scholarly journals An Efficient Approach to the Synthesis of Novel Oxazolidinones as Potential Antimicrobial Agents

2013 ◽  
Vol 2013 ◽  
pp. 1-5 ◽  
Author(s):  
Kavita Devi ◽  
Yumna Asmat ◽  
Sonika Jain ◽  
Swapnil Sharma ◽  
Jaya Dwivedi

Oxazolidinone, either mononuclear or condensed with other heterocyclics, has established its importance in medicinal chemistry. A variety of biological activities have been reported by oxazolidinone derivatives. The present work describes the synthesis of several oxazolidinone derivatives, 3-(2-(7-chloroquinoline-4-ylamino)ethyl)-2-imino-5-(4-chloro/nitro/methoxy benzylidene)oxazolidin-4-one 4(a–c) and 4-(2-(7-chloroquinolin-4-ylamino)ethyl)-2(4-chloro/nitro/methoxy-benzylidene)-1,6-diox-4,9-di-azaspiro[4,4]nonane-3,8-dione 5(a–c). Synthesized compounds (1, 3, 4a, 5a, and 5c) were screened against bacterial strains such asS. aureus(MTCC 96) andE. coli(MTCC119) and fungal strainsA. niger(MTCC 1344) andC. albicans(MTCC 871) compared with penicillin for bacteria and fluconazole for fungi as reference drugs by disk diffusion method. All synthesized compounds were identified by the means of IR, NMR, and MS.

INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (07) ◽  
pp. 5-9
Author(s):  
R. G Ingle ◽  
◽  
S. J. Wadher

A set of ten new 2,3-diphenyl-6-sulfonamido quinoxaline derivatives was synthesized and screened for antimicrobial activity by disk diffusion method. Test derivatives R3, R5, R’’1 and R’’2 show promising results against bacterial strains S. aureus gram positive and E. coli gram negative organism with the concentration 1000 μg/mL in disk diffusion method. Rest of the derivatives show sensitivity against the same organisms. All the synthesized derivatives were confirmed by their spectral data.


2020 ◽  
Vol 13 (2) ◽  
pp. 290-295
Author(s):  
Meki Boutaiba Benklaouz ◽  
Hebib Aggad ◽  
Qada Benameur

Background and Aim: Escherichia coli can cause a number of serious infections both in human and veterinary medicine. Their management is increasingly complicated by the emergence and dissemination of multiresistance to various first-line antimicrobial agents. This study aimed to evaluate the resistance level to the commonly used antibiotics, with a focus on the first-line antimicrobial agents, in E. coli strains isolated from poultry in Western Algeria. Materials and Methods: E. coli culture was done on MacConkey agar and their identification was determined by AP20E system. For susceptibility testing, disk diffusion method to 14 antimicrobials, including first-line antibiotics, was used according to Kirby–Bauer disk diffusion method in Mueller-Hinton agar and the results were interpreted according to the Clinical and Laboratory Standards Institute guidelines. E. coli isolates were considered as multidrug resistance (MDR) when found resistant to at least one antimicrobial agent of three different families of antibiotics. Double-disk synergy and combination disk tests were used for initial screening and confirmation for extended-spectrum β-lactamases (ESBLs) production, respectively. Results: A total of 145 E. coli strains were isolated in this study. High resistance levels to various antibiotics, including commonly used first-line antimicrobial agents, were recorded in this study. The highest resistance level was observed against nalidixic acid (90.34%, n=131), followed by tetracycline (86.89%, n=126), ampicillin (82.75%, n=120), enrofloxacin (80.68%, n=117) and neomycin (80.68%, n=117), trimethoprim/sulfamethoxazole (73.79%, n=107), norfloxacin (72.41%, n=105) and cephalothin (72.41%, n=105), amoxicillin/clavulanic acid (51.72%, n=75), chloramphenicol (22.75%, n=33), nitrofurantoin (17.24%, n=25), gentamicin (13.10%, n=19), and ceftiofur (3.44%, n=5). Moreover, resistance to multiple first-line antibiotics was also demonstrated in the present study. Overall, 139 out of 145 isolates (95.86%) demonstrated MDR (resistant to at least three antibiotics). In addition, five E. coli isolates (3.44%) were confirmed to be ESBL producers. Conclusion: The alarming rate of E. coli resistant to multiple first-line antibiotics in poultry demands intensified surveillance. These results call for taking drastic measures to preserve antibiotic effectiveness and reduce the emergence risks of extensively drug-resistant and pandrug-resistant E. coli isolates.


