scholarly journals One-Pot Multi Component Microwave Assisted Synthesis of 4H-Pyrano [2, 3-c] Pyrazoles in Methanol and their Antibacterial Study

2021 ◽  
Vol 11 (2) ◽  
pp. 3441-3448

Upon literature studies, pyrano-pyrazoles were found to exhibit the biological activity as antimicrobial agents. So literature employed conventional stirring and reflux condensing to afford different pyrano-pyrazoles. Recent researches adopted the Microwave method, which is a simple and convenient method for organic synthesis. In this work, we reported the synthesis of different 4H-pyrano [2, 3-c] pyrazoles via two different methods, such as microwave & conventional stirring at room temperature. Ethyl acetoacetate, hydrazine hydrate, malanonitrile, and different substituted carbonyl compounds were made to react in the presence of methanol solvent & potassium ter-butoxide, a base catalyst. The microwave method was adopted for all the reactions and found to be more potent than the conventional method. The prepared compounds were characterized by FT-IR, 1HNMR, and 13CNMR. These compounds were screened for anti-bacterial activity against Staphylococcus aureus and E. coli by well diffusion method and showed the excellent antibacterial property. Our In vitro test for antibacterial study involves excellent MIC (µg/ml) and zone inhibition (mm) measurements of all synthesized compounds. Microwave irradiation synthesis hastens the reaction and is completed very fast. Potassium ter-butoxide, a base catalyst, is proved to be a good catalyst for accelerating the reactions. The yield of all synthesized compounds was good. Different 4H-pyrano [2, 3-c] pyrazoles exhibited good potency against Staphylococcus aureus and E. coli. In the presence of a base catalyst, the reactions are faster than in the absence of a catalyst. The microwave method is a good methodology for the green syntheses. Derivatives of 4H-pyrano [2, 3-c] pyrazoles exhibited excellent MIC (µg/ml) and proved to be as good antibacterial agents.

2021 ◽  
Vol 38 ◽  
pp. 20-24
Author(s):  
S.A. Mohamed ◽  
C. Mathew

Resistance against synthetic antimicrobial agents is one of the major global public health challenges that compel scientists to search for alternatives including those of plants origin. Staphylococcus aureus and Escherichia coli are bacteria responsible for a variety of infections and diseases that causes significant morbidity and mortality in humans and animals. E. coli is widely distributed in nature and commonly found in lower gastro intestinal tracts of most warm-blooded animals associated with urinary tract infections and enterocolitis in humans and colibacillosis in poultry. This study was carried out to investigate antimicrobial activity of methanolic leaf extracts of Bidens pilosa against S. aureus and E. coli. Agar well diffusion method was used to assess antimicrobial activity of the leaf extracts at 20%, 50% and 70% concentrations respectively based on measured zone of inhibition. The leaf extracts of Bidens pilosa produced significant zone of inhibition indicating its antimicrobial activity against E. coli and S. aureus. The antimicrobial activity was demonstrated in all concentrations however, the highest zone of inhibition (18.5mm and 32mm) for E. coli and S. aureus respectively was at 70% concentration. The results shows that Bidens pilosa leaf extracts have antimicrobial activity against the tested bacteria and have the potential for further development including identification of active components that can be tested for treatment of E. coli and S. aureus associated conditions.


Author(s):  
Kyoung- Sun Seo ◽  
Seong Woo Jin ◽  
Seongkyu Choi ◽  
Kyeong Won Yun

The antibacterial activity of three Cupressaceae plants (Thujaoccidentalis,ThujaorientalisandChamaecyparisobtusa) was tested against three bacteria using the agar diffusion method. The ether and ethylacetate fraction of crude methanol extract from the three plants showed potent antibacterial activity against the tested microorganisms. The result showed that Staphylococcus aureus revealed the most sensitivity among the tested bacteria. Thujaoccidentalisether fraction and Thujaorientalis hexane fraction exhibited the highest antibacterial activity against Staphylococcus aureus. E. coli was shown the highest MIC values compared to the other two tested bacteria, which indicates the lowest antibacterial activity against the bacterium. This study promises an interesting future for designing a potentially active antibacterial agent from the three Cupressaceae plants.


