Pefloxacin aldolase 4-aryl thiosemicarbazides derivative and preparation method and application thereof

Abstract

The invention discloses a pefloxacin aldolase 4-aryl thiosemicarbazides derivative. The structural formula is shown in formula I in the specification, wherein the substituent group Ar is a benzene ring, a substituted benzene ring, a pyridine ring, a furan ring or a thiofuran ring. The invention also discloses a preparation method and an application of the pefloxacin aldolase 4-aryl thiosemicarbazides derivative. The pefloxacin aldolase 4-aryl thiosemicarbazides derivative has the advantages that the three types of superior pharmacophores of tricyclic fluoroquinolone keel, imine Schiff base and thiourea are compounded, so that the anti-tumor activity of a new compound is improved, and the toxic or side effect to normal cells is decreased; the derivative can be used as an anti-tumor active substance to develop an anti-tumor drug with a new structure.

Description

technical field

[0001] The invention belongs to the technical field of new drug discovery and innovative drug synthesis, and specifically relates to a pefloxacin acetal 4-aryl thiosemicarbazide derivative, a preparation method thereof, and an application thereof as an antitumor drug. Background technique

[0002] The innovation of new drugs originates from the discovery of leads, and the construction of lead molecules based on the combination of dominant pharmacophore skeletons is the most economical and effective strategy. The thiosemicarbazone derivatives constructed from aldehydes or ketones and thiosemicarbazides have attracted much attention because they are easy to form complexes or chelate with macromolecules or metal ions, and exhibit a wide range of pharmacological activities. However, most of the aldehydes or ketones used to construct thiosemicarbazone molecules are common benzenes or heterocyclic aromatic aldehydes and ketones, while quinoline aldehydes, especiall...

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