- Syntheses and biological activities of new N1-aryl substituted quinolone antibacterials
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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
- Juergens, Jens,Schedletzky, Holger,Heisig, Peter,Seydel, Joachim K.,Wiedemann, Bernd,Holzgrabe, Ulrike
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p. 179 - 190
(2007/10/03)
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- Intermediates for producing quinolone-3-carboxylic acids
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A process for producing a 1,4-dihydro-4-oxo-quinoline-3-carboxylic acid by reacting an acctophenone with a dialkoxycarbonate to obtain the corresponding β-ketoester, treating the β-ketoester with a trialkylorthoformate in the presence of an acid anhydride
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- Quinoline antibacterial compounds
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Quinoline compounds having the formula: STR1 wherein R is a phenyl group or an aromatic heterocyclic group, Z is an aliphatic heterocyclic group or an amine, and R1 is hydrogen or a carboxy-protecting group. The compounds here disclosed have an
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- Synthesis and Structure-Activity Relationships of Novel Arylfluoroquinolone Antibacterial Agents
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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.
- Chu, Daniel T. W.,Fernandes, Prabhavathi B.,Claiborne, Akiyo K.,Pihuleac, Eva,Nordeen, Carl W.,et al.
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p. 1558 - 1564
(2007/10/02)
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