A series of new fluorinated quinoline analogs were synthesized using Tebufloquin as the lead compound, 2-fluoroaniline, ethyl 2-methylacetoacetate, and substituted benzoic acid as raw materials. ...Their structures were confirmed by
H NMR,
C NMR, and HRMS. The compound 8-fluoro-2,3-dimethylquinolin-4-yl 4-(
-butyl)benzoate (
) was further determined by X-ray single-crystal diffraction. The antifungal activity was tested at 50 μg/mL, and the bioassay results showed that these quinoline derivatives had good antifungal activity. Among them, compounds
,
,
,
, and
exhibited good activity (>80%) against
, and compound
displayed good activity (80.8%) against
.
Flowering time has an important effect on regional adaptation and yields for crops. The tyrosine kinase-like (TKL) gene family is widely existed and participates in many biological processes in ...plants. Furthermore, only few TKLs have been characterized functions in controlling flowering time in wheat.
Here, we report that TaCTR1, a tyrosine kinase-like (TKL) gene, regulates flowering time in wheat. Based on identification and evolutionary analysis of TKL_CTR1-DRK-2 subfamily in 15 plants, we proposed an evolutionary model for TaCTR1, suggesting that occurrence of some exon fusion events during evolution. The overexpression of TaCTR1 caused early flowering time in transgenic lines. Transcriptomics analysis enabled identification of mass differential expression genes including plant hormone (ET, ABA, IAA, BR) signaling, flavonoid biosynthesis, phenolamides and antioxidant, and flowering-related genes in TaCTR1 overexpression transgenic lines compared with WT plants. qRT-PCR results showed that the expression levels of ethylene (ET) signal-related genes (ETR, EIN, ERF) and flowering-related genes (FT, PPD1, CO, PRR, PHY) were altered in TaCTR1-overexpressing wheat compared with WT plants. Metabonomics analysis showed that flavonoid contents were altered.
Thus, the results show that TaCTR1 plays a positive role in controlling flowering time by activating various signaling pathways and regulating flowering-related genes, and will provide new insights on the mechanisms of wheat flowering regulation.
Plants, as sessile organisms, uptake nutrients from the soil. Throughout their whole life cycle, they confront various external biotic and abiotic threats, encompassing harmful element toxicity, ...pathogen infection, and herbivore attack, posing risks to plant growth and production. Plants have evolved multifaceted mechanisms to cope with exogenous stress. The element defense hypothesis (EDH) theory elucidates that plants employ elements within their tissues to withstand various natural enemies. Notably, essential and non-essential trace metals and metalloids have been identified as active participants in plant defense mechanisms, especially in nanoparticle form. In this review, we compiled and synthetized recent advancements and robust evidence regarding the involvement of trace metals and metalloids in plant element defense against external stresses that include biotic stressors (such as drought, salinity, and heavy metal toxicity) and abiotic environmental stressors (such as pathogen invasion and herbivore attack). We discuss the mechanisms underlying the metals and metalloids involved in plant defense enhancement from physiological, biochemical, and molecular perspectives. By consolidating this information, this review enhances our understanding of how metals and metalloids contribute to plant element defense. Drawing on the current advances in plant elemental defense, we propose an application prospect of metals and metalloids in agricultural products to solve current issues, including soil pollution and production, for the sustainable development of agriculture. Although the studies focused on plant elemental defense have advanced, the precise mechanism under the plant defense response still needs further investigation.
In poplar cultivation, continuous cropping obstacles affect wood yield and soil-borne diseases, primarily due to structural changes in microbes and fungus infection. The bacterium
BJS-1-3 has strong ...antagonistic properties against pathogens that were isolated from the rhizosphere soil of poplars. Poplar rhizospheres were investigated for the effects of
BJS-1-3 on microbial communities. Three successive generations of soil were used to replant poplar seedlings. BJS-1-3 inoculated poplars were larger, had higher plant height and breast height diameter, and had a greater number of total and culturable bacteria than non-inoculated controls.
BJS-1-3 inoculated poplar rhizospheres were sequenced, utilizing the Illumina MiSeq platform to analyze changes in diversity and structure. The fungi abundance and diversity in the BJS-1-3 rhizosphere were significantly lower than in the control rhizosphere. In comparison to the control group,
sp. constituted 2.87% and 2.38% of the total bacterial community, while
sp. constituted 2.06% and 6.00% of the total fungal community. Among the potential benefits of
BJS-1-3 in poplar cultivation is that it enhances rhizosphere microbial community structure and facilitates the growth of trees.
In order to explore novel nematicidal and fungicidal lead compounds, two series of target compounds were designed and synthesized by introducing sulfide and sulfone substructures into fluopyram. The ...bioassays displayed that most compounds showed excellent nematicidal activities at 200 μg/mL in comparison with fluopyram. In terms of fungicidal activity, compound I-9 exhibited almost comparable inhibition rates to that of fluopyram, whose molecular docking simulation indicated the presence of the amide and its ortho-fluorinated groups had an important role on the fungicidal activity.
