Synthesis and Docking Study of N‑(Cinnamoyl)‑N′‑(substituted)acryloyl Hydrazide Derivatives
Containing Pyridinium Moieties as a Novel Class of Filamentous Temperature-Sensitive
Protein Z Inhibitors against the Intractable Xanthomonas
oryzae pv. oryzae Infections in Rice
Posted on 2020-07-22 - 20:17
Xanthomonas oryzae pv. oryzae (Xoo) is an offensive phytopathogen that can invade
a wide range of plant hosts to develop bacterial diseases, including
the well-known rice bacterial leaf blight. However, few agrochemicals
have been identified to effectively prevent and eliminate Xoo-induced diseases. Thus, designing novel antibacterial
compounds on the basis of the potential targets from Xoo may lead to the discovery of highly efficient and innovative anti-Xoo agents. Filamentous temperature-sensitive protein Z
(FtsZ), an important functional protein in the progression of cell
division, has been widely reported and exploited as a target for creating
antibacterial drugs in the field of medicine. Therefore, the fabrication
of innovative frameworks targeting XooFtsZ may be
an effective method for managing bacterial leaf blight diseases via
blocking the binary division and reproduction of Xoo. As such, a series of novel N-(cinnamoyl)-N′-(substituted)acryloyl hydrazide derivatives containing
pyridinium moieties were designed, and the anti-Xoo activity was determined. The bioassay results showed that compound A7 had excellent anti-Xoo activity
(EC50 = 0.99 mg L–1) in vitro and distinct
curative activity (63.2% at 200 mg L–1) in vivo.
Further studies revealed that these designed compounds were XooFtsZ inhibitors, validating by the reduced GTPase activity
of recombinant XooFtsZ, the nonfilamentous XooFtsZ assembly observed in the TEM images, and the prolonged Xoo cells from the fluorescence patterns. Computational
docking studies showed that compound A7 had
strong interactions with ASN34, GLN193, and GLN197 residues located
in the α helix regions of XooFtsZ. The present
study demonstrates the developed FtsZ inhibitors can serve as agents
to control Xoo-induced infections.
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Zhou, Xiang; Feng, Yu-Mei; Qi, Pu-Ying; Shao, Wu-Bin; Wu, Zhi-Bing; Liu, Li-Wei; et al. (2020). Synthesis and Docking Study of N‑(Cinnamoyl)‑N′‑(substituted)acryloyl Hydrazide Derivatives
Containing Pyridinium Moieties as a Novel Class of Filamentous Temperature-Sensitive
Protein Z Inhibitors against the Intractable Xanthomonas
oryzae pv. oryzae Infections in Rice. ACS Publications. Collection. https://doi.org/10.1021/acs.jafc.0c01565