N′-mono- and N, N′-diacyl derivatives of benzyl and arylhydrazines as contact insecticides against adult Anopheles gambiae

Clements, Joseph S.; Islam, Rafique; Sun, Bingrong; Tong, Fan; Gross, Aaron D.; Bloomquist, Jeffrey R.; Carlier, Paul R.

doi:10.1016/j.pestbp.2017.10.001

Cited by 10 publications

(16 citation statements)

References 24 publications

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“…The HEK-293 cell line is used in research on the potassium channel in insects. 6,40 Due to the lack of cell lines of P. xylostella with high transfection efficiency, HEK-293 cells were used to explore the pharmacological characterization of PxShab in this study. Although the sensitivity of PxShab to high concentration (10 mM) nonspecific potassium channel inhibitors, 4-AP, and TEA, was different (Fig.…”

Section: Discussionmentioning

confidence: 99%

Identification and pharmacological characterization of the voltage‐gated potassium channel Shab in diamondback moth, Plutella xylostella

Huo

Zhu

et al. 2022

Pest Management Science

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Background: Voltage-gated potassium channel Kv2 is the primarily delayed rectifier in insect nerves and muscles involved in several crucial biological processes, including action potential regulation, photoreceptor performance, and larval locomotor. It is a potential molecular target for developing a novel pesticide for mosquitos. However, there are few studies on the Kv2 channel in agricultural pests.Results: The only ⊍-subunit gene of the Kv2 channel in Plutella xylostella (L.), PxShab, was cloned, and its expression profile was analyzed. The relative expression level of PxShab was highest in the pupal stage of both sexes and male adults but lowest in female adults. Meanwhile, PxShab had the highest expression in the head in both larvae and adults. Then, PxShab was stably expressed in the HEK-293 T cell line. Whole cell patch clamp recordings showed an outward current whose current-voltage relationship conformed to a typical delayed-rectifier potassium channel. 20 ∼M quinidine could effectively inhibit the potassium current, while the channel was insensitive to 4-AP even at 10 mM. Several potential compounds and botanical pesticides were assessed, and carvedilol (IC 50 = 0.53 ∼M) and veratrine (IC 50 = 2.22 ∼M) had a good inhibitory effect on the channel. Conclusion:This study revealed the pharmacological properties of PxShab and screened out several high potency inhibitors, which laid the foundation for further functional research of PxShab and provides new insight into designing novel insecticides.

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Section: Discussionmentioning

confidence: 99%

Identification and pharmacological characterization of the voltage‐gated potassium channel Shab in diamondback moth, Plutella xylostella

Huo

Zhu

et al. 2022

Pest Management Science

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“…Each treatment was repeated three times with 30 adult aphids each time. 38 Systemic Insecticidal Activity of Compound I-9 against M. persicae. The inward-absorbent activity of compound I-9 in the laboratory was determined using the liquid culture method.…”

Section: ■ Materials and Methodsmentioning

confidence: 99%

“…The mortality rates were calculated 24 h after treatment. Each treatment was repeated three times with 30 adult aphids each time …”

Section: Methodsmentioning

confidence: 99%

Synthesis, Crystal Structure, and Insecticidal Activity of Steroidal N-Piperidone

Jiang

et al. 2022

J. Agric. Food Chem.

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A series of steroidal piperidone derivatives were synthesized, and their agricultural activities were evaluated against Myzus persicae, Aphis citricola, Brevicoryne brassicae Linn., and Bemisia tabaci (Gennadius). Most of the tested compounds exhibited potent insecticidal activity against these four pests. Compound I-9 displayed the highest activity against M. persicae, A. citricola, and Brevicoryne brassicae, with LC 50 values of 11.3, 10.4, and 8.68 μg/mL, respectively. The mode of action test indicated that these derivatives had superior contact and systemic insecticidal activity against M. persicae. In addition, we initially explored whether the foregut and midgut might be the action sites of the target derivatives against M. persicae. Furthermore, a field trial showed that the control of compound I-9 was similar to that of acetamiprid against M. persicae, at a dose of 50 μg/mL; the control rates were 97.8 and 99.2% after 14 and 21 days, respectively. The structure−activity relationship of these analogues provided some important insights for the discovery and development of new insecticides to solve the current pesticide resistance crisis.

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“…In our study, we focused on the diarylhydrazide compounds that have been found to show insecticidal and 15-lipoxygenase inhibitory effects, , although the research on their antifungal activities is still limited. , Forty-five kinds of diarylhydrazide compounds were afforded and screened for in vitro antifungal activities against eight strains of phytopathogenic fungi ( Alternaria alternate , Alternaria brassicae , Alternaria solani , Botryosphaeria dothidea , Fusarium bulbigenum , Fusarium graminearum , Fusarium solani , and Pyricularia oryza ). The systemic structure–activity relationship was deduced based on the experimental results of antifungal activities.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Structure–Activity Relationship, and Mechanism of a Series of Diarylhydrazide Compounds as Potential Antifungal Agents

Liu

et al. 2023

J. Agric. Food Chem.

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A series of simple diarylhydrazide derivatives (45 examples) were well-designed, prepared, and screened for their antifungal activities both in vitro and in vivo. Bioassay results suggested that all designed compounds had significant activity against Alternaria brassicae (EC 50 = 0.30−8.35 μg/mL). Among of them, 2c, as the highest activity compound, could effectively inhibit the growth of plant pathogens Pyricularia oryza, Fusarium solani, Alternaria solani, Alternaria brassicae, and Alternaria alternate and was more potent than carbendazim and thiabendazole. 2c showed almost 100% protection at 200 μg/mL in vivo activity against A. solani in tomato. Moreover, 2c did not affect the germination of cowpea seed and the growth of normal human hepatocytes. The preliminary mechanistic exploration documented that 2c could result in the abnormal morphology and irregular structure of the cell membrane, destroy the function of mitochondria, increase the reactive oxygen species, and inhibit the proliferation of hypha cell. The above results manifested that target compound 2c could be a potential fungicidal candidate against phytopathogenic diseases for its excellent fungicidal activities.

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N′-mono- and N, N′-diacyl derivatives of benzyl and arylhydrazines as contact insecticides against adult Anopheles gambiae

Cited by 10 publications

References 24 publications

Identification and pharmacological characterization of the voltage‐gated potassium channel Shab in diamondback moth, Plutella xylostella

Identification and pharmacological characterization of the voltage‐gated potassium channel Shab in diamondback moth, Plutella xylostella

Synthesis, Crystal Structure, and Insecticidal Activity of Steroidal N-Piperidone

Synthesis, Structure–Activity Relationship, and Mechanism of a Series of Diarylhydrazide Compounds as Potential Antifungal Agents

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