Synthesis, Characterization and in vitro Antimicrobial Evaluation of Pyrazole Based Oxothiazolidine Hybrids

2020 ◽  
Vol 5 (4) ◽  
pp. 295-300
Author(s):  
Yogesh J. Sanghani ◽  
Suresh B. Koradiya ◽  
Krushnakumar J. Jilariya

In this work, pyrazole based oxothiazolidine hybrids, 4-{4-[2-(1- phenyl-3-(substituted)phenyl-1H-pyrazol-4-yl)-4-oxo-thiazolidin-3- yl]-phenyl}-morpholin-3-one (11a-l) were synthesized using molecular hybridization approach through Vilsmeier-Haack reaction. The titled compounds 11a-l were characterized by elemental analysis, IR, 1H NMR and mass spectral studies. The antibacterial activity of 11a-l was evaluated in vitro by agar cup plate method against B. cocous, B. subtillis, E. coli and P. vulgaris. The antifungal activity of compounds 11a-l was evaluated in vitro by agar based disk diffusion method against A. niger. The results of antibacterial and antifungal evaluation were reported in terms of zone of inhibition measured in mm. The synthesized compounds 11a-l exhibited moderate to good antibacterial and antifungal potential. Compound 4-{4-[2-(1-phenyl-3-(2-methoxyphenyl) phenyl-1H-pyrazol-4-yl)-4-oxo-thiazolidin-3-yl]-phenyl}- morpholin-3-one (11h) emerged as a most potent antimicrobial agent displaying zone of inhibition 21, 20, 21, 24 and 20 mm against B. cocous, B. subtillis, E. coli, P. vulgaris and A. niger, respectively.

2013 ◽  
Vol 14 (5) ◽  
pp. 924-929 ◽  
Author(s):  
Reena Kulshrestha ◽  
J Kranthi ◽  
P Krishna Rao ◽  
Feroz Jenner ◽  
V Abdul Jaleel ◽  
...  

ABSTRACT Aim The present study was conducted to evaluate the efficacy of commercially available herbal toothpastes against the different periodontopathogens. Materials and methods Six herbal toothpastes that were commonly commercially available were included in the study. Colgate herbal, Babool, Meswak, Neem active, Dabur red toothpastes were tested for the study whereas sterile normal saline was used as control. Antimicrobial efficacies of dentifrices were evaluated against Streptococcus mutans and Actinobacillus actinomycetemcomitans. The antimicrobial properties of dentifrices were tested by measuring the maximum zone of inhibition at 24 hours on the Mueller Hinton Agar media inoculated with microbial strain using disk diffusion method. Each dentifrice was tested at 100% concentration (full strength). Results The study showed that all dentifrices selected for the study were effective against the entire test organism but to varying degree. Neem active tooth paste gave a reading of 25.4 mm as the zone of inhibition which was highest amongst all of the test dentifrices. Colgate Herbal and Meswak dentifrices recorded a larger maximum zone of inhibition, measuring 23 and 22.6 mm respectively, compared to other toothpastes. All other dentifrices showed the zone of inhibition to be between 17 and 19 mm respectively. Conclusion The antibacterial properties of six dentifrices were studied in vitro and concluded that almost all of the dentifrices available commercially had antibacterial properties to some extent to benefit dental health or antiplaque action. How to cite this article Jenner F, Jaleel VA, Kulshrestha R, Maheswar G, Rao PK, Kranthi J. Evaluating the Antimicrobial Activity of Commercially Available Herbal Toothpastes on Microorganisms Associated with Diabetes Mellitus. J Contemp Dent Pract 2013;14(5):924-929.


2020 ◽  
Vol 32 (6) ◽  
pp. 1437-1442
Author(s):  
Panneerselvam Kalaivani ◽  
Jayaraman Arikrishnan ◽  
Mannuthusamy Gopalakrishnan

In this study, a new series of (E)-N-(4-(3-(3,5-dialkylphenyl)acryloyl)phenyl)-2-(1H-1,2,4-triazol-1- yl)acetamide (32-41) was synthesized, characterized by FT-IR, 1H NMR, 13C NMR and Mass spectral analysis and evaluated for their in vitro antibacterial and antifungal activities. The docking study of the newly synthesized compounds was performed and results showed good binding mode in the active site of 1T9U protein. The zone of inhibition concentration was tested for the synthesized compounds against five bacterial and three fungal strains. Compounds 34 and 37 have good antibacterial activity. Compounds 3, 4 and 6 shows moderate inhibition against the antifungal activity.


