Synthesis and Anti‐Fungal/Oomycete Activity of Novel Sulfonamide Derivatives Containing Camphor Scaffold

Abstract

Twelve novel camphor sulfonamide derivatives 2a -2l were synthesized and characterized by 1 H-NMR, 13 C-NMR and HRMS spectra. The anti-fungal/oomycete activity bioassay showed that some of the title compounds displayed moderate to good anti-fungal/oomycete activities against B. dothidea and P. capsici. Compound 2d exhibited the best in vitro antifungal activity toward B. dothidea. The in vivo experiment revealed that compound 2d possessed considerable anti-B. dothidea effect at 200 mg/L. Mechanism study showed that compound 2d could increase the cell membrane permeability. In addition, the in vitro enzyme inhibition assay and molecular docking results indicated that compound 2d could be a potential SDH inhibitor.

Design, Synthesis, and Antifungal Activities of Novel Carboxamides Derivatives Bearing a Chalcone Scaffold as Potential SDHIs

“…Numerous studies demonstrate that modification of the polar moiety and the hydrophobic tail are beneficial to enhancing the antifungal efficacies and considered as effective strategies for discovery of novel SDHIs fungicides (Figure 1). [13–16] …”

“…Numerous studies demonstrate that modification of the polar moiety and the hydrophobic tail are beneficial to enhancing the antifungal efficacies and considered as effective strategies for discovery of novel SDHIs fungicides (Figure 1). [13][14][15][16] Chalcone is a privileged scaffold that has a α,β-unsaturated carbonyl group, which is abundant in natural products and served as precursors to the biosynthesis of flavonoids and isoflavonoids. [17] Chalcone derivatives have garnered foremost interest in medicine and pesticides fields because they have various biological activities such as anticancer, [18] antimicrobial, [19] anti-inflammatory, [20] antileishmanial, [21] antiviral, [22] antifungal, [23] insecticidal, [24] and herbicidal activities.…”