57results about How to "To achieve the effect of increasing efficiency and reducing toxicity" patented technology

The invention discloses a 3,3'-methene-difluoroquinolone derivative of a chiral oxazine quinoline ring as well as a preparation method and application of the 3,3'-methene-difluoroquinolone derivative. The 3,3'-methene-difluoroquinolone derivative has a chemical general structural formula I shown in the specification, wherein R represents cyclopropyl or ethyl or fluoroethyl; R1 represents a hydrogen atom or methyl or ethyl; R2 represents a hydrogen atom or methyl; X represents a nitrogen atom or a hydrocarbon (CH) group or a fluoro-substituted carbon atom (F-C) or a methoxyl-substituted carbon atom (CH3O-C). The 3,3'-methene-difluoroquinolone derivative of the chiral oxazine quinoline ring, disclosed by the invention, can be used for realizing the superposition of a difluoroquinolone framework and alpha, beta-unsaturated ketone pharmacophores, so that the antitumor activity of a new compound is improved, the toxic and side effects on normal cells can be reduced, and the 3,3'-methene-difluoroquinolone derivative can be used as an antitumor active substance for developing an antitumor drug of a totally new structure.

The invention provides a plant raw material composition with an anti-fatigue effect, a preparation method, an application and a product thereof. The composition is prepared from the following in proportion: 20 to 80 percent of rhodiola rosea plants, 10 to 60 percent of gynostemma pentaphylla plants, and 10 to 60 percent of lycium plants. Auxiliary materials can be added into the composition to prepare health-care products, foods or anti-fatigue medicament. The medicament can obviously improve the fatigue symptom of fatigue people, and improve sleep quality without affecting human normal physiologic indexes. The medicament can improve the oxygen supply capability of a body, and plays a role of resisting fatigue by potentially improving the function of red blood cells and platelets. The medicinal composition uses small effective dosage, has good water solubility, and is suitable for preparing various preparations.

The invention discloses N-methyl gatifloxacin aldehyde thiosemicarbazone derivative and a preparation method and application thereof. The N-methyl gatifloxacin aldehyde thiosemicarbazone derivative has a chemical structural formula as a following formula I. In the formula I, substituent R is an H atom or alkyl or cyclopropyl with 1 to 5 carbon atoms. According to the N-methyl gatifloxacin aldehyde thiosemicarbazone derivative disclosed by the invention, combination of three kinds of advantage pharmacophore of a fluoroquinolone framework, imine Schiff base, thiourea and the like is achieved; thus, antineoplastic activity of novel compound is improved, a toxic and side effect of normal cells is reduced, and the N-methyl gatifloxacin aldehyde thiosemicarbazone derivative can serve as antineoplastic activity substance to develop antineoplastic drug with a novel structure.

The invention discloses a levofloxacin (rhodanine unsaturated ketone) amide derivative and a preparation method and an application thereof. The levofloxacin (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. On the basis of a medicine molecule construction strategy of pharmacophore splice, the levofloxacin (rhodanine unsaturated ketone) amide derivative disclosed by the invention implements superposition of four pharmacophores of a chiral tricyclic fluoroquinolone skeleton, amide, rhodanine and alpha, beta-unsaturated ketone, so that the antineoplastic activity of a new compound is improved, the toxic or side effects on normal cells are reduced, and the levofloxacin (rhodanine unsaturated ketone) amide derivative can be used as an antineoplastic active substance for developing an antineoplastic medicament of a brand-new structure.

The invention discloses an N-methylmoxifloxacin aldehyde thiosemicarbazone derivative, and a preparation method and an application thereof. The N-methylmoxifloxacin aldehyde thiosemicarbazone derivative has a structure as shown in a general formula I in the specification. In the general formula I, R is selected from the group consisting of an H atom, or a hydrocarbyl group with 1 to 5 carbon atoms or a cyclopropyl group. The N-methylmoxifloxacin aldehyde thiosemicarbazone derivative provided by the invention realizes combination of three advantage pharmacophores like a fluoroquinolone skeleton, Schiff base imine and thiourea, thereby adding the antitumor activity of a novel compound, reducing the toxic and side effects on normal cells, and being able to be used as an antitumor active substance to develop an antitumor drug with a novel structure.

