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 journalArticle

16 Citations (Scopus)

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 languageEnglish
Pages (from-to)1433-1438
Number of pages6
JournalHeterocycles
Volume55
Issue number8
Publication statusPublished - Aug 1 2001
Externally publishedYes

ASJC Scopus subject areas

  • Analytical Chemistry
  • Pharmacology
  • Organic Chemistry

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