FR290581, a novel sordarin derivative: synthesis and antifungal activity.
Sordarin is a unique natural product antifungal agent that is an inhibitor of elongation factor 2. To improve biological activity, we synthesized various compounds by novel modification of the aglycone, sordaricin. As a result, we have discovered the novel sordarin derivative FR290581. This compound exhibited superior activity and a good pharmacokinetic profile, and also displayed good in vivo activity against Candida albicans.
Hanadate
Tadaatsu
T
Chemistry Research Labs., Astellas Pharma Inc., 2-1-6 Kashima, Yodogawa-ku, Osaka 532-8514, Japan.
Tomishima
Masaki
M
Shiraishi
Nobuyuki
N
Tanabe
Daisuke
D
Morikawa
Hiroshi
H
Barrett
David
D
Matsumoto
Satoru
S
Ohtomo
Kazumi
K
Maki
Katsuyuki
K
D000818:Animals; D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002176:Candida albicans / Q000187:drug effects / Q000378:metabolism; D007192:Indenes / Q000138:chemical synthesis* / Q000494:pharmacology; D051379:Mice; D011500:Protein Synthesis Inhibitors / Q000138:chemical synthesis; D013329:Structure-Activity Relationship
D000935:Antifungal Agents; C543156:FR290581; D007192:Indenes; D011500:Protein Synthesis Inhibitors; C003329:sordarin