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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Kakuta, H., Koiso, Y., Takahashi, H., Nagasawa, K., & Hashimoto, Y. (2001). 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. Heterocycles, 55(8), 1433-1438.