title: A-503083 A, B, E and F, novel inhibitors of bacterial translocase I, produced by Streptomyces sp. SANK 62799.
abstract: Novel nucleoside antibiotics were isolated from the cultured broth of the strain classified as Streptomyces sp. SANK 62799. The strain produced four novel capuramycin derivatives designated as A-503083 A, B, E and F. Their structures were elucidated as 2'-O-carbamoyl derivatives of A-500359 A, B (capuramycin), E and F, respectively. A-503083 A, B, E and F inhibited bacterial phospho-N-acetylmuramyl-pentapeptide-translocase (translocase I: EC 2.7.8.13) with IC50 values of 0.024, 0.038, 0.135 and 17.9 microM, respectively.
authors.affiliation: Lead Discovery Research Laboratories, Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan. yasuno@shina.sankyo.co.jp
authors.forename: Yasunori
authors.initials: Y
authors.lastname: Muramatsu
authors.forename: Takashi
authors.initials: T
authors.lastname: Ohnuki
authors.forename: Michiko Miyazawa
authors.initials: MM
authors.lastname: Ishii
authors.forename: Masaaki
authors.initials: M
authors.lastname: Kizuka
authors.forename: Ryuzo
authors.initials: R
authors.lastname: Enokita
authors.forename: Shunichi
authors.initials: S
authors.lastname: Miyakoshi
authors.forename: Toshio
authors.initials: T
authors.lastname: Takatsu
authors.forename: Masatoshi
authors.initials: M
authors.lastname: Inukai
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D001381:Azepines / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D001419:Bacteria / Q000201:enzymology*; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D013302:Streptomyces / Q000145:classification / Q000378:metabolism*; D017855:Transferases (Other Substituted Phosphate Groups) / Q000037:antagonists & inhibitors*; D014529:Uridine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology
chemical_list: C495801:A 503083 A; C495802:A 503083 B; C495803:A 503083 E; C495804:A 503083 F; D000900:Anti-Bacterial Agents; D001381:Azepines; D004791:Enzyme Inhibitors; D017855:Transferases (Other Substituted Phosphate Groups); C100130:phospho-N-acetylmuramoyl pentapeptide transferase; D014529:Uridine