# Synthesis of Farnesyloxy- and Drimanyloxy-Arene Scaffold-Based Hybrid Molecules as Antifungals against Botrytis cinerea

## TL;DR

This study creates and tests new antifungal compounds based on natural product scaffolds to combat the plant pathogen Botrytis cinerea.

## Contribution

The paper introduces novel farnesyloxy- and drimanyloxy-arene hybrid molecules with potent antifungal activity against Botrytis cinerea.

## Key findings

- Drimanyloxyarene derivatives showed higher fungitoxicity than farnesyloxyarene derivatives.
- Compounds (±)-12, (±)-31, and (±)-35 outperformed azoxystrobin at 391 × 10–5 mg/mL.
- (±)-12 exhibited antifungal inhibition comparable to triclosan.

## Abstract

There is an increasing
interest in the use of biopesticides, which
implies the use of living microorganisms, plant and microbial extracts,
and natural products isolated from the above-mentioned sources or
closely related derivatives. In this regard, 10 farnesyloxy-arenes
derivatives (21–25, (±)-26–(±)-30) and 12 drimanyloxyarenes
derivatives ((±)-12–(±)-14, (±)-31–(±)-40) were
synthesized and tested against the phytopathogenic fungus Botrytis cinerea. In general, the drimanyloxyarenes derivatives
were more fungitoxic than their farnesyloxyarene precursors. The most
active compounds were (±)-12, (±)-31, and (±)-35, which at a 391 × 10–5 mg/mL dose, were more active than azoxystrobin, while (±)-12 presented an inhibition comparable to that of triclosan.
Structure–activity relationships are discussed, as well as
the correlation with calculated physicochemical properties such as
logP and total polar surface area.