Important role of the position of a functional group in isomers for photophysical and antibacterial properties: a case study with naphthalenemaleonitrile positional isomers

2020 ◽  
Vol 44 (33) ◽  
pp. 14116-14128
Author(s):  
Monika ◽  
Abhineet Verma ◽  
Supriy Verma ◽  
Nidhi Pandey ◽  
Ragini Tilak ◽  
...  

The position of the functional group alters the interactions in the crystal packing, thereby altering the fluorescence responses as well as the antibacterial activities.

2017 ◽  
Vol 63 (3) ◽  
pp. 18-24 ◽  
Author(s):  
Mohaddese Mahboubi ◽  
Rezvan Heidarytabar ◽  
Elaheh Mahdizadeh

Summary Introduction: In Iranian traditional medicine, Zataria multiflora Boiss (Lamiaceae family) is reputed due to its antiseptic effects. Objective: The purpose of this study was to evaluate the antibacterial and biofilm killing effects of Z. multiflora essential oil and main components against Pseudomonas aeruginosa. Methods: The main components of essential oil were identified by gas chromatography (GC) and gas chromatography-mass spectrometry (GC-MS). The antibacterial properties of Z. multiflora oil and main components were determined by assessing the MIC and MBC values, and their inhibition percent of biofilm killing effects were determined by the evaluation of optical density. The role of each main component in these activities was determined according to the chemical profiles of essential oil. Results: Thymol (38.7%), carvacrol (30.6%), and p-cymene (8.3%) were main components of twenty five components of essential oil. Carvacrol had the higher role in antibacterial activity against P. aeruginosa, followed by thymol. P-cymene enhanced the antibacterial activities of thymol and carvacrol against P. aeruginosa. Carvacrol showed the weak role in biofilm killing effect. In spite of the low antibacterial activity of p-cymene against P. aeruginosa, it can enhance the antibacterial activity of thymol or carvacrol. Conclusion: Z. multiflora essential oil can be used for the management of P. aeruginosa infections. Determining the precise role of each components needs investigating in their behavior in different media.


Nano Hybrids ◽  
2013 ◽  
Vol 3 ◽  
pp. 37-49 ◽  
Author(s):  
Shweta Rajawat ◽  
M.S. Qureshi

Silver nanoparticles are the most promising nanomaterial with antibacterial properties. Recent study of resistance to most potential antibiotics promotes research in the bactericidal activity of the silver nanoparticles. In this work, the effect of biosynthesized silver nanoparticles, in combination with gentamicin and ampicillin, on Pseudomonas Aeruginosa bacteria has been studied. Pseudomonas Aeruginosa is a common bacterium that can cause infections which are generalized as inflammation and sepsis. The results show that the bactericidal properties of the nanoparticles depends on the size of the as-synthesized silver nanoparticles as nanoparticles of diameter ~120 nm only have a direct interaction with the bacteria. It is observed that the antibacterial activities of antibiotics increase in the presence of AgNPs against test strains. Silver nanoparticles were synthesized elctrolytically using silver wire of 99% purity as anode and carbon rod wrapped with LDPE as cathode. 0.01 N Silver nitrate was used as an electrolyte. The process is termed as biosynthesis, because tea extract was used used as the capping agent which is also a very mild reducing agent. The polyphenols theaflavins and thearubigins, present in tea perform the role of stabilizing or capping agents due to their bulky and steric nature. A brown colored colloidal solution of silver nanoparticles is obtained. The as-synthesized silver nanoparticles were characterized using XRD, TEM and UV-Vis spectroscopy.


2021 ◽  
Vol 4 (1) ◽  
Author(s):  
David Dailler ◽  
Andrea Dorst ◽  
Daniel Schäfle ◽  
Peter Sander ◽  
Karl Gademann

AbstractFidaxomicin (FDX) is a marketed antibiotic for the treatment of Clostridioides difficile infections (CDI). Fidaxomicin displays antibacterial properties against many Gram-positive bacteria, yet the application of this antibiotic is currently limited to treatment of CDI. Semisynthetic modifications present a promising strategy to improve its pharmacokinetic properties and also circumvent resistance development by broadening the structural diversity of the derivatives. Here, based on a rational design using cryo-EM structural analysis, we implement two strategic site-selective catalytic reactions with a special emphasis to study the role of the carbohydrate units. Site-selective introduction of various ester moieties on the noviose as well as a Tsuji–Trost type rhamnose cleavage allow the synthesis of novel fidaxomicin analogs with promising antibacterial activities against C. difficile and Mycobacterium tuberculosis.


2020 ◽  
Author(s):  
David Dailler ◽  
Andrea Dorst ◽  
Daniel Schäfle ◽  
Peter Sander ◽  
Karl Gademann

<div><div><div><p>Fidaxomicin (FDX) is a marketed antibiotic for the treatment Clostridium difficile infections (CDI). Although showing interesting antibacterial properties against many Gram-positive bacteria, the application of this antibiotic is currently limited to treatment of CDI. Semisynthetic modifications present a promising strategy to improve its pharmacokinetic properties and also circumvent resistance development by broadening the structural diversity of derivatives. Based on a rational design using a cryo-EM structure analysis, we implemented two strategic site- selective catalytic reactions with a special emphasis to study the role of the carbohydrate units. Site-selective introduction of various ester moieties on the noviose as well as a Tsuji-Trost type rhamnose cleavage allowed the synthesis of novel fidaxomicin analogs with promising antibacterial activities against C. difficile and M. tuberculosis.</p></div></div></div>


2020 ◽  
Author(s):  
David Dailler ◽  
Andrea Dorst ◽  
Daniel Schäfle ◽  
Peter Sander ◽  
Karl Gademann

<div><div><div><p>Fidaxomicin (FDX) is a marketed antibiotic for the treatment Clostridium difficile infections (CDI). Although showing interesting antibacterial properties against many Gram-positive bacteria, the application of this antibiotic is currently limited to treatment of CDI. Semisynthetic modifications present a promising strategy to improve its pharmacokinetic properties and also circumvent resistance development by broadening the structural diversity of derivatives. Based on a rational design using a cryo-EM structure analysis, we implemented two strategic site- selective catalytic reactions with a special emphasis to study the role of the carbohydrate units. Site-selective introduction of various ester moieties on the noviose as well as a Tsuji-Trost type rhamnose cleavage allowed the synthesis of novel fidaxomicin analogs with promising antibacterial activities against C. difficile and M. tuberculosis.</p></div></div></div>


1987 ◽  
Author(s):  
William A. Worrall ◽  
Ann W. Stockman

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