Synthesis, ADME Study, and Antimicrobial Evaluation of Novel Naphthalene-Based Derivatives

In recent times, many researchers in pharmaceutical chemistry have been preoccupied with the quest for new potent anti-infective agents to combat antimicrobial resistance. A novel series of naphthalene-based derivatives were synthesized as part of these studies. Different spectral techniques, such as UV–Vis, FTIR, ۱۳C-NMR, and ۱H-NMR were used to affirm the synthesized compounds’ chemical structures, while an ADME study was conducted to investigate their pharmacokinetics and drug-like properties. The potential of the synthesized naphthalene-based derivatives as anti-infective candidates versus pathogenic microbes was evaluated using a broth microdilution assay. These microbes involved six aerobic gram-negative bacteria, four anaerobic bacteria, and two fungi. In addition, their safety was assessed versus normal bacterial flora. From the obtained results, the authors reported the following principal outcomes: Compound SF۵ revealed a significant aerobic gram-negative bactericidal impact while indicating high safety versus the non-pathological bacterial strain. Most of the synthesized naphthalene-based derivatives demonstrated outstanding potential as fungicidal candidates, but compound SF۱ was the most potent one. According to ADME analysis, almost all of the synthesized derivatives have good theoretical pharmacokinetics and drug-likeness characteristics making them suitable as oral-derived agents.

Keywords:

Naphthalene-based derivatives , Antimicrobial , Bactericidal , Fungicidal , Normal flora