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Identification of a diverse synthetic abietane diterpenoid library and insight into the structure-activity relationships for antibacterial activity.
Hou, Wei; Zhang, Guanjun; Luo, Zhi; Li, Di; Ruan, Haoqiang; Ruan, Benfang Helen; Su, Lin; Xu, Hongtao.
Afiliación
  • Hou W; College of Pharmaceutical Science, Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals, Zhejiang University of Technology, Hangzhou 310014, PR China.
  • Zhang G; College of Chemical Engineering and Materials Science, Tianjin University of Science & Technology, Tianjin 300457, PR China.
  • Luo Z; Shanghai Evergene Biotech Co., Ltd., Shanghai 201499, PR China.
  • Li D; College of Pharmaceutical Science, Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals, Zhejiang University of Technology, Hangzhou 310014, PR China.
  • Ruan H; College of Pharmaceutical Science, Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals, Zhejiang University of Technology, Hangzhou 310014, PR China.
  • Ruan BH; College of Pharmaceutical Science, Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals, Zhejiang University of Technology, Hangzhou 310014, PR China.
  • Su L; College of Pharmaceutical Science, Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals, Zhejiang University of Technology, Hangzhou 310014, PR China. Electronic address: sulin8023@zjut.edu.cn.
  • Xu H; Shanghai Institute for Advanced Immunochemical Studies, ShanghaiTech University, Shanghai 201210, PR China. Electronic address: xuht@shanghaitech.edu.cn.
Bioorg Med Chem Lett ; 27(24): 5382-5386, 2017 12 15.
Article en En | MEDLINE | ID: mdl-29153424
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.
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Texto completo: 1 Bases de datos: MEDLINE Asunto principal: Abietanos / Antibacterianos Tipo de estudio: Diagnostic_studies Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2017 Tipo del documento: Article

Texto completo: 1 Bases de datos: MEDLINE Asunto principal: Abietanos / Antibacterianos Tipo de estudio: Diagnostic_studies Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2017 Tipo del documento: Article