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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

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

*Institute of Molecular and Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan

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.