2014 ◽  
Vol 44 (2) ◽  
pp. 287-290 ◽  
Author(s):  
Carolinie Batista Nobre da Cruz ◽  
Fabio Alessandro Pieri ◽  
Gislene Almeida Carvalho-Zilse ◽  
Patrícia Puccinelli Orlandi ◽  
Carlos Gustavo Nunes-Silva ◽  
...  

Honeys are described possessing different properties including antimicrobial. Many studies have presented this activity of honeys produced by Apis mellifera bees, however studies including activities of stingless bees honeys are scarce. The aim of this study was to compare the antimicrobial activity of honeys collected in the Amazonas State from Melipona compressipes, Melipona seminigra and Apis mellifera against Staphylococcus aureus, Enterococcus faecalis, Escherichia coli, Chromobacterium violaceum, and Candida albicans. Minimum inhibitory concentrations were determined using the agar dilution method with Müller-Hinton agar (for bacteria) or Saboraud agar (for yeast). Staphylococcus aureus and E. faecalis were inhibited by all honeys at concentrations below 12%, while E. coli and C. violaceum were inhibited by stingless bee honeys at concentrations between 10 and 20%. A. mellifera honey inhibited E. coli at a concentration of 7% and Candida violaceum at 0.7%. C. albicans were inhibited only with honey concentrations between 30 and 40%. All examined honey had antimicrobial activity against the tested pathogens, thus serving as potential antimicrobial agents for several therapeutic approaches.


2012 ◽  
Vol 45 (2) ◽  
pp. 189-193 ◽  
Author(s):  
Karinne Spirandelli Carvalho Naves ◽  
Natália Vaz da Trindade ◽  
Paulo Pinto Gontijo Filho

INTRODUCTION: Methicillin-resistant Staphylococcus aureus (MRSA) is spread out in hospitals across different regions of the world and is regarded as the major agent of nosocomial infections, causing infections such as skin and soft tissue pneumonia and sepsis. The aim of this study was to identify risk factors for methicillin-resistance in Staphylococcus aureus bloodstream infection (BSI) and the predictive factors for death. METHODS: A retrospective cohort of fifty-one patients presenting bacteraemia due to S. aureus between September 2006 and September 2008 was analysed. Staphylococcu aureus samples were obtained from blood cultures performed by clinical hospital microbiology laboratory from the Uberlândia Federal University. Methicillinresistance was determined by growth on oxacillin screen agar and antimicrobial susceptibility by means of the disk diffusion method. RESULTS: We found similar numbers of MRSA (56.8%) and methicillin-susceptible Staphylococcus aureus (MSSA) (43.2%) infections, and the overall hospital mortality ratio was 47%, predominantly in MRSA group (70.8% vs. 29.2%) (p=0.05). Age (p=0.02) was significantly higher in MRSA patients as also was the use of central venous catheter (p=0.02). The use of two or more antimicrobial agents (p=0.03) and the length of hospital stay prior to bacteraemia superior to seven days (p=0.006) were associated with mortality. High odds ratio value was observed in cardiopathy as comorbidity. CONCLUSIONS: Despite several risk factors associated with MRSA and MSSA infection, the use of two or more antimicrobial agents was the unique independent variable associated with mortality.


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%).


