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 (1-11) 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 r...

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Veröffentlicht in:	Journal of antibiotics 2001/10/25, Vol.54(10), pp.827-830
Hauptverfasser:	SUN, WON-SUCK, LEE, HYO-SUNG, PARK, JUNG-MIN, KIM, SUNG-HAN, YU, JU-HYUN, KIM, JUNG-HAN
Format:	Artikel
Sprache:	eng
Schlagworte:	Aldehyde Reductase - antagonists & inhibitors Animals Antibiotics, microbial producers, chemotherapic agents, antiseptics, disinfecting agents Applied microbiology Biological and medical sciences Corynebacterium - drug effects Corynebacterium - metabolism Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Fundamental and applied biological sciences. Psychology General aspects In Vitro Techniques Kidney - drug effects Kidney - enzymology Magnetic Resonance Spectroscopy Microbiology Spectrometry, Mass, Electrospray Ionization Swine Tyramine - analogs & derivatives Tyramine - chemistry Tyramine - pharmacology
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Zusammenfassung:	A series of novel N-substituted tyramine (2-p-hydroxyphenylethylamine) derivatives (1-11) 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 YUA0011).
ISSN:	0021-8820 1881-1469
DOI:	10.7164/antibiotics.54.827