1430731-75-1Relevant academic research and scientific papers
Design and Discovery of Novel Antifungal Quinoline Derivatives with Acylhydrazide as a Promising Pharmacophore
Yang, Yu-Dong,He, Ying-Hui,Ma, Kun-Yuan,Li, Hu,Zhang, Zhi-Jun,Sun, Yu,Wang, Yu-Ling,Hu, Guan-Fang,Wang, Ren-Xuan,Liu, Ying-Qian
, p. 8347 - 8357 (2021)
Inspired by natural 2-quinolinecarboxylic acid derivatives, a series of quinoline compounds containing acylhydrazine, acylhydrazone, sulfonylhydrazine, oxadiazole, thiadiazole, or triazole moieties were synthesized and evaluated for their fungicidal activity. Most of these compounds exhibited excellent fungicidal activity in vitro. Significantly, compound 2e displayed the superior in vitro antifungal activity against Sclerotinia sclerotiorum, Rhizoctonia solani, Botrytis cinerea, and Fusarium graminearum with the EC50 values of 0.39, 0.46, 0.19, and 0.18 μg/mL, respectively, and were more potent than those of carbendazim (EC50, 0.68, 0.14, >100, and 0.65 μg/mL, respectively). Moreover, compound 2e could inhibit spore germination of F. graminearum. Preliminary mechanistic studies showed that compound 2e could cause abnormal morphology of cell walls and vacuoles, loss of mitochondrion, increases in membrane permeability, and release of cellular contents. These results indicate that compound 2e displayed superior fungicidal activities and could be a potential fungicidal candidate against plant fungal diseases.
Application of quinoline 2-site derivative in preparation of medicine for preventing and treating agricultural plant diseases
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Paragraph 0227-0229; 0239-0241, (2021/03/18)
The invention relates to the technical field of pesticide chemistry, discloses a new application of a quinoline 2-site derivative, and particularly relates to an application of the quinoline 2-site derivative in preparation of drugs for preventing and treating rape sclerotinia sclerotiorum, rhizoctonia solani, tomato botrytis cinerea, wheat fusarium graminearum and magnaporthe oryzae. The compounddisclosed by the invention is a small molecular compound which is easy to synthesize and simple in structure, and is expected to be developed into a novel agricultural bactericide.
Novel method of synthesizing various five membered heterocycles from an aryl tribromomethyl group
Tynebor, Robert,Millings, Elizabeth
, p. 1902 - 1908 (2013/05/21)
Synthesis of five membered heterocycles from an aryl tribromomethyl functional group is discussed. Exposing a tribromomethyl group to subsequent nucleophilic attacks by a 1,2-di-nucleophilic species promotes the cyclization of five membered heterocycles. Such heterocycles as oxadiazoles, thiadiazole, benzimidazole, benzothioazole, and benzoxazole were synthesized in moderate to good yields. Supplemental materials are available for this article. Go to the publisher's online edition of Synthetic Communications to view the free supplemental file.