Author(s):  
Ganesamoorthy Thirunarayanan ◽  
R. Senbagam ◽  
M. Rajarajan ◽  
V. Manikandan ◽  
S. Balaji ◽  
...  

A series of ten substituted (E)-2-benzylidene-N-methylhydrazinecarbothioamides were synthesized from 4-methyl-3-thiosemicarbazide with substituted benzaldehydes. All the synthesized compounds were in good agreement with elemental and spectral data (UV, FT-IR, 1H NMR and 13C NMR). The assigned UV λmax (nm), IR νC=N (cm-1), NMR δ1H (ppm) CH=N and δ13C (ppm) C=N spectral data of (E)-2-benzylidene-N-methylhydrazinecarbothioamides correlated with Hammett constants using single and multi-regression analysis. From the results of correlation analysis substituent effects on the spectral data have been discussed. The antibacterial activity of (E)-2-benzylidene-N-methylhydrazinecarbothioamides have been studied with three Gram-positive pathogenic bacterial strains namely (B. subtilis, S. aureus and S. pyogens) and two Gram-negative strains (E. coli and P. aeruginosa). The antifungal activity of (E)-2-benzylidene-N-methyl hydrazones studied with three fungal species (A. flavus, A. niger, T. viride) using disk diffusion method. 


2015 ◽  
Vol 65 (4) ◽  
pp. 538-547 ◽  
Author(s):  
Valentina Urumova

AbstractThe aim of this study was to describe the prevalence of antibiotic resistance to beta-lactams and to evaluate two resistance genesblaTEMandblaOXA-1inEscherichia coliisolates from faeces on six swine farms in the Republic of Bulgaria. A total of 186E. coliisolates from 192 faecal swabs were tested by the disk diffusion method to determine resistance patterns to 11 antimicrobial agents. Resistance to beta-lactams was determined by disk diffusion method, E-test, micro-broth dilution method and PCR. About 40.3% of theE. coliisolates from swine were resistant to ampicillin. The highest resistance was observed inE.coliisolates from weaned pigs to ampicillin – 60.0% and to cephalotin – 45.5 %. TheE. coliisolates resistant to beta-lactams were examined for the presence ofblaTEMandblaOXA-1genes. The most commonblagene identified wasblaTEM, which was found in 92.0% of swine isolates.


2011 ◽  
Vol 2 (1) ◽  
pp. 8
Author(s):  
Ronak Bakhtiari ◽  
Jalil Fallah Mehrabadi ◽  
Hedroosha Molla Agamirzaei ◽  
Ailar Sabbaghi ◽  
Mohammad Mehdi Soltan Dallal

Resistance to b-lactam antibiotics by gramnegative bacteria, especially <em>Escherichia coli (E. coli)</em>, is a major public health issue worldwide. The predominant resistance mechanism in gram negative bacteria particularly <em>E. coli </em>is via the production of extended spectrum beta lactamase (ESBLs) enzymes. In recent years, the prevalence of b-lactamase producing organisms is increased and identification of these isolates by using disk diffusion method and no-one else is not satisfactory. So, this investigation focused on evaluating the prevalence of ESBL enzymes by disk diffusion method and confirmatory test (Combined Disk). Five hundred clinical samples were collected and 200 <em>E. coli </em>isolates were detected by standard biochemical tests. To performing initial screening of ESBLs was used from Disk diffusion method on <em>E. coli </em>isolates. A confirmation test (Combined Disk method) was performed on isolates of resistant to cephalosporin's indicators. Up to 70% isolates exhibited the Multi Drug Resistance phenotype. In Disk diffusion method, 128(64%) <em>E. coli </em>isolates which resistant to ceftazidime and cefotaxime while in Combined Disk, among 128 screened isolates, 115 (89.8%) isolates were detected as ESBLs producers. This survey indicate beta lactamase enzymes are playing a significant role in antibiotic resistance and correct detection of them in phenotypic test by using disk diffusion and combined Disk is essential for accurate recognition of ESBLs.


