Fluoronaphthyridines and quinolones as antibacterial agents. 1. Synthesis and structure-activity relationship of new 1-substituted derivatives
摘要:
A series of novel 7-piperazinyl-1-substituted-6-fluoroquinolones and naphthyridines have been prepared and their antibacterial activities evaluated. These derivatives are characterized by having alkyl, alkenyl, arylalkyl, cycloalkyl, and cycloalkenyl groups at the 1-position. As a result of this study, derivatives 7 and 26, which are substituted with tert-butyl groups at N-1, were found to possess excellent in vitro and in vivo potency, particularly against Staphylococcus aureus, comparable to that of norfloxacin or ciprofloxacin. Structure-activity relationships of N-1 substituted alkyls and cycloalkyls are also discussed.
Modular Access to Substituted Azocanes via a Rhodium-Catalyzed Cycloaddition–Fragmentation Strategy
作者:Megan H. Shaw、Rosemary A. Croft、William G. Whittingham、John F. Bower
DOI:10.1021/jacs.5b05215
日期:2015.7.1
A short entry to substituted azocanes by a Rh-catalyzed cycloaddition–fragmentation process is described. Specifically, exposure of diverse N-cyclopropylacrylamides to phosphine-ligated cationic Rh(I) catalyst systems under a CO atmosphere enables the directed generation of rhodacyclopentanone intermediates. Subsequent insertion of the alkene component is followed by fragmentation to give the heterocyclic
描述了通过 Rh 催化的环加成-断裂过程对取代的偶氮烷的简短介绍。具体来说,在 CO 气氛下将不同的 N-环丙基丙烯酰胺暴露于膦配位的阳离子 Rh(I) 催化剂体系可以直接生成罗达环戊酮中间体。随后插入烯烃组分,然后断裂,得到杂环目标。立体化学研究首次表明,烯烃插入到罗达环戊酮中是可逆的。
Fluoronaphthyridines and quinolones as antibacterial agents. 1. Synthesis and structure-activity relationship of new 1-substituted derivatives
作者:D. Bouzard、P. Di Cesare、M. Essiz、J. P. Jacquet、P. Remuzon、A. Weber、T. Oki、M. Masuyoshi
DOI:10.1021/jm00123a005
日期:1989.3
A series of novel 7-piperazinyl-1-substituted-6-fluoroquinolones and naphthyridines have been prepared and their antibacterial activities evaluated. These derivatives are characterized by having alkyl, alkenyl, arylalkyl, cycloalkyl, and cycloalkenyl groups at the 1-position. As a result of this study, derivatives 7 and 26, which are substituted with tert-butyl groups at N-1, were found to possess excellent in vitro and in vivo potency, particularly against Staphylococcus aureus, comparable to that of norfloxacin or ciprofloxacin. Structure-activity relationships of N-1 substituted alkyls and cycloalkyls are also discussed.