posted on 2021-10-28, 20:29authored byHua Li, Yu-Xia Wang, Xiao-Lei Zhu, Guang-Fu Yang
Succinate
dehydrogenase (SDH, EC 1.3.5.1) has proven to be an important
fungicidal target, and the inhibition of SDH is useful in the treatment
of plant pathogens. The discovery of a novel active SDH inhibitor
is of high value. Herein, we disclose the discovery of a potent, highly
active inhibitor as a fungicide candidate by using a computational
substitution optimization method, a fast drug design method developed
in our laboratory. The greenhouse experiments showed that compound 17c exhibited high protective activity against south corn
rust, soybean rust (SBR), and rice sheath blight at a very low dosage
of 0.781 mg/L. Moreover, the field trials indicated that compound 17c is comparable to and even better than commercial fungicides
against SBR and cucumber powdery mildew at 50 mg/L concentration.
Most surprisingly, compound 17c resulted to be strictly
better in curative activity than the commercial fungicide benzovindiflupyr.
The computation results indicated that 17c could form
another hydrogen bond with C_S42 and then lead to strong van der Waals
and electronic interactions with SDH. Our results suggested that 17c is a potential fungicide candidate for SDH.