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Editorial: Inspired by Nature: Towards Novel Anti-Infective Agents

机译:社论:受大自然的启发:朝着新型的抗感染剂

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Since the dawn of mankind natural sources have been explored due their valuable medicinal properties. Even in modern times several compounds are still being identified in the natural source(s) from which anti-microbial activity was originally isolated. However, the world of natural products is still the largest unexplored chemical space when compared with the largest of the known chemical databases. Although remaining one of the best sources of chemical inspiration for the development of new drugs, only around a quarter million natural products are available within public databases and no more that ten percent can be readily obtainable from commercial vendors for experimental testing. The identification of such molecular scaffolds, either derived from plants, microorganisms or marine products, followed by isolation of active molecules and further chemical modification, allows researchers to further improve their pharmacological properties. Having strong roots in traditional medicine, in which plants and plant extracts only known to the medicine caregivers are used to treat all sorts of diseases, the identification of each compound responsible for that given activity is usually the first step in increasing the pool of chemical templates. This is why many compounds were first isolated from natural sources and used to develop drugs targeting specific diseases, from which salicylic acid, morphine and quinine are classical examples. However, due to the intricate complexity of some molecules, hemi-synthetic derivatives as etoposide and teniposide, paclitaxel or vinblastine/vincristine remains as the most feasible approach for obtaining more potent compounds in selected instances. The main challenge within this topic was to use nature as an inspiration for new compounds that can pave the way for future pharmacological innovations. In this perspective, boron-containing DNA-binding ionic liquids as antimicrobial agents ( Rosa et al. ) or inspired by natural product nitrogen-containing 5-membered heterocyclic moieties ( Camargo et al. ) are two very interesting approaches in the development of new antibiotics. The identification of sugar-type compounds as antiviral agents is also remarkable ( Zhou et al. ), taking into account that generally sugar moieties are often ignored in drug development. Furthermore, novel techniques such as Molecular Dynamics, largely ignored in the natural products, are slowly increasing in importance as useful tools for the comprehension of more dynamic systems as nature-inspired eutectic solvents ( Monteiro et al. ). Taken together these papers present a glimpse on the opportunities that nature continues to provide, when properly addressed. Therefore, further inspiration can be obtained by harnessing the enormous potential delivered by nature throughout its natural selection and evolution.
机译:由于人类自然来源的黎明因其宝贵的药用特性而探讨。即使在近代,仍然在最初分离出抗微生物活性的自然来源中仍然鉴定出几种化合物。然而,与最大的已知化学数据库相比,天然产品的世界仍然是最大的未探索的化学空间。虽然剩余的最佳化学灵感来源是开发新药物的化学灵感之一,但仅在公共数据库中提供左右四分之一的天然产品,并且从商业供应商可以易于获得10%的人进行实验测试。鉴定这些分子支架,衍生自植物,微生物或海洋产品,然后分离活性分子和进一步的化学改性,允许研究人员进一步改善其药理学性质。在传统医学中具有强大的根源,其中仅针对药物护理人员唯一已知的植物和植物提取物用于治疗各种疾病,该疾病的鉴定通常是增加化学模板池的第一步。这就是为什么许多化合物首先从天然来源中分离出来并用于开发靶向特异性疾病的药物,从中含有水杨酸,吗啡和奎宁是典型的例子。然而,由于某些分子的复杂性,作为依托泊苷和萜醇,紫杉醇或植物苷/血管内的半合成衍生物仍然是在所选情况下获得更多有效化合物的最可行方法。本课题内的主要挑战是将大自然作为可以为未来药理学创新铺平道路的新化合物的灵感来源。在这种观点中,含硼DNA结合离子液体作为抗微生物剂(Rosa等)或由含天然产物含氮的5-元杂环部分的启发(Camargo等)是新的两个非常有趣的方法抗生素。作为抗病毒剂的鉴定也是显着的(周等人),考虑到通常在药物发育中忽略糖部分。此外,新颖的技术如分子动力学,在天然产物中很大程度上被忽略,这重要地增加了对自然灵感的共晶溶剂(Monteiro等)来理解更多动态系统的有用工具。占据了这些论文的瞥见,在适当的解决方面,对自然继续提供的机会。因此,通过在整个自然选择和进化中利用本质上的巨大潜力来获得进一步的灵感。

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