【作者】 张瑾； 彭菊芳； 张尊听；

【Author】 ZHANG Jin;PENG Jufang;ZHANG Zunting;Key Laboratory of the Ministry of Education for Medicinal Resources and Natural Pharmaceutical Chemistry,National Engineering Laboratory for Resource Development of Endangered Crude Drugs in Northwest of China,and School of Chemistry and Chemical Engineering,Shaanxi Normal University;

【机构】 陕西师范大学化学化工学院教育部药用资源与天然药物化学重点实验室西北濒危药材资源开发国家工程实验室；

【摘要】 本文通过色原酮和水合肼的缩合反应,设计合成了14种高收率的3,4-二苯基-1H-吡唑类化合物（5）和3-苯基-4-呋喃（噻吩/N-甲基吡咯）-1H-吡唑类化合物（7）,并评价了5和7体外对马铃薯干腐病菌（Fusariumsolani）、苹果炭疽病菌（Colletotrichumgloeosporioides）、苹果腐烂病菌（Cytosporasp.）、番茄早疫病菌（Alternariasolani）及番茄灰霉病菌（Botrytiscinerea）5种植物病原真菌的抑制活性。结果表明:5和7对植物病原真菌具有较好的抑制活性,尤其是3-（2-羟基-4-甲氧基）苯基-4-（4-氟）苯基-1H-吡唑（5g）分别针对苹果腐烂、苹果炭疽和番茄早疫表现出显著地抗真菌活性,IC50值分别为:11.91±0.51μg/mL、14.92±1.14μg/mL和16.98±0.50μg/mL;3-苯基-4-噻吩-1H-吡唑（7d）针对苹果炭疽的IC₅₀值为:12.86±6.21μg/mL。更多还原

【Abstract】 Fourteen compounds with 3,4-diphenyl-1 H-pyrazole derivatives（5） and 3-phenyl-4-furan（thiophen/N-methyl-pyrrol）-1 H-pyrazole derivatives（7） weredesigned and synthesized by the condensation of chromone and hydrazine hydrate in good yields,their antifungal abilities were evaluated against five phytopathogens fungi including Fusariumsolani,Colletotrichumgloeosporioides,Alternariasolani,Cytospora sp.and Botrytis cinerea in vitro.The results showed that some of those compounds exhibited good antifungal activities.For example,3-（2-hydroxy-4-methoxy）phenyl-4-（4-fluoro）phenyl-1 H-pyrazole（5 g） showed good antifungal properties against Cytospora sp.,Colletotrichumgloeosporioides and Alternariasolani with IC50 of 11.91,14.92 and 16.98 μg/mL,respectively.3-Phenyl-4-thiophen-1 H-pyrazole（7 d） displayed inhibition on Colletotrichumgloeosporioides with IC₅₀ of 12.86 μg/mL.更多还原