Novel Quinolone substituted 1,3,4-oxadiazole derivatives: Design, synthesis, antimicrobial and anti-inflammatory potential DOI Creative Commons
Vishal Sharma, Rina Das, Dinesh Kumar Mehta

et al.

Research Square (Research Square), Journal Year: 2024, Volume and Issue: unknown

Published: May 3, 2024

Abstract A novel series of quinolone-substituted 1,3,4-oxadiazole derivatives 4(a-l) have been designed and synthesized. The target compounds were investigated for their antibacterial activity against gram positive (Staphylococcus aureus, ATCC 25923, Enterococcus faecalis, 29212) negative bacterium (Escherichia coli, 25922, Pseudomonas aeruginosa, 27853) antifungal using candida albicans (ATCC 10231) anti-inflammatory as COX-II inhibitors, respectively. functionality was introduced at C-6 position pipemidic acid derivatives. structure synthesized confirmed by IR, 1H NMR Mass spectrometry techniques. quinolone (pipemidic acid)-oxadiazole hybrid found to be effective bacterial strains. When compared ciprofloxacin (MIC 16 µg/mL), the under consideration (4f, 4h, 4k) showed potent all strains except faecalis, with MICs 8 µg/mL. On other hand, (4a–l) did not respond well Candida albicans fungal strain. compound (4k) represents high % inhibition COX-II. (4f, 4h & 4k) exhibited highest hydrogen bonding interaction ARG57, ARG72, ARG78, LEU54 MET16 residues a binding energy -8.4, -8.6 -8.5 kcal/mol into active pocket DNA gyrase enzyme respectively even better in comparison reference ligands. Based on docking study, acid) oxadiazole structural ligands strong pockets enzyme.

Language: Английский

Combatting resistance: Understanding multi-drug resistant pathogens in intensive care units DOI Open Access

Jianying Teng,

Saber İmani, Aiping Zhou

et al.

Biomedicine & Pharmacotherapy, Journal Year: 2023, Volume and Issue: 167, P. 115564 - 115564

Published: Sept. 23, 2023

The escalating misuse and excessive utilization of antibiotics have led to the widespread dissemination drug-resistant bacteria, posing a significant global healthcare crisis. Of particular concern is increasing prevalence multi-drug resistant (MDR) opportunistic pathogens in Intensive Care Units (ICUs), which presents severe threat public health contributes substantial morbidity mortality. Among them, MDR ESKAPE account for vast majority these pathogens. This comprehensive review provides meticulous analysis current landscape ICUs, especially pathogens, illuminating their resistance mechanisms against commonly employed first-line antibiotics, including polymyxins, carbapenems, tigecycline. Furthermore, this explores innovative strategies aimed at preventing controlling emergence spread resistance. By emphasizing urgent need robust measures combat nosocomial infections caused by study serves as an invaluable reference future investigations field antibiotic

Language: Английский

Citations

32
Cyanomethylquinolones as a New Class of Potential Multitargeting Broad-Spectrum Antibacterial Agents DOI

Yi-Min Tan,

Jing Zhang, Yu-Jia Wei

et al.

Journal of Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 67(11), P. 9028 - 9053

Published: May 24, 2024

This work identified a class of cyanomethylquinolones (CQs) and their carboxyl analogues as potential multitargeting antibacterial candidates. Most the prepared compounds showed high activities against most tested bacteria, exhibiting lower MIC values (0.125–2 μg/mL) than those clinical norfloxacin, ciprofloxacin, clinafloxacin. The low hemolysis, drug resistance, cytotoxicity, well good predictive pharmacokinetics active CQs revealed development potential. Furthermore, they could eradicate established biofilm, facilitating bacterial exposure to these These induce death through effects, including intercalating into DNA, up-regulating reactive oxygen species, damaging membranes directly, impeding metabolism. Moreover, highly cyclopropyl CQ 15 exhibited more effective in vivo anti-MRSA potency ciprofloxacin. findings highlight broad-spectrum candidates for treating intractable infections.

Language: Английский

Citations

12
Synthesis of tetra-substituted thiophene derivatives as potential Hits combating antibiotic resistant bacteria ESKAPE DOI
Heba K. Abd El-Mawgoud, Asmaa M. AboulMagd, Ahmed Shaker

et al.

Bioorganic Chemistry, Journal Year: 2025, Volume and Issue: 155, P. 108101 - 108101

Published: Jan. 8, 2025

Language: Английский

Citations

1
A systematic review on the anti-microbial activities and structure-activity relationship (SAR) of quinoxaline derivatives DOI

Sri Mounika Bellapukonda,

Rani Bandela,

Anuradha Singampalli

et al.

