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Synonyms: Ro 09-1437
Compound class: Natural product or derivative
Comment: Cyclothialidine is a potent DNA gyrase inhibitor, isolated from Streptomyces filipinensis following microbial broth screening . It belongs to a novel class of antibacterial compounds, containing a unique 12-membered lactone ring that is partly integrated into a pentapeptide chain, that exhibit broad-spectrum in vitro activity against Gram-positive bacteria. Further development of cyclothialidine has been precluded due to low growth-inhibitory activity against intact bacterial cells but analogues with improved in vivo efficacy have been synthesized .
1. Angehrn P, Buchmann S, Funk C, Goetschi E, Gmuender H, Hebeisen P, Kostrewa D, Link H, Luebbers T, Masciadri R et al.. (2004)
New antibacterial agents derived from the DNA gyrase inhibitor cyclothialidine.
J Med Chem, 47 (6): 1487-513. [PMID:14998336]
2. Nakada N, Gmünder H, Hirata T, Arisawa M. (1994)
Mechanism of inhibition of DNA gyrase by cyclothialidine, a novel DNA gyrase inhibitor.
Antimicrob Agents Chemother, 38 (9): 1966-73. [PMID:7811004]
3. Nakada N, Shimada H, Hirata T, Aoki Y, Kamiyama T, Watanabe J, Arisawa M. (1993)
Biological characterization of cyclothialidine, a new DNA gyrase inhibitor.
Antimicrob Agents Chemother, 37 (12): 2656-61. [PMID:8109932]