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Capsaicin derivatives with nitrothiophene substituents: Design, synthesis and antibacterial activity against multidrug-resistant S. aureus.
Wang, Zhi-Cheng; Wei, Bingyan; Pei, Fang-Ning; Yang, Teng; Tang, Jie; Yang, Song; Yu, Li-Fang; Yang, Cai-Guang; Yang, Fan.
Affiliation
  • Wang ZC; Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, SCME, East China Normal University, Shanghai, 200062, China.
  • Wei B; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China; University of the Chinese Academy of Sciences, Beijing, 100049, China.
  • Pei FN; Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, SCME, East China Normal University, Shanghai, 200062, China.
  • Yang T; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China; State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Edu
  • Tang J; Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, SCME, East China Normal University, Shanghai, 200062, China.
  • Yang S; State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for R&D of Fine Chemicals, Guizhou University, 2708 South Huaxi Road, Guiyang, Guizhou, 550025, China.
  • Yu LF; Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, SCME, East China Normal University, Shanghai, 200062, China.
  • Yang CG; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China; University of the Chinese Academy of Sciences, Beijing, 100049, China. Electronic address: yangcg@simm.ac.cn.
  • Yang F; Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, SCME, East China Normal University, Shanghai, 200062, China. Electronic address: fyang@chem.ecnu.edu.cn.
Eur J Med Chem ; 198: 112352, 2020 Jul 15.
Article in En | MEDLINE | ID: mdl-32387838
To address the emergency caused by multi-drug resistant Staphylococcus aureus, a series of novel capsaicin derivatives with nitrothiophene substituents have been designed and evaluated for the antibacterial activities against S. aureus Newman and multidrug-resistant strains (NRS-1, NRS-70, NRS-100, NRS-108, and NRS-271). The structure-activity relationship was further revealed. Compound 13c, 13f, and 13g were highly active against staphylococcal growth, with minimal inhibition concentration (MIC) values of 0.39-1.56 µg/mL. The oxadiazole-derived compound 21, a bioisostere of ester 13f, is the most potent candidate for anti-growth of five multidrug-resistant S. aureus strains with MICs of 0.20-0.78 µg/mL, which is more active compared with vancomycin in vitro. Notably, these anti-staphylococcal compounds are much less cytotoxic to the normal kidney epithelial cell line (HK293T).
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Staphylococcal Infections / Thiophenes / Capsaicin / Methicillin-Resistant Staphylococcus aureus / Anti-Bacterial Agents Limits: Humans Language: En Journal: Eur J Med Chem Year: 2020 Document type: Article Affiliation country: China Country of publication: France
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Staphylococcal Infections / Thiophenes / Capsaicin / Methicillin-Resistant Staphylococcus aureus / Anti-Bacterial Agents Limits: Humans Language: En Journal: Eur J Med Chem Year: 2020 Document type: Article Affiliation country: China Country of publication: France