Three new 2,6-disubstituted thiosemicarbazone derivatives of pyridine, namely, 2-{amino[6-(pyrrolidin-1-yl)pyridin-2-yl]methylidene}-N,N-dimethylhydrazine-1-carbothioamide, C₁₃H₂₀N₆S, 2-{amino[6-(piperidin-1-yl)pyridin-2-yl]methylidene}-N,N-dimethylhydrazine-1-carbothioamide, C₁₄H₂₂N₆S, and 2-[amino(6-phenoxypyridin-2-yl)methylidene]-N,N-dimethylhydrazine-1-carbothioamide monohydrate, C₁₅H₁₇N₅OS·H₂O, have been synthesized and characterized by NMR spectroscopy and low-temperature single-crystal X-ray diffraction. In addition, their antibacterial and anti-yeast activities have been determined. The ability of the tested compounds to inhibit bacterial growth was comparable to vancomycin as a reference drug. Compared to isoniazid (MIC 0.125 and 8 µg ml⁻¹), the compounds showed the ability to inhibit the growth of Mycobacterium tuberculosis to a moderate degree for the standard strain and at the same level or higher (MIC 4–8 µg ml⁻¹) for the resistant strain. All three compounds adopt the zwitterionic form in the crystal structure regardless of the presence or absence of solvent molecules.

中文翻译：

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三种2,6-二取代缩氨基硫脲衍生物的合成、结构、ADME及生物活性

三种新的2,6-二取代缩氨基硫脲衍生物，即2-{氨基[6-(吡咯烷-1-基)吡啶-2-基]亚甲基}-N,N-二甲基肼-1-硫代硫酰胺， C ₁₃ H ₂₀ N ₆ S、2-{氨基[6-(哌啶-1-基)吡啶-2-基]亚甲基}-N , N-二甲基肼-1-硫代甲酰胺、C ₁₄ H ₂₂ N ₆ S和2-[氨基(6-苯氧基吡啶-2-基)亚甲基]-N , N-二甲基肼-1-硫代甲酰胺一水合物，C ₁₅ H ₁₇ N ₅ OS·H ₂O已合成并通过核磁共振波谱和低温单晶X射线衍射进行表征。此外，它们的抗菌和抗酵母活性也已确定。测试化合物抑制细菌生长的能力与作为参考药物的万古霉素相当。^{与异烟肼（MIC 0.125和8 µg ml -1} ）相比，这些化合物对标准菌株具有中等程度的抑制结核分枝杆菌生长的能力，对耐药菌株具有相同或更高的水平（MIC 4–8 µg ml ^{-1 ）。}无论是否存在溶剂分子，所有三种化合物在晶体结构中均采用两性离子形式。