Synthesis and characterization of pyridine-based organic salts: Their antibacterial, antibiofilm and wound healing activities.

Bioorg Chem

H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, Karachi University, Karachi 74200, Pakistan. Electronic address:

Published: July 2020

In treating wounds, long lasting infection is considered the major impediment. Drugs are rendered ineffective by pathogenic microorganisms via antibiotic resistance and calls for designing and development of new drugs. Herein, we report synthesis of eight different N-alkylated pyridine-based organic salts QAS 1-8 and their antibacterial, antibiofilm and wound healing activities. 3-(2-R-hydrazinecarbonyl)-1-propylpyridinium Bromide was the parent compound while R group was varying in each salt composed of different aromatic aldehyde moieties. In the antibacterial activity against S. aureus and E. coli, amoxicillin shows IC near to 25 µg/mL inhibiting 58 ± 0.4% S. aureus while ceftriaxone inhibited 55 ± 0.5% E. coli at a concentration of 10 µg/mL. The highest IC (56 ± 0.5% against S. aureus; 55 ± 0.5% against E. coli) was shown by compound QAS 7 at the concentration of 100 µg/mL; followed by the QAS 6 (55 ± 0.5% against E. coli) and QAS 2 (55 ± 0.5% against E. coli). In the antibiofilm activity, QAS 6, QAS 1 and QAS 8 inhibited 58 ± 0.4% S. aureus at a concentration of 75 µg/mL, while QAS 2 inhibited E. coli at the same concentration and amount. QAS 7, 3 and 1 inhibited almost 90% while QAS 6 inhibited 95 ± 1.1%of E. coli at a concentration of 250 µg/mL. Highest MBIC was provided by QAS 7 (52 ± 0.4%) against S. aureus at a concentration of 50 µg/mL that is very near to the standard amoxicillin. Antibacterial and antibiofilm activity results were also supported by the atomic force microscopy (AFM). In the wound healing activity, QAS 8 healed 90.8 ± 4.3% of the wound in 21 days with an average period of epithelialization (POE) of 19 ± 1.4 days; that is far better than povidone iodine ointment (81.5 ± 3.3% of the wound in the 21 days with 22.4 ± 2.9 days of POE). It is concluded from this study that the synthesized compounds QAS 2, 7 and 8 can be used for further mechanistic studies to be employed as antibacterial, antibiofilm and wound healing agents.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bioorg.2020.103937DOI Listing

Publication Analysis

Top Keywords

antibacterial antibiofilm
16
wound healing
16
55 ± 05% coli
16
qas inhibited
16
qas
13
antibiofilm wound
12
coli concentration
12
pyridine-based organic
8
organic salts
8
healing activities
8

Similar Publications

Combining antibacterial and wound healing features: Xanthan gum/guar gum 3D-printed scaffold tuned with hydroxypropyl-β-cyclodextrin/thymol and Zn.

Carbohydr Polym

March 2025

Departamento de Farmacología, Farmacia y Tecnología Farmacéutica, I+D Farma (GI-1645), Faculty of Pharmacy, Instituto de Materiales (iMATUS), and Health Research Institute of Santiago de Compostela (IDIS), Universidade de Santiago de Compostela, 15782 Santiago de Compostela, Spain. Electronic address:

Biofilm formation on biological and material surfaces represents a heavy health and economic burden for both patient and society. To contrast this phenomenon, medical devices combining antibacterial and pro-wound healing abilities are a promising strategy. In the present work, Xanthan gum/Guar gum (XG/GG)-based scaffolds were tuned with thymol and Zn to obtain wound dressings that combine antibacterial and antibiofilm properties and favour the healing process.

View Article and Find Full Text PDF

Biofilm formation and virulence factor production by Pseudomonas aeruginosa are identified as the main mechanisms of its antibiotic resistance and pathogenicity. In this context, the study of the chemical composition of three Algerian essential oils (EOs) and the screening of their antibacterial, anti-biofilm and virulence factor inhibitory activities enabled us to select the Thyme EO as the best oil to control the P. aeruginosa strain isolated from hospital environments.

View Article and Find Full Text PDF

Hospital surfaces are often contaminated with multidrug-resistant pathogenic bacteria that cause healthcare-associated infections and lead to increased mortality and morbidity. There is a need for new alternative antibacterial agents to overcome antibiotic resistance. Azadirachta indica and Simmondsia chinensis have been found to possess antibacterial activity and medicinal value.

View Article and Find Full Text PDF

Resistance by bacteria to available antibiotics is a threat to human health, which demands the development of new antibacterial agents. Considering the prevailing conditions, we have developed a library of new naphthalimide-coumarin moieties as broad-spectrum antibacterial agents to fight against awful drug resistance. Preliminary studies indicate that compounds and display excellent antibacterial activity against , exceeding the performance of marketed drug amoxicillin.

View Article and Find Full Text PDF

This study explores the development and characterization of spray-dried composite microparticles consisting of levofloxacin (LVX, a broad-spectrum antibiotic), and ambroxol (AMB, a mucolytic agent that has antibacterial and antibiofilm properties), for the intended application of the drug against lower respiratory tract infections (LRTIs). A range of LVX to AMB mass ratios (1:1, 1:0.5, and 1:0.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!