中文摘要：

根据活性亚结构拼接原理,将1,3,4-噻二唑环和哌嗪环通过磺酰基桥接,设计并合成了16个新型的1-取代-4-[5-（4-硝基苯基）-1,3,4-噻二唑-2-磺酰基]哌嗪类衍生物（4a ～4p）,其结构经1 H NMR,13C NMR,IR和元素分析表征.考察了溶剂、缚酸剂和反应温度对1-甲基-4-[5-（4-硝基苯基）-1,3,4-噻二唑-2-磺酰基]哌嗪（4a）产率的影响.合成4a的最佳反应条件为：乙腈为溶剂,三乙胺为缚酸剂,于25℃反应5h,产率75％.采用生长速率法研究了4a ～4p对小麦赤霉菌、苹果腐烂病菌和辣椒枯萎病菌的抑制活性.结果表明：在用药量为50 μg · mL^-1,1-（4-氟苄基）-4-[5-（4-硝基苯基）-1,3,4-噻二唑-2-磺酰基]哌嗪（4d）和1-丙炔基-4-[5-（2,4-二氯苯基）-1,3,4-噻二唑-2-磺酰基]哌嗪（4n）对三种病菌均具有较好的抑制活性.

英文摘要：

Sixteen novel 1-substituted-4-[5-（4-substituted phenyl）-1,3,4-thiadiazol-2-sulfonyl] piperazine derivatives（4a ～ 4p） were designed and synthesized by connection reaction of 1,3,4-thiadiazol with N-substitued piperazine.The structures were characterized by 1H NMR,13C NMR,IR and elemental analysis.Effects of the solvent,acid acceptor and reaction temperature on the yield of 1-methyl-4-[5-（4-nitrophenyl）-1,3,4-thiadiazol-2-sulfonyl] piperazine （4a） were investigated.The optimum reaction conditions for synthesizing 4a with the yield of 75% at 25 ℃ for 5 h were as follows：acetonitrile was solvent and triethylamine was acid acceptor.The antibacterial activities of 4a ～ 4p against G.zeae,C.mandshurica and F.oxysporum were investigated by growth rate method.The results indicated that 1-methyl-4-[5-（4-fluorobenzyl）-1,3,4-thiadiazol-2-sulfonyl] piperazine （4d） and 1-methyl-4-[5-（4-propinyl）-1,3,4-thiadiazol-2-sulfonyl] piperazine （4n） exhibited better antibacterial activities at 50 μg · mL^-1