The invention discloses an ofloxacin aldehyde thiosemicarbazone derivative, and a preparation method and an application thereof. A chemical structure general formula is as shown in the specification, wherein in the formula, R represents a hydrogen atom or alkyl or cyclopropyl of 1-5 carbon atoms. The ofloxacin aldehyde thiosemicarbazone derivative disclosed by the invention realizes the fusion of three advantageous pharmacophores, namely, tricyclic fluoroquinolone skeleton, schiff base imine and thiourea, thereby improving the antineoplastic activity of a new compound and reducing the toxic and side effects to normal cells, thus the ofloxacin aldehyde thiosemicarbazone derivative can be used as an antineoplastic drug of a brand-new structure developed for antineoplastic active substance.

The invention discloses a bis-fluoroquinolone thiadiazole ureas N-acetyl norfloxacin derivative and a preparation method and application thereof. The chemical structural general formula of the bis-fluoroquinolone thiadiazole ureas N-acetyl norfloxacin derivative is shown in the following formula I (shown in the specification), according to the formula I, R is ethyl or cyclopropyl or fluoroethyl oran oxazine ring formed with a C-8 position or a thiazine ring formed with the C-8 position, L is independent chlorine atom or fluorine atom or 1-piperazinyl or substituted piperazine-1-yl or a nitrogen fused heterocyclic ring, and X is hydrocarbon (CH) or nitrogen atom or fluorine-substituted carbon atom (F-C) or methoxy-group-substituted carbon atom (CH3O-C). According to the bis-fluoroquinolonethiadiazole ureas N-acetyl norfloxacin derivative and the preparation method and application thereof, organic combination of a bis-fluoroquinolone skeleton, the thiadiazole heterocyclic ring and functional group ureas is achieved, the charge transfer and superposition of different pharmacophore are further achieved, the anti-tumor activity and selectivity of fluoroquinolone are increased, toxic and side effects on normal cells are reduced, and the bis-fluoroquinolone thiadiazole ureas N-acetyl norfloxacin derivative can be used as anti-tumor active substances to develop anti-tumor drugs withbrand-new structures.

The invention discloses a pefloxacin aldehyde aminothiourea derivative as well as a preparation method and an application thereof. The following general chemical formula is as shown in the specification, wherein in the formula, R is hydrogen atom, or alkyl or cyclopropyl with 1-5 carbon atoms. The pefloxacin aldehyde aminothiourea derivative combines three advantageous pharmacophores including fluoroquinolone skeleton, Schiff base imine and thiourea, thus improving the anti-tumor activity of new compounds, reducing the toxic or side effect on normal cells, and being capable of being used as an anti-tumor activity material for developing brand-new anti-tumor medicaments.

The invention discloses an ofloxacin (rhodanine unsaturated ketone) amide derivative and a preparation method and an application thereof. The ofloxacin (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. On the basis of a medicine molecule construction strategy of pharmacophore splice, the ofloxacin (rhodanine unsaturated ketone) amide derivative disclosed by the invention implements superposition of four pharmacophores of a chiral tricyclic fluoroquinolone skeleton, amide, rhodanine and 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 ofloxacin (rhodanine unsaturated ketone) amide derivative can be used as an antineoplastic active substance for developing an antineoplastic medicament of a brand-new structure.

