Synthesis and antifungal activities of small molecule arylthiazolamine derivatives.

Mol Divers

College of Pharmacy, Guizhou Provincial Engineering Technology Research Center for Chemical Drug R&D, Guizhou Provincial Key Laboratory of Pathogenesis and Drug Research On Common Chronic Diseases, Guizhou Medical University, Guiyang, 550004, People's Republic of China.

Published: October 2024

AI Article Synopsis

  • Researchers are focusing on developing new fungicides due to the resistance issues of existing ones against harmful fungi that affect plants.
  • They successfully synthesized thirty-eight new arylthiazolamine derivatives through various chemical reactions to find effective antifungal agents.
  • Some of these compounds, particularly 4m, 5k, and 5n, showed strong antifungal properties and could be as effective as current fungicides, offering a potential new solution for managing plant diseases.

Article Abstract

Developing new fungicides to compensate for the deficiencies of existing fungicides resistance in phytopathogenic fungi is a research hotspot in the field of pesticides. Aiming to discover novel template small molecules with excellent antifungal activity, thirty-eight arylthiazolamine derivatives were synthesized through bromination, cyclization, halogenation, and acylation reactions. The synthesized compounds were screened for antifungal activity against ten typical fungal pathogens, and some halogenated arylthiazolamines and amides exhibited excellent broad-spectrum antifungal activity, especially compounds 4m (3.96-47.76 μg/mL), 5k (0.10-7.70 μg/mL) and 5n (2.08-11.21 μg/mL). Among them, compound 5k provided comparable protection and curative effects to chloroticonil and boscalid against B. dothidea and V. mali infection in apple and apple tree branches, respectively, and it could exert antifungal effects by inhibiting the differentiation of mycelium spores, spore germination, and bud tube growth. This study provides high-efficiency and inexpensive candidate compounds for managing of diseases caused by plant pathogenic fungi.

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Source
http://dx.doi.org/10.1007/s11030-024-11002-8DOI Listing

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