TY - JOUR
T1 - Novel specific puromycin-sensitive aminopeptidase inhibitors
T2 - 3-(2,6-diethylphenyl)-2,4(1H, 3H)-quinazolinedione and N-(2,6-diethylphenyl)-2-amino-4H-3,1-benzoxazin-4-one
AU - Kakuta, Hiroki
AU - Koiso, Yukiko
AU - Takahashi, Hiroyasu
AU - Nagasawa, Kazuo
AU - Hashimoto, Yuichi
PY - 2001/8/1
Y1 - 2001/8/1
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=0001691491&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0001691491&partnerID=8YFLogxK
M3 - Article
AN - SCOPUS:0001691491
VL - 55
SP - 1433
EP - 1438
JO - Heterocycles
JF - Heterocycles
SN - 0385-5414
IS - 8
ER -