申请人:Meiji Seika Kaisha, Ltd.
公开号:EP1054011A1
公开(公告)日:2000-11-22
Disclosed are novel compounds useful for prevention or control of diseases derived from fungi, a process for producing the same, and novel antifungal agents using the novel compounds. The compounds useful for prevention and treatment of diseases derived from fungi according to the present invention include novel compounds represented by formula (I). The compounds represented by formula (I) have potent antifungal activity against diseases derived from fungi, and do not have phytotoxicity to mammals and agricultural and garden plants, from which diseases should be eliminated, and, even when applied to agricultural and garden plants, have high photostability.
wherein
R1 represents isobutyryl, tigloyl, isovaleryl, or 2-methylbutanoyl;
R2 represents a hydrogen atom, an aromatic carboxylic acid residue, or a protective group of amino; and R3 represents a hydrogen atom, nitro, amino, acylamino, or N,N-dialkylamino, excluding the case where, when R1 represents isobutyryl, tigloyl, isovaleryl, or 2-methylbutanoyl with R3 representing a hydrogen atom, R2 represents a 3-hydroxypicolinic acid residue, 3-hydroxy-4-methoxypicolinic acid residue, or a 3,4-dimethoxypicolinic acid residue.
本发明公开了用于预防或控制由真菌引起的疾病的新型化合物、生产新型化合物的工艺以及使用新型化合物的新型抗真菌剂。根据本发明,用于预防和治疗由真菌引起的疾病的化合物包括由式(I)代表的新型化合物。式 (I) 所代表的化合物对真菌引起的疾病有很强的抗真菌活性,对哺乳动物和农业及园林植物无植物毒性,可消除这些植物的疾病,即使应用于农业和园林植物,也具有很高的光稳定性。
其中
R1 代表异丁酰基、丁酰基、异戊酰基或 2-甲基丁酰基;
R2 代表氢原子、芳香族羧酸残基或氨基保护基团;以及 R3 代表氢原子、硝基、氨基、酰氨基或 N,N-二烷基氨基,但不包括以下情况:当 R1 代表异丁酰基、虎杖酰基、异戊酰基或 2-甲基丁酰基且 R3 代表氢原子时,R2 代表 3-羟基吡啶羧酸残基、3-羟基-4-甲氧基吡啶羧酸残基或 3,4-二甲氧基吡啶羧酸残基。