93983-13-2Relevant articles and documents
Synthesis and in vitro antibacterial activity of gemifloxacin derivatives containing a substituted benzyloxime moiety
Feng, Lianshun,Lv, Kai,Liu, Mingliang,Wang, Shuo,Zhao, Jing,You, Xuefu,Li, Sujie,Cao, Jue,Guo, Huiyuan
, p. 125 - 136 (2012/11/07)
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
Heterocyclic compounds
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Page/Page column 12, (2010/02/14)
The inventive subject matter relates to compounds, pharmaceutical compositions, and kits containing a heterocyclic compound represented by the formula (I) wherein R is an alkyl group optionally having substituent(s) etc., X is an amino group optionally having substituent(s), Y1 and Y2 are nitrogen atoms etc., an isomer or solvate thereof or a pharmaceutically acceptable salt thereof as an active ingredient.
Synthesis and Renal Vasodilator Activity of 2-Chlorodopamine and N-Substituted Derivatives
McCarthy, James R.,McCowan, Jefferson,Zimmerman, Mark B.,Wenger, Marcia A.,Emmert, Lee W.
, p. 1586 - 1590 (2007/10/02)
A four-step synthesis of 2-chlorodopamine (2b) is presented as well as methods for the syntheses of the N-methyl, ethyl, and n-propyl analogues (2c-e).Compounds 2b and 2c were essentially equipotent to dopamine for increasing renal blood flow in anesthesized dogs that had been treated with the α-adrenergic antagonist phenoxybenzamine.The increases in renal blood flow were blocked by the DA1 antagonist (R)-(+)-8-chloro-2,3,4,5-tetrahydro-3-methyl-5-phenyl-1H-3-benzazepine.Compounds 2d and 2e were significantly less potent than dopamine in the same model; the increases in renal blood flow were attenuated by propanolol and blocked by a combination of propanolol and (R)-(+)-8-chloro-2,3,4,5-tetrahydro-3-methyl-5-phenyl-1H-3-benzazepine.The significance of an o-chloro substituent on dopamine analogues for the activation of the DA1 receptor is briefly discussed.
