# Design, Synthesis, Antifungal Activity, and 3D-QSAR Study of Novel Quinoxaline-2-Oxyacetate Hydrazide

## TL;DR

Researchers designed and tested new antifungal compounds based on a quinoxaline scaffold, showing strong activity against several plant pathogenic fungi.

## Contribution

A novel quinoxaline-2-oxyacetate hydrazide scaffold was designed, synthesized, and shown to have superior antifungal activity compared to existing fungicides.

## Key findings

- Most compounds exhibited strong antifungal activity against tested pathogens.
- Compound 15 and compound 1 showed better efficacy than ridylbacterin against specific fungi.
- 3D-QSAR analysis provided insights for optimizing future antifungal drug design.

## Abstract

Plant pathogenic fungi pose a major threat to global food security, ecosystem services, and human livelihoods. Effective and broad-spectrum fungicides are needed to combat these pathogens. In this study, a novel antifungal 2-oxyacetate hydrazide quinoxaline scaffold as a simple analogue was designed and synthesized. Their antifungal activities were evaluated against Botrytis cinerea (B. cinerea), Altemaria solani (A. solani), Gibberella zeae (G. zeae), Rhizoctonia solani (R. solani), Colletotrichum orbiculare (C. orbiculare), and Alternaria alternata (A. alternata). These results demonstrated that most compounds exhibited remarkable inhibitory activities and possessed better efficacy than ridylbacterin, such as compound 15 (EC50 = 0.87 μg/mL against G. zeae, EC50 = 1.01 μg/mL against C. orbiculare) and compound 1 (EC50 = 1.54 μg/mL against A. alternata, EC50 = 0.20 μg/mL against R. solani). The 3D-QSAR analysis of quinoxaline-2-oxyacetate hydrazide derivatives has provided new insights into the design and optimization of novel antifungal drug molecules based on quinoxaline.