Antimicrobial and Drug Releasing Studies of Novel Acrylate Polymer based on Triazine

This work is focused on the synthesis and characterization of versatile acrylate polymer of chalcone based triazine for their antibacterial activity and cumulative drug release behaviour studies. The novel acrylate monomer 4-(3-(4-((4-(4-(3-(4-((7-chloroquinolin-4-yl)amino)-phenyl)-3-oxoprop-1-en-1- yl)phenoxy)-6-((4-nitrophenyl)amino)-1,3,5-triazin-2-yl)oxy)phenyl)-3-oxoprop-1-en-1- yl)phenylacrylate (SCP) is from novel chalcone and acryloyl chloride. Homo and copolymers of SCP were prepared using acrylic acid and hydroxyethyl acrylate. Physical characterization confirms the formation of the above compounds. Prepared drug molecules possess chalcone moiety as well as quinoline so it has the greater effect to inhibit the growth of the Gram-negative bacteria (15.63 ± 0.4 μg/mL) was confirmed by MIC method. The weight average molecular weight of the polymer is 10,000 g/mol. The polymer decomposes at 325 ºC. Drug releasing in vitro behaviour of the synthesized drug is controlled by the nature of comonomer, pH and the temperature.

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Synthesis and characterization of the novel pyrimidine’s derivatives, as a promising tool for antimicrobial agent and in-vitro cytotoxicity

Journal of the Iranian Chemical Society ◽

10.1007/s13738-021-02448-w ◽

2021 ◽

Author(s):

Arwa M. Abd-Elaziz ◽

Hala M. Aly ◽

Nashwa M. Saleh ◽

Sawsan A. Fouad ◽

Abla A. Ismail ◽

...

Keyword(s):

Antimicrobial Agent ◽

In Vitro Cytotoxicity ◽

Synthesis And Characterization ◽

The Novel ◽

Promising Tool

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Structure-Guided Discovery of Novel Aminoglycoside Mimetics as Antibacterial Translation Inhibitors

Antimicrobial Agents and Chemotherapy ◽

10.1128/aac.49.12.4942-4949.2005 ◽

2005 ◽

Vol 49 (12) ◽

pp. 4942-4949 ◽

Cited By ~ 33

Author(s):

Yuefen Zhou ◽

Vlad E. Gregor ◽

Zhongxiang Sun ◽

Benjamin K. Ayida ◽

Geoffrey C. Winters ◽

...

Keyword(s):

Respiratory Pathogen ◽

Gram Negative Bacteria ◽

The Novel ◽

Guided Discovery ◽

Initial Characterization ◽

Low Toxicity ◽

Translation Inhibitor

ABSTRACT We report the structure-guided discovery, synthesis, and initial characterization of 3,5-diamino-piperidinyl triazines (DAPT), a novel translation inhibitor class that targets bacterial rRNA and exhibits broad-spectrum antibacterial activity. DAPT compounds were designed as structural mimetics of aminoglycoside antibiotics which bind to the bacterial ribosomal decoding site and thereby interfere with translational fidelity. We found that DAPT compounds bind to oligonucleotide models of decoding-site RNA, inhibit translation in vitro, and induce translation misincorporation in vivo, in agreement with a mechanism of action at the ribosomal decoding site. The novel DAPT antibacterials inhibit growth of gram-positive and gram-negative bacteria, including the respiratory pathogen Pseudomonas aeruginosa, and display low toxicity to human cell lines. In a mouse protection model, an advanced DAPT compound demonstrated efficacy against an Escherichia coli infection at a 50% protective dose of 2.4 mg/kg of body weight by single-dose intravenous administration.

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Synthesis and characterization of new copper(II) complex compounds with chlorhexidine. Part I

Open Chemistry ◽

10.2478/s11532-010-0028-9 ◽

2010 ◽

Vol 8 (3) ◽

pp. 543-549 ◽

Cited By ~ 5

Author(s):

Mirela Călinescu ◽

Ticuţa Negreanu-Pîrjol ◽

Rodica Georgescu ◽

Octavian Călinescu

Keyword(s):

Antimicrobial Activity ◽

Metal Salt ◽

Complex Compounds ◽

Synthesis And Characterization ◽

Gram Negative Bacteria ◽

Reaction Conditions ◽

Gram Negative ◽

Imine Nitrogen

AbstractThree new copper(II) complex compounds with chlorhexidine diacetate as a ligand have been prepared and characterized by elemental and thermogravimetrical analyses, molar conductances, magnetic susceptibility measurements, infrared, electronic and EPR spectra. The complexes correspond to the formulas: [Cu2(CHX)Cl4]·2C2H5OH, [Cu2(CHX)Br4]·2C2H5OH and [Cu2(CHX)(CH3COO)2] (CH3COO)2·2C2H5OH, where CHX = chlorhexidine, their composition and stereochemistry depending on the reaction conditions and the metal salt used. Chlorhexidine acts as neutral tetradentate NNNN donor, coordinating through the four imine nitrogen atoms. Investigations on antimicrobial activity in vitro show that all the complexes are active against the tested microorganisms, the complex with chloride being more active against Gram negative bacteria than chlorhexidine diacetate..

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Synthesis and Characterization of Novel N-(Benzo[d]Thiazol-2-yl)-2-(2-(6-Chloroquinolin-4-yl)Hydrazinyl)Acetamide Derivatives Containing Quinoline Linkage as Potent Antibacterial Agents

International Letters of Chemistry Physics and Astronomy ◽

10.18052/www.scipress.com/ilcpa.53.114 ◽

2015 ◽

Vol 53 ◽

pp. 114-121 ◽

Cited By ~ 3

Author(s):

Manoj N. Bhoi ◽

Mayuri A. Borad ◽

Hitesh B. Parmar ◽

Hitesh D. Patel

Keyword(s):

Antibacterial Activity ◽

Antibacterial Agent ◽

Antibacterial Agents ◽

Spectroscopic Techniques ◽

Gram Negative Bacteria ◽

The Novel ◽

Elemental Analyses ◽

In Vitro Antibacterial Activity

As part of ongoing studies in developing new antibacterial agent, a novel series of N-(benzo[d]thiazol-2-yl)-2-(2-(6-chloroquinolin-4-yl)hydrazinyl)acetamide derivatives was synthesized by sequencing reaction of 2-aminobenzothiazole with chloroacetylchloride, hydrazine hydrate and 4,7-dichloroquinoline. The novel heterocycles were characterized by elemental analyses and various spectroscopic techniques. The synthesized compounds were tested in-vitro antibacterial activity against two Gram-positive and two Gram-negative bacteria with standard drugs. Microbiological results showed that the synthesized compounds possessed a broad spectrum of antibacterial activity against the tested microorganisms.

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