- Synthesis and in vitro antibacterial activity of gemifloxacin derivatives containing a substituted benzyloxime moiety
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A series of novel gemifloxacin (GMFX) derivatives containing a substituted benzyloxime moiety with remarkable improvement in lipophilicity were synthesized. The target compounds evaluated for their in vitro antibacterial activity against representative strains. Our results reveal that most of the target compounds have considerable potency against all of the tested Gram-positive strains including MRSA and MRSE (MIC: 90: 1 μg/mL) is 8-fold more active than GMFX, and 2-fold more active than GMFX and moxifloxacin against MRSE clinical isolates (MIC90: 4 μg/mL). Crown Copyright
- Feng, Lianshun,Lv, Kai,Liu, Mingliang,Wang, Shuo,Zhao, Jing,You, Xuefu,Li, Sujie,Cao, Jue,Guo, Huiyuan
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p. 125 - 136
(2012/11/07)
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- Gold(I)-catalyzed synthesis of benzoxocines by an 8-endo-dig cyclization
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A golden dig! Gold-catalyzed direct access to functionalized 2H-1-benzoxocines, eight-membered-ring ethers, is described. This unprecedented synthesis of benzoxocines occurs by an 8-endo-dig cyclization of the 1,7-enyne substrates. Copyright
- Wittstein, Kathrin,Kumar, Kamal,Waldmann, Herbert
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supporting information; experimental part
p. 9076 - 9080
(2011/10/12)
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- Low molecular weight dendritic compounds as pharmaceutical agents
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This invention is for low molecular weight dendritic polymers (dendroids) of Formula I are useful as agents in the treatment of cancer, Alzheimers disease, thrombosis, inflammatory diseases, and bacterial resistance.
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- 1-benzyl-1,3-dihydroindol-2-one derivatives, their preparation and the pharmaceutical compositions in which they are present
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The present invention relates to 1-benzyl-1,3-dihydroindol-2-one derivatives of the formula (I). The invention also relates to preparation of these derivatives as well as to the pharmaceutical compositions in which they are present. These derivatives have
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- ANTIVIRAL ETHERS OF ASPARTATE PROTEASE SUBSTRATE ISOSTERES
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Antiretroviral compounds (which are effective, for example, against HIV) of the formula I STR1 in which R 1 is an acyl radical lower-alkoxyl-lower-alkanoyl whose lower alkoxy radical is unsubstituted or is substituted by halogen, phenyl, lower alkoxy or a heterocyclic radical selected from piperidinyl, pyrrolidinyl, tetrahydropyranyl, tetrahydrofuranyl, thiazolidinyl, thiazolyl, indolyl or 4H-1-benzopyranyl which is unsubstituted or substituted by oxo, hydroxyl, amine, lower alkyl, lower-alkoxycarbonyl and/or phenyl-lower-alkoxycarbonyl; lower alkanoyl which is unsubstituted or is substituted by one of the said unsubstituted or substituted heterocyclic radicals; arylcarbonyl or heterocyclylcarbonyl which are substituted by heterocyclyl or heterocyclyl-lower-alkyl; phenyl-lower-alkanoyl which is substituted by hydroxyl and lower alkyl; or arylsulfonyl;or the residue of an amino acid which is defined in accordance with the description (and which may be acylated on the amino nitrogen by one of the abovementioned acyl radicals);R 2 and R 3 are in each case cyclohexyl, cyclohexenyl, phenyl, naphthyl or tetrahydronaphthyl which are unsubstituted or substituted by lower alkyl, phenyl, cyanophenyl, phenyl-lower-alkyl, halogen, halo-lower-alkyl, cyano, hydroxyl, lower alkoxy, phenyl-lower-alkoxyl, pyridyl-lower-alkoxy, lower-alkoxy-lower-alkoxy, lower-alkoxycarbonyl-lower-alkoxy, carboxyl-lower-alkoxy, hydroxyl-lower-alkoxy, carbamoyl-lower-alkoxy, cyano-lower-alkoxy, and phenyl-lower-alkanesulfonyl which is unsubstituted or substituted by halogen;R 4 is lower alkyl, cyclohexyl or phenyl; and R 5 is lower alkyl; and n is 1 or 2, or salts thereof, are novel.
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- 1-benzyl-1,3-dihydro-2H-benzimidazol-2-one derivatives, their preparation and the pharmaceutical compositions containing them
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The present invention relates to 1-benzyl-1,3-dihydro-2H-benzimidazol-2-one derivatives, of formula: STR1 and to the possible salts thereof, to a process for their preparation and to the pharmaceutical compositions containing them.These compounds have an
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- Synthesis of potent and orally active HIV-protease inhibitors
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A series of potent HIV-protease inhibitors has been prepared. Several of the newly synthesized compounds showed high plasma levels after oral administration to animals. Based on the overall biological profile, CGP 61755 was chosen for further preclinical evaluation. For this compound, a 10 step synthesis potentially suitable for large scale production was developed.
- Capraro, Hans-Georg,Bold, Guido,Faessler, Alexander,Cozens, Robert,Klimkait, Thomas,Lazdins, Janis,Mestan, Juergen,Poncioni, Bernard,Roesel, Johannes L.,Stover, David,Lang, Marc
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p. 273 - 278
(2007/10/03)
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