Levo-fluoroquinolone C3 bisazole methyl sulfide, preparation method and application thereof
A technology of levofluoroquinolones and fluoroquinolones, which is applied in the field of medicine, can solve the problems that the study of electron isosteres has not been reported, and achieve the effects of strong in vitro cytotoxicity and strong anti-tumor activity
Inactive Publication Date: 2012-03-28
河南省健康伟业生物医药研究股份有限公司
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Problems solved by technology
In addition, although there are a large number of synthetic reports on azole compounds, the research on the isosteres of the C-3 carboxyl group of levofloxacin has not been reported yet.
Method used
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Embodiment 1
[0042] (S)-8,1-[1,2-(oxypropyl)]-6-fluoro-7-(4-methylpiperazin-1-yl)-3-[5-(5-phenyl- 1,3,4-oxadiazol-2-methylthio)-1,3,4-oxadiazol-2-yl]-4(1H)-quinolinone, the structural formula is:
[0043]
Embodiment 2
[0045] (S)-8,1-[1,2-(oxypropyl)]-6-fluoro-7-(4-methylpiperazin-1-yl)-3-[5-(5-p-methoxy Phenyl-1,3,4-oxadiazol-2-methylthio)-1,3,4-oxadiazol-2-yl]-4(1H)-quinolinone, the structural formula is:
[0046]
Embodiment 3
[0048] (S)-8,1-[1,2-(oxypropyl)]-6-fluoro-7-(4-methylpiperazin-1-yl)-3-[5-(5-p-tolyl -1,3,4-oxadiazol-2-methylthio)-1,3,4-oxadiazol-2-yl]-4(1H)-quinolinone, the structural formula is:
[0049]
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The invention belongs to the technical field of medicine, and in particular discloses a levo-fluoroquinolone C3 bisazole methyl sulfide, a preparation method and application thereof in the field of pharmacy. The chemical structural formula of the levo-fluoroquinolone C3 bisazole methyl sulfide is shown as a general formula I, wherein in the general formula I, X is selected from any one of O, S and -NH; and Ar is selected from any one of phenyl, substituent-containing phenyl and heterocyclic aromatic hydrocarbon. The levo-fluoroquinolone C3 bisazole methyl sulfide has strong in vitro cytotoxin effect on experimental leukemia cancer cell strains, has strong anti-tumor activity, and can be mixed with a human acceptable acid salt or a medicinal carrier to prepare an anti-tumor medicament.
Description
technical field [0001] The invention relates to the technical field of medicine, in particular to levofluoroquinolone C3 bisazole methide, and also relates to a preparation method of levofluoroquinolone C3 bisazole methide and its application in the field of pharmacy. Background technique [0002] Fluoroquinolones (FQ) are clinical antibacterial drugs developed in the 1980s, represented by norfloxacin. Based on the similar function of its target topoisomerase (TOPO) and mammalian TOPO, it is a new research direction to transform antibacterial FQ into antitumor FQ. Although anti-tumor FQ compounds including bicyclic quinolones, tricyclic quinolones, tetracyclic quinolones, chiral quinolones, flavonoids and other anti-tumor FQ compounds have been designed and synthesized, at present, these compounds have toxicity and activity in parallel to varying degrees, and poor solubility in vivo Lead to common problems such as low bioavailability and easy metabolic inactivation in vivo ...
Claims
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IPC IPC(8): C07D498/06A61K31/5383A61P35/00
Inventor 胡国强叶乾堂于振艳陈蕴刘浩李建勋康建党黄福生
Owner 河南省健康伟业生物医药研究股份有限公司
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