Over the past decade, considerable scientific attention has been given to adapting cobalt bis(dicarbollide) as innovative agent with various biomedical applications. Although the studied compounds show great potential in this field, only a few reports have explored broad, well-thought-out libraries of derivatives to correlate their structure with biological activity. In this study, we investigate a panel of [CoSAN]⁻ derivatives substituted with fluorine, chlorine, bromine and iodine in order to elucidate the impact of the halogen presence on antimicrobial action and selectivity over mammalian cells. We present the first evidence that increasing the atomic mass of a substituent improves the biological activity of a derivative. Our results demonstrate that the addition of a single iodine atom to the [CoSAN]⁻ core results in the most selective antibacterial outcome, especially toward Staphylococcus aureus ATCC 6538. The described correlation between the lipophilicity and the activity of the compounds toward both bacteria and human cell lines highlights the importance of a conscious design method to obtain the most desirable [CoSAN]⁻-based derivatives.

中文翻译：

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揭示钴双（双羧内酯）中生物效应与卤素取代基之间的相关性


在过去的十年中，人们给予了相当大的科学关注，将双钴（双羧藻）作为创新剂应用于各种生物医学应用。尽管所研究的化合物在该领域显示出巨大的潜力，但只有少数报告探索了广泛的、经过深思熟虑的衍生物库，以将其结构与生物活性相关联。在这项研究中，我们研究了一组用氟、氯、溴和碘取代的 [CoSAN] ^- 衍生物，以阐明卤素的存在对哺乳动物细胞的抗菌作用和选择性的影响。我们提出了第一个证据，证明增加取代基的原子质量可以提高衍生物的生物活性。我们的结果表明，在 [CoSAN] ^- 核心中添加单个碘原子会导致最具选择性的抗菌效果，尤其是对金黄色葡萄球菌 ATCC 6538。所描述的亲脂性与化合物对细菌和人类细胞系的活性之间的相关性突出了有意识的设计方法以获得最理想的基于 [CoSAN] ⁻ 的衍生物的重要性。