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Discovery of novel pyridine carboxamides with antifungal activity as potential succinate dehydrogenase inhibitors.

ABSTRACT: Fifteen novel pyridine carboxamide derivatives bearing a diarylamine-modified scaffold were designed, synthesized, and their antifungal activity was evaluated. Preliminary bioassay results showed that some of the synthesized compounds exhibited moderate to good in vitro antifungal activity. Further, compound 6-chloro-N-(2-(phenylamino)phenyl)nicotinamide (3f) displayed good in vivo antifungal activity against Botrytis cinerea. The enzymatic test on B. cinerea succinate dehydrogenase (SDH) showed that the inhibitory activity possessed by compound 3f equally matches that of thifluzamide. Molecular docking results demonstrated that compound 3f could commendably dock with the active site of SDH via stable hydrogen bonds and hydrophobic interactions, suggesting the possible binding modes of the title compounds with SDH. The results above revealed that the target compounds would be the leading fungicide compound for further investigation.

SUBMITTER: Yan Z 

PROVIDER: S-EPMC9706280 | biostudies-literature | 2022 Aug

REPOSITORIES: biostudies-literature

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Discovery of novel pyridine carboxamides with antifungal activity as potential succinate dehydrogenase inhibitors.

Yan Zhongzhong Z   Yang Zihui Z   Qiu Longjian L   Chen Yan Y   Li Aijun A   Chang Taopeng T   Niu Xinzhe X   Zhu Jingyan J   Wu Shihao S   Jin Feng F  

Journal of pesticide science 20220801 3

Fifteen novel pyridine carboxamide derivatives bearing a diarylamine-modified scaffold were designed, synthesized, and their antifungal activity was evaluated. Preliminary bioassay results showed that some of the synthesized compounds exhibited moderate to good <i>in vitro</i> antifungal activity. Further, compound 6-chloro-<i>N</i>-(2-(phenylamino)phenyl)nicotinamide (<b>3f</b>) displayed good <i>in vivo</i> antifungal activity against <i>Botrytis cinerea</i>. The enzymatic test on <i>B. cinere  ...[more]

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