新型4(3H)-喹唑啉酮席夫碱衍生物的合成及抗烟草花叶病毒活性（英文）

Synthesis and anti-TMV activity of novel 4(3H)-quinazolinone derivatives containing a Schiff base moiety

合成了一系列含席夫碱的4(3H)-喹唑啉酮衍生物,并采用半叶枯斑法测试了目标化合物抗烟草花叶病毒活性。结果表明:目标化合物在500μg/m L下对烟草花叶病毒的治疗活性为40.4%~53.1%,保护活性为51.2%~72.6%,钝化活性为46.0%~90.7%,其中,化合物3d的保护活性较好,有效抑制中浓度(EC_(50))值为203.89μg/m L,略优于商业化抗病毒剂宁南霉素(EC50值214.90μg/m L)。初步构效关系结果表明:在苯环的R^1及R^2位上引入吸电子基团有利于活性的提高。本研究结果表明,含席夫碱的4(3H)-喹唑啉酮衍生物能较好地控制烟草花叶病毒。

A series of 4（3H）-quinazolinone derivatives containing a Schiff base moiety were synthesized and their antiviral activity against tobacco mosaic virus（TMV） was evaluated using halfleaf method in vivo. Bioactivity results exhibited that the target compounds 3a-3x under 500 μg/m L displayed moderate to good anti-TMV activities with the curative activity, protection activity, and inactivation activity values of 40.4%-53.1%, 51.2%-72.6%, and 46.0%-90.7%, respectively. Especially,compound 3d showed excellent protection activity against TMV, with a half-maximal effective concentration（EC_（50）） value of 203.89 μg/m L, which was even superior to that of ningnanmycin（214.90μg/m L）. SAR analysis showed that compounds with electron-withdrawing groups at R^1 and R^2 positions displayed better anti-TMV activity. These results indicated that the series of 4（3H）-quinazolinone derivatives containing a Schiff base moiety can effectively control TMV.