Naphthalene, a versatile platform in medicinal chemistry: Sky-high perspective

Area of Science:

• Medicinal Chemistry
• Pharmacology
• Drug Discovery

Background:

• Naphthalene is a versatile aromatic scaffold with diverse biological activities.
• Naphthalene metabolites, like epoxides and quinones, contribute to its cytotoxic effects.
• Numerous natural and synthetic naphthalene-based compounds exhibit therapeutic properties.

Purpose of the Study:

• To review the pharmacological aspects of chemically modified naphthalene-based molecules.
• To compile the activity profiles of various naphthalene derivatives.
• To provide a benchmark for designing novel naphthalene-based therapeutics.

Main Methods:

• Literature review of naphthalene derivatives and their pharmacological activities.
• Analysis of structure-activity relationships for naphthalene-based compounds.
• Compilation of FDA-approved naphthalene-based drugs and natural phytoconstituents.

Main Results:

• Naphthalene derivatives possess a wide range of activities including anticancer, antimicrobial, anti-inflammatory, and neuroprotective effects.
• Specific naphthalene-based drugs like Etoposide, Rifampicin, Naproxen, and Bedaquiline are approved therapeutics.
• Structural modifications of the naphthalene scaffold lead to varied biological activities and therapeutic applications.

Conclusions:

• The naphthalene scaffold is a crucial building block in drug discovery due to its broad biological activity spectrum.
• Understanding the pharmacological profiles of existing naphthalene derivatives can guide the design of new potent drugs with reduced side effects.
• Further research into naphthalene-based molecules holds promise for developing novel therapeutics for various diseases.