A bis-fluoroquinolone oxadiazuron pefloxacin derivative and its preparation method and application

A technology of fluoroquinolone oxadiazoles and pefloxacin, applied to antineoplastic drugs, the field of bis-fluoroquinolone oxadiazoles and pefloxacin derivatives
CN109369675BInactive Publication Date: 2021-07-06ZHENGZHOU UNIV OF IND TECH
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
ZHENGZHOU UNIV OF IND TECH
Publication Date
2021-07-06
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a bis-fluoroquinolone oxadiazuron pefloxacin derivative and its preparation method and application. Its general chemical structure is shown in the following formula: in the formula, R is ethyl, cyclopropyl, Fluoroethyl, oxazine ring formed with C-8 position or thiazine ring formed with C-8 position; L is an independent chlorine atom, fluorine atom, 1-piperazinyl, substituted piperazin-1-yl Or nitrogen-fused heterocycle; X is ‑CH, N, ‑CF or ‑C‑O‑CH 3 . The bis-fluoroquinolone oxadiazole urea pefloxacin derivatives of the present invention realize the organic combination of bis-fluoroquinolone skeleton, oxadiazole heterocycle and functional urea, and then realize the migration of different pharmacophore The superposition of more and more innovates the new structure of drug molecules, which in turn increases the anti-tumor activity and selectivity of fluoroquinolones, reduces the toxic and side effects on normal cells, and can be used as an anti-tumor active substance to develop anti-tumor drugs with a new structure.
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Description

technical field

[0001] The invention is a drug innovation research, and specifically relates to a bis-fluoroquinolone oxadiazuron pefloxacin derivative, and also relates to a preparation method of the derivative and its application in antitumor drugs. Background technique

[0002] The research and development of new drugs originates from the discovery of lead substances, and the structural optimization of lead substances is the key link to promote their development into finished drugs. A rational drug design strategy based on structure or mechanism, using the dominant skeleton or pharmacophore fragments of existing drugs to create new small molecule leads with therapeutic and functional regulation for major diseases such as malignant tumors is the most economical and effective strategy for new drug development. Based on this, on the one hand, it is considered that fluoroquinolones (FQs) are widely used as a class of clinical antibacterial drugs, and their antibacterial domin...

Claims

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