European Journal of Medicinal Chemistry, Journal Year: 2025, Volume and Issue: 289, P. 117472 - 117472

Published: March 3, 2025

Language: Английский

Citations

1
Photodynamic therapy for ESKAPE pathogens: An emerging approach to combat antimicrobial resistance (AMR) DOI

Akansha Mathur,

Ajayraj Singh Parihar,

S.I. Patel A.N. Modi

et al.

Microbial Pathogenesis, Journal Year: 2023, Volume and Issue: 183, P. 106307 - 106307

Published: Aug. 19, 2023

Language: Английский

Citations

21
Discovery of indolylacryloyl-derived oxacins as novel potential broad-spectrum antibacterial candidates DOI

Yue-Gao Hu,

Narsaiah Battini,

Bo Fang

et al.

European Journal of Medicinal Chemistry, Journal Year: 2024, Volume and Issue: 270, P. 116392 - 116392

Published: April 1, 2024

Language: Английский

Citations

6
Discovery of benzopyridone cyanoacetates as new type of potential broad-spectrum antibacterial candidates DOI
Jing Zhang,

Yi-Min Tan,

Shu-Rui Li

et al.

European Journal of Medicinal Chemistry, Journal Year: 2023, Volume and Issue: 265, P. 116107 - 116107

Published: Dec. 30, 2023

Language: Английский

Citations

14
ESKAPE: Navigating the Global Battlefield for Antimicrobial Resistance and Defense in Hospitals DOI Creative Commons

Kamna Ravi,

Baljit Singh

Bacteria, Journal Year: 2024, Volume and Issue: 3(2), P. 76 - 98

Published: April 16, 2024

The current healthcare environment is at risk due to the facilitated transmission and empowerment of ESKAPE pathogens, comprising Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, Enterobacter species. These pathogens have posed significant challenges global public health threat has only amplified over time. multidrug-resistant bacteria become adept escaping effects conventional antibiotics utilized, leading severe healthcare-associated infections compromising immunocompromised patient outcomes a greater extent. impact evident in rapidly rising rates treatment failures, increased mortality, elevated costs. To combat this looming crisis, diverse strategies been adopted, ranging from development novel antimicrobial agents combination therapies implementation stringent infection control measures. Additionally, there growing emphasis on promoting stewardship programs optimize use existing reduce selective pressure driving evolution resistance. While progress made some extent, rapid adaptability these enhancement resistance mechanisms proves be major hurdle yet crossed by professionals. In viewpoint, impending heralded proliferation need for concerted effort via international collaborations assurance effective sustainable solutions, are explored. curb possibility outbreaks future safeguard health, better preparation awareness defense should given paramount importance.

Language: Английский

Citations

5
Epidemiology, Clinical, and Microbiological Characteristics of Multidrug-Resistant Gram-Negative Bacteremia in Qatar DOI Creative Commons
Hamad Abdel Hadi, Soha R. Dargham,

Faiha Eltayeb

et al.

Antibiotics, Journal Year: 2024, Volume and Issue: 13(4), P. 320 - 320

Published: March 31, 2024

Antimicrobial resistance is a global healthcare threat with significant clinical and economic consequences peaking at secondary tertiary care hospitals where multidrug-resistant Gram-negative bacteria (MDR GNB) lead to poor outcomes. A prospective study was conducted between January December 2019 for all invasive bloodstream infections (BSIs) MDR GNB in Qatar identified during routine microbiological service examine their clinical, microbiological, genomic characteristics. Out of 3238 episodes BSIs, the prevalence 13% (429/3238). The predominant pathogens were Escherichia coli (62.7%), Klebsiella pneumoniae (20.4%), Salmonella species (6.6%), Pseudomonas aeruginosa (5.3%), while out 245 clinically evaluated patients, majority adult males, elderly constituting almost one-third cohort highest observed risk prolonged hospital stays. factors included multiple comorbidities, recent contact, previous antimicrobial therapy, admission critical care. in-hospital mortality rate recorded 25.7%, associated care, acquisition aeruginosa. Resistant demonstrated high levels but noticeable susceptibility amikacin carbapenems. Genomic analysis revealed that ST131 enterica ST1 clones not other pathogens.

Language: Английский

Citations

4
Pharmacophore-guided computational modeling of quinolone-ATPase conjugate inhibitors targeting DNA GyrB subunit of Staphylococcus aureus DOI
Md. Al Amin,

Md. Jakir Hossain,

Md. Kawsar Habib

et al.

Computers in Biology and Medicine, Journal Year: 2025, Volume and Issue: 186, P. 109727 - 109727

Published: Jan. 25, 2025

Language: Английский

Citations

0