Synthesis and antifungal activity of substituted salicylaldehyde hydrazones, hydrazides and sulfohydrazides
作者:Gregory L. Backes、Donna M. Neumann、Branko S. Jursic
DOI:10.1016/j.bmc.2014.07.022
日期:2014.9
Efficient synthetic procedures for the preparation of acid hydrazines and hydrazides were developed by converting the corresponding carboxylic acid into the methyl ester catalyzed by Amberlyst-15, followed by a reaction with hydrazine monohydrate. Sulfohydrazides were prepared from the corresponding sulfonyl chlorides and hydrazine monohydrate. Both of these group of compounds were condensed with substituted
通过将相应的羧酸转化成由Amberlyst-15催化的甲酯,然后与一水合肼反应,开发出了用于制备酰肼和酰肼的有效合成方法。磺酰肼由相应的磺酰氯和肼一水合物制备。使用梯度浓缩方法将这两组化合物与取代的水杨醛缩合,生成大量的,、酰肼和磺酰肼类似物库。制备的类似物的抗真菌活性表明,水杨醛hydr和酰肼是有效的真菌生长抑制剂,几乎没有哺乳动物细胞毒性,这使这些类似物成为未来治疗发展的新靶标。