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6-hydroxy derivative as new desfluoroquinolone (DFQ): synthesis and DNA-binding study.

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1
Istituto di Chimica e Tecnologia del Farmaco, Università degli Studi di Perugia, Italy.

Abstract

A new 6-desfluoroquinolone derivative, characterized by the presence of a 6-hydroxyl group instead of the usual fluorine atom at the C-6 position, was synthesized with the aim to better understand the mechanistic role of the C-6 substituent in the quinolone/DNA/DNA-gyrase interaction. The antibacterial activity unambiguously shows that the hydroxyl group is a good substitute for the C-6 fluorine atom, especially against Gram-positive bacteria. On the contrary, it is a very weak inhibitor of the target DNA gyrase, displaying the highest IC50 value observed for all the C-6 substituted analogues. This behaviour could be explained on the basis of its DNA binding properties.

PMID:
11097062
DOI:
10.1080/15257770008033055
[Indexed for MEDLINE]
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