Cyclothialidine analogs, novel DNA gyrase inhibitors.
DNA gyrase inhibitors, cyclothialidines B, C, D and E were isolated from four Streptomycete strains (NR 0659, NR 0660, NR 0661 and NR 0662). Their structures have been elucidated based on the amino acid analysis of the hydrolysates, NMR and HRFAB-MS experiments and shown to be cyclothialidine analogs. The absolute stereochemistry has been determined by the chiral HPLC analysis of the hydrolysates. Cyclothialidines B, D and E are novel and potent inhibitors of DNA gyrase.
Yamaji
K
K
Nippon Roche Research Center, Kanagawa, Japan.
Masubuchi
M
M
Kawahara
F
F
Nakamura
Y
Y
Nishio
A
A
Matsukuma
S
S
Fujimori
M
M
Nakada
N
N
Watanabe
J
J
Kamiyama
T
T
D002851:Chromatography, High Pressure Liquid; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000302:isolation & purification* / Q000494:pharmacology; D015394:Molecular Structure; D010456:Peptides, Cyclic / Q000737:chemistry* / Q000302:isolation & purification* / Q000494:pharmacology; D013237:Stereoisomerism; D013302:Streptomyces; D013329:Structure-Activity Relationship; D059005:Topoisomerase II Inhibitors
D004791:Enzyme Inhibitors; D010456:Peptides, Cyclic; D059005:Topoisomerase II Inhibitors; C085889:cyclothialidine