4.5 Article

Identification of a diverse synthetic abietane diterpenoid library and insight into the structure-activity relationships for antibacterial activity

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 27, Issue 24, Pages 5382-5386

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2017.11.014

Keywords

Diterpenoid; Natural product-like (NPL); Dehydroabietic acid (DHAA); Abietic acid (AA); Click chemistry; Antibacterial

Funding

  1. Zhejiang University of Technology, China [2017116002229]
  2. China Postdoctoral Science Foundation, China [2017M612024]

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A diverse natural product-like (NPL) synthetic abietane diterpenoid library containing 86 compounds were obtained and the SARs were studied based on their antibacterial potential. Further in vitro cytotoxic and in silico drug-like properties evaluation showed that the potent antibacterial compound 84 had good drug-like properties and displayed low cytotoxicity toward noncancerous mammalian cells, indicating the study of AA and DHAA might be a good starting point for the search of novel antimicrobial molecules. Future work should be focused on the optimization of their potency and selectivity. (C) 2017 Elsevier Ltd. All rights reserved.

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