The invention discloses bis-fluoroquinolone oxadiazole urea derivatives containing N-methyl gatifloxacin as well as a preparation method and an application of the derivatives. The general chemical structural formula of the derivatives is represented as the formula I shown in the description; in the general formula, R is -CH2-CH3, cyclopropyl or -CH2-CH2F, L is -Cl, -F, 1-piperazinyl, substituted piperazine-1-yl or nitrogenous heterocyclic ring, X is -CH, -N, -CF or -COCH3, or R and X jointly constitute an oxazine ring or a thiazine ring. According to the bis-fluoroquinolone oxadiazole urea derivatives, organic splicing of a bis-fluoroquinolone skeleton, an oxadiazole heterocyclic ring and functional ureas is realized, hopping and stacking of different pharmacophores are realized, antitumoractivity and selectivity of fluoroquinolone are improved, toxic and side effects on normal cells are reduced, and the derivatives can be used as antitumor active substances to develop antitumor drugswith brand-new structure.

The invention discloses a Rufloxacin aldolase 4-aryl thiosemicarbazides derivative and a preparation method and an application thereof. The structural formula is shown in formula I in the specification, wherein Ar is phenyl, substituted phenyl, pyridyl, furyl or thienyl. The Rufloxacin 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.

The invention discloses N-methyl ciprofloxacin aldehyde thiosemicarbazone derivatives as well as a preparation method and application thereof. The chemical structure general formula of the derivatives is described in the description, wherein R is a hydrogen atom, or an alkyl or a cyclopropyl which has 1 to 5 carbon atoms. The N-methyl ciprofloxacin aldehyde thiosemicarbazone derivatives realize the splicing of three dominant pharmacophores, i.e. fluoroquinolone skeleton, Schiff base imine and thiourea, thus improving the antitumor activity of a new compound and reducing the toxic and side effects for normal cells; therefore, the N-methyl ciprofloxacin aldehyde thiosemicarbazone derivatives can be taken as anti-tumor active substances for developing anti-tumor drugs with brand-new structures.

The invention discloses an ofloxacin aldehyde thiosemicarbazone derivative, and a preparation method and an application thereof. A chemical structure general formula is as shown in the specification, wherein in the formula, R represents a hydrogen atom or alkyl or cyclopropyl of 1-5 carbon atoms. The ofloxacin aldehyde thiosemicarbazone derivative disclosed by the invention realizes the fusion of three advantageous pharmacophores, namely, tricyclic fluoroquinolone skeleton, schiff base imine and thiourea, thereby improving the antineoplastic activity of a new compound and reducing the toxic and side effects to normal cells, thus the ofloxacin aldehyde thiosemicarbazone derivative can be used as an antineoplastic drug of a brand-new structure developed for antineoplastic active substance.

The invention discloses a 3,3'-methene-difluoroquinolone derivative of a chiral oxazine quinoline ring as well as a preparation method and application of the 3,3'-methene-difluoroquinolone derivative. The 3,3'-methene-difluoroquinolone derivative has a chemical general structural formula I shown in the specification, wherein R represents cyclopropyl or ethyl or fluoroethyl; R1 represents a hydrogen atom or methyl or ethyl; R2 represents a hydrogen atom or methyl; X represents a nitrogen atom or a hydrocarbon (CH) group or a fluoro-substituted carbon atom (F-C) or a methoxyl-substituted carbon atom (CH3O-C). The 3,3'-methene-difluoroquinolone derivative of the chiral oxazine quinoline ring, disclosed by the invention, can be used for realizing the superposition of a difluoroquinolone framework and alpha, beta-unsaturated ketone pharmacophores, so that the antitumor activity of a new compound is improved, the toxic and side effects on normal cells can be reduced, and the 3,3'-methene-difluoroquinolone derivative can be used as an antitumor active substance for developing an antitumor drug of a totally new structure.

