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

Abstract

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.

Synthesis and Biological Evaluation of 1,2,4-Triazole Thioethers as Both Potential Virulence Factor Inhibitors against Plant Bacterial Diseases and Agricultural Antiviral Agents against Tobacco Mosaic Virus Infections

“…Compound A 10 with concentrations of 500 and 200 μg/mL and an equivalent DMSO solution were sprayed uniformly onto the adult rice leaves. After being cultured for 7 days in the greenhouse, the lesion symptoms were observed and photographed …”

“…After being cultured for 7 days in the greenhouse, the lesion symptoms were observed and photographed. 20 2.7. GFP-Labeled TMV Inoculation and Photographing.…”

“…The former T3SS encoded by more than 20 genes exemplified by hpa , hrc , and hrp genes is a highly conserved transmembrane secretion apparatus that mainly consists of a needle tip spanning the host cell membrane and a sophisticated supramolecular framework that mediates the passage of the secreted proteins across the bacterial inner and outer membrane. − Given the privileged characteristics and their correlative functions, T3SS and TALE proteins were widely recognized as the important targets for novel bactericide discovery via interacting bacterial virulence mechanisms. − Currently, plant bacterial diseases caused by various virulent pathogens are a huge obstacle to the global food security, and only a small amount of commercial agrochemicals were exploited to manage these intractable and ever-expanding epidemic diseases, such as copper/zinc preparations, antibiotics (examples of zhongshengmycin, kasugamycin, tetramycin, etc. ), bismerthiazol, and thiadiazole copper. − Depressingly, the quick development of chemoresistant pathogens and the achieved implacable field control efficiency have aggravated the complicated situation. , Therefore, excavating and developing novel molecular frameworks targeting the virulence factors of pathogens should be a feasible and promising plan for alleviating or eliminating the pathogenicity and rapid outbreak of plant bacterial diseases.…”

Transcriptome Analysis on the Mechanism of Ethylicin Inhibiting Pseudomonas syringae pv. actinidiae on Kiwifruit

“…The Psa flagella form was then detected by TEM according to the method reported by Zhou [28]. Psa bacterial suspensions (10 µL, OD 600 = 0.1) were added to an agar plate with nutrient broth medium containing different concentrations (0, 1.8, 3.6, and 5.4 µg/mL) of ethylicin at 28 • C and incubated for 24 h. Then, a piece of bacterial agar was picked using a copper mesh with a carbon support film and then stained with 1% phosphotungstic acid followed by sterile water rinsing.…”

Novel Cinnamic Acid Derivatives Containing the 1,3,4-Oxadiazole Moiety: Design, Synthesis, Antibacterial Activities, and Mechanisms

“…Cinnamic acid is a natural plant metabolite that is usually found in fruits, vegetables, and honey. , Cinnamic acid and its derivatives have diverse biological activities, such as herbicidal, fungicidal, , antiviral, insecticidal, and bactericidal activities. , Therefore, cinnamic acid derivatives are an up-and-coming class of lead compounds for new pesticides. Moreover, 1,3,4-oxadiazole has insecticidal, herbicidal, antiviral, nematicidal, antibacterial, − and antifungal activities, and it has an essential use in the creation of pesticides.…”