农药学学报
農藥學學報
농약학학보
CHINESE JOURNAL OF PESTICIDE SCIENCE
2014年
3期
252-258
,共7页
崔紫宁%梁志彬%田芳%刘诗胤%闫晓静
崔紫寧%樑誌彬%田芳%劉詩胤%閆曉靜
최자저%량지빈%전방%류시윤%염효정
5-苯基2-呋喃%5-肼基-3(2H)哒嗪酮%酰肼%合成%杀虫活性%杀菌活性
5-苯基2-呋喃%5-肼基-3(2H)噠嗪酮%酰肼%閤成%殺蟲活性%殺菌活性
5-분기2-부남%5-정기-3(2H)달진동%선정%합성%살충활성%살균활성
5-phenyl-2-furan%5-hydrazino-pyridazin-3(2H)-one%hydrazide%synthesis%insecticidal activity%fungicidal activity
为探索新的农药先导化合物,经取代苯基呋喃甲酰氯与5-肼基-3(2H)哒嗪酮反应,得到15个未见文献报道的含呋喃环3(2H)哒嗪酮类化合物,其结构均通过了红外光谱、核磁共振氢谱和元素分析确认。初步生物活性测定结果表明,目标化合物具有良好的杀菌活性,但杀虫活性较弱。其中化合物3 k在50 mg/L时对灰霉病菌的抑制率为86.29%±1.51%,与对照药剂腐霉利相当。初步的构效关系研究结果显示,苯环上取代基的种类和位置对杀菌活性有重要影响。
為探索新的農藥先導化閤物,經取代苯基呋喃甲酰氯與5-肼基-3(2H)噠嗪酮反應,得到15箇未見文獻報道的含呋喃環3(2H)噠嗪酮類化閤物,其結構均通過瞭紅外光譜、覈磁共振氫譜和元素分析確認。初步生物活性測定結果錶明,目標化閤物具有良好的殺菌活性,但殺蟲活性較弱。其中化閤物3 k在50 mg/L時對灰黴病菌的抑製率為86.29%±1.51%,與對照藥劑腐黴利相噹。初步的構效關繫研究結果顯示,苯環上取代基的種類和位置對殺菌活性有重要影響。
위탐색신적농약선도화합물,경취대분기부남갑선록여5-정기-3(2H)달진동반응,득도15개미견문헌보도적함부남배3(2H)달진동류화합물,기결구균통과료홍외광보、핵자공진경보화원소분석학인。초보생물활성측정결과표명,목표화합물구유량호적살균활성,단살충활성교약。기중화합물3 k재50 mg/L시대회매병균적억제솔위86.29%±1.51%,여대조약제부매리상당。초보적구효관계연구결과현시,분배상취대기적충류화위치대살균활성유중요영향。
A series of novel pyridazin-3(2H)-one derivative with 5-phenyl-2-furan were designed and synthesized. All the title compounds were characterized by IR,1 H NMR and elemental analysis. Bioassay indicated that the title compounds had low insecticidal effects on Plutella xylostella, Mythimna separate and Culex pipiens pallens, but most compounds exhibited good fungicidal activities against Botrytis cinerea, Fusarium oxysporum and Corynespora cassiicola. In particular, compounds 3k showed considerable activity (86.29% ± 1.51%) against B. cinerea at 50 mg/L, which was equal to the fungicide procymidone. The preliminary structure-activity relationship showed that the difference of R group affected the fungicidal activity.