Synthesis and evaluation of new quinazolin-4(3H)-one derivatives as potent antibacterial agents against multidrug resistant Staphylococcus aureus and Mycobacterium tuberculosis

2019 ◽  
Vol 175 ◽  
pp. 287-308 ◽  
Author(s):  
Srikanth Gatadi ◽  
Jitendra Gour ◽  
Manjulika Shukla ◽  
Grace Kaul ◽  
Arunava Dasgupta ◽  
...  
2019 ◽  
Vol 92 ◽  
pp. 103252 ◽  
Author(s):  
Srikanth Gatadi ◽  
Y.V. Madhavi ◽  
Sidharth Chopra ◽  
Srinivas Nanduri

2017 ◽  
Vol 61 (9) ◽  
Author(s):  
Timothy E. Long

ABSTRACT Thiram and disulfiram were evaluated as antibacterial agents against multidrug-resistant Staphylococcus aureus. Against a 30-member panel comprised of vancomycin-susceptible, vancomycin-intermediate, and vancomycin-resistant S. aureus strains, the MIC90 values of the respective test agents were 4 and 16 μg/ml. Additional analyses revealed that thiram and disulfiram are rapid-acting bacteriostatic agents with narrow, Gram-positive-bacterium spectrum activity. Synergy studies further determined that disulfiram increases the vancomycin susceptibility of three clinical vancomycin-resistant S. aureus strains in vitro, thus establishing a potential use in combination therapy.


2021 ◽  
Vol 854 (1) ◽  
pp. 012024
Author(s):  
S Djukanovic ◽  
S Cvetkovic ◽  
T Ganic ◽  
B Nikolic ◽  
D Mitic-Culafic

Abstract Contamination by numerous food-borne pathogens is a major challenge facing the food industry daily. Even though there are many strategies in the fight against contamination, pathogens able to attach to different surfaces and form biofilms are the biggest concern. Staphylococcus aureus is a common food-borne pathogen capable of forming biofilms on foods and food contact surfaces. The prevalence of multidrug resistant S. aureus is high in raw products, high-protein foods and processed products. Bearing in mind S. aureus resistance to numerous antibacterial agents, the aim of this study was to investigate antibiofilm activity of an ethyl-acetate extract of the medicinal plant, Frangula alnus, against S. aureus ATCC 25923 and S. aureus ATCC 43300. It was demonstrated that extract reduced survival of both tested strains by up to 67%. Furthermore, quantification of biofilm biomass showed that extract possesses the extraordinary ability to inhibit biofilm formation of both tested strains (up to 91%). On the other hand, the effect on preformed biofilm was less pronounced and measured only for S. aureus ATCC 43300, wherein about 28% of preformed biofilm was eradicated. The results obtained in this study encourage further investigation of F. alnus as a novel antibiofilm agent or preservative in the food industry.


2016 ◽  
Vol 2016 ◽  
pp. 1-10 ◽  
Author(s):  
Sin-Yeang Teow ◽  
Kitson Liew ◽  
Syed A. Ali ◽  
Alan Soo-Beng Khoo ◽  
Suat-Cheng Peh

Curcumin, the major constituent of Curcuma longa L. (Zingiberaceae family) or turmeric, commonly used for cooking in Asian cuisine, is known to possess a broad range of pharmacological properties at relatively nontoxic doses. Curcumin is found to be effective against Staphylococcus aureus (S. aureus). As demonstrated by in vitro experiment, curcumin exerts even more potent effects when used in combination with various other antibacterial agents. Hence, curcumin which is a natural product derived from plant is believed to have profound medicinal benefits and could be potentially developed into a naturally derived antibiotic in the future. However, there are several noteworthy challenges in the development of curcumin as a medicine. S. aureus infections, particularly those caused by the multidrug-resistant strains, have emerged as a global health issue and urgent action is needed. This review focuses on the antibacterial activities of curcumin against both methicillin-sensitive S. aureus (MSSA) and methicillin-resistant S. aureus (MRSA). We also attempt to highlight the potential challenges in the effort of developing curcumin into a therapeutic antibacterial agent.


2020 ◽  
Vol 15 (16) ◽  
pp. 1527-1534
Author(s):  
Beatriz C de Freitas ◽  
Paula A Queiroz ◽  
Vanessa P Baldin ◽  
Pedro HR do Amaral ◽  
Lucas LF Rodrigues ◽  
...  

Aim: To evaluate the activity of (-)-camphene-based thiosemicarbazide (TSC) and 4-hydroxy-thiosemicarbazone (4-OH-TSZ), alone and in combination against Gram-positive. Material & methods: MIC were determined for Staphylococcus aureus, Enterococcus spp. reference strains and clinical isolates. Drug combination, time–kill and cytotoxicity assays were also performed. Results: TSC and 4-OH-TSZ demonstrated potent inhibitory activity against S. aureus and Enterococcus spp., including multidrug-resistant isolates (MIC ranging from 1.9 to 31.2 μg/ml), and were bactericidal for the reference strains of both Gram-positive tested. The derivatives proved to be selective for the bacteria and synergistic with oxacillin and vancomycin. Conclusion: (-)-Camphene-based derivatives can represent promising drug candidates against critical pathogens, such as S. aureus and Enterococcus spp., including MRSA and vancomycin resistance Enterococcus spp. isolates.


2018 ◽  
Vol 157 ◽  
pp. 1056-1067 ◽  
Author(s):  
Srikanth Gatadi ◽  
Jitendra Gour ◽  
Manjulika Shukla ◽  
Grace Kaul ◽  
Swetarka Das ◽  
...  

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