Abstract A series of benzothiazole derivatives bearing a 1,3,4-thiadiazole moiety were designed, synthesized and evaluated for their antibacterial, antifungal and antiviral activities. The bioassay results indicated that most of target compounds showed good antiviral activities against tobacco mosaic virus (TMV) and antibacterial activities against Xanthomonas oryzae pv. oryzae (Xoo) and Ralstonia solanacearum (Rs). Especially, the anti-Xoo effect of title compounds 5k (N-(5-methoxybenzo[d]thiazol-2-yl)-2-((5-(2-tolyl)-1,3,4-thiadiazol-2-yl)thio)acetamide) and the anti-Rs effect of title compounds 5a (N-(5-nitrobenzo[d]thiazol-2-yl)-2-((5-(4-(trifluorom ethyl)phenyl)-1,3,4-thiadiazol-2-yl)thio)acetmide) respectively reached 52.4% and 71.6% at 100 µg/mL, which are superior to that of bismerthiazol (32.0% and 52.3%). In addition, the protective and inactivation activities of title compound 5i (N-(5-methoxybenzo [d]thiazol-2-yl)-2-((5-(4-nitrophenyl)-1,3,4-thiadiazol-2-yl)thio)acetamide) against TMV were 79.5% and 88.3%, respectively, which are better than that of ningnanmycin (76.4% and 86.8%). The above research showed that benzothiazole derivatives bearing a 1,3,4-thiadiazole moiety may be used as potential molecular templates in searching for highly-efficient antiviral and antibacterial agents. Graphical Abstract

中文翻译：

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带有 1,3,4-噻二唑部分的苯并噻唑衍生物的合成和生物活性

摘要 设计、合成了一系列带有 1,3,4-噻二唑部分的苯并噻唑衍生物，并评估了它们的抗菌、抗真菌和抗病毒活性。生物测定结果表明，大多数目标化合物对烟草花叶病毒（TMV）表现出良好的抗病毒活性和对米黄单胞菌的抗菌活性。oryzae (Xoo) 和青枯病菌 (Rs)。特别是，标题化合物 5k (N-(5-甲氧基苯并[d]噻唑-2-基)-2-((5-(2-甲苯基)-1,3,4-噻二唑-2-基)硫代)乙酰胺)和标题化合物5a(N-(5-硝基苯并[d]噻唑-2-基)-2-((5-(4-(三氟甲基)苯基)-1)的抗-Rs作用) ,3,4-噻二唑-2-基）硫代）乙酰胺）在 100 µg/mL 时分别达到 52.4% 和 71.6%，优于双甲噻唑（32.0% 和 52.3%）。此外，标题化合物5i (N-(5-甲氧基苯并[d]噻唑-2-基)-2-((5-(4-硝基苯基)-1,3,4-噻二唑-2-基)的保护和灭活活性)硫）乙酰胺）对 TMV 分别为 79.5% 和 88.3%，优于宁南霉素（76.4% 和 86.8%）。上述研究表明，带有 1,3,4-噻二唑部分的苯并噻唑衍生物可作为潜在的分子模板，用于寻找高效的抗病毒和抗菌剂。图形概要 4-噻二唑部分可用作寻找高效抗病毒和抗菌剂的潜在分子模板。图形概要 4-噻二唑部分可用作寻找高效抗病毒和抗菌剂的潜在分子模板。图形概要