“…In fact, although Pseudomonas aeruginosa does not express TSPO, its large genome encodes many sensors (receptors) and transporters and different porins, including OprF. In addition, other studies indicated that benzodiazepine analogs can exhibit in vitro direct antibacterial activities on Pseudomonas aeruginosa ( Sharma et al, 2013 ), suggesting that Pseudomonas aeruginosa can sense benzodiazepines. Considering these findings, we cannot exclude the possibility that a sensor protein showing functional homologies with TSPO is expressed in Pseudomonas aeruginosa .…”
The translocator protein (TSPO), which was previously designated as the peripheral-type benzodiazepine receptor, is a 3.5 billion year-old evolutionarily conserved protein expressed by most Eukarya, Archae and Bacteria, but its organization and functions differ remarkably. By taking advantage of the genomic data available on TSPO, we focused on bacterial TSPO and attempted to define functions of TSPO in Pseudomonas via in silico approaches. A tspo ortholog has been identified in several fluorescent Pseudomonas. This protein presents putative binding motifs for cholesterol and PK 11195, which is a specific drug ligand of mitochondrial TSPO. While it is a common surface distribution, the sense of insertion and membrane localization differ between α- and γ-proteobacteria. Experimental published data and STRING analysis of common TSPO partners in fluorescent Pseudomonas indicate a potential role of TSPO in the oxidative stress response, iron homeostasis and virulence expression. In these bacteria, TSPO could also take part in signal transduction and in the preservation of membrane integrity.
“…In fact, although Pseudomonas aeruginosa does not express TSPO, its large genome encodes many sensors (receptors) and transporters and different porins, including OprF. In addition, other studies indicated that benzodiazepine analogs can exhibit in vitro direct antibacterial activities on Pseudomonas aeruginosa ( Sharma et al, 2013 ), suggesting that Pseudomonas aeruginosa can sense benzodiazepines. Considering these findings, we cannot exclude the possibility that a sensor protein showing functional homologies with TSPO is expressed in Pseudomonas aeruginosa .…”
The translocator protein (TSPO), which was previously designated as the peripheral-type benzodiazepine receptor, is a 3.5 billion year-old evolutionarily conserved protein expressed by most Eukarya, Archae and Bacteria, but its organization and functions differ remarkably. By taking advantage of the genomic data available on TSPO, we focused on bacterial TSPO and attempted to define functions of TSPO in Pseudomonas via in silico approaches. A tspo ortholog has been identified in several fluorescent Pseudomonas. This protein presents putative binding motifs for cholesterol and PK 11195, which is a specific drug ligand of mitochondrial TSPO. While it is a common surface distribution, the sense of insertion and membrane localization differ between α- and γ-proteobacteria. Experimental published data and STRING analysis of common TSPO partners in fluorescent Pseudomonas indicate a potential role of TSPO in the oxidative stress response, iron homeostasis and virulence expression. In these bacteria, TSPO could also take part in signal transduction and in the preservation of membrane integrity.
“…Anthelmintic activity was evaluated against Eisenia foetida . The hybrids 103 showed promising anthelmintic properties at low concentrations as compared to reference drug, piperazine citrate, with mean paralysis time in the range of 22.80–32.60 vs. 34.4 min [ 185 ]. …”
This review is aimed to provide extensive survey of quinolones and fluoroquinolones for a variety of applications ranging from metal complexes and nanoparticle development to hybrid conjugates with therapeutic uses. The review covers the literature from the past 10 years with emphasis placed on new applications and mechanisms of pharmacological action of quinolone derivatives. The following are considered: metal complexes, nanoparticles and nanodrugs, polymers, proteins and peptides, NO donors and analogs, anionic compounds, siderophores, phosphonates, and prodrugs with enhanced lipophilicity, phototherapeutics, fluorescent compounds, triazoles, hybrid drugs, bis-quinolones, and other modifications. This review provides a comprehensive resource, summarizing a broad range of important quinolone applications with great utility as a resource concerning both chemical modifications and also novel hybrid bifunctional therapeutic agents.Graphical abstract
“…Many other biological pharmacophores such as azole/hydrozone , benzofuroxan , bisphosphonate , catecholate , citrate , glycoside , isoniazid , kanamycin , kojic acid , β ‐lactams , lactone , imidazole , sideromycins , peptide , phenothiazinium , pyochelin , pyoverdin , pyrazine , pyridyl , pyrimidine , pyrrazole , quinolone , sulfonamide , siderophore , tetrahydroquinoline , 1,3,4‐thiadiazol/oxadiazol , thiazole , triazine , and trifluoroacetimidoyl have been introduced into the piperazinyl subunit of FQs; although some of them such as lactone‐CPFX hybrid 23 (MIC of 0.11 μg/mL against multidrug‐resistant E . coli , which was 50 times more potent than the parent CPFX ) showed promising activity against Gram‐negative pathogens, the majority of them were less active than the parents.…”
Gram‐negative pathogens represent a significant global health threat, while the emergency and widespread of drug resistance make the situation even worse. As “privileged building blocks,” 4‐quinolones including fluoroquinolones are mainstays of chemotherapy against various bacterial infections. However, as other antibiotics, the resistance of Gram‐negative bacteria to 4‐quinolones develops rapidly and spreads widely throughout the world. To overcome the resistance and improve the potency, a number of 4‐quinolone derivatives were designed, synthesized, and screened for their in vitro and in vivo activities against representative Gram‐negative pathogens. This review aims to summarize the recent advances made towards the discovery of 4‐quinolone derivatives as anti‐Gram‐negative agents as well as their structure–activity relationship. The enriched structure–activity relationship paves the way to the further rational development of 4‐quinolones with excellent potency against both drug‐susceptible and drug‐resistant Gram‐negative pathogens.
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