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源自自然界化学宝库的新型抗生素。

New antibiotics from Nature's chemical inventory.

作者信息

Wencewicz Timothy A

机构信息

Department of Chemistry, Washington University in St. Louis, One Brookings Drive, St. Louis, MO 63130, United States.

出版信息

Bioorg Med Chem. 2016 Dec 15;24(24):6227-6252. doi: 10.1016/j.bmc.2016.09.014. Epub 2016 Sep 13.

Abstract

The doom and gloom of antibiotic resistance dominates public perception of this drug class. Many believe the world has entered the post-antibiotic era. Classic and modern approaches to antibacterial drug discovery have delivered a plethora of lead molecules with a great majority being natural products of ancient microbial origin. The failure of antibiotics in the resistance era comes from an inability to develop new leads into clinical candidates, which is a costly and risky endeavor for any therapeutic area, especially when resistance is at play. The world needs new antibiotic molecules to replace the exhausted pipeline and the second 'golden era' is certain to come from Nature's chemical inventory once again.

摘要

抗生素耐药性带来的悲观情绪主导了公众对这类药物的认知。许多人认为世界已进入后抗生素时代。经典和现代的抗菌药物发现方法已产生了大量先导分子,其中绝大多数是古老微生物来源的天然产物。在耐药性时代,抗生素的失败源于无法将新的先导分子开发成临床候选药物,对于任何治疗领域来说,这都是一项成本高昂且风险巨大的工作,尤其是在存在耐药性的情况下。世界需要新的抗生素分子来填补枯竭的产品线,而第二个“黄金时代”肯定会再次来自大自然的化学宝库。

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