Structures and biological activity of three 2-(pyridin-2-yl)-1H-benzimidazole derivatives,Acta Crystallographica Section C

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Structures and biological activity of three 2-(pyridin-2-yl)-1H-benzimidazole derivatives
Acta Crystallographica Section C ( IF 0.7 ) Pub Date : 2023-11-08 , DOI: 10.1107/s2053229623009452
Jarosław Sukiennik ₁ , Andrzej Olczak ₁ , Katarzyna Gobis ₂ , Izabela Korona-Głowniak ₃ , Katarzyna Suśniak ₃ , Andrzej Fruziński ₁ , Małgorzata Szczesio ₁

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Two new 2-(pyridin-2-yl)-1H-benzimidazole derivatives, namely, 2-(4-phenoxypyridin-2-yl)-1H-benzimidazole, C₁₈H₁₃N₃O, and 2-[4-(4-fluorophenoxy)pyridin-2-yl]-1H-benzimidazole, C₁₈H₁₂FN₃O, were synthesized and characterized by NMR spectroscopy. Crystal structure, biological activity and ADME analyses were performed for these two new compounds and a third compound, namely, 5,6-dimethyl-2-[4-(4-phenylpiperazin-1-yl)pyridin-2-yl]-1H-benzimidazole methanol monosolvate, C₂₄H₂₅N₅·CH₃OH, the synthesis of which had been described previously. All three compounds have a similar chain hydrogen-bonding pattern. One of them (the fluorophenoxy derivative) showed good antimicrobial activity against Gram-positive bacteria. The ADME analysis indicates that the compounds could be good drug candidates.

中文翻译：

三种2-(吡啶-2-基)-1H-苯并咪唑衍生物的结构和生物活性

两种新的2-(吡啶-2-基)-1 H-苯并咪唑衍生物，即2-(4-苯氧基吡啶-2-基)-1 H-苯并咪唑、C ₁₈ H ₁₃ N ₃ O和2-[4合成了-(4-氟苯氧基)吡啶-2-基]-1 H-苯并咪唑C ₁₈ H ₁₂ FN ₃ O，并通过NMR光谱进行表征。对这两种新化合物和第三种化合物（即 5,6-二甲基-2-[4-(4-苯基哌嗪-1-基)吡啶-2-基]-1）进行了晶体结构、生物活性和 ADME 分析。 H-苯并咪唑甲醇单溶剂化物C ₂₄ H ₂₅ N ₅ ·CH ₃ OH，其合成先前已描述。所有三种化合物都具有相似的链氢键模式。其中一种（氟苯氧基衍生物）对革兰氏阳性菌表现出良好的抗菌活性。 ADME 分析表明这些化合物可能是良好的候选药物。

更新日期：2023-11-08

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