YUA001, a novel aldose reductase inhibitor isolated from alkalophilic Corynebacterium sp. YUA25. II. Chemical modification and biological activity.
A series of novel N-substituted tyramine (2-p-hydroxyphenylethylamine) derivatives (1 to approximately 11) were synthesized and evaluated for their inhibitory activity against pig kidney aldose reductase (EC 1, 1, 1, 21). Of these compounds, N-2-p-hydroxyphenylethyl maleamic acid (10) exhibits the strongest aldose reductase inhibitory activity, which is 22 times more potent than that of YUA001.
Sun
W S
WS
Department of Biotechnology, College of Engineering, Yonsei University, Sodaemun-ku, Seoul, Korea.
Lee
H S
HS
Park
J M
JM
Kim
S H
SH
Yu
J H
JH
Kim
J H
JH
D000449:Aldehyde Reductase / Q000037:antagonists & inhibitors*; D000818:Animals; D003352:Corynebacterium / Q000187:drug effects / Q000378:metabolism*; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D066298:In Vitro Techniques; D007668:Kidney / Q000187:drug effects / Q000201:enzymology; D009682:Magnetic Resonance Spectroscopy; D021241:Spectrometry, Mass, Electrospray Ionization; D013552:Swine; D014439:Tyramine / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology*
D004791:Enzyme Inhibitors; C444199:YUA001; D000449:Aldehyde Reductase; D014439:Tyramine