2013 ◽  
Vol 2013 ◽  
pp. 1-12 ◽  
Author(s):  
Reena Jain ◽  
Rajeev Singh ◽  
N. K. Kaushik

A new series of organotin(IV) complexes with purine bases theophylline (HL1) and theobromine (L2) of the types R3Sn(L1), R2Sn(L1)Cl, R3Sn(L2)Cl, and R2Sn(L2)Cl2(R = C6H5CH2–;p-ClC6H4CH2–) have been synthesized in anhydrous THF. The complexes were characterized by elemental analysis, conductance measurements, molecular weight determinations, UV-vis, IR,1H,13C NMR, and mass spectral studies. Various kinetic and thermodynamic parameters of these complexes have also been determined using TG/DTA technique. The thermal decomposition techniques indicate the formation of SnO2as a residue. The results show that the ligands act as bidentate, forming a five-member chelate ring. All the complexes are 1 : 1 metal-ligand complexes. In order to assess their antimicrobial activity, the ligands and their corresponding complexes have also been testedin vitroagainst bacteria (E. coli, S. aureus, andP. pyocyanea) and fungi (Rhizopus oryzaeandAspergillus flavus). All the complexes exhibit remarkable activity, and the results provide evidence that the studied complexes might indeed be a potential source of antimicrobial agents.


2019 ◽  
Vol 31 (9) ◽  
pp. 2015-2021
Author(s):  
Ashok K. Singh ◽  
Suresh K. Patel ◽  
Asif Jafri

A series of eight Co(III) complexes [CoL1-8(H2O)2Cl] (I-1 to I-8) incorporating 4-(2-substituted phenylimino)-2-(4-substituted phenyl)-4H-chromen-3-ol, as a tridentate imino flavone ligands (L1 to L8, 2-sub. = NH2, SH, 4-sub. = OMe, OH, Cl, NMe2) have been synthesized, characterized and the geometry of the complexes were optimized by DFT. The chemical structure of synthesized imino flavone ligands and their complexes were characterized by elemental analysis, 1H NMR, 13C NMR, UV-visible, IR, ESI-mass spectral data, conductometric and magnetic measurements. The synthesized compounds have been screened for their in vitro antibacterial activities against bacteria Vibrio cholerae, Salmonella typhi, Staphylococcus aureus, Escherichia coli and antifungal activities against fungi Candida albicans and Aspergillus flavus by paper disc diffusion method. The complexes I-3, I-4, I-7 and I-8 showed good antimicrobial activities against pathogens.


Author(s):  
Anjani Solankee ◽  
Riki Tailor

In our present investigation a new class of diverse sets of acetyl pyrazolines (6a-e), amino pyrimidines (7a-e) and 1,5-benzodiazepines (8a-e) bearing 1,3,5-triazine core were synthesised from chalcones (5a-e). Treatment of chalcone with hydrazine hydrate, guanidine hydrochloride and o-phenylenediamine afforded the corresponding acetyl pyrazoline, amino pyrimidine and 1,5-benzodiazepine derivatives respectively. The structures of all the newly synthesised compounds were assigned on the basis of FTIR, 1H NMR, 13C NMR, mass spectral data as well as elemental analysis. In vitro antimicrobial proficiency of the title compounds were assessed against selected pathogens S. aureus MTCC 96, S. pyogeneus MTCC 442, E. coli MTCC 443 and P. aeruginosa MTCC 1688 bacteria for antibacterial activities as well as antifungal activities against C. albicans MTCC 227, A. niger MTCC 282 and A. clavatus MTCC 1323 were used. The minimum inhibitory concentration (MIC) was determined by broth dilution method and recorded at the lowest concentration inhibiting growth of the organism. Among the synthesised compounds 6b, 6c, 7b, 8b, 8d and 8e exhibited excellent antimicrobial activity and said to be the most proficient members of the series.


2015 ◽  
Vol 43 (2) ◽  
pp. 327-334 ◽  
Author(s):  
Mihaela NICULAE ◽  
Laura STAN ◽  
Emoke PALL ◽  
Anamaria Ioana PAȘTIU ◽  
Iulia Maria BALACI ◽  
...  

The study was aimed to characterize the chemical composition and the antimicrobial activity of Romanian propolis ethanolic extracts (EEP) against antibiotic-sensitive and antibiotic-resistant E. coli strains isolated from bovine mastitis. The preliminary antimicrobial screening was performed by a disk diffusion method, followed by determination of minimum inhibitory concentrations (MIC) and minimum bactericidal concentrations (MBC) based on broth microdilution assay; further, the synergistic action of propolis with antimicrobial drugs was assessed by a disk diffusion method on agar containing subinhibitory concentrations of propolis. For the chemical characterisation of EEP, the flavonoids (flavones/flavonols, flavanones/dihydroflavonols) and total phenolics were evaluated by spectrophotometric methods. The phenolic compounds of these extracts were also determined using HPLC. The results indicated for Romanian propolis ethanolic extracts the typical poplar composition profile with flavonoids and phenolic acids as main biological active compounds, with chromatographic analysis data confirmed also spectrophotometrically. In addition, positively correlated with the chemical composition, a strong antimicrobial efficacy was exhibited towards E. coli strains, along with interesting synergistic interaction with antibiotics that can be further investigated to obtain propolis-based formulation with antibacterial properties. Subsequent in vitro and in vivo studies evaluating the safety and efficacy are intended to consider propolis in veterinary therapeutic protocols.


