scholarly journals Synthesis and antibacterial activity of novel myricetin derivatives containing sulfonylpiperazine

2020 ◽  
Author(s):  
Jun He ◽  
Xue-Mei Tang ◽  
Ting-Ting Liu ◽  
Feng Peng ◽  
Qing Zhou ◽  
...  

Abstract Myricetin derivatives containing sulfonylpiperazine were synthesized and their structures were confirmed by NMR and HRMS. The antibacterial activity results indicated that some compounds showed good antibacterial activity against Xanthomonas oryzaepv. oryzae (Xoo), Xanthomonas axonopodispv. citri (Xac) and Ralstonia solanacearum (Rs). Among them, compounds 4m and 4p revealed excellent antibacterial activities against Rs with a concentration for 50% of maximal effect (EC50) value of 4 and 4 μg/mL, which were better than the control drugs bismerthiazol (13 μg/mL) and thiodiazole-copper (185 μg/mL). As observed using scanning electron microscope (SEM), these compounds act by causing folding and deformation of the bacterial surface, resulting in incomplete bacterial structure, so as to achieve the goal of bacteriostasis. The myricetin derivatives synthesized are expected to guide the research direction of new antibacterial agents.

2012 ◽  
Vol 550-553 ◽  
pp. 1026-1029
Author(s):  
Jian Xi Ren ◽  
Jing Ya Li ◽  
Zhi Feng Cai ◽  
Jin Ming Dai ◽  
Mei Niu ◽  
...  

Carbon microspheres (CMSs) were used as the carrier to prepare the Ag-loading CMSs (Ag/CMSs) antibacterial agent through the method of chemical adsorption. The morphologies and structures of modified CMSs were characterized by using the field emission Scanning Electron Microscope (SEM). The results showed that silver was absorbed on the surface of CMSs. The bacterial inhibition ring experiment showed that Ag/CMSs had good antibacterial activity against Staphylococcus aureus and Escherichia coli, meanwhile the diameters of the bacterial inhibition rings were 19 mm against Staphylococcus aureus and 21 mm against Escherichia coli, respectively.


Author(s):  
Olufunmiso O. Olajuyigbe ◽  
Morenike O. Adeoye-Isijola ◽  
Otunola Adedayo

Background: Black soap is a medicinal product that could be harnessed for economic purpose if properly packaged, and misconception about its traditional use by herbalists is thrown overboard.Aims: To promote the relevance of these soaps for economic development, this study compared the antibacterial activity of black soaps with medicated soaps widely used against bacterial infections.Methods: The antibacterial activities of these soap samples were determined by agar diffusion and macrobroth dilution methods.Results: In this study, the statistical analysis of the inhibition zones showed that black soaps were significantly (p < 0.05) more active than medicated soaps used against the test bacterial isolates. The black soaps inhibited and killed the isolates better than the medicated soaps at the different concentrations used. The minimum inhibitory concentration for Klebsiella pneumoniae and Enterococcus faecalis ranged between 0.125 mg/mL and 2 mg/mL, Staphylococcus aureus (0.25–4) mg/mL, Escherichia coli (0.125–4) mg/mL and Pseudomonas aeruginosa (1–4) mg/mL. The result showed that K. pneumoniae and E. faecalis were the most susceptible, followed by E. faecalis > E. coli > S. aureus > P. aeruginosa.Conclusion: As a valuable medicinal output derivable from organic waste product that could be converted to wealth, African black soap production, utilisation and commercialisation have tremendous economic potentials. These soaps showed significant antibacterial activity greater than those of the medicated soaps. Hence, their use could be a better option in place of commercially available medicated and antiseptic soaps because of the degree of antibacterial activities they exhibited.


