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Selective COX-2 inhibitor celecoxib was found directly inhibiting the growth of tested phytopathogenic fungi with the inhibitory rate ranging from 30 to 40% at 100 µg/ml. Lead optimization of celecoxib led to the identification of compound 12 among its derivatives as the most active antifungal candidate. The antifungal effect of compound 12 was supposed to be independent of COX-2 inhibition. Transcriptome profiling analysis of Fusarium graminearium (PH-1) treated with compound 12 brought about 406 up-regulated and 572 down-regulated differentially express genes (DEGs) respectively. Copyright © 2020 Elsevier Inc. All rights reserved.

Citation

Yihui Ma, Lirong Yang, Xiuxiu Liu, Jun Yang, Xianglong Sun. Development of celecoxib-derived antifungals for crop protection. Bioorganic chemistry. 2020 Apr;97:103670

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PMID: 32088417

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