  
Author(s):  
Daniela Nikolovska-Nedelkoska ◽  
Natalija Atanasova-Pancevska ◽  
Haris Amedi ◽  
Dafina Veleska ◽  
Emilija Ivanova ◽  
...  

Regarding the development of novel safe antimicrobials of natural origin, macrofungi became attractive for the researchers in the last decade. In this study, antimicrobial potential of methanolic extracts of six wild macromycetes (Boletus lupinus, Flammulina velutypes, Phellinus igniarius, Sarcodon imbricatus, Tricholoma aurantium, Xerocomus ichnusanus) was evaluated. In vitro antimicrobial activity was investigated by the microdilution method and minimum inhibitory concentration (MIC) was determined. Testing was conducted against eleven microorganisms, including six strains of bacteria and five species of fungi. Extracts showed selective antimicrobial properties while the activities depended both on the species of microorganism and on the type and concentration of extract. The evaluated extracts demonstrated antimicrobial activity, exhibiting more potent inhibitory effects on the growth of bacteria than on fungi. The highest antibacterial and antifungal activity was observed in methanolic extract of polypore fungus P. igniarius.


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