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Trienomycin A-simplified analogs: Synthesis and anti-neuroinflammatory activity.
Luo, Yu-Qing; Bian, Zhao-Yuan; Xu, Dan-Dan; Tang, Jiang-Jiang; Gao, Jin-Ming.
Afiliación
  • Luo YQ; Shaanxi Key Laboratory of Natural Products & Chemical Biology, College of Chemistry & Pharmacy, Northwest A&F University, Yangling 712100, Shaanxi, PR China.
  • Bian ZY; Shaanxi Key Laboratory of Natural Products & Chemical Biology, College of Chemistry & Pharmacy, Northwest A&F University, Yangling 712100, Shaanxi, PR China.
  • Xu DD; School of Foundational Education, Tibet Agricultural and Animal Husbandry University, Nyingchi 860000, Tibet, PR China.
  • Tang JJ; Shaanxi Key Laboratory of Natural Products & Chemical Biology, College of Chemistry & Pharmacy, Northwest A&F University, Yangling 712100, Shaanxi, PR China. Electronic address: tangjiang11@nwafu.edu.cn.
  • Gao JM; Shaanxi Key Laboratory of Natural Products & Chemical Biology, College of Chemistry & Pharmacy, Northwest A&F University, Yangling 712100, Shaanxi, PR China.
Bioorg Med Chem Lett ; 80: 129122, 2023 01 15.
Article en En | MEDLINE | ID: mdl-36592870
A series of novel trienomycin A (TA)-mimetic compounds (5a-p) have been designed, synthesized, and evaluated for their in vitro anti-neuroinflammatory and neuroprotective activities. Among them, compounds 5h, 5n, and 5o exhibits relatively strong NO inhibitory activity in LPS-activated BV-2 cells with the EC50 values of 12.4, 17.3, and 8.9 µM, respectively. Moreover, 5h showed evidently neuroprotective effect against H2O2-induced PC-12 cells without cytotoxicity at 20 µM. Overall, these compounds can provide a better understanding of the structure-activity relationship of TA and furnish research ideas for anti-neuroinflammatory and neuroprotective agents.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Fármacos Neuroprotectores / Peróxido de Hidrógeno Límite: Animals Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2023 Tipo del documento: Article Pais de publicación: Reino Unido
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Fármacos Neuroprotectores / Peróxido de Hidrógeno Límite: Animals Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2023 Tipo del documento: Article Pais de publicación: Reino Unido