2007 ◽  
Vol 59 (2) ◽  
pp. 508-512 ◽  
Author(s):  
B.R. Paneto ◽  
R.P. Schocken-Iturrino ◽  
C. Macedo ◽  
E. Santo ◽  
J.M. Marin

The occurrence of toxigenic Escherichia coli in raw milk cheese was surveyed in Middle Western Brazil. Fifty samples of cheese from different supermarkets were analyzed for E.coli. The isolates were serotyped and screened for the presence of verotoxigenic E. coli (VTEC) and enterotoxigenic E. coli (ETEC) by Polymerase Chain Reaction (PCR). The susceptibility to thirteen antimicrobial agents was evaluated by the disk diffusion method. E.coli were recovered from 48 (96.0%) of the samples. The serogroups identified were O125 (6.0%), O111 (4.0%), O55 (2.0%) and O119 (2.0%). Three (6.0%) and 1(2.0%) of the E.coli isolates were VTEC and ETEC, respectively. Most frequent resistance was observed to the following antimicrobials: cephalothin (60.0%), nalidixic acid (40.0%), doxycyclin (33.0%), tetracycline (31.0%) and ampicillin (29.0%).


2019 ◽  
Vol 12 (5) ◽  
pp. 629-637 ◽  
Author(s):  
Sarah Rose Fitzpatrick ◽  
Mary Garvey ◽  
Kieran Jordan ◽  
Jim Flynn ◽  
Bernadette O'Brien ◽  
...  

Background and Aim: Teat disinfection is an important tool in reducing the incidence of bovine mastitis. Identifying the potential mastitis-causing bacterial species in milk can be the first step in choosing the correct teat disinfectant product. The objective of this study was to screen commercial teat disinfectants for inhibition against mastitis-associated bacteria isolated from various types of milk samples. Materials and Methods: Twelve commercially available teat disinfectant products were tested, against 12 mastitis-associated bacteria strains isolated from bulk tank milk samples and bacterial strains isolated from clinical (n=2) and subclinical (n=3) quarter foremilk samples using the disk diffusion method. Results: There was a significant variation (7-30 mm) in bacterial inhibition between teat disinfection products, with products containing a lactic acid combination (with chlorhexidine or salicylic acid) resulting in the greatest levels of bacterial inhibition against all tested bacteria (p<0.05). Conclusion: In this study, combined ingredients in teat disinfection products had greater levels of bacterial inhibition than when the ingredients were used individually. The disk diffusion assay is a suitable screening method to effectively differentiate the bacterial inhibition of different teat disinfectant products.


2008 ◽  
Vol 52 (No. 4) ◽  
pp. 169-174
Author(s):  
M. Holasova ◽  
R. Karpiskova ◽  
S. Karpiskova ◽  
V. Babak ◽  
J. Schlegelova

With a microdilution method, using the commercial diagnostic test Sensititre Susceptibility Plates for Campylobacter MIC (Trek Diagnostic Systems, Cleveland, OH, USA), disk diffusion and agar dilution method, resistance to six antimicrobial agents were examined in a reference strain <i>Campylobacter jejuni</i> ATCC 33560 and 73 thermo-tolerant isolates of <i>Campylobacter</i> spp. For the microdilution method and all tested antimicrobial agents, our determined values of microbiological breakpoints of resistant strains were suggested as the minimum inhibitory concentration (MIC<sub>R</sub>) for ciprofloxacin &ge; 0.5, erythromycin &ge; 4, gentamicin &ge; 4, nalidixic acid &ge; 32 and tetracycline &ge; 4 &mu;g/ml. On the basis of our study results, strains resistant to clindamycin were MIC<sub>R</sub> &ge; 2 &mu;g/ml for the dilution methods and a zone diameter R ≤ 16 mm for the disk diffusion method. Comparison of the results of the resistance examination, a microdilution method and disk diffusion method with the reference agar dilution method, showed that all compared methods yielded identical results with the exception of the resistance determination in erythromycin and nalidixic acid. The errors were mostly the result of the interpretation criteria for MIC<sub>R</sub> of agar dilution method and different conditions of cultivation used. However, the compared methods, provide results comparable with the reference method having greater convenience of measurement.


