[Studies on pyridonecarboxylic acids as antibacterial agents. XII. Synthesis and antibacterial activity of 6-chloro-1-cyclopropyl-7-(1-piperazinyl)-1, 4-dihydro-4-oxo-quinoline-3-carboxylic acid and analogues]. 1997

X H Li, and Z M Tian, and H Miao, and L X Yu, and H Y Guo
Institute of Medicinal Biotechnology, Chinese Acadeny of Medical Sciences, Peking Union Medical College, Beijing 100050.

Sixteen pyridonecarboxylic acids, characterized by having a chlorine atom and a cyclopropyl group at the 6- and 1-position respectively, substituted amino groups at the 7-position, and some substituted groups (chloro, nitro, amino, dimethylamino) at the 8-position, were synthesized. In vitro antibacterial activities of these compounds were tested. The fluoroquinolones ciprofloxacin and norfloxacin were included for comparative purposes. The results showed that both 11 Ca and 11 Cc were 4-8 times more active than ciprofloxacin and norfloxacin against S. aureus-15 in vitro, but with the same activity as ciprofloxacin against E. coli-22 and P. aeruginosa-29.

UI MeSH Term Description Entries
D009643 Norfloxacin A synthetic fluoroquinolone (FLUOROQUINOLONES) with broad-spectrum antibacterial activity against most gram-negative and gram-positive bacteria. Norfloxacin inhibits bacterial DNA GYRASE. AM-0715,AM-715,MK-0366,MK-366,MK0366,MK366,Noroxin,AM 0715,AM 715,AM0715,MK 0366,MK 366
D011550 Pseudomonas aeruginosa A species of gram-negative, aerobic, rod-shaped bacteria commonly isolated from clinical specimens (wound, burn, and urinary tract infections). It is also found widely distributed in soil and water. P. aeruginosa is a major agent of nosocomial infection. Bacillus aeruginosus,Bacillus pyocyaneus,Bacterium aeruginosum,Bacterium pyocyaneum,Micrococcus pyocyaneus,Pseudomonas polycolor,Pseudomonas pyocyanea
D011728 Pyridones Pyridine derivatives with one or more keto groups on the ring. Pyridinones
D002264 Carboxylic Acids Organic compounds containing the carboxy group (-COOH). This group of compounds includes amino acids and fatty acids. Carboxylic acids can be saturated, unsaturated, or aromatic. Carboxylic Acid,Acid, Carboxylic,Acids, Carboxylic
D002939 Ciprofloxacin A broad-spectrum antimicrobial carboxyfluoroquinoline. Bay-09867,Ciprinol,Cipro,Ciprofloxacin Hydrochloride,Ciprofloxacin Hydrochloride Anhydrous,Ciprofloxacin Monohydrochloride Monohydrate,Anhydrous, Ciprofloxacin Hydrochloride,Bay 09867,Bay09867,Hydrochloride Anhydrous, Ciprofloxacin,Hydrochloride, Ciprofloxacin,Monohydrate, Ciprofloxacin Monohydrochloride,Monohydrochloride Monohydrate, Ciprofloxacin
D004926 Escherichia coli A species of gram-negative, facultatively anaerobic, rod-shaped bacteria (GRAM-NEGATIVE FACULTATIVELY ANAEROBIC RODS) commonly found in the lower part of the intestine of warm-blooded animals. It is usually nonpathogenic, but some strains are known to produce DIARRHEA and pyogenic infections. Pathogenic strains (virotypes) are classified by their specific pathogenic mechanisms such as toxins (ENTEROTOXIGENIC ESCHERICHIA COLI), etc. Alkalescens-Dispar Group,Bacillus coli,Bacterium coli,Bacterium coli commune,Diffusely Adherent Escherichia coli,E coli,EAggEC,Enteroaggregative Escherichia coli,Enterococcus coli,Diffusely Adherent E. coli,Enteroaggregative E. coli,Enteroinvasive E. coli,Enteroinvasive Escherichia coli
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D000890 Anti-Infective Agents Substances that prevent infectious agents or organisms from spreading or kill infectious agents in order to prevent the spread of infection. Anti-Infective Agent,Anti-Microbial Agent,Antimicrobial Agent,Microbicide,Microbicides,Anti-Microbial Agents,Antiinfective Agents,Antimicrobial Agents,Agent, Anti-Infective,Agent, Anti-Microbial,Agent, Antimicrobial,Agents, Anti-Infective,Agents, Anti-Microbial,Agents, Antiinfective,Agents, Antimicrobial,Anti Infective Agent,Anti Infective Agents,Anti Microbial Agent,Anti Microbial Agents
D013203 Staphylococcal Infections Infections with bacteria of the genus STAPHYLOCOCCUS. Infections, Staphylococcal,Staphylococcus aureus Infection,Staphylococcal Infection,Staphylococcus aureus Infections
D013211 Staphylococcus aureus Potentially pathogenic bacteria found in nasal membranes, skin, hair follicles, and perineum of warm-blooded animals. They may cause a wide range of infections and intoxications.

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