title: Cyclothialidine analogs, novel DNA gyrase inhibitors.
abstract: 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.
authors.affiliation: Nippon Roche Research Center, Kanagawa, Japan.
authors.forename: K
authors.initials: K
authors.lastname: Yamaji
authors.forename: M
authors.initials: M
authors.lastname: Masubuchi
authors.forename: F
authors.initials: F
authors.lastname: Kawahara
authors.forename: Y
authors.initials: Y
authors.lastname: Nakamura
authors.forename: A
authors.initials: A
authors.lastname: Nishio
authors.forename: S
authors.initials: S
authors.lastname: Matsukuma
authors.forename: M
authors.initials: M
authors.lastname: Fujimori
authors.forename: N
authors.initials: N
authors.lastname: Nakada
authors.forename: J
authors.initials: J
authors.lastname: Watanabe
authors.forename: T
authors.initials: T
authors.lastname: Kamiyama
mesh_terms: 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
chemical_list: D004791:Enzyme Inhibitors; D010456:Peptides, Cyclic; D059005:Topoisomerase II Inhibitors; C085889:cyclothialidine