4-羰基-2-戊烯醛与硫代乙酸加成的研究

以2-甲基-2,5-二甲氧基-2,5-二氢呋喃水解产物与硫代乙酸加成并在不同条件下关环,制得了β-乙酰硫基呋喃、噻吩和毗咯的各种异构产物,提供了按需要制备不同α-甲基-β-巯基呋喃、噻吩和吡咯衍生物的途径。     

Novel 1,3,4-oxadiazole thioether and sulfone derivatives bearing a flexible N-heterocyclic moiety: Synthesis,characterization, and anti-microorganism activity

In the search for more efficient and versatile anti-phytopathogen agents, a series of new 1,3,4-oxadiazole thioether/sulfone analogues bearing a flexible N-containing heterocyclic pattern were elaborately prepared, and their bioactivities against plant pathogenic microorganisms were systematically evaluated. Bioassay screening results demonstrated that compounds 32 and 33 significantly inhibited the growth of Xanthomonas oryzae pv. oryzae (Xoo) in vitro (32, EC₅₀ = 5.17 mg L^?1; 33, EC₅₀ = 1.19 mg L^?1), which were significantly surpass commercial bismerthiazol (BT) and thiodiazole copper (TC). Meanwhile, pot experiments confirmed the prospective applications of compound 33 in managing rice bacterial leaf blight and its good safety toward rice plants. Further studies showed that compound 33 interfered with the formation of bacterial biofilms and inhibited bacterial virulence factors. Furthermore, an in vitro antifungal bioassay showed that compound 32 possessed remarkable growth inhibitory activity against Sclerotinia sclerotiorum (S.s., EC₅₀ = 22.16 mg L^?1) and Verticillium dahlia (V.d. EC₅₀ = 32.78 mg L^?1). These results all confirmed that the designed 1,3,4-oxadiazole compounds displayed potential for managing plant microbial diseases through targeting dihydrolipoamide S-succinyltransferase (DLST).     

蛇床子素酯类/磺酸酯类衍生物的合成与抗菌活性研究

为了寻找抗菌苗头化合物,以蛇床子素为原料,对其7位结构改造,经脱甲基化制得中间体Ⅰ,中间体Ⅰ再分别与酰氯、磺酰氯反应,合成了12个目标化合物,经_¹H NMR 、_¹³C NMR和MS确认结构。体外抗菌活性筛选结果表明：两类衍生物对金葡菌有较好的抗菌活性,磺酸酯衍生物的活性优于羧酸酯衍生物,尤以化合物Ⅲd和Ⅲe的抗金葡菌的活性最为显著,MIC值均为32mg/L,远优于蛇床子素的活性,接近对照药苯唑西林。该研究也表明蛇床子素7位的结构修饰能改善其抗菌活性,值得进一步研究。