Graduate Program in Technology of Chemical and Biochemical Processes, Technology Center, Federal University of Rio de Janeiro (UFRJ), EQ/UFRJ, Centro de Tecnologia, Bloco E, Ilha do Fundão, Rio de Janeiro-RJ 21949-900, Brazil.
Brazilian National Institute of Industrial Property, INPI/Rua Mayrink Veiga No. 9/19 andar, CEP 20090-910, Rio de Janeiro-RJ 20090-910, Brazil.
Antibiotics (Basel). 2013 Dec 6;2(4):500-34. doi: 10.3390/antibiotics2040500.
Many approaches are used to discover new antibiotic compounds, one of the most widespread being the chemical modification of known antibiotics. This type of discovery has been so important in the development of new antibiotics that most antibiotics used today belong to the same chemical classes as antibiotics discovered in the 1950s and 1960s. Even though the discovery of new classes of antibiotics is urgently needed, the chemical modification of antibiotics in known classes is still widely used to discover new antibiotics, resulting in a great number of compounds in the discovery and clinical pipeline that belong to existing classes. In this scenario, the present article presents an overview of the R&D pipeline of new antibiotics in known classes of antibiotics, from discovery to clinical trial, in order to map out the technological trends in this type of antibiotic R&D, aiming to identify the chemical classes attracting most interest, their spectrum of activity, and the new subclasses under development. The result of the study shows that the new antibiotics in the pipeline belong to the following chemical classes: quinolones, aminoglycosides, macrolides, oxazolidinones, tetracyclines, pleuromutilins, beta-lactams, lipoglycopeptides, polymyxins and cyclic lipopeptides.
许多方法被用于发现新的抗生素化合物，其中最广泛的方法之一是对已知抗生素进行化学修饰。这种发现类型在新抗生素的开发中非常重要，以至于今天使用的大多数抗生素都属于与 20 世纪 50 年代和 60 年代发现的抗生素相同的化学类别。尽管迫切需要发现新的抗生素类别，但对已知类别中的抗生素进行化学修饰仍广泛用于发现新的抗生素，从而导致发现和临床管道中属于现有类别的化合物数量众多。在这种情况下，本文概述了已知类别抗生素中新抗生素的研发管道，从发现到临床试验，以绘制出这种抗生素研发的技术趋势，旨在确定最受关注的化学类别、它们的活性谱以及正在开发的新子类。研究结果表明，管道中的新抗生素属于以下化学类别：喹诺酮类、氨基糖苷类、大环内酯类、恶唑烷酮类、四环素类、截短侧耳素类、β-内酰胺类、糖肽类、多粘菌素类和环脂肽类。