2009 ◽  
Vol 63 (4) ◽  
Author(s):  
Neela Bhatia ◽  
Kakasaheb Mahadik ◽  
Manish Bhatia

AbstractA series of 1,3-diaryl-2-propen-1-ones and their indole analogs were synthesized and evaluated for antibacterial activity. Structures of newly synthesized compounds were confirmed by physicochemical, spectral and elemental analysis. All the compounds were screened for their antibacterial activities against four different bacterial strains. The QSAR studies were performed using Vlife MDS 3.5 software. QSAR equation revealed that selected electronic, steric and lipophilic parameters have good correlation with antibacterial activity. Best equations were selected on basis of the correlation coefficient (r 2) and the predictable ability of the equations. The present findings suggest that the 1,3-diaryl-2-propen-1-ones framework is an attractive template for structure optimization to achieve higher potency, lower toxicity, and a wider spectrum of antibacterial activity.


2011 ◽  
Vol 287-290 ◽  
pp. 1947-1951 ◽  
Author(s):  
Jing Xian Xu ◽  
Ye Ting Lin ◽  
Qiang Lin ◽  
Wen Yuan ◽  
Xue Qiong Yin ◽  
...  

Two Schiff bases of chitosan (CTS) were synthesized from 4-methoxylbenzylaldehyde (CH3O-CTS) and 4-methylbenzylaldehyde(CH3-CTS). The Schiff bases were characterized by FTIR, DSC-TGA, solid13C CP-Mas NMR, and elemental analysis. Antibacterial activities of the Schiff bases against Escherichia coli and Staphylococcus aureus were measured by the optical density method. The antibacterial activity of the Schiff bases is better than that of the original CTS. The IC50of CH3O-CTS and CH3-CTS againstEscherichia coliis respectively 40.3 ppm and 43 ppm, which being 38.5 ppm and 39.5 ppm against Staphylococcus aureus, lower than IC50of chitosan, being 59.5 ppm and 52 ppm againstEscherichia coliand Staphylococcus aureus, respectively.


Author(s):  
Sarath Sasikumar ◽  
Haripriya M. ◽  
Anjali T.

Objective: A series of 1, 2-Benzisoxazole derivatives were synthesized and characterized by various analytical techniques like Melting point, Rf, FTIR, and NMR spectra.Methods: Structures of the compounds were elucidated and evaluated for anti-inflammatory activity by HRBC membrane stabilization method, antibacterial activity against Escherichia coli and Staphylococcus aureus by cup plate method.Results: The compounds 4a and 4e showed good anti-inflammatory activity compared with standard drug Diclofenac sodium and compounds 4b and 4d showed good antibacterial activity on compared with standard drug Gentamycin.Conclusion: These compounds may serve as future leads for anti-inflammatory and antibacterial drug discovery.


Molecules ◽  
2018 ◽  
Vol 23 (12) ◽  
pp. 3132 ◽  
Author(s):  
Xianghui Ruan ◽  
Cheng Zhang ◽  
Shichun Jiang ◽  
Tao Guo ◽  
Rongjiao Xia ◽  
...  

A series of myricetin derivatives containing amide, thioether, and 1,3,4-thiadiazole moieties were designed and synthesized, and their antiviral and antibacterial activities were assessed. The bioassays showed that all the title compounds exhibited potent in vitro antibacterial activities against Xanthomonas citri (Xac), Ralstonia solanacearum (Rs), and Xanthomonas oryzae pv. Oryzae (Xoo). In particular, the compounds 5a, 5f, 5g, 5h, 5i, and 5l, with EC50 values of 11.5–27.3 μg/mL, showed potent antibacterial activity against Xac that was better than the commercial bactericides Bismerthiazol (34.7 μg/mL) and Thiodiazole copper (41.1% μg/mL). Moreover, the in vivo antiviral activities against tobacco mosaic virus (TMV) of the target compounds were also tested. Among these compounds, the curative, protection, and inactivation activities of 5g were 49.9, 52.9, and 73.3%, respectively, which were better than that of the commercial antiviral Ribavirin (40.6, 51.1, and 71.1%, respectively). This study demonstrates that myricetin derivatives bearing amide, thioether, and 1,3,4-thiadiazole moieties can serve as potential alternative templates for the development of novel, highly efficient inhibitors against plant pathogenic bacteria and viruses.


