- Expedient discovery for novel antifungal leads: 1,3,4-Oxadiazole derivatives bearing a quinazolin-4(3H)-one fragment
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Developing novel fungicide candidates are intensively promoted by the rapid emergences of resistant fungi that outbreak on agricultural production. Aiming to discovery novel antifungal leads, a series of 1,3,4-oxadiazole derivatives bearing a quinazolin-4(3H)-one fragment were constructed for evaluating their inhibition effects against phytopathogenic fungi in vitro and in vivo. Systematically structural optimizations generated the bioactive molecule I32 that was identified as a promising inhibitor against Rhizoctonia solani with the in vivo preventative effect of 58.63% at 200 μg/mL. The observations that were captured by scanning electron microscopy and transmission electron microscopy demonstrated that the bioactive molecule I32 could induce the sprawling growth of hyphae, the local shrinkage and rupture on hyphal surfaces, the extreme swelling of vacuoles, the striking distortions on cell walls, and the reduction of mitochondria numbers. The above results provided an indispensable complement for the discovery of antifungal lead bearing a quinazolin-4(3H)-one and 1,3,4-oxadiazole fragment.
- Chai, Jianqi,Chen, Min,Jin, Fei,Kong, Xiangyi,Wang, Xiaobin,Xue, Wei,Yang, Chunlong
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- Design, synthesis and bioactivity evaluation of novel thioether derivatives containing a sulfonohydrazide moiety
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A series of novel thioether derivatives containing a sulfonohydrazide moiety were synthesized and determined using 1H NMR, 13C NMR, HRMS, and elemental analysis. Their in vitro antibacterial activities against Xanthomonas oryzae pv.
- Li, Pei,Zhou, Junliang,Liu, Yan,Wang, Xiang
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p. 976 - 980
(2020/07/03)
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- Disulfide derivative containing 1,3,4-oxa(thia)diazole and preparation method and application of derivative
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The invention discloses a disulfide derivative containing 1,3,4-oxa(thia)diazole and a preparation method and application of the derivative. The disulfide derivative has the following general formula (as shown in the specification), wherein R1 is selected from 4-chlorphenyl, 4-fluoro-phenyl, benzyl, 4-chloro-benzyl and other substituent groups; R2 is selected from methyl, ethyl, benzyl, 4-chloro-benzyl, ethyl acetate and other substituent groups; X is O or S. The disulfide derivative disclosed by the invention can serve as a medicine or agent for killing nematodes and inhibiting crop bacterium diseases.
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Paragraph 0028
(2017/07/08)
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- 2, 5-substituent-1, 3, 4-oxadiazole thioether derivative, preparation method and application thereof
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The invention discloses a chalcone derivative containing 1, 1-dichloropropene, a preparation method and application thereof. The derivative has a general formula (I) shown as the specification, wherein R1 is selected from 4-chlorphenyl, 4-fluorophenyl, benzyl, 4-chlorobenzyl and other substituents; R2 is selected from methyl, ethyl, benzyl, 4-chlorobenzyl, ethyl acetate and other substituents. The derivative provided by the invention has the characteristics of simple structure, simple preparation process and low production cost, and has good activity to rice bacterial leaf blight, rice baeterial leaf streak pathogens and caenorhabditis elegans.
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Paragraph 0017
(2017/01/02)
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