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Natural Products as a Source for Novel Antibiotics

机译:天然产物是新型抗生素的来源

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Natural products have historically been of crucial importance in the identification and development of antibacterial agents. Interest in these systems has waned in recent years, but the rapid emergence of resistant bacterial strains has forced their re-evaluation as a route to identify novel chemical skeletons with antibacterial activity for elaboration in drug development. This overview examines the current situation, highlights new natural product systems which have been found, together with re-examination of some old ones, and new technologies for their identification. While natural products certainly have the potential to re-emerge as a key start-point in antibacterial drug discovery, reports of new or reinvestigated structures need to be supported with sufficient quality chemical (solubility, stability), biochemical (including toxicity in particular, along with target information) and microbiological [minimum inhibitory concentration (MIC) and resistance frequency] validation data to assist in the identification of promising hit structures and to avoid wasted effort from trawling over already cultivated territory. This is particularly important in a resource-limited research environment.
机译:天然产物在历史上一直对鉴定和开发抗菌剂至关重要。近年来,对这些系统的兴趣减弱了,但是耐药细菌菌株的迅速出现迫使其重新评估,以鉴定具有抗菌活性的新型化学骨架,从而在药物开发中进行精心设计。本概述检查了当前情况,重点介绍了已发现的新天然产品系统,以及对某些旧系统的重新检验以及用于识别它们的新技术。虽然天然产物肯定有可能重新出现,成为抗菌药物发现的关键起点,但新的或重新研究的结构的报告需要有足够质量的化学物质(溶解性,稳定性),生物化学物质(尤其包括毒性)来支持。包含目标信息)和微生物学数据(最低抑菌浓度(MIC)和耐药频率)验证数据,可帮助鉴定有前途的命中结构,并避免在已经耕种的土地上拖网而浪费精力。这在资源有限的研究环境中尤其重要。

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