98105-69-2Relevant academic research and scientific papers
Syntheses and biological activities of new N1-aryl substituted quinolone antibacterials
Juergens, Jens,Schedletzky, Holger,Heisig, Peter,Seydel, Joachim K.,Wiedemann, Bernd,Holzgrabe, Ulrike
, p. 179 - 190 (2007/10/03)
A series of quinolones with a systematically varied substitution at the phenyl ring at N1 has been synthesized. Three lipophilicity descriptors (log K, log P, R(m)) and the pK(a) values have been determined as well as the microbiological activity: The MIC
Synthesis and Structure-Activity Relationships of Novel Arylfluoroquinolone Antibacterial Agents
Chu, Daniel T. W.,Fernandes, Prabhavathi B.,Claiborne, Akiyo K.,Pihuleac, Eva,Nordeen, Carl W.,et al.
, p. 1558 - 1564 (2007/10/02)
A series of novel arylfluoroquinolones has been prepared.These derivatives are characterized by having a fluorine atom at the 6-position, substituted amino groups at the 7-position, and substituted phenyl groups at the 1-position.Structure-activity relationship (SAR) studies indicate that the in vitro antibacterial potency is greatest when the 1-substituent is either p-fluorophenyl or p-hydroxyphenyl and the 7-substituent is either 1-piperazinyl, 4-methyl-1-piperazinyl, or 3-amino-1-pyrrolidinyl.The electronic and spatial properties of the 1-substituent, as well as the steric bulk, play important roles in the antimicrobial potency in this class of antibacterials.As a result of this study, compounds 45 and 41 were found to possess excellent in vitro potency and in vivo efficacy.
