The Synthesis of (1,3,4-Oxadiazol-2-yl)Acrylic Acid Derivatives with Antibacterial and Protistocidal Activities
作者:L. D. Popov、A. A. Zubenko、L. N. Fetisov、Yu. D. Drobin、A. I. Klimenko、A. N. Bodryakov、S. A. Borodkin、I. E. Melkozerova
DOI:10.1134/s1068162018010132
日期:2018.3
A series of new 1,3,4-oxadiazol-2-yl-acrylic acids was synthesized by cyclization of 4-(2-R-hydrazino)- 4-oxo-2-butenic acids, and their antibacterial and protistocidal activities were studied. The p-substituted benzyl derivatives in the Z-form were shown to exhibit a high protistocidal activity, which exceeded that of the reference drug Baycox (toltrazuril) by several times, whereas the 3-hydroxy-2-naphthyl
4-(2-R-肼基)-4-氧代-2-丁烯酸环化合成了一系列新的1,3,4-恶二唑-2-基-丙烯酸,并研究了它们的抗菌和杀虫活性. Z 型的对位取代苄基衍生物显示出高杀原虫活性,超过参考药物 Baycox (toltrazuril) 的数倍,而 3-羟基-2-萘基衍生物,除了非常高的杀原生生物活性,也表现出中等的抗菌活性。