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Isothiazolopyridones: synthesis, structure, and biological activity of a new class of antibacterial agents.

Abstract：

:We report the syntheses of first-generation derivatives of isothiazolopyridones and their in vitro evaluation as antibacterial agents. These compounds, containing a novel heterocyclic nucleus composed of an isothiazolone fused to a quinolizin-4-one (at C-2 and C-3 of the quinolizin-4-one), were prepared using a sequence of seven synthetic transformations. The solid-state structure of 7-chloro-9-ethyl-1-thia-2,4a-diazacyclopenta[b]naphthalene-3,4-dione was determined by X-ray diffraction. The prepared derivatives of desfluoroisothiazolopyridones exhibited (a) antibacterial activity against Gram-negative and Gram-positive organisms, (b) inhibitory activities against DNA gyrase and topoisomerase IV, and (c) no inhibitory activity against human topoisomerase II.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Wiles JA,Hashimoto A,Thanassi JA,Cheng J,Incarvito CD,Deshpande M,Pucci MJ,Bradbury BJ

doi

10.1021/jm051066d

keywords:

subject

Has Abstract

pub_date

2006-01-12 00:00:00

pages

39-42

issue

1

eissn

0022-2623

issn

1520-4804

journal_volume

49

pub_type

杂志文章

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