摘要
为了制备天然产物基抑菌剂,以去氢枞酸为原料,设计并合成得到20个新型去氢枞酸基B环并噻唑-酰胺化合物(Ⅵa^t)。初步探索了合成条件,并利用FTIR、1HNMR、13CNMR和ESI-MS对目标产物进行了结构表征。还测试了化合物对黄瓜枯萎病菌、番茄早疫病菌、苹果轮纹病菌、花生褐斑病菌和小麦赤霉病菌等5种植物病原菌的抑菌活性。初步的生物活性测试表明,在50 mg/L质量浓度下,目标产物去氢枞酸基B环并噻唑-苯甲酰胺(Ⅵj)和中间体去氢枞酸基B环并噻唑-胺(Ⅴ)对苹果轮纹病菌的抑制率分别为90.0%和92.4%(活性级别为A级)。
In an attempt to search for natural product-based antifungal agents,twenty novel dehydroabietic acid-based B ring-fused-thiazole-amide compounds（ Ⅵ a ~ t） were designed and synthesized by using dehydroabietic acid as starting materials. The synthetic conditions were investigated preliminarily,and the target products were characterized by FTIR,1HNMR,13 CNMR,and ESI-MS. The antifungal activity was also evaluated against the following 5 plant pathogens： Fusarium oxysporum f. cucumerinum,Cercospora arachidicola,Physalospora piricola,Alternaria solani and Gibberella zeae. The preliminary bioassay showed that,at the concentration of 50 mg / L,the target product dehydroabietic acid-based B ring-fused-thiazole-benzamide（ Ⅵ j） and the intermediate dehydroabietic acid-based B ring-fused-thiazole-amine（ Ⅴ） had inhibition rates of 90. 0% and92. 4% against Physalospora piricola（ A-class activity level）,respectively.
出处
《精细化工》
EI
CAS
CSCD
北大核心
2016年第7期811-819,共9页
Fine Chemicals
基金
国家自然科学基金项目(31060100)
广西植物功能物质研究与利用重点实验室开放基金课题(FPRU2016-1)~~
关键词
去氢枞酸
噻唑-酰胺
抑菌活性
精细化工中间体
医药原料
dehydroabietic acid
thiazole-amide
antifungal activity
fine chemical intermediates
drug materials
