摘要
我们已报道了1-芳基-4-乙氧羰基-5-氨基-1,2,3-连三唑类衍生物(1)的合成及抗菌活性,为研究药物构效关系,我们利用1的酰肼3同甲酸反应,制得了尚未报道的5-醛胺基-1-芳基-1,2,3-连三唑[2,3-d]嘧啶-4-酮(4_(a-c))及5-氨基-6-羟基-7H-1-(间硝基)苯基-1,2,3-连三唑[2,3-d]嘧啶-4-酮(5_d).并观察了它们对枯草杆菌,金黄色葡萄球菌等繁殖的抑制作用。
5-Formylamino-1-aryl-1,2,3-triazolo(2, 3-d)pyrimidin-4-one (4s,b,c) and 5-amino-6-hydroxyl-7H-1-(m-nitrophenyl)-1,2,3-triazolo(2,3-d)pyrimidin-4-one (5d) have been synthesised fromthe reaction of 1-aryl-4-carbonhydrazide-5-amino-1, 2, 3-triazoles 3a,b,c,d prepared by hydrazinolysis of either 1-aryl- 4- ethoxycarbonyl- 5- amino- 1, 2, 3-triazoles 1a,b,c,d or their benzoylamino derivatives (2a,d), with an excess of formic acid under the fluxing condition. The structures of all heterocyclic compounds were confirmed by elemental analysis, IR,1H NMR, MS, and the inhibiting effects on B. Substilis; E. coli; E. aerogenes;S. aureus were also screened.
出处
《高等学校化学学报》
SCIE
EI
CAS
CSCD
北大核心
1991年第10期1344-1346,共3页
Chemical Journal of Chinese Universities
关键词
连三唑并嘧啶酮
合成
抗菌活性
Triazolopyrimidinone, Synthesis, Antibacterial activity