2015 ◽  
Vol 80 (9) ◽  
pp. 1101-1111 ◽  
Author(s):  
Gokula Krishnan ◽  
R. Sivakumar ◽  
V. Thanikachalam

Fifteen novel biologically active piperidin-4-one oxime esters (8-22) have been synthesized with good yields. These compounds were prepared from in-situ activated carboxylic acids using POCl3 and pyridine with piperidin-4- one oximes. The structure of the title compounds were elucidated on the basis of FT-IR, NMR (1D and 2D) and mass spectral analyses. The single crystal XRD study of compounds 12 and 20 were the further evidence for the proposed structure unambiguously. All the synthesized compounds were tested for in vitro antibacterial and antifungal activities. Many of these derivatives exhibited good activity against Bacillus subtilis, Pseudomonas aeruginosa, Escherichia coli, Trigoderma veride and Aspergillus flavus.


2021 ◽  
Author(s):  
Bondy Lourenço ◽  
Asimbawe Kiza ◽  
Abrão Amândio João ◽  
Clemência Félix Odala Niconte ◽  
Pompílio Armando Vintuar ◽  
...  

Abstract Background: Currently, several studies are being conducted to test antibacterial activity of various medicinal plants, in attempt to develop new antibiotics or to potentiate the action of antibiotics of known clinical use. In this research, phytochemical analysis and in vitro antibacterial activity of leaf extracts of Lantana camara L were performed.Methods The extracts were obtained through maceration with 90% ethanol. In phytochemical analysis, alkaloids, flavonoids, tannins and saponins were identified using specific reagents for each class.The antibacterial activity was analyzed using the disk diffusion method according to Kirby-Bauer, against Escherichia coli and Staphylococus aureus.Key findings The diameters of the inhibition halos varied between 0.7 and 12 mm, with an average of 8.26 mm for strains of S. aureus and there was no inhibition for E. coli. The results showed a significant difference between the inhibition halos and the tested concentrations for S. aureus. In conclusion L. camara leaf extracts are rich in bioactive compounds and have a good antibacterial potential against S. aureus and not for E. coli. And there was no relationship between the concentration of the extract and the diameter of the halo of inhibition of the evaluated microorganism.


Author(s):  
V. V. Pantyo ◽  
M. M. Fizer ◽  
O. I. Fizer ◽  
G. M. Koval ◽  
E.M. Danko

Annotation. The development and rapid pace of the spread of resistance to antimicrobial agents predetermines the search for new methods of counteracting pathogenic and conditionally pathogenic microorganisms. In this context, studies of the antimicrobial activity of newly synthesized chemicals, which in the future can be considered as candidates for antiseptic and disinfectants, are relevant. The aim of the work was to determine the antimicrobial activity of new ionic associates based on the surface-active cetylpyridinium cation with respect to certain opportunistic microorganisms. The antimicrobial activity of four ionic associates based on the cetylpyridinium cation with respect to clinical isolates of E. coli, P. vulgaris, K. pneumonia, P. aeruginosa, S. aureus, as well as the collection test strains of S. aureus ATCC 25923, E. coli ATCC 29522 and P. aeruginosa ATCC 27853 was studied. Screening studies were performed by the disk diffusion method. With substances that showed an antimicrobial effect, quantitative studies were carried out by the method of serial macro-dilutions in a liquid nutrient media. Screening studies revealed the antibacterial activity of the substances against E. coli ATCC 25923, E. coli (clinical isolate), P. vulgaris and K. pneumonia. With these microorganisms quantitative studies were carried out with the determination of the minimum inhibitory and minimum bactericidal concentrations. The most pronounced antimicrobial activity for the investigated microflora was shown by tetraphenylborate and cetylpyridinium perchlorate. The MIC and MBC values of these substances ranged between 1.625–3.125 mmol / L and 3.125–12.5 mmol / L, respectively. The studied associates showed high antimicrobial activity against representatives of the Enterobacteriaceae family in in vitro studies. Promising is the further study of the effect of the counter-anion associates of cationic surfactants on the biofilm formation of conditionally pathogenic microorganisms.


2014 ◽  
Vol 1 (1) ◽  
pp. 1-3 ◽  
Author(s):  
Deepkumar Joshi ◽  
Rinku Patel ◽  
Nupur Patel ◽  
Devendra Patel ◽  
Chintan Pandya

The leaf and stem of cordia macleodii plant were investigated for evaluating antibacterial and antifungal properties.Different extracts of leaf and stem viz. double distilled water, methanol, ethyl acetate ane n-hexane were collectedand content was optimized for the maximum amount of extraction with varying time of 6 and 12 h. The extracts weretested for their antimicrobial activities against gram-positive bacteria (B. sutilis), gram-negative bacteria (E. coli) andfungi (A. niger). The extracts were found to be more active against bacteria as compared to fungi. It was also observedthat the antibacterial and antifungal potential of the water extracts were found to be excellent as 1A (38 mm) and 1B (22mm) compared to the other extracts. Graphical Abstract:


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