摘要
为了快速获得具有杀菌活性的先导化合物,按照苯环上取代基的性质,将18个N-取代苯基-2-羟基环己烷基磺酰胺分成8个大小不等的原料库(A),分别与过量的2-乙氧基乙酰氯(B1)和4-氟苯甲酰氯(B2)反应,获得16个2-酰氧基环己烷基磺酰胺类组合库。通过气相色谱-质谱联用仪(GC-MS)和红外光谱分析了组合库中36个化合物的结构和含量。以番茄灰霉病菌Botrytis cinerea Pers.为供试靶标,菌丝生长速率法测试结果表明:当A的苯环上含有多个Cl或CF3等吸电子基团时,与B1反应生成的组合库的活性普遍较高,其中活性组合库A5B1、A6B1和A7B1的杀菌活性均高于对照药剂腐霉利;黄瓜离体叶片试验表明,活性组合库A6B1和A7B1的防效也与腐霉利相当。在组合库生物活性筛选中化合物的结构、含量和数量是影响筛选结果的3个因素,其中结构为主要因素。
In order to rapidly prepare novel lead compounds of fungicides,18 N-substituted phenyl-2-hydroxycyclohexylsulfonamides w ere divided into 8 material libraries（ A） basing on the type of substituents on the phenyl ring. In total,36 compounds in 16 liquid phase combinatorial libraries w ere obtained by the reaction of A w ith 2-ethoxyacetyl chloride（ B1） or 4-fluorobenzoylchloride（ B2）.Structure and content of each compound w ere determined by GC-M S and IR. Activities of combinatorial libraries formed by the reaction of A bearing electron w ithdraw ing group,such as Cl or CF3,on the phenyl ring and B1 w ere generally higher basing on the mycelial grow th rate method of Botrytis cinerea Pers. In particular,A5B1,A6B1 and A7B1are more active than procymidone. The A6B1 and A7B1show ed similar effect as procymidone in detached leaves of cucumber. Activities of combinatorial libraries w ere influenced by compound structure,content and quantity and structure w as the major parameters.
出处
《农药学学报》
CAS
CSCD
北大核心
2014年第6期651-658,共8页
Chinese Journal of Pesticide Science
基金
国家自然科学基金资助项目(31101466)
辽宁省高等学校优秀人才支持计划项目(LJQ2012059)
沈阳农业大学天柱山英才基金
关键词
磺酰胺
羧酸酯
组合化学
灰霉病菌
杀菌活性
结构-活性关系
sulfonamides
carboxylic ester
combinatorial chemistry
Botrytis cinerea
fungicidal activity
structure-activity relationship
