新型喹唑啉二酮乙酰腙类化合物的合成与抗菌活性研究（英文）

Syntheses and Antimicrobial Activities of Novel Quinazolin-2,4-dione Acetyl Hydrazones

以邻氨基苯甲酸甲酯为原料,经过甲基化、取代、关环、肼解反应制得含有喹唑啉二酮的中间体乙酰肼,进一步与多种取代醛和酮反应得到目标化合物9a^9t,所有化合物结构均经~1H NMR、^(13)C NMR和MS确证,并进行了体外抗菌活性测试。初步测试结果表明,所有化合物均对测试菌株有一定的抗菌活性,且部分化合物对测试菌株的抑制活性接近甚至优于现有药物硫酸链霉素和多抗霉素B。

Methyl 2-aminobenzoate was reacted with iodomethane to get methyl N-methylanthranilate. The key intermediate 2-（6-chloro-l-methyl-2,4-dioxo-1,2-dihydroquinazolin-3 （4H）-yl） acetohydrazide （7） was synthesized from methyl N-methylanthranilate via substitution, hydrolysis, cyclization and hydrazinolysis reactions. Then the key intermediate 7 was reacted with various substituted aromatic aldehydes or ketones to afford a series of quinazolin-2,4- dione acetyl hydrazone compounds 9a - 9t. The structures of all target compounds were characterized by means of 1 H NMR, 13C NMR and MS. The preliminary bioassay indicated that the as-synthesized compounds had certain antibacterial activities against the tested strains. At the same time, some of them showed better antibacterial activities than the commercial drugs such as streptomycin sulfate and polyoxin B.