- Studies on prodrugs. 7. Synthesis and antimicrobial activity of 3-formylquinolone derivatives
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Several 3-formylquinolone derivatives (8a-c) were synthesized to assay the antibacterial activity both in vitro and in vivo. In vitro, all of the compounds 8a-c showed lower activity than that of the corresponding 3-carboxyl compounds 1a-c, and in vivo, they showed higher activity than that of compounds 1a-c. After oral administration of 3-formyl compounds 8a-c to mice, the compounds were rapidly metabolized into 3-carboxyl compounds 1a-c. In particular, the 3-formyl derivative (8a) of norfloxacin (NFLX, 1a) gave a 2-fold higher serum level than that of NFLX and functioned as a prodrug of NFLX.
- Kondo,Sakamoto,Kawakami,Tsukamoto
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- Mechlorethamine quinolone derivative and preparing method and application thereof
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The invention relates to a mechlorethamine quinolone derivative (I). A preparing method of the derivative comprises the steps of firstly, conducting reduction and formylation on a quinolone compound to prepare 3-formyl quinolone (IV), and then carrying ou
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Paragraph 0014; 0020; 0022
(2019/06/07)
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- Pefloxacin aldehyde aminothiourea derivative as well as preparation method and application thereof
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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.
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Paragraph 0031; 0032
(2017/07/14)
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- Pefloxacin aldolase 4-aryl thiosemicarbazides derivative and preparation method and application thereof
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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.
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Paragraph 0031; 0032
(2017/07/19)
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- REDOX DRUG DERIVATIVES
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The present invention provides redox drug derivatives. In particular, 9-fluoro-2,3- dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7H-pyrido[1,2,3-de]-1,4- benzoxazine-6-carboxylic acid, 1-ethyl-6-fluoro-1,4-dihydro-7-(4-methyl-1-piperazinyl)-4- oxo-3-quinolinecarboxylic acid, (3R, 4R, 5S)-4-(acetylamino)-5-amino-3-(1- ethylpropoxy)-1-cyclohexene-1-carboxylic acid ethyl ester, (3S)-3-(aminomethyl)-5- methylhexanoic acid, (3S)-1 -[2-(2,3-dihydro-5-benzofuranyl)ethyl]-α-α-diphenyl-3- pyrrolidineacetamide, (1S,2S,3S,4R)-3-[(1S)-1 -acetamido-2-ethyl-butyl]-4- (diaminomethylideneamino)-2-hydroxy-cyclopentane-1-carboxylic acid and (2R,3R,4S)- 4-[(diaminomethylidene)amino]-3-acetamido-2-[(1R,2R)-1,2,3-trihydroxypropyl]-3,4- dihydro-2H-pyran-6-carboxylic acid redox derivatives.
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Page/Page column 40
(2010/12/17)
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