Novel specific puromycin-sensitive aminopeptidase inhibitors: 3-(2,6-diethylphenyl)-2,4(1H, 3H)-quinazolinedione and N-(2,6-diethylphenyl)-2-amino-4H-3,1-benzoxazin-4-one

Hiroki Kakuta; Yukiko Koiso; Hiroyasu Takahashi; Kazuo Nagasawa; Yuichi Hashimoto

Novel specific puromycin-sensitive aminopeptidase inhibitors: 3-(2,6-diethylphenyl)-2,4(1H, 3H)-quinazolinedione and N-(2,6-diethylphenyl)-2-amino-4H-3,1-benzoxazin-4-one

Hiroki Kakuta, Yukiko Koiso, Hiroyasu Takahashi, Kazuo Nagasawa, Yuichi Hashimoto

Research output: Contribution to journal › Article › peer-review

Abstract

Novel specific PSA (puromycin-sensitive aminopeptidase) inhibitors, 3-(2,6-diethylphenyl)-2,4(1H, 3H)-quinazolinedione (3: PAQ-22) and N-(2,6-diethylphenyl)-2-amino-4H-3,1-benzoxazin-4-one (4: PAZOX-22), were designed and synthesized. These compounds are chemically much more stable than the known specific PSA inhibitor PIQ-22 (2), and the enzyme specificity and inhibitory activity to PSA are similar to those of 2. The inhibitory manner of these compounds was found to be a non-competitive mode by Lineweaver- Burk plot analysis.

Original language	English
Pages (from-to)	1433-1438
Number of pages	6
Journal	Heterocycles
Volume	55
Issue number	8
Publication status	Published - Aug 1 2001
Externally published	Yes

ASJC Scopus subject areas

Analytical Chemistry
Pharmacology
Organic Chemistry

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Novel specific puromycin-sensitive aminopeptidase inhibitors : 3-(2,6-diethylphenyl)-2,4(1H, 3H)-quinazolinedione and N-(2,6-diethylphenyl)-2-amino-4H-3,1-benzoxazin-4-one. / Kakuta, Hiroki; Koiso, Yukiko; Takahashi, Hiroyasu; Nagasawa, Kazuo; Hashimoto, Yuichi.

In: Heterocycles, Vol. 55, No. 8, 01.08.2001, p. 1433-1438.

Research output: Contribution to journal › Article › peer-review

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AU - Hashimoto, Yuichi

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