Title of article :
Novel naphthalene-derived coumarin composites: synthesis, antibacterial, and antifungal activity assessments
Author/Authors :
Waheed ، Sarah Ahmed Pharmaceutical Chemistry Department - College of Pharmacy - University of Mosul , Mustafa ، Yasser Fakri Pharmaceutical Chemistry Department - College of Pharmacy - University of Mosul
Abstract :
Composites with a coumarin-based chemical structure have sparked a lot of interest in the scientific community. This is because of their diverse structural properties and also, their wide range of biological activities. In this work, eight novel naphthalene-derived coumarin composites were synthesised, confirmed by various spectrophotometers, and assessed for antibacterial and anti-fungal activities. The pharmacokinetic parameters were evaluated in silico using pre-ADMET, a free online program. The antimicrobial activity was tested using the method of broth-dilution towards six aerobic gram-negative bacterial strains (Klebsiella pneumonia, Pseudomonas aeruginosa, Escherichia coli, Haemophilus influenzae, Shigella dysenteriae, and Salmonella typhi), four anaerobic bacterial strains (Prevotella melaninogenica, Bacteroides fragilis, Clostridium perfringens, and Fusobacterium necrophorum), as well as two fungal strains (Aspergillus niger and Candida albicans). The safety profile was inspected by testing the toxicity for normal flora bacteria. Pharmacokinetic investigations demonstrated that the synthesised naphthalene-derived coumarin composites have good penetration across the GIT mucosa and most of them have poor penetration across the blood-brain barrier. These findings suggest good oral bioavailability along with low neurological toxicity profiles. The evaluations of the antimicrobial activity revealed that our composites have a weak bactericidal influence on gram-negative aerobic as well as anaerobic bacteria. The foremost discovery in this report was that most of these composites have an extremely potent fungicidal influence. The authors hope that this realization, along with the apparent safety of these compounds, can be utilized in the coming time for the production of new powerful fungicidal influence drugs.
Keywords :
Synthesis , Antimicrobial , Broth , dilution , Bactericidal influence , Fungicidal influence