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In recent years, the damage caused by soil nematodes has become increasingly serious; however, the varieties and structures of the nematicides available on the market are deficient. Fluopyram, a succinate dehydrogenase inhibitor (SDHI) fungicide developed by Bayer AG in Germany, has been widely used in the prevention and control of soil nematodes due to its high efficiency and novel mechanism of action. In this paper, two series of novel target compounds were designed and synthesized with nematicidal and fungicidal fluopyram as the molecular skeleton in order to introduce sulfide and sulfone substructures. The structures were identified and characterized by 1H nuclear magnetic resonance (NMR), 13C NMR, and high-resolution mass spectrometer (HRMS). The bioassays revealed that most of the compounds showed excellent nematicidal activities at 200 µg·mL−1 in comparison with fluopyram, while the nematode mortality rate dropped sharply at 100 µg·mL−1, except for compounds I-11 and II-6. In terms of fungicidal activity, compound I-9 was discovered to have an excellent inhibitory rate, and a molecular docking simulation was performed that can provide important guidance for the design and exploration of efficient fungicidal lead compounds.
Structural optimization based on natural products has become an effective way to develop new fungicides, which provides important guiding significance for practicing the new development concept and ...promoting the green development of pesticides. In this project, the target compounds containing 4-quinolone and piperazine substructures based on waltherione F were synthesized through the combination of the fungicidal amide lead compound
X
-
I
-
4
discovered in our previous work and various of fungicidal piperazine derivatives. Screening of their biological activities suggested that products
I
-
3
,
I
-
5
,
II
-
3
,
II
-
7
,
II
-
10
,
II
-
11
and
II
-
13
displayed higher inhibition rates against
Rhizoctonia solani
than other tested compounds. The in vitro cellular cytotoxicity assay revealed that compounds
II
-
6
and
II
-
11
exhibited higher cytotoxicity against HepG2 than other tested compounds. The fluorescence characteristics investigation showed that the absolute fluorescence QY value of the methanol solution of the compound
I
-
6
was higher than those of
I
-
2
,
I
-
3
,
I
-
7
and
I
-
8
, which was further elucidated by TD-DFT.
Graphical abstract
The cultivation of poplar trees is hindered by persistent cropping challenges, resulting in reduced wood productivity and increased susceptibility to soil-borne diseases. These issues primarily arise ...from alterations in microbial structure and the infiltration of pathogenic fungi. To investigate the impact on soil fertility, we conducted an analysis using soil samples from both perennial poplar trees and three successive generations of continuously cropped poplar trees. The quantity and community composition of bacteria and fungi in the rhizosphere were assessed using the Illumina MiSeq platform. The objective of this study is to elucidate the impact of continuous cropping challenges on soil fertility and rhizosphere microorganisms in poplar trees, thereby establishing a theoretical foundation for investigating the mechanisms underlying these challenges. The study found that the total bacteria in the BT group is 0.42 times higher than the CK group, and the total fungi is 0.33 times lower than the CK group. The BT and CK groups presented relatively similar bacterial richness and diversity, while the indices showed a significant (
< 0.05) higher fungal richness and diversity in the CK group. The fractions of
were 2.22% and 2.41% in the BT and CK groups, respectively. There was a 35.29% fraction of
in the BT group, whereas this was barely observed in the CK group. The fractions of
were 26.25% and 5.99%, respectively in the BT and CK groups. Modifying the microbial community structure in soil subjected to continuous cropping is deemed as the most effective approach to mitigate the challenges associated with this agricultural practice.
To further explore the structure-activity relationship(SAR) of amide bridge moeity of anthranilic diamides derivatives, a series of
N
-pyridylpyrazole derivatives was designed, synthesized and their ...biological activities were evaluated. The chemical structures of novel target compounds were confirmed by
1
H nuclear magnetic resonance (NMR),
13
C NMR and elemental analyses(EA). Bioassay results of insecticidal activity demonstrated that the target compound
6
h displayed 70% lethality rate against oriental armyworms at 200 mg/L. Moreover, most compounds displayed moderate to excellent antifungicidal activities against
Fusarium oxysporum f. sp
.
cucumerinum
,
Cercospora arachidicola Hori
,
Botryosphaeria dothidea
,
Alternaria solani
,
Gibberella zeae
and
Phytophthora capsici
at 50 mg/L. In particular, compound
6
e showed 61.5% and 92.3% inhibition rate against
Cercospora arachidicola Hori
and
Botryosphaeria dothidea
, which was superior to the commercial positive control
Chlorothalonil
. These results will provide a potential clue for exploring novel high-effective agrochemicals.
In order to develop a novel herbicide containing the 2,1-benzothiazine motif, a series of 3-acetyl-4-hydroxy-2,1-benzothiazine derivatives was synthesized. All the target compounds were confirmed by
...1
H NMR,
13
C NMR, and high-resolution mass spectrometry(HRMS). In addition, the crystal structure of compound T27 was determined by single crystal X-ray diffraction. The bioassay results showed that some of the 3-acetyl-4-hydroxy-2,1-benzothiazine derivatives(T13, T15, T22, and T24) showed good herbicidal activity at a dosage of 100 μg/mL. Among them, compounds T22 and T24 showed promising post-emergent herbicidal activities against
Brassica campestris
and
Amaranthus retroflexus
even at a dosage of 375 g/ha(1 ha=10
4
m
2
) in the greenhouse test. Studies on the structure-activity relationship demonstrated that the type of acetyl group played an important role in the herbicidal activity, and that the introduction of a phenoxyacetyl group at the 3-position of 2,1-benzothiazine was beneficial in improving the herbicidal activity. The present study also indicated that 3-phenoxyacetyl-4-hydroxy-2,1-benzothiazine could be a potential lead compound for further development of novel 2,1-benzothiazine-containing herbicides.
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