Function-Oriented Synthesis of Simplified Caprazamycins: Discovery of Oxazolidine-Containing Uridine Derivatives as Antibacterial Agents against Drug-Resistant Bacteria

2010 ◽  
Vol 53 (9) ◽  
pp. 3793-3813 ◽  
Author(s):  
Kensuke Ii ◽  
Satoshi Ichikawa ◽  
Bayan Al-Dabbagh ◽  
Ahmed Bouhss ◽  
Akira Matsuda
Keyword(s):  
Antibacterial Agents ◽  
Resistant Bacteria ◽  
Drug Resistant ◽  
Drug Resistant Bacteria

scholarly journals Novel Seleno- and Thio-Urea Containing Dihydropyrrol-2-One Analogues as Antibacterial Agents

Antibiotics ◽  
2021 ◽  
Vol 10 (3) ◽  
pp. 321
Author(s):  
Shekh Sabir ◽  
Tsz Tin Yu ◽  
Rajesh Kuppusamy ◽  
Basmah Almohaywi ◽  
George Iskander ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Antibiotic Resistance ◽  
Quorum Sensing ◽  
Antibacterial Agents ◽  
Inhibitory Concentration ◽  
Resistant Bacteria ◽  
Drug Resistant ◽  
Positive Bacterium ◽  
Quorum Sensing Inhibition ◽  
Drug Resistant Bacteria

The quorum sensing (QS) system in multi-drug-resistant bacteria such as P. aeruginosa is primarily responsible for the development of antibiotic resistance and is considered an attractive target for antimicrobial drug discovery. In this study, we synthesised a series of novel selenourea and thiourea-containing dihydropyrrol-2-one (DHP) analogues as LasR antagonists. The selenium DHP derivatives displayed significantly better quorum-sensing inhibition (QSI) activities than the corresponding sulphur analogues. The most potent analogue 3e efficiently inhibited the las QS system by 81% at 125 µM and 53% at 31 µM. Additionally, all the compounds were screened for their minimum inhibitory concentration (MIC) against the Gram-positive bacterium S. aureus, and interestingly, only the selenium analogues showed antibacterial activity, with 3c and 3e being the most potent with a MIC of 15.6 µM.

An unexpected discovery toward novel membrane active sulfonyl thiazoles as potential MRSA DNA intercalators

2020 ◽  
Vol 12 (19) ◽  
pp. 1709-1727 ◽  
Author(s):  
Yuan-Yuan Hu ◽  
Juan Wang ◽  
Tie-Jun Li ◽  
Rammohan R Yadav Bheemanaboina ◽  
Mohammad Fawad Ansari ◽  
...  
Keyword(s):  
Mammalian Cells ◽  
Antibacterial Agents ◽  
Antimicrobial Agents ◽  
Methicillin Resistant Staphylococcus Aureus ◽  
Inhibitory Concentration ◽  
Resistant Bacteria ◽  
Drug Resistant ◽  
Dna Intercalators ◽  
Dna Targeting ◽  
Drug Resistant Bacteria

Aim: With the increasing emergence of drug-resistant bacteria, the need for new antimicrobial agents has become extremely urgent. This work was to develop sulfonyl thiazoles as potential antibacterial agents. Results & methodology: Novel hybrids of sulfonyl thiazoles were developed from commercial acetanilide and acetylthiazole. Hybrids 6e and 6f displayed excellent inhibitory efficacy against clinical methicillin-resistant Staphylococcus aureus (MRSA) (minimum inhibitory concentration = 1 μg/ml) without obvious toxicity toward normal mammalian cells (RAW 264.7). The combination uses were found to improve the antimicrobial ability. Further preliminary antibacterial mechanism experiments showed that the active molecule 6f could effectively interfere with MRSA membrane and insert into MRSA DNA. Conclusion: Compounds 6e and 6f could serve as potential DNA-targeting templates toward the development of promising antimicrobial agents.

scholarly journals Biofabricated platinum nanoparticles: therapeutic evaluation as a potential nanodrug against breast cancer cells and drug-resistant bacteria

RSC Advances ◽  
2021 ◽  
Vol 11 (40) ◽  
pp. 24900-24916
Author(s):  
Saliha Manzoor ◽  
Dar Junaid Bashir ◽  
Khalid Imtiyaz ◽  
M. Moshahid A. Rizvi ◽  
Irshad Ahamad ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Green Synthesis ◽  
Cancer Cells ◽  
Platinum Nanoparticles ◽  
Breast Cancer Cells ◽  
Antibacterial Agents ◽  
Resistant Bacteria ◽  
Drug Resistant ◽  
Drug Resistant Bacteria ◽  
Therapeutic Evaluation