The invention discloses a 3,3'-methylene-bisfluoroquinolone derivative containing ethylquinoline rings as well as a preparation method and application thereof. The 3,3'-methylene-bisfluoroquinolone derivative containing ethylquinoline rings is a compound having the following structural general formula (I) as shown in the specification, wherein R1 is ethyl, cyclopropyl or fluoroethyl; R2 is H or methyl; R3 is H, methyl or ethyl; R4 is H or methyl; and X is CH, N, F-C or CH3O-C. The preparation method comprises the following steps of effectively combining fluoroquinolone pharmacophores and alpha, beta-unsaturated ketone pharmacophores and constructing two quinolone structural units into the 3,3'-methylene-bisfluoroquinolone derivative by virtue of condensation reaction, the anti-tumor activity is increased, the toxic and side effects to normal cells are decreased, the synergistic and toxicity-reducing effects are achieved and the 3,3'-methylene-bisfluoroquinolone derivative can be used as an anti-tumor active material to develop anticancer drugs having novel structures.

The invention discloses a bis-fluoroquinolone-based oxadiazole urea derivative containing N-methyloxacin and a preparation method and application of the bis-fluoroquinolone-based oxadiazole urea derivative. The chemical structural general formula is shown in formula I as shown in specification, in the general formula I, R is -CH2-CH3, cyclopropyl or -CH2-CH2F; L is -Cl, -F, 1-piperazinyl, substituted piperazine-1-yl or nitrogen-containing fused heterocycle; X is -CH, -N, -CF or -COCH3; or R and X jointly form an oxazine ring or phenothiazine ring. By the bis-fluoroquinolone-based oxadiazole urea derivative, organic combination of a bis-fluoroquinolone framework, an oxadiazole heterocyclic ring and functional urea is realized, therefore, transferring and overlapping of different pharmacophores are realized, the anti-tumor activity and selectivity of the fluoroquinolone are improved, toxic and side effects to normal cells are reduced, and the bis-fluoroquinolone-based oxadiazole urea derivative can serve as an anti-tumor active substance to develop an anti-tumor drug with a brand-new structure.

The invention discloses N-methyl ciprofloxacin aldolase 4-aryl thiosemicarbazide derivative. A chemical structural formula of the N-methyl ciprofloxacin aldolase 4-aryl thiosemicarbazide derivative is shown in the specification, wherein a substituent group Ar is a benzene ring, a substituent benzene ring, a pyridine ring, a furan ring or a thiophene ring. The invention further discloses a preparation method and application of the N-methyl ciprofloxacin aldolase 4-aryl thiosemicarbazide derivative. The N-methyl ciprofloxacin aldolase 4-aryl thiosemicarbazide derivative disclosed by the invention achieves combination of three kinds of advantageous pharmacophore of fluoroquinolone keel, Schiff base imine and thiourea, so that antineoplastic activity of the new compound is improved, toxic and side effects on normal cells are reduced, and the N-methyl ciprofloxacin aldolase 4-aryl thiosemicarbazide derivative can serve as an antineoplastic activity material to develop antineoplastic medicine of a full-novel structure.

The invention discloses bis-fluoroquinolone thiadiazole urea fleroxacin derivatives as well as a preparation method and an application thereof. The general chemical structure formula of the derivatives is shown in the formula I as follows in the description. In the formula I, R is ethyl, cyclopropyl, fluoroethyl, an oxazine ring formed with C-8 or a thiazine ring formed with C-8; L is an independent Cl or F atom, 1-piperazinyl, substituted piperazine-1-yl or a nitrogen fused heterocyclic ring; X is CH, N atom or F-substituted C atom (F-C) or a methoxy substituted C atom (CH3O-C). The bis-fluoroquinolone thiadiazole urea fleroxacin derivatives realize organic combination of a bis-fluoroquinolone skeleton and the thiadiazole heterocyclic ring with functional urea pharmacophores, so that transition and superposition of different pharmacophores are realized, anti-tumor activity and selectivity of fluoroquinolone are increased, toxic and side effects on normal cells are reduced, and the derivatives can be taken as an anti-tumor active substance for developing anti-tumor drugs with novel structures.

