Solid-phase combinatorial synthesis of aeruginosin derivatives and their biological evaluation.
A 24-member combinatorial library based on the structure of aeruginosin 298-A (1a) was synthesized utilizing solid-phase, and their inhibitory activity against trypsin was evaluated. Among the library, we found that D-Hpla-D-Leu-L-Choi-Agma (1h) is 300 times more potent than the parent natural product 1a.
Doi
Takayuki
T
Department of Applied Chemistry, Tokyo Institute of Technology, 2-12-1 Ookayama, Meguro, Tokyo 152-8552, Japan.
Hoshina
Yoichiro
Y
Mogi
Hiroyuki
H
Yamada
Yoshifumi
Y
Takahashi
Takashi
T
D002851:Chromatography, High Pressure Liquid; D020650:Combinatorial Chemistry Techniques; D007930:Leucine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D019151:Peptide Library; D011480:Protease Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D013056:Spectrophotometry, Ultraviolet; D013237:Stereoisomerism; D014357:Trypsin / Q000378:metabolism
D019151:Peptide Library; D011480:Protease Inhibitors; C419325:aeruginosin 298-A; D014357:Trypsin; D007930:Leucine