Functionalized Cyclic Beta-Amino Acid Derivatives With Antiviral Potential

Area of Science:

• Medicinal Chemistry
• Organic Synthesis
• Virology

Background:

• Cyclic beta (β)-amino acids are valuable scaffolds in medicinal chemistry.
• Developing novel antiviral agents is crucial for public health.

Purpose of the Study:

• To synthesize diverse, highly functionalized cyclic β-amino acid derivatives.
• To evaluate the antiviral potential of these novel compounds against key human viruses.

Main Methods:

• Modified and improved literature synthetic protocols were employed.
• Synthesis of various derivatives including azido-, triazole-, fluoro-, and hydroxyl-substituted compounds, as well as lactams and piperidine/azepane skeletons.
• Antiviral activity screening including Human cytomegalovirus (HCMV), Human rhinovirus 8 (HRV8), and Human herpesvirus 1 (HSV-1) using CC50 and IC50 determinations.

Main Results:

• A library of regio- and stereoisomers of functionalized cyclic β-amino esters and lactams was successfully synthesized.
• Initial screening provided data on the anti-HCMV, anti-HRV8, and anti-HSV-1 activities of the synthesized compounds.

Conclusions:

• The study established a versatile synthetic route to novel cyclic β-amino acid derivatives.
• These compounds represent a promising starting point for the development of new antiviral therapeutics.