N-methyl ciprofloxacin (rhodanine unsaturated ketone) amide derivative and preparation method and application thereof

A technology of methyl ciprofloxacin and rhodanine, applied in the directions of drug combination, organic chemistry, anti-tumor drugs, etc.
CN104844590AInactive Publication Date: 2015-08-19HENAN UNIVERSITY
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
HENAN UNIVERSITY
Publication Date
2015-08-19
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses an N-methyl ciprofloxacin (rhodanine unsaturated ketone) amide derivative and a preparation method and an application thereof. The N-methyl ciprofloxacin (rhodanine unsaturated ketone) amide derivative adopts the following chemical structural general formula I (shown in the specification); and in the formula I, Ar represents a benzene ring or a substituted benzene ring or a furan ring or a pyridine ring. The N-methyl ciprofloxacin (rhodanine unsaturated ketone) amide derivative disclosed by the invention implements superposition of three pharmacophores of a chiral tricyclic fluoroquinolone skeleton, amide and rhodanine alpha, beta-unsaturated ketone, so that the antineoplastic activity of a new compound is improved, and the toxic or side effects on normal cells are reduced, and the N-methyl ciprofloxacin (rhodanine unsaturated ketone) amide derivative can be used as an antineoplastic active substance for developing an antineoplastic medicament of a brand-new structure.
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Description

technical field

[0001] The invention belongs to the technical field of innovative drug synthesis, and specifically relates to a kind of N-methylciprofloxacin (rhodanine unsaturated ketone) amide derivative, and also relates to N-methylciprofloxacin (rhodanine not saturated ketone) A preparation method of saturated ketone) amide derivatives and its application in the preparation of antitumor drugs. Background technique

[0002] New drug innovation originates from the discovery of lead substances, and structure-based rational drug design is an effective method to discover lead substances. Among the various pharmacophore structures, five-membered heterocyclic ketones with a wide range of pharmacological activities, especially rhodanine, have become the dominant framework in medicinal chemistry and are widely used in the construction of new drug molecular chemical frameworks. It mainly includes α, β-unsaturated ketone derivatives constructed by the condensation reaction of acti...

Claims

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