Author(s):  
Maysa Serpa ◽  
Juliana Amália Fonte Bôa do Nascimento ◽  
Mirian Fátima Alves ◽  
Maria Isabel Maldonado Coelho Guedes ◽  
Adrienny Trindade Reis ◽  
...  

Antimicrobial resistance is a current and important issue to public health, and it is usually associated with the indiscriminate use of antimicrobials in animal production. This study aimed to evaluate the antimicrobial susceptibility profile in bacterial isolates from pigs with clinical respiratory signs in Brazil. One hundred sixty bacterial strains isolated from pigs from 51 pig farms in Brazil were studied. In vitro disk-diffusion method was employed using 14 antimicrobial agents: amoxicillin, penicillin, ceftiofur, ciprofloxacin, enrofloxacin, chlortetracycline, doxycycline, oxytetracycline, tetracycline, erythromycin, tilmicosin, florfenicol, lincomycin, and sulfadiazine/trimethoprim. The majority of isolates were resistant to at least one antimicrobial agent (98.75%; 158/160), while 31.25% (50/160) of the strains were multidrug resistant. Streptococcus suis and Bordetella bronchiseptica were the pathogens that showed higher resistance levels. Haemophilus parasuis showed high resistance levels to sulfadiazine/trimethoprim (9/18=50%). We observed that isolates from the midwestern and southern regions exhibited four times greater chance of being multidrug resistant than the isolates from the southeastern region studied. Overall, the results of the present study showed a great level of resistance to lincomycin, erythromycin, sulfadiazine/trimethoprim, and tetracycline among bacterial respiratory pathogens isolated from pigs in Brazil. The high levels of antimicrobial resistance in swine respiratory bacterial pathogens highlight the need for the proper use of antimicrobials in Brazilian pig farms.


Antibiotics ◽  
2020 ◽  
Vol 9 (7) ◽  
pp. 375
Author(s):  
Vanessa Silva ◽  
Sara Hermenegildo ◽  
Catarina Ferreira ◽  
Célia M. Manaia ◽  
Rosa Capita ◽  
...  

In this study we aimed to characterize antimicrobial resistance in methicillin-resistant Staphylococcus aureus (MRSA) isolated from bloodstream infections as well as the associated genetic lineages of the isolates. Sixteen MRSA isolates were recovered from bacteremia samples from inpatients between 2016 and 2019. The antimicrobial susceptibility of these isolates was tested by the Kirby–Bauer disk diffusion method against 14 antimicrobial agents. To determine the macrolide–lincosamide–streptogramin B (MLSB) resistance phenotype of the isolates, erythromycin-resistant isolates were assessed by double-disk diffusion (D-test). The resistance and virulence genes were screened by polymerase chain reaction (PCR). All isolates were characterized by multilocus sequence typing (MLST), spa typing, staphylococcal chromosomal cassette mec (SCCmec) typing, and accessory gene regulator (agr) typing. Isolates showed resistance to cefoxitin, penicillin, ciprofloxacin, erythromycin, fusidic acid, clindamycin, and aminoglycosides, confirmed by the presence of the blaZ, ermA, ermC, mphC, msrA/B, aac(6’)-Ie-aph(2’’)-Ia, and ant(4’)-Ia genes. Three isolates were Panton–Valentine-leukocidin-positive. Most strains (n = 12) presented an inducible MLSB phenotype. The isolates were ascribed to eight spa-types (t747, t002, t020, t1084, t008, t10682, t18526, and t1370) and four MLSTs (ST22, ST5, ST105, and ST8). Overall, most (n = 12) MRSA isolates had a multidrug-resistance profile with inducible MLSB phenotypes and belonged to epidemic MRSA clones.


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