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以5-甲基-2-氨基苯甲酸和2-氨基苯甲酸为原料,通过酯化、酰化、环合再酯化的路线,合成了15个新型喹啉酮类衍生物(5a～5o),其结构均经红外、电喷雾串联质谱(ESI-MS)和核磁共振氢谱确证。初步的生物活性测定结果表明:在100 mg/L质量浓度下,化合物5c对6种供试病原菌均具有较好活性,抑制率在61.7%～92.9%之间;同时,化合物5i对棉花枯萎病菌Fusariumoxysporum f.sp.Vasinfectum的抑制率达96.1%,接近对照药剂嘧菌酯。
Fifteen novel quinolinone derivatives (5a ~ 5o) were synthesized from 5-methyl-2-aminobenzoic acid and 2-aminobenzoic acid via esterification, acylation and cyclization re-esterification. ). Their structures were confirmed by IR, ESI-MS and 1H-NMR. The preliminary bioassay results showed that compound 5c had good activity against 6 tested pathogenic bacteria at a concentration of 100 mg / L with the inhibition rates between 61.7% and 92.9%. At the same time, Fusarium oxysporum f.sp.Vasinfectum inhibition rate of 96.1%, close to the control agent azoxystrobin.