Synthesis and Evaluation of Guanidine-Containing Schiff Base Copper(II), Zinc(II), and Iron(III) Chelates as Trypsin Inhibitors
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概要
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3-Formyl-4-hydroxyphenylguanidine hydrochloride and its Schiff base copper(II), zinc(II), and iron(III) chelates were synthesized and their inhibitory activity against bovine β-trypsin were determined. Syntheses of Schiff base metal chelates were carried out from 3-formyl-4-hydroxyphenylguanidine, various L-amino acids, and divalent metal acetate. Their structures were established on the basis of spectroscopic evidence and elemental analysis. The inhibitory activity of these chelates against bovine β-trypsin was determined. The guanidine-containing copper(II) and zinc(II) chelates behaved as potent competitive inhibitors of trypsin. However, similar inhibitory activity was not observed for guanidine-containing iron(III) chelates. The inhibition constants (K_1 values, ca. 10^<-5>M) of guanidine-containing Schiff base copper(II) and zinc(II) chelates were slightly lower than those (ca. 10^<-6>M) of the corresponding amidine-containing Schiff base chelates with regard to bovine trypsin.
- 2003-06-01
著者
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Toyota Eiko
Faculty of Pharmaceutical Sciences, Health Sciences University of Hokkaido
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Sekizaki Haruo
Faculty of Pharmaceutical Sciences, Health Sciences University of Hokkaido
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Toyota E
Faculty Of Pharmaceutical Sciences Health Sciences University Of Hokkaido
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Toyota Eiko
Faculty Of Pharmaceutical Sciences Health Sciences University Of Hokkaido
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Itoh Kunihiko
Faculty Of Pharmaceutical Sciences Health Sciences University Of Hokkaido
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Sekizaki H
Faculty Of Pharmaceutical Sciences Health Sciences University Of Hokkaido
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Sekizaki Haruo
Faculty Of Pharmaceutical Sciences Health Science University Of Hokkaido
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TANIZAWA Kazutaka
Faculty of Pharmaceutical Sciences, Health Sciences University of Hokkaido
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Tanizawa K
Faculty Of Pharmaceutical Sciences Health Sciences University Of Hokkaido
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Sekizaki Haruo
Faculty of Pharmaceutical Science, Higashi Nippon Gakuen University
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Toyota Eiko
Faculty of Pharmaceutical Science, Higashi Nippon Gakuen University
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