Synthesis and antimycobacterial activity of capuramycin analogues. Part 1: substitution of the azepan-2-one moiety of capuramycin.
Capuramycin analogues with a variety of substituents in place of the azepan-2-one moiety were synthesized from A-500359E and were tested for their translocase I inhibitory activity and in vitro antimycobacterial activity. Phenyl-type moieties were found to be effective substituents for capuramycin analogues.
Hotoda
Hitoshi
H
Exploratory Chemistry Research Laboratories, Sankyo Co., Ltd., Tokyo, Japan. hotoda@hq.sankyo.co.jp
Furukawa
Miyuki
M
Daigo
Makiko
M
Murayama
Kazuhiro
K
Kaneko
Masakatsu
M
Muramatsu
Yasunori
Y
Ishii
Michiko Miyazawa
MM
Miyakoshi
Shun-ichi
S
Takatsu
Toshio
T
Inukai
Masatoshi
M
Kakuta
Masayo
M
Abe
Tomomi
T
Harasaki
Tamako
T
Fukuoka
Takashi
T
Utsui
Yukio
Y
Ohya
Satoshi
S
D000617:Aminoglycosides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001381:Azepines / Q000737:chemistry* / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D008826:Microbial Sensitivity Tests; D009161:Mycobacterium / Q000187:drug effects; D013329:Structure-Activity Relationship; D014166:Transferases / Q000037:antagonists & inhibitors
D000617:Aminoglycosides; D000900:Anti-Bacterial Agents; D001381:Azepines; D004791:Enzyme Inhibitors; C049983:capuramycin; D014166:Transferases