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Design, synthesis, and antibacterial activity of pleuromutilin derivatives.
Liu, Hui-Xian; Yao, Wen-Yu; Cui, Ge; Zhou, Jing; Yan, Hao; Guo, Hui; Wang, Yu-Wei; Zhang, Yue.
Afiliación
  • Liu HX; College of Pharmacy, Shaanxi University of Chinese Medicine, Xianyang, PR China.
  • Yao WY; Jinan University College of Pharmacy, Guangzhou, PR China.
  • Cui G; School of Chemical and Pharmaceutical Engineering, Hebei University of Science and Technology, Shijiazhuang, PR China.
  • Zhou J; College of Pharmacy, Shaanxi University of Chinese Medicine, Xianyang, PR China.
  • Yan H; College of Pharmacy, Shaanxi University of Chinese Medicine, Xianyang, PR China.
  • Guo H; College of Pharmacy, Shaanxi University of Chinese Medicine, Xianyang, PR China.
  • Wang YW; College of Pharmacy, Shaanxi University of Chinese Medicine, Xianyang, PR China.
  • Zhang Y; School of Chemical and Pharmaceutical Engineering, Hebei University of Science and Technology, Shijiazhuang, PR China.
Chem Biol Drug Des ; 103(6): e14554, 2024 Jun.
Article en En | MEDLINE | ID: mdl-38806405
ABSTRACT
This paper reports the design, synthesis, and antibacterial activity study of pleuromutilin derivatives with 2-methyl-4-nitroaniline and 2-methoxy-4-nitroaniline side chains at the C22 position. The structures of the new compounds were characterized by 1H-NMR, 13C-NMR and HRMS. The inhibitory activity of the compounds against MSSA, pyogeniccoccus, streptococcus, and MRSA strains was determined using the micro broth dilution method. The results showed that the compounds exhibited certain activity against Gram-positive bacteria, among which compounds A8a, A8b, A8c, A8d, and A7 demonstrated superior antibacterial activity against MSSA, MRSA, and pyogeniccoccus compared to tiamulin, although the derivatives showed lower antibacterial activity against streptococcus compared to the control drug. Based on the favorable in vitro activity of A8c, the time-kill kinetics against MRSA were evaluated, revealing that compound A8c could inhibit bacterial proliferation in a concentration-dependent manner.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Compuestos Policíclicos / Diseño de Fármacos / Pruebas de Sensibilidad Microbiana / Diterpenos / Staphylococcus aureus Resistente a Meticilina / Pleuromutilinas / Antibacterianos Idioma: En Revista: Chem Biol Drug Des Asunto de la revista: BIOQUIMICA / FARMACIA / FARMACOLOGIA Año: 2024 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: Compuestos Policíclicos / Diseño de Fármacos / Pruebas de Sensibilidad Microbiana / Diterpenos / Staphylococcus aureus Resistente a Meticilina / Pleuromutilinas / Antibacterianos Idioma: En Revista: Chem Biol Drug Des Asunto de la revista: BIOQUIMICA / FARMACIA / FARMACOLOGIA Año: 2024 Tipo del documento: Article Pais de publicación: Reino Unido