Potential antibacterial activity of triazine dendrimer: Synthesis and controllable drug release properties

Vembu, Sandhirakasu; Pazhamalai, S.; Gopalakrishnan, Mahesh

doi:10.1016/j.bmc.2015.06.009

Cited by 34 publications

(14 citation statements)

References 36 publications

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“…Victorious foreword of biologically applicable piperazine ring in some of our previous cases act as important core moiety to produced the higher generation dendrimer through the bond formation between norfloxacin and macromolecule. 35 Here with, we focus on norfloxacin piperazin ring bonded novel drug delivery system synthesis, β-cyclodextrin The MTT assay is a colorimetric assay for measuring cell viability through increased metabolism of tetrazolium salt (Moshmann, 1983). Cultured Escherichia coli, Staphylococcus aureus were taken into 96 well plates.…”

Section: Anti Bacterial Activitymentioning

confidence: 99%

“Design and Synthesis of Some Cyclic Carbohydrates with Norfloxacin as Surface moiety. A Study of Sustained Relax of Drugs”.

et al. 2019

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Biocompatible and biodegradable sustained drug delivery system has been constructed from reaction between norfloxacin and cyclodextrin through secondary amine of piperazine ring and hydroxyl group of the carbohydrate. Covalent bond polymeric structure is designed by the help of chloroacetyl chloride, target dendrimer formed by removing two hydrochloride molecules. The development of cyclodextrin core drug delivery system with twenty one norfloxacin surface moiety has been synthesized by only two steps. The synthesized polymeric structure was thoroughly studied by NMR, FT-IR, MALDI and UV- spectrometry. Sustained release assessment of synthetic polymer studied through different buffer solution by UV spectrometry and norfloxacin releases rate of synthetic polymer was controlled by the concentration and the experimental medium. The microbial assessments through kinetic studies by using Escherichia coli also reveal that the norfloxacin released possesses potential antimicrobial activity. Antibacterial activity of synthesized drug delivery system has been investigated with gram-negative and gram-positive species like Escherichia coli (mtcc 443), bacillus subtilis (mtcc 2063), pseudomonas (mtcc 741), staphylococcus (mtcc 737) and proteus mirabilis (mtcc 425). The hydrophobic and hydrophilic balance and the repeat drug unit of this synthesized system are responsible for effective antibacterial activity. The minimum inhibitor concentration values of this system are very small to 100 µg/mL-1, synthesized compound shown five times improved activity against organism on comparism with standard drug. The in-vitro release of norfloxacin from obtained dendrimer was investigated.

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Section: Anti Bacterial Activitymentioning

confidence: 99%

“Design and Synthesis of Some Cyclic Carbohydrates with Norfloxacin as Surface moiety. A Study of Sustained Relax of Drugs”.

et al. 2019

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“…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.…”

Section: Structure–activity Relationshipmentioning

confidence: 99%

4‐Quinolone Derivatives and Their Activities Against Gram‐negative Pathogens

Jiang

2018

Journal of Heterocyclic Chem

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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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“…Eight ciprofloxacin molecules were attached in an interesting dendrimer designed with piperazine and 1,3,5-triazine [57]. The compound was characterized by MALDI-TOF MS, NMR and IR.…”

Section: General Applications Of Dendrimer Prodrugsmentioning

confidence: 99%

Dendrimer Prodrugs

2016

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Abstract:The main objective of this review is to describe the importance of dendrimer prodrugs in the design of new drugs, presenting numerous applications of these nanocomposites in the pharmaceutical field. Therefore, the use of dendrimer prodrugs as carrier for drug delivery, to improve pharmacokinetic properties of prototype, to promote drug sustained-release, to increase selectivity and, consequently, to decrease toxicity, are just some examples of topics that have been extensively reported in the literature, especially in the last decade. The examples discussed here give a panel of the growing interest dendrimer prodrugs have been evoking in the scientific community.

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Potential antibacterial activity of triazine dendrimer: Synthesis and controllable drug release properties

Cited by 34 publications

References 36 publications

“Design and Synthesis of Some Cyclic Carbohydrates with Norfloxacin as Surface moiety. A Study of Sustained Relax of Drugs”.

“Design and Synthesis of Some Cyclic Carbohydrates with Norfloxacin as Surface moiety. A Study of Sustained Relax of Drugs”.

4‐Quinolone Derivatives and Their Activities Against Gram‐negative Pathogens

Dendrimer Prodrugs

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