The present study involves the green synthesis of platinum nanoparticles and their application as anticancer and antibacterial agents.

scholarly journals Mechanistic Insights into the Antimicrobial Actions of Metallic Nanoparticles and Their Implications for Multidrug Resistance

2019 ◽  
Vol 20 (10) ◽  
pp. 2468 ◽  
Author(s):  
Sibhghatulla Shaikh ◽  
Nazia Nazam ◽  
Syed Mohd Danish Rizvi ◽  
Khurshid Ahmad ◽  
Mohammad Hassan Baig ◽  
...  
Keyword(s):  
Metallic Nanoparticles ◽  
Bacterial Infections ◽  
Antibacterial Agents ◽  
Health Concern ◽  
Resistant Bacteria ◽  
Multiple Drug ◽  
Drug Resistant ◽  
Drug Resistant Bacteria ◽  
Multiple Drug Resistant ◽  
Bacterial Drug Resistance

Multiple drug-resistant bacteria are a severe and growing public health concern. Because relatively few antibiotics have been approved over recent years and because of the inability of existing antibiotics to combat bacterial infections fully, demand for unconventional biocides is intense. Metallic nanoparticles (NPs) offer a novel potential means of fighting bacteria. Although metallic NPs exert their effects through membrane protein damage, superoxide radicals and the generation of ions that interfere with the cell granules leading to the formation of condensed particles, their antimicrobial potential, and mechanisms of action are still debated. This article discusses the action of metallic NPs as antibacterial agents, their mechanism of action, and their effect on bacterial drug resistance. Based on encouraging data about the antibacterial effects of NP/antibiotic combinations, we propose that this concept be thoroughly researched to identify means of combating drug-resistant bacteria.

scholarly journals Metallic Antibacterial Surface Treatments of Dental and Orthopedic Materials

Materials ◽  
2020 ◽  
Vol 13 (20) ◽  
pp. 4594
Author(s):  
Rushui Bai ◽  
Liying Peng ◽  
Qiannan Sun ◽  
Yunfan Zhang ◽  
Lingyun Zhang ◽  
...  
Keyword(s):  
Antibacterial Agents ◽  
Bacterial Resistance ◽  
Antibacterial Properties ◽  
Surface Treatments ◽  
Resistant Bacteria ◽  
Drug Resistant ◽  
Clinical Issue ◽  
Drug Resistant Bacteria ◽  
Antibacterial Surface ◽  
Orthopedic Materials

The oral cavity harbors complex microbial communities, which leads to biomaterial-associated infections (BAI) during dental and orthopedic treatments. Conventional antibiotic treatments have met great challenges recently due to the increasing emergency of drug-resistant bacteria. To tackle this clinical issue, antibacterial surface treatments, containing surface modification and coatings, of dental and orthopedic materials have become an area of intensive interest now. Among various antibacterial agents used in surface treatments, metallic agents possess unique properties, mainly including broad-spectrum antibacterial properties, low potential to develop bacterial resistance, relative biocompatibility, and chemical stability. Therefore, this review mainly focuses on underlying antibacterial applications and the mechanisms of metallic agents in dentistry and orthopedics. An overview of the present review indicates that much work remains to be done to deepen the understanding of antibacterial mechanisms and potential side-effects of metallic agents.

scholarly journals Alternative Antimicrobial Approach: Nano-Antimicrobial Materials

2015 ◽  
Vol 2015 ◽  
pp. 1-16 ◽  
Author(s):  
Nurit Beyth ◽  
Yael Houri-Haddad ◽  
Avi Domb ◽  
Wahid Khan ◽  
Ronen Hazan
Keyword(s):  
Mechanism Of Action ◽  
Bacterial Infections ◽  
Antibacterial Agents ◽  
Multidrug Resistant ◽  
Resistant Bacteria ◽  
Drug Resistant ◽  
Bacterial Strains ◽  
Drug Resistant Bacteria ◽  
Antimicrobial Materials ◽  
Nanoparticle Effect

Despite numerous existing potent antibiotics and other antimicrobial means, bacterial infections are still a major cause of morbidity and mortality. Moreover, the need to develop additional bactericidal means has significantly increased due to the growing concern regarding multidrug-resistant bacterial strains and biofilm associated infections. Consequently, attention has been especially devoted to new and emerging nanoparticle-based materials in the field of antimicrobial chemotherapy. The present review discusses the activities of nanoparticles as an antimicrobial means, their mode of action, nanoparticle effect on drug-resistant bacteria, and the risks attendant on their use as antibacterial agents. Factors contributing to nanoparticle performance in the clinical setting, their unique properties, and mechanism of action as antibacterial agents are discussed in detail.

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