The invention discloses N-methyl ciprofloxacin aldolase 4-aryl thiosemicarbazide derivative. A chemical structural formula of the N-methyl ciprofloxacin aldolase 4-aryl thiosemicarbazide derivative is shown in the specification, wherein a substituent group Ar is a benzene ring, a substituent benzene ring, a pyridine ring, a furan ring or a thiophene ring. The invention further discloses a preparation method and application of the N-methyl ciprofloxacin aldolase 4-aryl thiosemicarbazide derivative. The N-methyl ciprofloxacin aldolase 4-aryl thiosemicarbazide derivative disclosed by the invention achieves combination of three kinds of advantageous pharmacophore of fluoroquinolone keel, Schiff base imine and thiourea, so that antineoplastic activity of the new compound is improved, toxic and side effects on normal cells are reduced, and the N-methyl ciprofloxacin aldolase 4-aryl thiosemicarbazide derivative can serve as an antineoplastic activity material to develop antineoplastic medicine of a full-novel structure.

The invention discloses an N-methylmoxifloxacin aldehyde thiosemicarbazone derivative, and a preparation method and an application thereof. The N-methylmoxifloxacin aldehyde thiosemicarbazone derivative has a structure as shown in a general formula I in the specification. In the general formula I, R is selected from the group consisting of an H atom, or a hydrocarbyl group with 1 to 5 carbon atoms or a cyclopropyl group. The N-methylmoxifloxacin aldehyde thiosemicarbazone derivative provided by the invention realizes combination of three advantage pharmacophores like a fluoroquinolone skeleton, Schiff base imine and thiourea, thereby adding the antitumor activity of a novel compound, reducing the toxic and side effects on normal cells, and being able to be used as an antitumor active substance to develop an antitumor drug with a novel structure.

The invention discloses levofloxacin aldolase thiosemicarbazide derivative and a preparation method and application thereof. A chemical structure general formula shown in the formula is adopted, wherein R is hydrogen atom and alkyl or cyclopropyl with 1-5 carbon atoms. According to the levofloxacin aldolase thiosemicarbazide derivative, splicing of advantageous pharmacophores of a chiral fluoroquinolone skeleton, schiff base imine and thiourea is achieved, so that the anti-tumor activity of a novel compound is improved, the toxic or side effect on a normal cell is reduced, and the levofloxacin aldolase thiosemicarbazide derivative can be used for developing an anti-tumor drug of a bran-new structure as an anti-tumor active material.

The invention discloses a fleroxacinaldehyde-4-aryl thiosemicarbazide derivative, as well as a preparation method and application thereof. The following chemical structural formula I is adopted: the formula is shown in the description, where a substituent Ar is a benzene ring or a substituted benzene ring or a pyridine ring or a furan ring or a thiophene ring. According to the fleroxacinaldehyde-4-aryl thiosemicarbazide derivative, three advantageous pharmacophores, i.e. a polyfluoroquinolone framework, Schiff base imine and thiourea, are mixed, thereby improving the anti-tumor activity of a new compound and reducing toxic or side effects on normal cells; the fleroxacinaldehyde-4-aryl thiosemicarbazide derivative can be used for developing an anti-tumor medicament of a new structure as an anti-tumor active substance.

The invention discloses an N-methyl enoxacin aldehyde-4-aryl thiosemicarbazide derivative, and a preparation method and application thereof. The N-methyl enoxacin aldehyde-4-aryl thiosemicarbazide derivative has a structure formula as shown in formula (1), wherein Ar is a phenyl group, a substituted phenyl group, a pyridyl group, a furan group or a thienyl group. According to the N-methyl enoxacin aldehyde-4-aryl thiosemicarbazide derivative disclosed by the invention, the combination of three advantaged pharmacophores, including fluorine naphthyridine ketone framework, Schiff base imine and thiourea can be realized, so that the anti-tumor activity of the new compound can be increased and the toxic and side effects to normal cells can be reduced. The N-methyl enoxacin aldehyde-4-aryl thiosemicarbazide derivative can be used as an anti-tumor active substance for developing an anti-tumor drug with a brand new structure.