Author(s):  
Susmita Phattepuri ◽  
Prince Subba ◽  
Arjun Ghimire ◽  
Shiv Nandan Sah

Milk is an excellent medium for the growth of many bacteria. This study aimed to determine antibiotic profiling and thermal inactivation of Staphylococcus aureus and Escherichia coli isolated from raw milk of Dharan. Total viable count, total Staphylococcal count, and total coliform count were carried out by conventional microbiological methods. Identification was done on the basis of Gram staining and biochemical tests. The antibiotic susceptibility test of the isolates carried out by the modified Kirby-Baur disc diffusion method. Thermal inactivation of S. aureus and E. coli were carried out by subjecting to thermal treatment in a water bath. Total plate count ranged from 204×104 CFU/mL to 332×105 CFU/mL. Total staphylococcal count and total coliform count ranged from 14×105 CFU/mL to 8×106 CFU/mL and 11×104 CFU/mL to 3×106 CFU/mL respectively. S. aureus showed an increasing resistance patterns towards Ampicillin, Cefotixin, Carbenicillin and Cefotaxime. Ciprofloxacin, Erythromycin, Amikacin, Gentamycin, Azithromycin, and Chloramphenicol were found to be effective against S. aureus. All the E. coli isolates were resistant to Ampicillin and least resistant to Cefotixin. Chloramphenicol, Amikacin, Azithromycin, and Nalidixic acid were found highly effective to E. coli. The D-values for S. aureus at 56°C, 58°C and 60°C were 1.36 min, 1.19 min, and 1.09 min respectively. The Z-value was 14.92°C. While D-values were obtained as 0.98 min, 0.75 min, and 0.57 min for E. coli at 56° C, 58° C and 60° C respectively, and Z-value was 9.75° C. Hence, S. aureus was found to be more heat resistant than E. coli.


2016 ◽  
Vol 9 (2) ◽  
pp. 15
Author(s):  
Emil Salim ◽  
Hasnirwan ◽  
Sanusi Ibrahim ◽  
Afrizal

Kitooligosakarida-2,5-anhidro-D-mannofuranosa (KOSamf) dipersiapkan dengan derajat polimerisasi tertentu melalui reaksi nitrous deaminasi dari kitosan parsial N-deasetilasi. KOSamf kemudian diubah menjadi turunan KOSamf dengan mengkopling gugus aldehid yang terdapat pada unit 2,5-anhidro-D-mannofuranosa (amf). KOSamf dengan 3,5-dikloroanilin dan NaBH3CN dalam pelarut buffer ammonium asetat direaksikan melalui metoda one-pot aminasi reduktif untuk menghasilkan turunan KOSamf yang berpotensi sebagai senyawa antibakteri dan antijamur. Struktur kimia dari turunan KOSamf yang telah disintesis dikarakterisasi dengan Spektroskopi FT-IR dan NMR. Senyawa turunan KOSamf memiliki aktivitas sebagai antibakteri terhadap bakteri Staphylococcus aureus dengan zona inhibisi 12,5 mm dan bakteri E. coli dengan zona inhibisi 10,5 mm.


2020 ◽  
Vol 28 (2) ◽  
pp. 81
Author(s):  
Raouia Ben Rhouma ◽  
Ahlem Jouini ◽  
Amira Klibi ◽  
Safa Hamrouni ◽  
Aziza Boubaker ◽  
...  

