128073-03-0Relevant articles and documents
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 (2021/08/16)
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.
Synthetic method of novel monoamine oxidase inhibitor (malabemide)
-
Paragraph 0020-0021, (2019/03/26)
The invention discloses a synthetic method of a novel monoamine oxidase inhibitor (malabemide). According to the synthetic method, 5-chloro-2-pyridine carboxylic acid is taken as the primary raw material, after acyl-chlorination reactions, 5-chloro-2-pyridine formyl chloride is generated; then after amidation reactions, 5-chloro-N-(2-hydroxyethyl)-2-pyridine formyl chloride is generated, and finally 5-chloro-N-(2-hydroxyethyl)-2-pyridine formyl chloride and morpholine carry out condensation reactions to generate malabemide. Ethanolamine, 5-chloro-2-pyridine carboxylic acid, and morpholine aretaken as the main raw materials to prepare the novel monoamine oxidase inhibitor (malabemide); and the raw materials are easily available. The synthetic method has the advantages of simple operation,high product purity, and high yield, and is suitable for industrial production.
New compound Malabemide, preparation method and uses thereof
-
Paragraph 0024; 0027-0028, (2018/11/03)
The invention discloses a new compound Malabemide with a molecule formula represented by a formula h, a preparation method and pharmaceutical applications thereof, wherein ethanolamine and 5-chloro-2-pyridinecarboxylic acid are used as starting raw materials, corresponding intermediates 2-bromoethylamine hydrobromide and 5-chloro-2-pyridinecarbonyl chloride are respectively synthesized, and are subjected to a reaction to generate 5-chloro-N-(2-bromoethyl)-2-pyridinecarboxamide, and the 5-chloro-N-(2-bromoethyl)-2-pyridinecarboxamide and morpholine are subjected to condensation to generate Malabemide h. According to the present invention, the preparation method has characteristics of easily available raw materials, simple operation, good product purity and high yield, and is suitable for industrial production. The formula h is defined in the specification.