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. 1996 Jan;40(1):274–277. doi: 10.1128/aac.40.1.274

Antibacterial activity and pharmacokinetics of four new 7-azetidinyl fluoroquinolones.

R Coll 1, D Gargallo-Viola 1, E Tudela 1, M A Xicota 1, S Llovera 1, J Guinea 1
PMCID: PMC163101  PMID: 8787924

Abstract

The activity of E-4535, E-4534, E-4528, and E-4527, four new 7-azetidinyl-6-fluoroquinolones, was studied to evaluate the role played by the C-2' and C-3' substitutions of the azetidinyl group, together with a C-8 fluorine atom. In general, like other 6,8-difluoroquinolones, E-4534 and E-4527 showed higher levels of activity than the corresponding monofluorinated derivatives, E-4535 and E-4528. E-4535 and E-4534, having a 7-(2-methyl-3-aminoazetidinyl) substituent, demonstrated higher levels of activity in vitro than their corresponding structural analogs, E-4528 and E-4527, distinguished by a 3-methyl-3-methylaminoazetidinyl group at position 7 of the quinolone nucleus. In consequence, E-4534 was the most potent of the new agents tested.

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Selected References

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