2. Academic Validation
  3. Synthesis and biological evaluation of fluoroquinolones containing a pyridoxine derivatives moiety

Synthesis and biological evaluation of fluoroquinolones containing a pyridoxine derivatives moiety

  • Eur J Med Chem. 2023 Sep 7:261:115798. doi: 10.1016/j.ejmech.2023.115798.
Nikita V Shtyrlin 1,  Airat R Kayumov 2,  Maria N Agafonova 2,  Marsel R Garipov 2,  Alina E Gatina 2,  Mikhail V Pugachev 2,  Elena S Bulatova 2,  Denis Y Grishaev 2,  Alfiya G Iksanova 2,  Rail M Khaziev 2,  Ilnur M Ganiev 2,  Aleksandr M Aimaletdinov 2,  Oleg I Gnezdilov 3,  Yurii G Shtyrlin 4
Affiliations

Affiliations

  • 1 Kazan (Volga region) Federal University, Kremlyovskaya St. 18, Kazan, 420008, Russian Federation. Electronic address: Nikita.Shtyrlin@kpfu.ru.
  • 2 Kazan (Volga region) Federal University, Kremlyovskaya St. 18, Kazan, 420008, Russian Federation.
  • 3 Kazan E. K. Zavoisky Physical-Technical Institute, Federal Research Center "Kazan Scientific Center of the Russian Academy of Sciences", 10/7 ul. Sibirskiy trakt, Kazan, 420029, Russian Federation.
  • 4 Kazan (Volga region) Federal University, Kremlyovskaya St. 18, Kazan, 420008, Russian Federation. Electronic address: Yurii.Shtyrlin@kpfu.ru.
PMID: 37729692 DOI: 10.1016/j.ejmech.2023.115798
Abstract

We report herein the design, synthesis and biological evaluation of series of 7-substituted fluoroquinolones with pyridoxine derivatives. In vitro screening of Antibacterial activity and toxicity of 39 synthesized fluoroquinolones defined compounds 7 and 28 as lead compounds for further investigations. On various clinical isolates lead compounds 7 and 28 exhibited Antibacterial activity comparable with reference fluoroqinolones. Mutagenic effects haven't been observed for these compounds in SOS-chromotest. Compound 7 are non-toxic in vivo on mice (LD50 > 2000 mg/kg, oral) and rats (LD50 > 2000 mg/kg, oral). Compound 28 was more toxic (LD50 = 474 mg/kg, oral, mice). Moreover compound 7 showed greater in vivo efficacy compared to ciprofloxacin in a murine model of staphylococcal sepsis. Taken together the described active compound are promising candidate for preclinical trials.

Keywords

Antibacterial activity; Fluoroquinolone; In vivo efficacy; Pyridoxine; Toxicity.

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