A-503083 A, B, E and F, novel inhibitors of bacterial translocase I, produced by Streptomyces sp. SANK 62799.
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.
Muramatsu
Yasunori
Y
Lead Discovery Research Laboratories, Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan. yasuno@shina.sankyo.co.jp
Ohnuki
Takashi
T
Ishii
Michiko Miyazawa
MM
Kizuka
Masaaki
M
Enokita
Ryuzo
R
Miyakoshi
Shunichi
S
Takatsu
Toshio
T
Inukai
Masatoshi
M
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
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