Synthesis and bacterial DNA gyrase inhibitory properties of a spirocyclopropylquinolone derivative
- 1 September 1988
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 31 (9) , 1694-1697
- https://doi.org/10.1021/jm00117a005
Abstract
A novel conformationally restricted 1-cyclopropylquinolone (1) that incorporates structural features of both ofloxacin and ciprofloxacin has been prepared. Compound 1 was found to be a DNA gyrase inhibitor having potency similar to ofloxacin but less than ciprofloxacin. The cellular inhibitory and in vivo antibacterial potencies of 1 were found to be less than those of the two reference agents.This publication has 7 references indexed in Scilit:
- Chiral DNA gyrase inhibitors. 2. Asymmetric synthesis and biological activity of the enantiomers of 9-fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid (ofloxacin)Journal of Medicinal Chemistry, 1987
- Synthesis and structure-activity relationship of 1-aryl-6,8-difluoroquinolone antibacterial agentsJournal of Medicinal Chemistry, 1987
- Inactivation of .gamma.-aminobutyric acid aminotransferase by (S,E)-4-amino-5-fluoropent-2-enoic acid and effect on the enzyme of (E)-3-(1-aminocyclopropyl)-2-propenoic acidJournal of Medicinal Chemistry, 1986
- Mechanism of inhibition of DNA gyrase by analogues of nalidixic acid: the target of the drugs is DNA.Proceedings of the National Academy of Sciences, 1985
- Novel amino-substituted 3-quinolinecarboxylic acid antibacterial agents: synthesis and structure-activity relationshipsJournal of Medicinal Chemistry, 1984
- Cloning and simplified purification of Escherichia coli DNA gyrase A and B proteins.Journal of Biological Chemistry, 1984
- Structure-activity relationships of antibacterial 6,7- and 7,8-disubstituted 1-alkyl-1,4-dihydro-4-oxoquinoline-3-carboxylic acidsJournal of Medicinal Chemistry, 1980