Design, synthesis, X‐ray crystal structure, and antifungal evaluation of new acetohydrazide derivatives containing a 4‐thioquinazoline moiety DOI

Guangmin Tian,

Mingyan Yi,

T F Yan

и другие.

Pest Management Science, Год журнала: 2024, Номер unknown

Опубликована: Дек. 4, 2024

Abstract BACKGROUND To find efficient agricultural fungicides, 29 new 4‐thioquinazoline‐containing acetohydrazide derivatives were prepared and tested for their fungicidal properties. RESULTS All of the target compounds characterized by 1 H 13 C nuclear magnetic resonance high‐resolution mass spectrometry techniques, molecular structure compound A2 was verified single‐crystal X‐ray diffraction measurement. The experimental results revealed that many from this series had impressive inhibition efficacies in vitro against fungi. For example, A25 identified as best agent Rhizoctonia solani with an EC 50 (half‐maximal effective concentration) value 0.66 μg mL −1 , superior to those commercial fungicides chlorothalonil, carbendazim boscalid. Additionally, displayed favorable protection curative activities vivo rice sheath blight caused R . Antifungal mechanistic studies on indicated exerted its strong anti ‐R effects probably through fungal succinate dehydrogenase activity [half‐maximal inhibitory concentration (IC ) = 4.88 μ m ] impairment cell membrane integrity, based enzymatic bioassays, docking studies, scanning transmission electron microscopy observations. CONCLUSION Acetohydrazide containing 4‐thioquinazoline moiety potential be employed lead developing more near future. © 2024 Society Chemical Industry.

Язык: Английский

Design, synthesis and antifungal activity of arylhydrazine analogs containing diphenyl ether fragments DOI

Longjian Qiu,

Yaru Liu, Lijuan Zhang

и другие.

Pest Management Science, Год журнала: 2024, Номер unknown

Опубликована: Окт. 28, 2024

Abstract BACKGROUND Succinate dehydrogenase (SDH) represents a critical target in the development of novel fungicides. To address growing issue resistance and safeguard economic viability agricultural production, pursuit new succinate inhibitors (SDHIs) has emerged as significant focus contemporary research. RESULTS In this project, 32 arylhydrazine derivatives containing diphenyl ether structural units were synthesized evaluated for their fungicidal activities against Rhizoctonia solani , Sclerotinia sclerotiorum Alternaria alternata Gibberella zeae Colletotrichum gloeosporioides . an vitro activity assay, compound D6 showed inhibitory R. with half‐maximum effective concentration (EC 50 ) 0.09 mg L −1 The vivo demonstrated that inhibited by 95.39% rice leaves, which was significantly better than boscalid (85.76%). results SDH enzyme molecular docking simulation, mitochondrial membrane potential cytoplasmic release studies morphological observations not only had activity, but also affected integrity mycelium. CONCLUSION Bioactivity screening validation mechanism action indicated potentially unique SDHI, acting on while affecting cell permeability, deserved further study. © 2024 Society Chemical Industry.

Язык: Английский

Процитировано

0
Design, Synthesis, and Biological Evaluations of 5-aryl-pyrazole-3-carboxamide Derivatives as Selective CB2 Receptor Agonists for the Treatment of Colitis DOI

Beier Jiang,

Ying He, Jie Chen

и другие.

European Journal of Medicinal Chemistry, Год журнала: 2024, Номер 283, С. 117117 - 117117

Опубликована: Дек. 2, 2024

Язык: Английский

Процитировано

0
Design, synthesis, X‐ray crystal structure, and antifungal evaluation of new acetohydrazide derivatives containing a 4‐thioquinazoline moiety DOI

Guangmin Tian,

Mingyan Yi,

T F Yan

и другие.

Pest Management Science, Год журнала: 2024, Номер unknown

Опубликована: Дек. 4, 2024

Abstract BACKGROUND To find efficient agricultural fungicides, 29 new 4‐thioquinazoline‐containing acetohydrazide derivatives were prepared and tested for their fungicidal properties. RESULTS All of the target compounds characterized by 1 H 13 C nuclear magnetic resonance high‐resolution mass spectrometry techniques, molecular structure compound A2 was verified single‐crystal X‐ray diffraction measurement. The experimental results revealed that many from this series had impressive inhibition efficacies in vitro against fungi. For example, A25 identified as best agent Rhizoctonia solani with an EC 50 (half‐maximal effective concentration) value 0.66 μg mL −1 , superior to those commercial fungicides chlorothalonil, carbendazim boscalid. Additionally, displayed favorable protection curative activities vivo rice sheath blight caused R . Antifungal mechanistic studies on indicated exerted its strong anti ‐R effects probably through fungal succinate dehydrogenase activity [half‐maximal inhibitory concentration (IC ) = 4.88 μ m ] impairment cell membrane integrity, based enzymatic bioassays, docking studies, scanning transmission electron microscopy observations. CONCLUSION Acetohydrazide containing 4‐thioquinazoline moiety potential be employed lead developing more near future. © 2024 Society Chemical Industry.

Язык: Английский

Процитировано

0