The purpose of this study was to identify <em>Escherichia coli</em> isolates in diarrhoeic and healthy rabbits in Tunisia and characterise their virulence and antibiotic resistance genes. In the 2014-2015 period, 60 faecal samples from diarrhoeic and healthy rabbits were collected from different breeding farms in Tunisia. Susceptibility to 14 antimicrobial agents was tested by disc diffusion method and the mechanisms of gene resistance were evaluated using polymerase chain reaction and sequencing methods. Forty <em>E. coli</em> isolates were recovered in selective media. High frequency of resistance to tetracycline (95%) was detected, followed by different levels of resistance to sulphonamide (72.5%), streptomycin (62.5%), trimethoprim-sulfamethoxazole (60%), nalidixic acid (32.5%), ampicillin (37.5%) and ticarcillin (35%). <em>E. coli</em> strains were susceptible to cefotaxime, ceftazidime and imipenem. Different variants of bla<sub>TEM</sub>, <em>tet</em>, <em>sul</em> genes were detected in most of the strains resistant to ampicillin, tetracycline and sulphonamide, respectively. The presence of class 1 integron was studied in 29 sulphonamide-resistant <em>E. coli</em> strains from which 15 harboured class 1 integron with four different arrangements of gene cassettes, <em>dfrA17</em>+<em>aadA5</em> (n=9), <em>dfrA1</em> + <em>aadA1</em> (n=4), <em>dfrA12</em> + <em>addA2</em> (n=1), <em>dfrA12</em>+<em>orf</em>+<em>addA2</em> (n=1). The <em>qnrB</em> gene was detected in six strains out of 13 quinolone-resistant <em>E. coli</em> strains. Seventeen <em>E. coli</em> isolates from diarrhoeic rabbits harboured the enteropathogenic eae genes associated with different virulence genes tested (<em>fimA</em>, <em>cnf1</em>, <em>aer</em>), and affiliated to B2 (n=8) and D (n=9) phylogroups. Isolated <em>E. coli</em> strains from healthy rabbit were harbouring <em>fim A</em> and/or <em>cnf1</em> genes and affiliated to A and B1 phylogroups. This study showed that <em>E. coli</em> strains from the intestinal tract of rabbits are resistant to the widely prescribed antibiotics in medicine. Therefore, they constitute a reservoir of antimicrobial-resistant genes, which may play a significant role in the spread of antimicrobial resistance. In addition, the eae virulence gene seemed to be implicated in diarrhoea in breeder rabbits in Tunisia.


2016 ◽  
Vol 6 (2) ◽  
pp. 70-76
Author(s):  
Soumia Keddari ◽  
Narimen Benaoum ◽  
Yasmina Mokhtaria Boufadi ◽  
Mansouria Belhocine ◽  
Ali Riazi

Medicinal plants have been used for countries as cures for human diseases because they contain components of therapeutic value. Among these medi-cinal plants, Ammi visnage which have an immense reservoir of potential compounds attributed to the secondary metabolites which have the advan-tage of being of great diversity of chemical structure and have a very wide range of biological activities. The objectives of the present work were to stu-dy the antioxidant and antimicrobial activity of phenolic compounds ex-tracted from A. visnaga L. Its extraction is performed by two methods, etha-nol extraction and water extraction. The results showed that A. visnaga L.. ethanolic extract contains a mixture of phytochemical classes as polyphenol, flavonoids and revealed that this plant has high antioxidant activity (IC50 0.069 mg/ml). Regarding the antimicrobial activity results expressed by the diameter of the inhibition zones by diffusion method AWDT, the most signifi-cant inhibition was observed against to Staphylococcus aureus (12 mm) to the ethanol extract at concentration of 100mg / ml. Thus the aqueous ex-tract had a significant inhibitory activity against on the strains Staphylococ-cus aureus (8 mm), E. coli ATCC 10536 (8 mm) to a concentration of 100 mg / ml. The results for the antibacterial properties have shown that Gram-positive bacteria (Staphylococcus aureus, Listeria monocytogenes and M. luteus.) were more sensitive than gram-negative (Pseudomonas aeruginosa, E. coli ATCC 10536) against from the action of phenolic compounds of the Ammi visnaga ethanolic extract.


2019 ◽  
Vol 31 (5) ◽  
pp. 1077-1080
Author(s):  
Kottakki Naveen Kumar ◽  
Karteek Rao Amperayani ◽  
V. Ravi Sankar Ummdi ◽  
Uma Devi Parimi

A series 1,2,4-triazole piperine analogues (TP1-TP6) were designed and synthesized. The structures were confirmed using 1H NMR and 13C NMR. Antibacterial study was done using Gram-positive (Staphylococcus aureus and Bacillus cereus) and Gram-negative micro-organisms (E. coli and Pseudomonas aeruginosa) by disc diffusion method. Compound containing chloro substitution (TP6) showed the highest effect, while compound TP1, TP3, TP4, TP5 showed the moderate activity.


Sign in / Sign up

Export Citation Format

Share Document