2018 ◽  
Vol 24 (6) ◽  
pp. 327-332 ◽  
Author(s):  
Yogesh D. Mane ◽  
Smita S. Patil ◽  
Dhanraj O. Biradar ◽  
Bhimrao C. Khade

Abstract Ten 5-bromoindole-2-carboxamides were synthesized, characterized and evaluated for antibacterial activity against pathogenic Gram-negative bacteria Klebsiella pneumoniae, Escherichia coli, Pseudomonas aeruginosa and Salmonella Typhi using gentamicin and ciprofloxacin as internal standards. Compounds 7a–c, 7g and 7h exhibit high antibacterial activity with a minimum inhibitory concentration (MIC) of 0.35–1.25 μg/mL. Compounds 7a–c exhibit antibacterial activities that are higher than those of the standards against E. coli and P. aeruginosa.


Coumarin is a heterocyclic moiety containing benzo pyran ring structure. It is widely distributed in the plant kingdom as a glycoside. Many compounds of medicinal and pharmaceutical importance possess coumarin ring structure. Drugs with coumarin structure can be synthesized by many well-known synthetic reactions. Coumarin derivatives were found to be antibacterial, anticoagulant, antiinflammatory, anti-HIV, anti-cancer and antioxidant. As part of the search for new and effective antibacterial agents, eight novel derivatives of coumarins were synthesized by Mannich reaction. All the compounds were evaluated for antibacterial activity against Staphylococcus aureus and Escherichia coli using ciprofloxacin as standard and DMSO as solvent. Three of the synthesized derivatives exhibited good antibacterial activity against Staphylococcus aureus and Escherichia coli. The work must be extended so as to develop coumarin derivatives into highly effective antibacterial agents.


2020 ◽  
Vol 20 (3) ◽  
pp. 229-236
Author(s):  
Jinwei Zhang ◽  
Qiuyue Tang ◽  
Wuyong Chen ◽  
Hongbin Sun ◽  
Qiming Ou ◽  
...  

In order to evaluate leather antibacterial activity rapidly and accurately, an improved halo method was developed based on conventional halo method and the agar diffusion plate method. During the new method, there were two layers of medium, the bottom was sterile medium and the top was medium containing microbes; more than one leather sample could be tested in a culture dish. The antibacterial activities of leather treated by nano-silver, nano-ZnO and butyl paraben against Escherichia coli, Staphylococcus aureus, Aspergillus niger and Rhodotorula mucilaginosa were tested by the new method. The results indicated intraclass correlation coefficient values were greater than 0.7 but the P values were less than 0.05 during improved halo method testing, thus, the repeatability and reliability was comparable or even better than conventional method. Nano-silver showed excellent and broad antibacterial activity and the difference between each antibacterial agent could be observed clearly and intuitively during improved halo method testing. In sum, improved halo method was a fast, accurate, qualitative and quantitative testing method and would be a new choice for evaluating leather antibacterial activity.


2017 ◽  
Vol 19 (4) ◽  
pp. 128-136 ◽  
Author(s):  
Saviour A. Umoren ◽  
Alexis M. Nzila ◽  
Saravanan Sankaran ◽  
Moses M. Solomon ◽  
Peace S. Umoren

Abstract Silver nanoparticles (AgNPs) have been synthesized in the presence of Strawberry fruit extract (SBFE) at room temperature. The synthesized AgNPs was characterized by UV-vis spectroscopy, SEM, EDS, XRD, TEM and FTIR. The UV-vis spectra of the AgNPs show SPR band at 450 nm. TEM results indicate that AgNPs are spherical in shape and size range between 7–65 nm. Antibacterial activity of the synthesized AgNPs has been assessed against Pseudomonas aeruginosa and Bacillus licheniformis. The results show that AgNPs exhibit inhibitory effect and effect is a function of AgNPs concentration. The antibacterial activity of the prepared AgNPs has been compared with two antibiotics, amoxicillin and ciprofloxacin. It is found that the antibiotics perform better than AgNPs.


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